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1

Comparative Plasma Exposure of Albendazole after Administration of Rapidly Disintegrating Tablets in Dogs  

PubMed Central

The main objectives of this study were (a) to evaluate the in vitro performance of the rapid disintegration tablets as a way to improve the solid dispersions and (b) to study the in vivo pharmacokinetics of the albendazole modified formulation in dogs. Rapid disintegration of tablets seems to be a key factor for efficiency of solid dispersions with regard to improvement of the albendazole bioavailability. The in vivo assays performed on dogs showed a marked increase in drug plasma exposure when albendazole was given in solid dispersions incorporated into rapid disintegration tablets compared with conventional solid dosage form. PMID:24063016

Castro, Silvina G.; Dib, Alicia; Suarez, Gonzalo; Allemandi, Daniel; Lanusse, Carlos; Sanchez Bruni, Sergio; Palma, Santiago D.

2013-01-01

2

Comparative plasma exposure of albendazole after administration of rapidly disintegrating tablets in dogs.  

PubMed

The main objectives of this study were (a) to evaluate the in vitro performance of the rapid disintegration tablets as a way to improve the solid dispersions and (b) to study the in vivo pharmacokinetics of the albendazole modified formulation in dogs. Rapid disintegration of tablets seems to be a key factor for efficiency of solid dispersions with regard to improvement of the albendazole bioavailability. The in vivo assays performed on dogs showed a marked increase in drug plasma exposure when albendazole was given in solid dispersions incorporated into rapid disintegration tablets compared with conventional solid dosage form. PMID:24063016

Castro, Silvina G; Dib, Alicia; Suarez, Gonzalo; Allemandi, Daniel; Lanusse, Carlos; Sanchez Bruni, Sergio; Palma, Santiago D

2013-01-01

3

[Fast-disintegration oral tablets having sustained release property].  

PubMed

Fast-disintegrating (FD) tablets containing nicorandil-loaded dry emulsions were prepared and their controlled-release properties were examined and compared with the plain FD tablets (FD tablets without dry emulsions) and commercial tablets. The dry emulsions were prepared with myristyl alcohol and stearyl alcohol and their property was modified by mixing the ratio of the two alcohols. Disintegration time of the prepared FD tablets was sufficiently fast (i.e., 12 to 23 s). In vitro release of nicorandil from the FD tablets containing the dry emulsions was sustained over 6 h, while that from plain FD and commercial tablets was complete within 5 min. In vivo absorption of nicorandil from the tablets was evaluated by oral administration in beagle dogs. FD tablets containing dry emulsions showed a similar AUC, lower Cmax, and delayed Tmax compared to the plain FD and commercial tablets. These results suggest that the dry emulsion-loaded FD tablets can be utilized to improve the sustained-release property of active drugs. PMID:12440156

Jin, Yi; Ohkuma, Hideki; Wang, Hua; Natsume, Hideshi; Sugibayashi, Kenji; Morimoto, Yasunori

2002-11-01

4

Assessment of disintegration of rapidly disintegrating tablets by a visiometric liquid jet-mediated disintegration apparatus.  

PubMed

The aim of this study was to develop a responsive disintegration test apparatus that is particularly suitable for rapidly disintegrating tablets (RDTs). The designed RDT disintegration apparatus consisted of disintegration compartment, stereomicroscope and high speed video camera. Computational fluid dynamics (CFD) was used to simulate 3 different designs of the compartment and to predict velocity and pressure patterns inside the compartment. The CFD preprocessor established the compartment models and the CFD solver determined the numerical solutions of the governing equations that described disintegration medium flow. Simulation was validated by good agreement between CFD and experimental results. Based on the results, the most suitable disintegration compartment was selected. Six types of commercial RDTs were used and disintegration times of these tablets were determined using the designed RDT disintegration apparatus and the USP disintegration apparatus. The results obtained using the designed apparatus correlated well to those obtained by the USP apparatus. Thus, the applied CFD approach had the potential to predict the fluid hydrodynamics for the design of optimal disintegration apparatus. The designed visiometric liquid jet-mediated disintegration apparatus for RDT provided efficient and precise determination of very short disintegration times of rapidly disintegrating dosage forms. PMID:22985772

Desai, Parind M; Liew, Celine V; Heng, Paul W S

2013-02-14

5

Hordeum Vulgare Hull in the Design of Fast Disintegrating Tablets  

PubMed Central

In the present study, fast disintegrating tablets were designed with a view to enhance patient compliance. In this method, the hull of Hordeum vulgare, cross carmellose sodium, and sodium starch glycolate were used as superdisintegrants (4 and 6%), along with microcrystalline cellulose and mannitol, to enhance mouth feel. The prepared batches of tablets were evaluated for hardness, friability, drug content uniformity, wetting time, water absorption ratio and in vitro dispersion time. Based on the in vitro dispersion time, the formulations were tested for the in vitro drug release pattern. Tablets having H. vulgare hull showed the release profile comparable to those tablets having sodium starch glycolate and cross carmellose sodium. PMID:21897660

Rajpurohit, H; Sharma, P; Sharma, S; Purohit, S; Bhandari, A

2011-01-01

6

Fast disintegrating tablets of nisoldipine for intra-oral administration.  

PubMed

Nisoldipine is a calcium channel blocker with low and variable oral bioavailability. This was attributed to slow dissolution and presystemic metabolism. Accordingly, the objective of this work was to enhance the dissolution rate of nisoldipine to formulate fast disintegrating tablets with rapid dissolution. Binary solid dispersions (SD) were prepared for the drug with hydroxypropyl methyl cellulose E5 (HPMC), polyvinylpyrrolidone (PVP), Pluronic F68 or polyethylene glycol 6000 (PEG 6000). SD formation increased the dissolution rate compared to pure drug with the corresponding physical mixtures failing to provide the same dissolution enhancement. This indicates that the SD enhanced dissolution is not due to the solubilizing effect of the polymer and can be due to physical change in the drug crystal which was confirmed by thermal analysis. SD with HPMC and PVP were selected for preparation of fast disintegrating tablets as they liberated most of the drug in the first 5?min. HPMC-based tablets disintegrated rapidly and released most of the drug in the first 2?min which correlated with the corresponding SD. In contrast, PVP-based tablets disintegrated slowly with gradual dissolution. This can be attributed to the binding effect of PVP. The study developed fast disintegrating tablet for intra-oral administration. PMID:23841582

El Maghraby, Gamal M; Elsergany, Ramy N

2014-09-01

7

Evaluation of coprocessed disintegrants produced from tapioca starch and mannitol in orally disintegrating paracetamol tablet.  

PubMed

The study evaluated two novel coprocessed excipients (with two methods) as disintegrants in an orally disintegrating paracetamol tablet formulation. The tablets produced were assessed for mechanical properties with the use of friability and tensile strength while the release properties were assessed with wetting time, water absorption ratio, disintegration time and dissolution profile. The results obtained showed that the methods of coprocessing and disintegrant incorporation influenced the activities of the disintegrants. The novel disintegrant enhanced the mechanical properties of the tablets containing them as shown by lower friability and higher tensile strength of the tablets. The result further showed that the rate and amount of water absorbed, type of disintegrant and the method of disintegrant incorporation influenced the total amount of paracetamol released. The study concluded that the novel disintegrants will be effective in the formulation of orally disintegrating paracetamol tablets. PMID:25362809

Adeoye, Oluwatomide; Alebiowu, Gbenga

2014-01-01

8

Mimosa pudica seed mucilage: isolation; characterization and evaluation as tablet disintegrant and binder.  

PubMed

In the present study Mimosa pudica seed mucilage was isolated, characterized and evaluated as tablet binder and disintegrant. Several properties of mucilage like high swelling index and gelling nature prompted us to explore its applications as disintegrating and binding agent. Disintegrant properties were evaluated by formulating directly compressed hydrochlorothiazide tablets containing 1%-10% (w/w) of seed mucilage as disintegrant and compared with the standard disintegrants. The disintegration time of mucilage containing tablets was found to be in the order of 3%>1%>5%>7.5%>10%. On comparative evaluation with standard disintegrants, it was observed that the order of disintegration of tablets was Ac-Di-Soldisintegration time studies. The binding and granulating properties of mucilage were evaluated by formulating the paracetamol tablets using the Mimosa mucilage at 6%, 8%, and 10% (w/w) concentration as the binder and compared with tablets prepared using PVP-K25 (1.7%, w/w) and acacia (6.8%, w/w) as the binder. Mimosa mucilage at 10% (w/w) concentration provided tablets with adequate hardness and friability. In conclusion, M. pudica seed mucilage is a potential tablet disintegrant and binder. PMID:23500434

Ahuja, Munish; Kumar, Ashok; Yadav, Parvinder; Singh, Kuldeep

2013-06-01

9

Formulation and optimization of orally disintegrating tablets of sumatriptan succinate.  

PubMed

The aims of the present research were to mask the intensely bitter taste of sumatriptan succinate and to formulate orally disintegrating tablets (ODTs) of the taste masked drug. Taste masking was performed by coating sumatriptan succinate with Eudragit EPO using spray drying technique. The resultant microspheres were evaluated for thermal analysis, yield, particle size, entrapment efficiency and in vitro taste masking. The tablets were formulated by mixing the taste masked microspheres with different types and concentrations of superdisintegrants and compressed using direct compression method followed by sublimation technique. The prepared tablets were evaluated for weight variation, thickness, hardness, friability, drug content, water content, in vitro disintegration time and in vitro drug release. All the tablet formulations disintegrated in vitro within 37-410 s. The optimized formulation containing 5% Kollidon CL-SF released more than 90% of the drug within 15 min and the release was comparable to that of commercial product (Suminat®). In human volunteers, the optimized formulation was found to have a pleasant taste and mouth feel and disintegrated in the oral cavity within 41 s. The optimized formulation was found to be stable and bioequivalent with Suminat®. PMID:21804234

Sheshala, Ravi; Khan, Nurzalina; Darwis, Yusrida

2011-01-01

10

Effect of a Disintegration Mechanism on Wetting, Water Absorption, and Disintegration Time of Orodispersible Tablets  

PubMed Central

The aim of this study was to evaluate the influence of disintegration mechanism of various types of disintegrants on the absorption ratio (AR), wetting time (WT), and disintegration time (DT) of orodispersible tablets (ODTs). ODTs were prepared by direct compression using mannitol as filler and disintegrants selected from a range of swellable, osmotic, and porous disintegrants. Tablets formed were characterized for their water AR, WT, and DT. The porosity and mechanical strength of the tablets were also measured. Results show that the DT of formulated ODTs was directly related to the WT and was a function of the disintegration mechanism of the disintegrant used. The lowest WT and DT were observed for tablets formulated using the osmotic disintegrant sodium citrate and these tablets also showed the lowest AR and porosity. The wetting and disintegration of tablets containing the highly swellable disintegrant, sodium starch glycollate, was slowest despite their high water AR and high tablet porosity. Rapid wetting and disintegration of ODTs were therefore not necessarily related to the porosity of the tablets. PMID:23112534

Pabari, RM; Ramtoola, Z

2012-01-01

11

Design and evaluation of microwave-treated orally disintegrating tablets containing polymeric disintegrant and mannitol.  

PubMed

Microwave (MW) treatment was used to develop a formulation process for the preparation of wet molded orally disintegrating tablets (ODTs) consisting of mannitol and polymeric disintegrant with improved hardness and disintegration properties. The wet molded tablets were prepared in accordance with the conventional methods and subsequently heated by MW irradiation to induce the swelling of the tablet. Croscarmellose sodium, crospovidone, and low-substituted hydroxypropylcellulose (L-HPC) were evaluated for their use with this technology. NBD-020, which is a grade of L-HPC, provided the better hardness and disintegration results. In addition, the crystalline forms of mannitol impacted on hardness and disintegration properties of the ODT upon MW irradiation. The effects of the disintegrant ratio, ? and ? crystalline mannitol ratio, amount of water, and compression force on the ODT properties were evaluated using the design of experiment method. MW-induced swelling was enhanced by an increase in the disintegrant ratio. Although the hardness of the tablet increased following MW treatment, the disintegration time became less than that of the MW-untreated tablets as the ?-mannitol ratios increased. Taken together, the results indicated that the polymeric disintegrant greatly improved the properties of the molded tablets in combination with MW treatment. PMID:23524122

Sano, Syusuke; Iwao, Yasunori; Noguchi, Shuji; Kimura, Susumu; Itai, Shigeru

2013-05-01

12

Effect of disintegrants on the properties of multiparticulate tablets comprising starch pellets and excipient granules.  

PubMed

A design of experiments (DOE) approach (2-level full factorial design) was used to investigate the effect of several formulation and process variables on the properties of fast disintegrating tablets comprising starch-based pellets and excipient granules and to optimize and validate the design space. The percentage of starch pellets (30-50%, w/w), type of disintegrants (Ac-di-sol, Explotab, Polyplasdone), percentage of external disintegrant (4-8%, w/w) and compression force (5-15 kN) were the evaluated factors (24 runs+9 centre points=33 experiments), while tablet hardness, friability and disintegration time were the studied tablet properties (responses). Starch pellets were prepared by extrusion-spheronisation. Excipient granules containing microcrystalline cellulose, lactose, internal disintegrant (8%) and polyvinylpyrrolidone K-30 (4%) were prepared by wet granulation. Pellets, granules (700-1000 ?m) and external disintegrant were mixed and compressed into oblong tablets (17.1mm long, 8.2mm wide). Evaluation of the effects calculated from the DOE results showed that a lower concentration of starch pellets and higher compression force were required to yield tablets with a high hardness, a low friability (<1%) and short disintegration time (<3 min). Polyplasdone granules had the lowest porosity and friability which was reflected in the DOE study, where the Polyplasdone-containing tablets were harder, less friable and disintegrated faster compared to Ac-di-sol and Explotab-containing tablets. Monte carlo simulations at the optimal factor settings (30% starch pellets, 4% Polyplasdone and 10 kN compression force) indicated that a robust system was formed as the probability to exceed the limits was low for all responses. Validation of the design space (at optimal settings) showed that the results predicted via the DOE models correlated well with the observed experimental data. PMID:22101283

Mehta, Samata; De Beer, Thomas; Remon, Jean Paul; Vervaet, Chris

2012-01-17

13

Disintegrants combination: development and optimization of a cefadroxil fast disintegrating tablet.  

PubMed

Fast Disintegrating Tablets (FDTs) is a rapidly growing dosage form preferred for special population (pediatric, geriatric and psychotic patients). It is also developed with the aim of improving bioavailability and patient compliance. During the present study, cefadroxil fast disintegrating tablets formulations (n=9) were designed and optimized by central composite design with two independent variables (croscarmellose and crospovidone) using design expert® software. The effects of independent variables on formulation properties such as friability, hardness, in vitro dispersion and disintegration were assessed by drawing response surface graphs with design expert® software. Tablets were assessed for pharmacopeial and non-pharmacopeial parameters to ensure the quality of compressed tablets. Among all formulations, F3, F8 and F9 have shown better results. The formulation F9 containing 15mg croscarmellose and 33.075mg crospovidone showed good pharmacotechnical attributes as well as shelf life. F 9 showed improved dissolution with t90% of> 2 min and will lead to better bioavailability. PMID:25176230

Rahim, Najia; Naqvi, Syed Baqir-Shyum; Bibi, Rehana; Iffat, Wajiha; Shakeel, Sadia; Muhammad, Iyad Naeem

2014-09-01

14

Effects of disintegration-promoting agent, lubricants and moisture treatment on optimized fast disintegrating tablets.  

PubMed

Effects of calcium silicate (disintegration-promoting agent) and various lubricants on an optimized beta-cyclodextrin-based fast-disintegrating tablet formulation were investigated. Effects of moisture treatment were also evaluated at 75, 85 and 95% relative humidities. A two factor, three levels (3(2)) full factorial design was used to optimize concentrations of calcium silicate and lubricant. Magnesium stearate, being commonly used lubricant, was used to optimize lubricant concentration in optimization study. Other lubricants were evaluated at an obtained optimum concentration. Desiccator with saturated salt solutions was used to analyze effects of moisture treatments. Results of multiple linear regression analysis revealed that concentration of calcium silicate had no effect; however concentration of lubricant was found to be important for tablet disintegration and hardness. An optimized value of 1.5% of magnesium stearate gave disintegration time of 23.4 s and hardness of 1.42 kg. At an optimized concentration, glycerol dibehenate and L-leucine significantly affected disintegration time, while talc and stearic acid had no significant effect. Tablet hardness was significantly affected with L-leucine, while other lubricants had no significant effect. Hardness was not affected at 75% moisture treatment. Moisture treatment at 85 and 95% increased hardness of the tablets; however at the same time it negatively affected the disintegration time. PMID:18778759

Late, Sameer G; Yu, Yi-Ying; Banga, Ajay K

2009-01-01

15

Plantago ovata Mucilage in the Design of Fast Disintegrating Tablets.  

PubMed

In the present work, fast disintegrating tablets of prochlorperazine maleate were designed with a view to enhance patient compliance by direct compression method. In this method mucilage of Plantago ovata and crospovidone were used as superdisintegrants (2-8% w/w) along with microcrystalline cellulose (20-60% w/w) and directly compressible mannitol (Pearlitol SD 200) to enhance mouth feel. The prepared batches of tablets were evaluated for hardness, friability, drug content uniformity, wetting time, water absorption ratio and in vitro dispersion time. Based on in vitro dispersion time (approximately 8 s), the two formulations were tested for the in vitro drug release pattern (in pH 6.8 phosphate buffer), short-term stability (at 40 degrees /75% relative humidity for 3 mo) and drug-excipient interaction (IR spectroscopy). Among the two promising formulations, the formulation prepared by using 8% w/w of Plantago ovata mucilage and 60% w/w of microcrystalline cellulose emerged as the overall best formulation (t(50%) 3.3 min) based on the in vitro drug release characteristics compared to conventional commercial tablets formulation (t(50%) 17.4 min). Short-term stability studies on the formulations indicated that there are no significant changes in drug content and in vitro dispersion time (p<0.05). PMID:20177454

Shirsand, S B; Suresh, Sarasija; Para, M S; Swamy, P V; Kumar, D Nagendra

2009-01-01

16

Obtaining fast dissolving disintegrating tablets with different doses of melatonin.  

PubMed

Fast dissolving disintegrating tablets (FDDTs) containing different dosages of melatonin have been manufactured for administration to a specific target population: pediatric patients, having potential difficulties taking other oral forms. The lower dosages (3 and 5mg) are intended for epileptic children, migraine prevention, neurodevelopmental disability, sleep disorders and blindness. Dosages of 10 and 60 mg are intended for Duchenne muscular dystrophy. Two FDDT groups have been designed, one which has excipients for direct compression and others having direct compression and effervescent excipients. Tablets have been produced having disintegration times of less than 25s and with friability and hardness values that require no special storage or packaging conditions. PMID:24699354

Muñoz, H; Castan, H; Clares, B; Ruiz, M A

2014-06-01

17

Comparative disintegrant activities of breadfruit starch and official corn starch  

Microsoft Academic Search

A Comparative evaluation of starch powder extracted from breadfruit (Artocarpus communis, Frost) as tablet disintegrant was made with corn starch BP using a 2×4 factorial experiment in a randomized complete block design. Two factors (type of starch: 2 i.e. breadfruit and corn) at four levels (concentrations of starch disintegrant: 4 i.e. 2.5%, 5%, 7.5% and 10%) were studied. One (1)

Sarafadeen A. Adebayo; Eugenie Brown-Myrie; Oludele A. Itiola

2008-01-01

18

Formulation of multiparticulate systems as lyophilised orally disintegrating tablets.  

PubMed

The current study aimed to exploit the electrostatic associative interaction between carrageenan and gelatin to optimise a formulation of lyophilised orally disintegrating tablets (ODTs) suitable for multiparticulate delivery. A central composite face centred (CCF) design was applied to study the influence of formulation variables (gelatin, carrageenan and alanine concentrations) on the crucial responses of the formulation (disintegration time, hardness, viscosity and pH). The disintegration time and viscosity were controlled by the associative interaction between gelatin and carrageenan upon hydration which forms a strong complex that increases the viscosity of the stock solution and forms tablet with higher resistant to disintegration in aqueous medium. Therefore, the levels of carrageenan, gelatin and their interaction in the formulation were the significant factors. In terms of hardness, increasing gelatin and alanine concentration was the most effective way to improve tablet hardness. Accordingly, optimum concentrations of these excipients were needed to find the best balance that fulfilled all formulation requirements. The revised model showed high degree of predictability and optimisation reliability and therefore was successful in developing an ODT formulation with optimised properties that were able deliver enteric coated multiparticulates of omeprazole without compromising their functionality. PMID:21693189

Alhusban, Farhan; Perrie, Yvonne; Mohammed, Afzal R

2011-11-01

19

Application of a novel automatic disintegration apparatus for the development and evaluation of a direct compression rapidly disintegrating tablet.  

PubMed

An automatic disintegration tester was developed and used to explore disintegration mechanism and times of rapidly disintegrating tablets. DT50, the time required for a tablet to decrease in its thickness by half, allowed an unbiased determination of disintegration time. Calcium silicate concentration, Explotab® concentration, DiPac®/Xylitab® ratio as fillers, and compression pressure were evaluated using a central composite model design analysis for their DT50, tensile strength, and friability. Tablets that could reasonably be handled (friability <10%) could be produced. The expansion coefficient (n) and the exponential rate constant (k) for disintegrating tablets, originally measured by Caramella et al. using force kinetics, could be determined from axial displacement data measured directly without the need to assume that disintegration force generation was indicative of changes in tablet volume. The n values of tablets containing calcium silicate, Ditab® and/or Xylitab®, magnesium stearate, and Explotab® suggested that the amount of Explotab® was not a significant factor in determining the disintegration mechanism; however, the type of disintegrant used did alter the n value. Primojel® and Explotab®, which are in the same class of disintegrants, exhibited similar DT50, n, and k. Polyplasdone® XL exhibited a much higher n, while yielding faster DT50, suggesting that its performance is more dependent on facilitating the interfacial separation of particles. AcDiSol® showed no apparent moisture sensitivity in regards to disintegration efficiency. The use of the novel apparatus proved to be useful in measuring disintegration efficiency of rapidly disintegrating tablets and in providing valuable information on the disintegration phenomena. PMID:22091970

Jung, Huijeong Ashley; Augsburger, Larry L

2012-07-01

20

Fabrication and optimization of fast disintegrating tablets employing interpolymeric chitosan-alginate complex and chitin as novel superdisintegrants.  

PubMed

The objective of the present work was to optimize the formulation of fast disintegrating tablets (FDTs) of ondansetron HCl containing novel superdisintegrants, possessing sufficient mechanical strength and disintegration time comparable to those containing crospovidone or croscarmellose sodium. The FDTs were formulated using a novel superdisintegrant (chitosan-alginate (1:1) interpolymer complex and chitin) to achieve a sweet tasting disintegrating system. The results revealed that chitin (5-20%) increased the porosity and decreased the DT of tablets. At higher concentrations chitin maintained tablet porosity even at 5.5 kg crushing strength. Ondansetron HCl was found to antagonize the wicking action of glycine. Further, evaluation of the mechanism of disintegration revealed that glycine transported the aqueous medium to different parts of the tablets while the chitosan-alginate complex swelled up due to transfer of moisture from glycine. This phenomenon resulted in breakage of the tablet within seconds. For preparing optimized FDTs, the reduced model equations generated from Box-Behnken design (BBD) were solved after substituting the known disintegration time of FDTs containing superdisintegrants in the reduced model equations. The results suggested that excipient system under investigation not only improved the disintegration time but also made it possible to prepare FDTs with higher crushing strength as compared to tablets containing known superdisintegrants. PMID:21796940

Goel, Honey; Tiwary, Ashok K; Rana, Vikas

2011-01-01

21

Preparation of cross-linked carboxymethyl jackfruit starch and evaluation as a tablet disintegrant.  

PubMed

The main purposes of this study are to prepare cross-linked carboxymethyl jackfruit starch (CL-CMJF) and to evaluate its pharmaceutical property as a tablet disintegrant. CL-CMJF was prepared by a dual carboxymethyl-crosslinking reaction in a flask containing jackfruit seed starch (JFS), chloroacetic acid (CAA), sodium hydroxide (NaOH) and sodium trimetaphosphate (STMP). The reaction was carried out using methanol as a solvent for 60 min at 70°C and at JFS:CAA:NaOH:STMP ratio of 1.0:0.29:0.28:0.07. The obtained CL-CMJF, with degree of substitution and degree of crosslinking calculated to be 0.34 and 0.06, respectively, was insoluble but swellable in water. Rheological study revealed a decreased in solution viscosity compared to the non-crosslinked CMJF. The water uptake of CL-CMJF was 23 times higher than that of native starch and was comparable to that of a commercial superdisintegrant, sodium starch glycolate (SSG). The swelling ability of CL-CMRS was similar to that of crosscarmellose sodium (CCS), another commercial superdisintegrant. Disintegration test of aspirin tablets containing 2%w/w of JFS, CL-CMJF, SSG and CCS showed disintegration times in the order of SSG < CCS ~ CL-CMJF < JFS. The results suggested that CL-CMJF could be developed as a tablet disintegrant. PMID:21959799

Kittipongpatana, Nisit; Suwakon, Janta; Kittipongpatana, Ornanong

2011-10-01

22

Stability of benzocaine formulated in commercial oral disintegrating tablet platforms.  

PubMed

Pharmaceutical excipients contain reactive groups and impurities due to manufacturing processes that can cause decomposition of active drug compounds. The aim of this investigation was to determine if commercially available oral disintegrating tablet (ODT) platforms induce active pharmaceutical ingredient (API) degradation. Benzocaine was selected as the model API due to known degradation through ester and primary amino groups. Benzocaine was either compressed at a constant pressure, 20 kN, or at pressure necessary to produce a set hardness, i.e., where a series of tablets were produced at different compression forces until an average hardness of approximately 100 N was achieved. Tablets were then stored for 6 months under International Conference on Harmonization recommended conditions, 25°C and 60% relative humidity (RH), or under accelerated conditions, 40°C and 75% RH. Benzocaine degradation was monitored by liquid chromatography-mass spectrometry. Regardless of the ODT platform, no degradation of benzocaine was observed in tablets that were kept for 6 months at 25°C and 60% RH. After storage for 30 days under accelerated conditions, benzocaine degradation was observed in a single platform. Qualitative differences in ODT platform behavior were observed in physical appearance of the tablets after storage under different temperature and humidity conditions. PMID:23990120

Köllmer, Melanie; Popescu, Carmen; Manda, Prashanth; Zhou, Leon; Gemeinhart, Richard A

2013-12-01

23

Formulation development and evaluation of fast disintegrating tablets of salbutamol sulphate for respiratory disorders.  

PubMed

Recent developments in fast disintegrating tablets have brought convenience in dosing to pediatric and elderly patients who have trouble in swallowing tablets. The objective of the present study was to prepare the fast disintegrating tablet of salbutamol sulphate for respiratory disorders for pediatrics. As precision of dosing and patient's compliance become important prerequisites for a long-term treatment, there is a need to develop a formulation for this drug which overcomes problems such as difficulty in swallowing, inconvenience in administration while travelling, and patient's acceptability. Hence, the present investigation were undertaken with a view to develop a fast disintegrating tablet of salbutamol sulphate which offers a new range of products having desired characteristics and intended benefits. Superdisintegrants such as sodium starch glycolate was optimized. Different binders were optimized along with optimized superdisintegrant concentration. The tablets were prepared by direct compression technique. The tablets were evaluated for hardness, friability, weight variation, wetting time, disintegration time, and uniformity of content. Optimized formulation was evaluated by in vitro dissolution test, drug-excipient compatibility, and accelerated stability study. It was concluded that fast disintegrating tablets of salbutamol sulphate were formulated successfully with desired characteristics which disintegrated rapidly; provided rapid onset of action; and enhanced the patient convenience and compliance. PMID:23956881

Sharma, Deepak

2013-01-01

24

Formulation Development and Evaluation of Fast Disintegrating Tablets of Salbutamol Sulphate for Respiratory Disorders  

PubMed Central

Recent developments in fast disintegrating tablets have brought convenience in dosing to pediatric and elderly patients who have trouble in swallowing tablets. The objective of the present study was to prepare the fast disintegrating tablet of salbutamol sulphate for respiratory disorders for pediatrics. As precision of dosing and patient's compliance become important prerequisites for a long-term treatment, there is a need to develop a formulation for this drug which overcomes problems such as difficulty in swallowing, inconvenience in administration while travelling, and patient's acceptability. Hence, the present investigation were undertaken with a view to develop a fast disintegrating tablet of salbutamol sulphate which offers a new range of products having desired characteristics and intended benefits. Superdisintegrants such as sodium starch glycolate was optimized. Different binders were optimized along with optimized superdisintegrant concentration. The tablets were prepared by direct compression technique. The tablets were evaluated for hardness, friability, weight variation, wetting time, disintegration time, and uniformity of content. Optimized formulation was evaluated by in vitro dissolution test, drug-excipient compatibility, and accelerated stability study. It was concluded that fast disintegrating tablets of salbutamol sulphate were formulated successfully with desired characteristics which disintegrated rapidly; provided rapid onset of action; and enhanced the patient convenience and compliance. PMID:23956881

Sharma, Deepak

2013-01-01

25

Development of orally disintegrating tablets of Perphenazine/hydroxypropyl-?-cyclodextrin inclusion complex.  

PubMed

The aim of the present work was to prepare perphenazine (PPZ) orally disintegrating tablets (ODTs) based on the use of hydroxypropyl-?-cyclodextrin (HP-?-CD) forming inclusion complex with PPZ to improve the solubility and dissolution of this practically insoluble drug. Phase solubility studies were performed to evaluate the complexation of PPZ with HP-?-CD in three aqueous systems. The inclusion complex prepared by evaporation method was characterized by different physicochemical techniques, including the dissolution studies. The prepared complex was incorporated into ODTs containing different fillers and disintegrants. The ODTs prepared by direct compression were evaluated for drug content, hardness, porosity, friability, in vitro disintegration time (DT), wetting time (WT) and dissolution profiles. The solubility and dissolution rate were substantially improved compared with that of PPZ. Differential scanning calorimetry (DSC), X-ray powder diffraction (XRD) and Fourier-transform infrared spectroscopy (FTIR) analyses suggested that PPZ could form true inclusion complex with HP-?-CD. The optimized formulation F6 exhibited short DT (15.5 ± 1.9 s) and WT (34.2 ± 2.3 s), sufficient hardness (30.4 ± 1.6 N/mm) and rapid drug dissolution. The developed tablet formulation could be a promising drug delivery system with improvements in PPZ bioavailability and patient compliance. PMID:22759202

Wang, Ling; Zeng, Fan; Zong, Li

2013-01-01

26

Oral Disintegration Tablets of Stavudine for HIV Management: A New Technological Approach.  

PubMed

Stavudine oral disintegration tablets were formulated to minimize the bitter taste and to reduce the first-pass hepatic metabolism. The various precompression parameters like the angle of repose, bulk density, compressibility index and Hausner's ratio were determined for the powder blend. In this study, 14 formulations of stavudine oral disintegration tablet were prepared by direct compression method. The tablets were evaluated for weight variation, percentage friability, disintegration time, hardness, wetting time and water absorption ratio. The in vitro dissolution study results of the batch S1 (stavudine+crospovidone+sodium starch glycollate) are encouraging as highest dissolution rate (99.2% in 100 min) and lowest time of disintegration (56 s) was achieved. The in vivo drug release studies were carried out in rabbits and the relative bioavailability of formulation S1 was found to be 2.83 times greater than that of conventional tablets. PMID:23798782

Sankar, V; Ramakrishna, B; Devi, P Shalini; Karthik, S

2012-11-01

27

Fast disintegrating crystalline solid dispersions of simvastatin for incorporation into orodispersible tablets  

PubMed Central

Aim: Spray dried solid dispersion (SDP) of crystalline simvastatin (SIM) in a fast disintegrating matrix of superdisintegrants was studied as a method to enhance SIM dispersibility, rheology, compactibility and compressibility for incorporation into orodispersible tablets (ODTs). Materials and Methods: The superdisintegrants investigated were crospovidone (CP), sodium starch glycollate (SSG) and calcium silicate (CS) were spray dried with simvastatin to form SDPs. Results: The SDPs were characterized and the median particle size of SDPs was similar or greater than the SIM, contributing to good rheology of SDPs, while the low bulk density of SDPs indicated a high compactibility. Interestingly electron micrographs for SDPs showed a CP or CS carrier coating of the SIM crystals, contributing to its rheology. Thermal analysis and X-ray diffraction confirmed that SIM was crystalline in the SDPs and no interaction between SIM and any of the carrier(s) was shown by Fourier transform-infra red. Drug content analysis showed a SIM content of 90-95% in SDPs containing CP or CS, while a higher SIM content of 143% was found in SDP containing SSG. When formulated as ODTs, blend containing SIM SDPs in CP showed ease of tableting, regardless of the turret speed. In comparison, tablet blend consisting of a physical mix (PM) of SIM and CP could only be tableted at the lower turret speed of 7 rpm. ODTs formulated using SIM SDPs in CP showed a higher extent of dissolution, compared to the ODTs containing corresponding PM or the commercially available SIM Zocor® tablets (ANOVA, P < 0.05). Conclusion: SDP using disintegrants as carriers may offer an alternative formulation approach for ODTs of poorly soluble drugs. PMID:25006549

Pabari, Ritesh M; Jamil, Asha; Kelly, John G; Ramtoola, Zebunnissa

2014-01-01

28

Formulation and evaluation of diclofenac potassium fast-disintegrating tablets and their clinical application in migraine patients.  

PubMed

The aim of this study was to prepare fast-disintegrating tablets (FDTs) of diclofenac potassium with sufficient integrity as well as a pleasant taste, using two different fillers and binders: Tablettose 70(®) and Di-Pac(®). Tablets were made with direct compression method. Tablet properties such as porosity, hardness, and disintegration time were determined. Diclofenac potassium determinations were carried out using a validated spectrophotometric method for the analysis of drug. Furthermore, in vivo experiments were carried out to compare the analgesic effect and the time to relieve migraine headache between the commercial tablets and FDTs of diclofenac potassium against placebo. Results showed that FDTs of diclofenac potassium with durable structure and desirable taste can be prepared using both fillers and binders but tablets prepared with Di-Pac had a better taste so the tablet formulation containing Di-Pac was chosen for in vivo experiments. Placebo controlled in vivo trial demonstrated that 50 mg diclofenac potassium, administered as a single dose of FDTs or commercial tablets, was effective in relieving the pain and both of them were superior to placebo. PMID:20704458

Comoglu, Tansel; Dogan, Aysegul; Comoglu, Selcuk; Basci, Nursabah

2011-03-01

29

Preparation and evaluation of taste-masked donepezil hydrochloride orally disintegrating tablets.  

PubMed

The purpose of this research was to prepare and evaluate a non-bitter donepezil hydrochloride (DH) orally disintegrating tablet (ODT) for enhanced patient compliance. Taste masking was done by preparing microspheres with different ratios of drug and Eudragit EPO using spray drying method. The entrapment of the drug into microspheres was confirmed by scanning electron microscope (SEM) and X-ray powder diffraction. It was found that microspheres with a drug-polymer ratio of 1 : 2 could mask the taste obviously by inhibiting the release of DH in simulated salivary fluid. Microspheres-loaded tablets containing Polyplasdone NF and Low substituted Hydroxypropyl Cellulose (L-HPC) both at a 10% level showed rapid disintegration, in vitro (15.5 s) and in vivo (19.8 s), which were faster than that of marketed tablets (36.7, 41.3 s, respectively). Results from taste evaluation in human volunteers revealed that the ODTs with taste-masked microspheres had significantly enhanced palatability. Dissolution in vitro and pharmacokinetics in rats were evaluated for the tested ODTs compared to the donepezil hydrochloride commercial product (ARICEPT). Both tablets showed comparable dissolution patterns in vitro and similar area under curve from 0 to 24 h (AUC(0-24)), C(max) and T(max) of DH in vivo to each other, suggesting that the tested ODTs might give the similar drug efficacy in rats compared to that of ARICEPT. Thus, it was concluded that DH ODTs with masked taste were obtained by Eudragit EPO-based microspheres, drug loaded microspheres neither decreased the bioavailability nor delayed the release of DH. PMID:20686233

Yan, Yi-Dong; Woo, Jong Soo; Kang, Joon Heok; Yong, Chul Soon; Choi, Han-Gon

2010-01-01

30

Development and evaluation of orally disintegrating tablets (ODTs) containing Ibuprofen granules prepared by hot melt extrusion  

Microsoft Academic Search

In the current study Ibuprofen was embedded in a methacrylate copolymer (Eudragit® EPO) matrix to produce solid dispersions by hot-melt extrusion (HME) processing. The obtained granules were incorporated in orally disintegrating tablets (ODTs). The tablets were developed by varying the ratio of superdisintegrants such as sodium croscarmellose and crosslinked polyvinylpyrrolidone grades while a direct compression process was used to compress

Andreas Gryczke; Silke Schminke; Mohammed Maniruzzaman; Julien Beck; Dennis Douroumis

2011-01-01

31

Formulation and evaluation of clozapine orally disintegrating tablets prepared by direct compression.  

PubMed

In this study, clozapine orally disintegrating tablets (ODTs) were prepared by direct compression method. Disintegration time, resistance to crushing of tablets, porosity, friability, dissolution tests were performed and dissolution profiles of ODTs were investigated. Morphological and interaction studies were also performed. Friability values were found to be less than 1%. All tablet formulations disintegrated within 1 min and fulfilled the 3 min disintegration time required for ODTs given in the European Pharmacopoeia. More than 85% of the labeled amount of clozapine was dissolved in 15 min from the ODTs. No interaction or changes were found between active substance and excipients. As a result of the studies, ODT formulations developed in this study can be suggested as promising formulations, which assist development and manufacturing a generic product of clozapine. PMID:23469682

Olmez, S S; Vural, I; Sahin, S; Ertugrul, A; Capan, Y

2013-02-01

32

Influence of disintegrants in different substrate physical form on dimensional recovery of multi-component tablet.  

PubMed

This study investigated the influence of different disintegrants, present in different substrate physical forms, on dimensional recovery of multi-component tablets prepared at different compression pressures. Formulations containing model drug, metformin, (10%, w/w), different disintegrants (10%, w/w), and lactose (80%, w/w) were compressed directly or after granulation using polyvinyl pyrrolidone (1%, w/w) as binder, into tablets (350mg, 10mm diameter) at 150, 200, and 250N/mm(2) compression pressures. Tablets were characterized for immediate dimensional recovery (IR) after ejection from the die, latent dimensional recovery (LR) over 24h, tensile strength, and disintegration. The IR was predominantly contributed by crystalline components whereas LR was brought about by polymeric materials. With increased compression pressure, higher degree of plastic deformation of the polymeric disintegrants resulted in tablet with lower LR and higher tensile strength. Presence of polyvinyl pyrrolidone in the granules contributed considerably to plastic deformation, and the tablets produced had lower LR, higher tensile strength, and longer disintegration time. This study indicated that use of granules as the feed substrate physical form and a prudent selection of components may enable the coating of resultant tablets immediately after compression without the risk of coat damage due to LR. PMID:25218488

Sarkar, Srimanta; Ooi, Shing Ming; Liew, Celine Valeria; Tan, Bing Xun; Heng, Paul Wan Sia

2014-11-20

33

Influence of dissolution media pH and USP1 basket speed on erosion and disintegration characteristics of immediate release metformin hydrochloride tablets.  

PubMed

Abstract Purpose: To investigate the influence of the pH of the dissolution medium on immediate release 850?mg metformin hydrochloride tablets. Methods: A traditional wet granulation method was used to manufacture metformin hydrochloride tablets with or without a disintegrant. Tablet dissolution was conducted using the USP apparatus I at 100?rpm. Results: In spite of its pH-independent high solubility, metformin hydrochloride tablets dissolved significantly slower in 0.1?N HCl (pH 1.2) and 50?mM pH 4.5 acetate buffer compared with 50?mM pH 6.8 phosphate buffer, the dissolution medium in the USP. Metformin hydrochloride API compressed into a round 1200?mg disk showed a similar trend. When basket rotation speed was increased from 100 to 250?rpm, the dissolution of metformin hydrochloride tablets was similar in all three media. Incorporation of 2% w/w crospovidone in the tablet formulation improved the dissolution although the pH-dependent trend was still evident, but incorporation of 2% w/w croscarmellose sodium resulted in rapid pH-independent tablet dissolution. Conclusion: In absence of a disintegrant in the tablet formulation, the dissolution was governed by the erosion-diffusion process. Even for a highly soluble drug, a super-disintegrant was needed in the formulation to overcome the diffusion layer limitation and change the dissolution mechanism from erosion-diffusion to disintegration. PMID:24621340

Desai, Divyakant; Wong, Benjamin; Huang, Yande; Tang, Dan; Hemenway, Jeffrey; Paruchuri, Srinivasa; Guo, Hang; Hsieh, Daniel; Timmins, Peter

2014-03-12

34

Impact of chitosan as a disintegrant on the bioavailability of furosemide tablets: in vitro evaluation and in vivo simulation of novel formulations.  

PubMed

To determine the effect of chitosan, starch powder, polyvinylpyrrolidone (PVP), Avicel PH 101 powder, Avicel PH 102 granules as a function of different concentrations on the solubility, disintegration and hence dissolution of furosemide from immediate release tablet dosage forms. The tablets were prepared by the wet granulation method and evaluated for hardness, friability, disintegration and in vitro dissolution. Chitosan 7% w/w showed the fastest disintegration of furosemide tablets among the other disintegrants studied. This was attributed to its highest swelling properties and velocity constant of water uptake. The step of adding chitosan during tablet preparation had a great effect on the physical properties and dissolution profiles of the prepared tablets with external addition of chitosan showed best results compared to best results comparing to internal-external or internal addition. The most appropriate force of compression was 4ton/cm(2). The selected formula F15 containing 7% w/w chitosan was successful and showed a high significant (p<0.001) enhancement in disintegration and dissolution behaviors of furosemide tablets in comparison with the commercially available Furosemide ® tablets. These results were supported by the simulated data where F15 formula showed the highest plasma concentration C-max 1.89mcg/mL after 0.5 hr compared to C-max 1.05mcg/mL after 1hr for the reference. The present study demonstrated that chitosan is a very good candidate to be used as a tablet disintegrant and was able to enhance the dissolution of poorly absorbable drugs. PMID:23009999

Rasool, Bazigha Kadhim Abdul; Fahmy, Sahar Abdelsattar; Galeel, Omar Waleed Abdul

2012-10-01

35

Fast and pH-dependent release of domperidone from orally disintegrating tablets.  

PubMed

There has been growing interest in orally disintegrating tablets (ODTs) during the last decade due to their better patient acceptance and compliance. Further, drug dissolution and absorption may be significantly improved. This work describes the preparation of fast and pH-dependent release ODTs for domperidone by direct compression using crospovidone as superdisintegrant. Solid dispersions of domperidone and Eudragit L100-55, at different weight ratios, were prepared and characterized by DSC, TGA, X-ray diffraction, and FTIR, which indicated the presence of drug-polymer interaction. Disintegration time, friability, and hardness of ODTs were evaluated. In vitro drug release in 0.1N HCl and in phosphate buffer (pH 5.8 and 6.8) was investigated. All domperidone ODTs had fast disintegration times (6 KP) and acceptable friability (<1%). Drug release from fast release ODTs was highly improved; reaching 97% after 10 min in 0.1N HCl, compared to the dissolution of the free drug. Drug release from solid dispersions was pH dependent; showing higher release rates at pH 6.8 than at lower pH values. The controlled-release ODT resulted in 47% drug release in 0.1N HCl, with the rest of drug released at pH 6.8. Domperidone ODTs were considered suitable for ODT formulation. PMID:22304659

Assaf, Shereen M; Qandil, Amjad M; Al-Ani, Enas A

2013-01-01

36

Effects of plantain and corn starches on the mechanical and disintegration properties of paracetamol tablets.  

PubMed

The effects of plantain starch obtained from the unripe fruit of the plant Musa paradisiaca L. (Musaceae) on the mechanical and disintegration properties of paracetamol tablets have been investigated in comparison with the effects of corn starch BP using a 2(3) factorial experimental design. The individual and combined effects of nature of starch binder (N), concentration of starch binder (C), and the relative density of tablet (RD) on the tensile strength (TS), brittle fracture index (BFI), and disintegration time (DT) of the tablets were investigated. The ranking of the individual effects on TS was RD > C > N, on BFI was C > RD > N and on DT was N > C > RD. The ranking for the interaction effects on TS and DT was N-C > N-RD > C-RD, while that on BFI was N-C > C-RD > N-RD. Changing nature of starch from a "low" (plantain starch) to a "high" (corn starch) level, increasing the concentration of starch binding agent from 2.5% to 10.0% wt/wt, and increasing relative density of the tablet from 0.80 to 0.90, led to increase in the values of TS and DT, but a decrease in BFI. Thus, tablets containing plantain starch had lower tensile strength and disintegration time values than those containing corn starch, but showed better ability to reduce the lamination and capping tendency in paracetamol tablet formulation. The interaction between N and C was significantly (P < .001) higher than those between N and RD and between C and RD. There is therefore the need to carefully choose the nature (N) and concentration (C) of starch used as binding agent in tablet formulations to obtain tablets of desired bond strength and disintegration properties. Furthermore, plantain starch could be useful as an alternative binding agent to cornstarch, especially where faster disintegration is required and the problems of lamination and capping are of particular concern. PMID:16354005

Akin-Ajani, Olufunke D; Itiola, Oludele A; Odeku, Oluwatoyin A

2005-01-01

37

Magnetic images of the disintegration process of tablets in the human stomach by ac biosusceptometry  

NASA Astrophysics Data System (ADS)

Oral administration of solid dosage forms is usually preferred in drug therapy. Conventional imaging methods are essential tools to investigate the in vivo performance of these formulations. The non-invasive technique of ac biosusceptometry has been introduced as an alternative in studies focusing on gastrointestinal motility and, more recently, to evaluate the behaviour of magnetic tablets in vivo. The aim of this work was to employ a multisensor ac biosusceptometer system to obtain magnetic images of disintegration of tablets in vitro and in the human stomach. The results showed that the transition between the magnetic marker and the magnetic tracer characterized the onset of disintegration (t50) and occurred in a short time interval (1.1 ± 0.4 min). The multisensor ac biosusceptometer was reliable to monitor and analyse the in vivo performance of magnetic tablets showing accuracy to quantify disintegration through the magnetic images and to characterize the profile of this process.

Corá, L. A.; Andreis, U.; Romeiro, F. G.; Américo, M. F.; Oliveira, R. B.; Baffa, O.; Miranda, J. R. A.

2005-12-01

38

Response Surface Methodology to Optimize Novel Fast Disintegrating Tablets Using ? Cyclodextrin as Diluent  

Microsoft Academic Search

The objective of this work was to apply response surface approach to investigate main and interaction effects of formulation\\u000a parameters in optimizing novel fast disintegrating tablet formulation using ? cyclodextrin as a diluent. The variables studied\\u000a were diluent (? cyclodextrin, X\\u000a 1), superdisintegrant (Croscarmellose sodium, X\\u000a 2), and direct compression aid (Spray dried lactose, X\\u000a 3). Tablets were prepared by

Sameer G. Late; Ajay K. Banga

2010-01-01

39

Direct compression of cushion-layered ethyl cellulose-coated extended release pellets into rapidly disintegrating tablets without changes in the release profile.  

PubMed

The aim of this study was to develop and optimize a segregation-free ethyl cellulose-coated extended release multiparticulate formulation to be compressed into tablets without affecting the drug release. Standard tableting excipients (e.g., microcrystalline cellulose, lactose or sorbitol) were layered onto ethyl cellulose-coated propranolol hydrochloride pellets to form a cushion layer in order to eliminate segregation problems normally resulting from particle size difference between coated pellets and excipient powders and second to protect the integrity of the brittle ethyl cellulose coating during compression. The disintegration behavior of the tablets depended strongly on the composition of the cushion layer. Rapid tablet disintegration was obtained with microcrystalline cellulose and the disintegrant sodium croscarmellose. However, the drug release from these cushion-layered pellets still increased upon compression. Incorporation of a glidant into the cushion layer or between the cushion layer and the ethyl cellulose coating reduced the compression effect on drug release markedly. Glidant-containing formulations showed a delayed deformation and damage of the ethyl cellulose-coated pellet upon mechanical stress. In summary, cushion layer based on microcrystalline cellulose facilitated segregation-free compression of a highly compression-sensitive extended release ethyl cellulose-coated pellets into fast-disintegrating and hard tablets without compromising the release properties of the multiparticulates. Directly compressible cushion-layered pellets protected the pellet coating significantly better from damages during tabletting when compared to the conventional compression of blends of coated pellets and excipient powders. PMID:23892153

Hosseini, Armin; Körber, Martin; Bodmeier, Roland

2013-12-01

40

Taste Masking of Lornoxicam by polymer carrier system and formulation of oral disintegrating tablets  

Microsoft Academic Search

Lornoxicam is a non steroidal anti-inflammatory drug with analgesic properties and belongs to the class oxicams. It is extremely bitter in taste. The purpose of this research was to develop a bitterless oral disintegrating tablet of Lornoxicam. Taste masking was done by complexing Lornoxicam with aminoalkyl methacrylate copolymer (Eudragit EPO) in different ratios. In vitro release profile obtained at pH

Rajesh S. Jadon; Swadesh Nayak; Sabita Amlan; Vikas Deep Vaidya; Prashant Khemariya; Sandip Sumbhate

2009-01-01

41

Selection of generic preparations of famotidine orally disintegrating tablets for use in unit-dose packages.  

PubMed

Changes in the hardness, dissolution, and the disintegration time of brand name and generic preparations (6 preparations) of famotidine orally disintegrating tablets were investigated. Tablets had been stored in a thermo-hygrostat-controlled environment set to simulate the home conditions of patients up to 8 weeks after unit-dose packaging. Among the tablets in unit-dose packaging prepared immediately after blister packs (BP) were opened, one generic had decreased hardness to less than 2.0 kg after 1 week, 55.1% of its initial hardness value, and a shorter disintegration time of about 1/5 of its initial disintegration time. Generics met the standard for dissolution 8 weeks after unit-dose packaging. The decrease in hardness after unit-dose packaging is presumed to be associated with additives, and particularly the types and amounts of binding agents, but evidence of this association was lacking. The hardness noted in drug interview forms (IFs) and the state of sales of bulk tablet packages must be determined to facilitate the selection of generics that remain hard even after unit-dose packaging. PMID:23229147

Yamazaki, N; Iizuka, R; Miyazawa, S; Wada, Y; Shimokawa, K; Ishii, F

2012-10-01

42

Impact of active ingredients on the swelling properties of orally disintegrating tablets prepared by microwave treatment.  

PubMed

The impact of different active pharmaceutical ingredients (APIs) loading on the properties of orally disintegrating tablets (ODTs) prepared according to our previously reported microwave (MW) treatment process was evaluated using famotidine (FAM), acetaminophen (AAP), and ibuprofen (IBU). None of the APIs interrupted the tablet swelling during the MW treatment and the tablet hardness were improved by more than 20 N. MW treatment, however, led to a significant increase in the disintegration time of the ODTs containing IBU, but it had no impact on that of the ODTs containing FAM or AAP. This increased disintegration time of the ODTs containing IBU was attributed to the relatively low melting point of IBU (Tm=76 °C), with the IBU particles melting during the MW treatment to form agglomerates, which interrupted the penetration of water into the tablets and delayed their disintegration. The effects of the MW treatment on the chemical stability and dissolution properties of ODTs were also evaluated. The results revealed that MW treatment did not promote the degradations of FAM and AAP or delay their release from the ODTs, while dissolution of the ODTs containing IBU delayed by MW treatment. Based on these results, the MW method would be applicable to the preparation of ODTs containing APIs with melting points higher than 110 °C. PMID:24709215

Sano, Syusuke; Iwao, Yasunori; Kimura, Susumu; Noguchi, Shuji; Itai, Shigeru

2014-07-01

43

Development and optimization of dextromethorphan hydrobromide oral disintegrating tablets: effect of formulation and process variables.  

PubMed

Orally disintegrating tablets (ODTs), which disintegrate rapidly (<1?min) in the mouth and do not require water for administration, have become a very popular dosage form. The study aims to develop a simple and inexpensive method of manufacturing ODTs of a sparingly water-soluble drug, Dextromethorphan hydrobromide. Two factors, three levels (3(2)) full factorial design was used to optimize the diluent, microcrystalline cellulose (X(1)) and superdisintegrant, croscarmellose sodium (X(2)) concentrations. Disintegration time, hardness and T(50) values for all the formulations varied from 12.5 to 152.6 s, 3.58 to 4.92 kp and 0.8 to 2.8?min, respectively. The results indicated that the selected variables have a strong influence on disintegration time, hardness and T(50) of the ODTs. The manufactured ODTs formula composed of 30% microcrystalline cellulose in combination with 3% croscarmellose sodium was chosen as optimized formula, as it showed the lowest disintegration time (12.5?±?1.22 s), low T(50) (0.8?min.) and hard tablets (4.92?±?0.28 kp) amongst other tested ODTs formulations. Hardness of DM ODTs was not affected by changing the type of superdisintegrant and lubricant. The disintegration time was significantly (p < 0.05) increased by using sodium starch glycolate instead of croscarmellose sodium. PMID:22881389

Mostafa, Haitham Fady; Ibrahim, Mohamed Abbas; Sakr, Adel

2013-01-01

44

Preparation and evaluation of taste-masked dextromethorphan oral disintegrating tablet.  

PubMed

This study was aimed at preparing and evaluating oral disintegrating tablets (ODTs) using a strongly cationic resin, Amberlite(®) IRP-69, to mask the bitter taste of a delivered drug, i..e. dextromethorphan hydrobromide. The drug was loaded into the resin (referred to as resinate) or physically mixed with the resin (referred to as physical mixture), and was then incorporated into ODTs by direct compression. A variety of formulae was developed to acquire the optimal formulations of taste-masked ODTs that had acceptable hardness and mouth feel (grittiness). The optimized ODTs were further evaluated for thickness, diameter, weight, friability, disintegration time, wetting time, wetting rate, drug content, drug release and degree of bitter taste, respectively. The thickness, diameter, weight and friability of the tablet with resinate were slightly higher than those with physical mixture. The tablet with resinate had a longer disintegration time, corresponding with its slower wetting time and rate. Both tablets with resinate and physical mixture provided a sustained pattern of drug release. However, only tablets with resinate successfully masked the bitter taste of the drug. In conclusion, the combination of drug and ion exchange resin as resinate could increase the palatability and acceptability of ODTs containing bitter drugs. PMID:21142821

Samprasit, Wipada; Opanasopit, Praneet; Akkaramongkolporn, Prasert; Ngawhirunpat, Tanasait; Wongsermsin, Kaewnapa; Panomsuk, Suwannee

2012-01-01

45

Development of Corn Starch-Neusilin UFL2 Conjugate as Tablet Superdisintegrant: Formulation and Evaluation of Fast Disintegrating Tablets  

PubMed Central

In the present study, corn Starch-Neusilin UFL2 conjugates were prepared by physical, chemical, and microwave methods with the aim of using the conjugates as tablet superdisintegrant. Various powder tests, namely, angle of repose, bulk density, tapped density, Hausner's ratio, Carr's index, swelling index, and powder porosity were conducted on the samples. The conjugates were characterized by ATR-FTIR, XRD, DSC, and SEM techniques. Heckel and Kawakita models were applied to carry out compression studies for the prepared conjugates. Fast disintegrating tablets of domperidone were prepared using corn starch and corn Starch-Neusilin UFL2 conjugates as tablet superdisintegrants in different concentrations. Conjugates were found to possess good powder flow and tabletting properties. Heckel analysis indicated that the conjugates prepared by microwave method showed the slowest onset of plastic deformation while Kawakita analysis indicated that the conjugates prepared by microwave method exhibited the highest amount of total plastic deformation. The study revealed that the corn Starch-Neusilin UFL2 conjugates possess improved powder flow properties and could be a promising superdisintegrant for preparing fast disintegrating tablet. Also, the results sugessted that the microwave method was found to be most effective for the preparation of corn Starch-Neusilin UFL2 conjugates. PMID:25328710

Juneja, Prateek; Kaur, Birender; Odeku, Oluwatoyin A.; Singh, Inderbir

2014-01-01

46

Meloxicam taste-masked oral disintegrating tablet with dissolution enhanced by ion exchange resins and cyclodextrin.  

PubMed

The purpose of this study was to develop taste-masked oral disintegrating tablets (ODTs) using the combination of ion exchange resin and cyclodextrin, to mask the bitter taste and enhance drug dissolution. Meloxicam (MX) was selected as a model drug with poor water solubility and a bitter taste. Formulations containing various forms of MX (free drug, MX-loaded resin or resinate, complexes of MX and 2-hydroxypropyl-?-cyclodextrin (HP?CD) or MX/HP?CD complexes, and a mixture of resinate and MX/HP?CD complexes) were made and tablets were prepared by direct compression. The ODTs were evaluated for weight variation, thickness, diameter, hardness, friability, disintegration time, wetting time, MX content, MX release, degree of bitter taste, and stability. The results showed that thickness, diameter, weight, and friability did not differ significantly for all of these formulations. The tablet hardness was approximately 3 kg/in.(2), and the friability was less than 1%. Tablets formulated with resinate and the mixture of resinate and MX/HP?CD complexes disintegrated rapidly within 60 s, which is the acceptable limit for ODTs. These results corresponded to the in vivo disintegration and wetting times. However, only tablets containing the mixture of resinate and MX/HP?CD complexes provided complete MX dissolution and successfully masked the bitter taste of MX. In addition, this tablet was stable at least 6 months. The results from this study suggest that the appropriate combination of ion exchange resin and cyclodextrin could be used in ODTs to mask the bitter taste of drug and enhance the dissolution of drugs that are weakly soluble in water. PMID:23835739

Samprasit, Wipada; Akkaramongkolporn, Prasert; Ngawhirunpat, Tanasait; Rojanarata, Theerasak; Opanasopit, Praneet

2013-09-01

47

Orally disintegrating tablet of novel salt of antiepileptic drug: formulation strategy and evaluation.  

PubMed

The aim of present research was to design and evaluate orally disintegrating tablet (ODT) of novel lamotrigine-cyclamate salt. Box-Behnken response surface methodology was selected to design the optimized formulation. The independent factors selected were tablet hardness (X1), disintegrant (X2) and lubricant (X3) levels, and responses chosen were disintegration time (DT, Y1), friability (Y2), T50 (Y3), and T90 (Y4). The tablets were also characterized for drug uniformity by near infrared chemical imaging (NIR-CI) and taste masking evaluation by electronic tongue. All the selected independent variables were statistically (p<0.05) effect the Y1 while Y2, Y3, and Y4 affected only by X2. The optimized ODT was found to meet the regulatory requirement of DT and friability specification. The NIR-CI images indicated uniform distribution of active and inactive ingredients within the tablets. The electronic tongue results were analyzed by principle component analysis (PCA). It indicated that novel salt of lamotrigine and its ODT formulation have a taste similar to cyclamic acid which is indicated by close proximity on PCA score plot, lower Euclidean distance, and high discrimination index values. Furthermore, these parameters were very close to ODT placebo formulation. On the other hand, lamotrigine, its ODT, and placebo formulation were far from each other. In summary, lamotrigine salt provides another avenue for pediatric friendly formulation for children and will enhance patience compliance. PMID:23800704

Rahman, Ziyaur; Siddiqui, Akhtar; Khan, Mansoor A

2013-11-01

48

QbD approach of rapid disintegrating tablets incorporating indomethacin solid dispersion.  

PubMed

The development of rapid disintegrating tablets (RDT) requires the use of highly soluble components to support the intended use of these products. In an attempt to prepare RDT of indomethacin, its solid dispersion with polyvinyl pyrrolidone K25 (PVP) was incorporated in a fast disintegrating matrix. Drug polymer interactions were investigated using X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR). Indomethacin 1:1 solid dispersion with PVP was used to prepare its RDT. Two factors at 3 levels full factorial design were employed as a statistical approach to optimize the amount of superdisintegrant (Ac-di-sol) and hardness value regarding the desired disintegration and release characteristics. Drug to carrier ratio was the controlling factor for dissolution improvement. XRD and FTIR data revealed a remarkable interaction between the drug and the carrier that might be responsible for the dissolution enhancement. Multiple regression analysis revealed a significant effect of the polynomial terms for obtaining rapid disintegrating tablets. It was inferred that the hardness value is the most important factor controlling the disintegration time and the release characteristics. In conclusion, this study demonstrated that quality by design (QbD) is a potential paradigm for understanding the quality and optimizing the formulation of RDT containing indomethacin solid dispersion. PMID:20163325

Sammour, Omaima A; Hammad, Mohammed A; Zidan, Ahmed S; Mowafy, Ayman G

2011-06-01

49

Formulation design for orally disintegrating tablets containing enteric-coated particles.  

PubMed

The purpose of this study was to investigate the applicability of our newly developed technology (RACTAB® technology) for preparing orally disintegrating tablets (ODTs) containing enteric-coated particles. Tamsulosin hydrochloride (TAM) was used as a model drug contained in the enteric-coated particles. Enteric-coated particles containing TAM (ECP-T) were prepared by spray coating a mixture of TAM with controlled-release materials. ECP-T was then mixed with rapidly disintegrating granules (RDGs), which were prepared using the suspension spray-coating method, and was tableted to form ODTs (ODTRAC). ODTRAC was evaluated for its hardness, thickness, internal structure (X-ray-CT scanning), functional properties (controlled-release profile), and in vivo disintegration time. Since RDGs with micronized ethylcellulose (MEC) increased tablet hardness by increasing the contact frequency between granules, ODTRAC containing ECP-T exhibited high hardness (>50?N) and low friability (<0.5%) with a relatively low compression force. After tableting, the structure of ECP-T in ODTRAC remained intact and no damage was observed on the surface. ECP-T recovered from ODTRAC showed the same dissolution profile of TAM in Japanese Pharmacopoeia (JP) 1st and JP 2nd media as that of intact ECP-T, which indicated that the tableting process did not affect the acid-resistibility of the particle. In addition, ODTRAC rapidly disintegrated in vivo (< 30?s), even at a high compression force (at 9 kN). These findings clearly suggest that RACTAB® technology is a useful approach to prepare ODTs containing enteric-coated particles. PMID:24789923

Okuda, Yutaka; Okamoto, Yasunobu; Irisawa, Yosuke; Okimoto, Kazuto; Osawa, Takashi; Yamashita, Shinji

2014-01-01

50

Development and Evaluation of Cetirizine HCl Taste-Masked Oral Disintegrating Tablets  

Microsoft Academic Search

The purpose of the current study was to mask the taste of cetirizine HCl and to incorporate the granules produced in oral\\u000a disintegrating tablets (ODT). The bitter, active substance was coated by fluidized bed coating using Eudragit® RL30-D at levels\\u000a between 15% and 40% w\\/w. The ODTs were developed by varying the ratio of superdisintegrants such as sodium croscarmellose, crospovidone

Dionysios Dennis Douroumis; Andreas Gryczke; Silke Schminke

2011-01-01

51

Evaluation of Rapidly Disintegrating Vaginal Tablets of Tenofovir, Emtricitabine and Their Combination for HIV-1 Prevention  

PubMed Central

Vaginal tablets are being developed as an alternative to gels as an inexpensive, discreet dosage form for the administration of microbicides. This work describes the pharmacokinetic (PK) evaluation of rapidly disintegrating vaginal tablets containing tenofovir (TFV, 10 mg), emtricitabine (FTC, 10 mg), and the combination of TFV and FTC (10 mg each) under in vitro and in vivo conditions, and in direct comparison to the clinical TFV 1% gel, a microbicide product in Phase III clinical testing. The PK of TFV and FTC from tablets were also evaluated in female rabbits following intravaginal administration. Direct comparison of a single dose of TFV tablets (intact or predissolved at 10 mg/mL) and TFV 1% gel showed no differences in the vaginal PK of TFV between groups; however systemic bioavailability of TFV was significantly higher from the gel. When rabbits were dosed either once or daily for seven days with intact tablets of TFV, FTC, or the combination of TFV/FTC, vaginal and systemic concentrations of TFV and FTC were unaffected by co-formulation. Moreover, plasma PK parameters were similar following a single dose or seven once-daily doses. Tissue concentrations of TFV and FTC in the cranial vagina 4 h after administration ranged between 104 and 105 ng/g. Concentrations of TFV-diphospate (TFV-DP, the active metabolite) were also high (over 103 ng/g or about 3000 to 6000 fmol/mg) in the cranial vagina 4 h after administration and similar to those measured following administration of TFV 1% gel. These data demonstrate that rapidly disintegrating vaginal tablets may be a suitable topical microbicide dosage form providing similar vaginal TFV PK to that of TFV 1% gel. The data also support co-administration of FTC with TFV in a single vaginal tablet to create a combination microbicide in a simple and inexpensive dosage form. PMID:25494201

Clark, Meredith R.; Peet, M. Melissa; Davis, Sarah; Doncel, Gustavo F.; Friend, David R.

2014-01-01

52

Evaluation of Rapidly Disintegrating Vaginal Tablets of Tenofovir, Emtricitabine and Their Combination for HIV-1 Prevention.  

PubMed

Vaginal tablets are being developed as an alternative to gels as an inexpensive, discreet dosage form for the administration of microbicides. This work describes the pharmacokinetic (PK) evaluation of rapidly disintegrating vaginal tablets containing tenofovir (TFV, 10 mg), emtricitabine (FTC, 10 mg), and the combination of TFV and FTC (10 mg each) under in vitro and in vivo conditions, and in direct comparison to the clinical TFV 1% gel, a microbicide product in Phase III clinical testing. The PK of TFV and FTC from tablets were also evaluated in female rabbits following intravaginal administration. Direct comparison of a single dose of TFV tablets (intact or predissolved at 10 mg/mL) and TFV 1% gel showed no differences in the vaginal PK of TFV between groups; however systemic bioavailability of TFV was significantly higher from the gel. When rabbits were dosed either once or daily for seven days with intact tablets of TFV, FTC, or the combination of TFV/FTC, vaginal and systemic concentrations of TFV and FTC were unaffected by co-formulation. Moreover, plasma PK parameters were similar following a single dose or seven once-daily doses. Tissue concentrations of TFV and FTC in the cranial vagina 4 h after administration ranged between 104 and 105 ng/g. Concentrations of TFV-diphospate (TFV-DP, the active metabolite) were also high (over 103 ng/g or about 3000 to 6000 fmol/mg) in the cranial vagina 4 h after administration and similar to those measured following administration of TFV 1% gel. These data demonstrate that rapidly disintegrating vaginal tablets may be a suitable topical microbicide dosage form providing similar vaginal TFV PK to that of TFV 1% gel. The data also support co-administration of FTC with TFV in a single vaginal tablet to create a combination microbicide in a simple and inexpensive dosage form. PMID:25494201

Clark, Meredith R; Peet, M Melissa; Davis, Sarah; Doncel, Gustavo F; Friend, David R

2014-01-01

53

Comparative evaluation of the binding properties of two species of Khaya gum polymer in a paracetamol tablet formulation.  

PubMed

A study was made of the comparative effects of polymers obtained from two species of khaya tree - Khaya senegalensis and Khaya grandifoliola - as binding agents in a paracetamol tablet formulation. The mechanical properties of the tablets were assessed using the tensile strength (T), brittle fracture index (BFI) and friability (F) of the tablets while the drug release properties of the tablets were assessed using disintegration and dissolution times. The tensile strength, disintegration and the dissolution times of tablets increased with the increase in binder concentration while F and BFI decreased. K. senegalensis gum produced tablets with stronger mechanical properties with less tendency to laminate, and longer disintegration and dissolution times than K. grandifoliola gum. The results suggest that the polymer gum from K. senegalensis will be more appropriate as a binding agent than the gum from K. grandifoliola when higher mechanical strength and slower release profiles of tablets are desired. PMID:18720239

Adenuga, Yedunni A; Odeku, Oluwatoyin A; Adegboye, Temidayo A; Itiola, Oludele A

2008-01-01

54

Freeze drying of orally disintegrating tablets containing taste masked naproxen sodium granules in blisters.  

PubMed

Abstract Orally disintegrating tablets (ODTs) were freeze dried in blisters using the Lyostar® II SMART™ Freeze Dryer Technology. ODT formulations either without non-water soluble particles (placebo) or containing large fractions (717?mg) of taste-masked naproxen sodium (NaS) granules were freeze dried. The process data revealed differences between ODTs with and without embedded granules in the pressure rise curves as well as in the shelf (inlet) temperature adjustments during freeze-drying. Pressure rise curves of the placebo ODTs from eight hours process time showed no distinct temperature-dominated part, and the last optimization step of the shelf temperature to achieve -24.4?°C might be prone to errors. The final shelf temperature of ODTs containing granules was -23.3?°C. The detection of primary drying endpoints using SMART™ Technology or comparative pressure measurements was reliable for both ODT formulations, whereas the application of thermocouples resulted in premature endpoint indication. Product resistance of ODTs containing granules was generally elevated in comparison to ODTs without granules, but increased only slightly over the course of the drying process. In summary, the developed freeze-drying cycle was found applicable for production of elegant ODTs with incorporated taste masked NaS granules. PMID:25220888

Stange, Ulrike; Führling, Christian; Gieseler, Henning

2014-09-15

55

In situ, real time observation of the disintegration of paracetamol tablets in aqueous solution by magnetic resonance imaging.  

PubMed

The disintegration behavior of paracetamol tablets was studied by magnetic resonance imaging (MRI) using the Snapshot FLASH method. The total time of the single experiment is 425 ms and allows the study of the disintegration process in real time. The study was carried out in vitro under acidic gastric pH conditions and may help to predict the behavior of paracetamol tablets in the stomach after oral administration. It was shown that in spite of identical conditions, the disintegration of the tablets under study was different. The distribution of protons of 4-(N-acetyl)aminophenol within the paracetamol tablet was shown to be homogeneous. The study was carried out in a non-destructive way by the SPI MRI method. PMID:11988395

Tritt-Goc, Jadwiga; Kowalczuk, Joanna

2002-05-01

56

Effect of mode of incorporation of disintegrants on the characteristics of fluid-bed wet-granulated tablets.  

PubMed

A full factorial experimental design was employed to investigate the effects of mode of disintegrant incorporation and concentration in wet-granulated paracetamol tablets manufactured by top-spray fluid-bed. Disintegrants (croscarmellose sodium, sodium starch glycolate, or crospovidone) were incorporated either intragranularly, extragranularly, or distributed equally between the two phases. The results were analysed by a general quadratic equation and response surfaces generated. On examining the results for dissolution studies the combined mode resulted in significantly faster dissolution rates than did the extragranular mode which, in turn, was superior to the intragranular mode of inclusion. These results were reflected in the disintegration studies where the combined mode exhibited the shortest disintegration times for all the disintegrants. Tablet crushing strength was not affected by the mode of incorporation of concentration of the disintegrants. Main as well as interaction effects between the types, mode of incorporation and percent disintegrant employed were significant (P < 0.05) for disintegration time and percent release at 15 min. Croscarmellose sodium exhibited the shortest while crospovidone displayed significantly (P < 0.05) longer disintegration times. Formulations containing crospovidone did not meet official compendial (USP XXII) requirements of 80% in 30 min. In general, croscarmellose sodium and sodium starch glycolate were found to be less sensitive to the mode of incorporation than crospovidone. PMID:7901364

Khattab, I; Menon, A; Sakr, A

1993-08-01

57

Evidence-Based Nanoscopic and Molecular Framework for Excipient Functionality in Compressed Orally Disintegrating Tablets  

PubMed Central

The work investigates the adhesive/cohesive molecular and physical interactions together with nanoscopic features of commonly used orally disintegrating tablet (ODT) excipients microcrystalline cellulose (MCC) and D-mannitol. This helps to elucidate the underlying physico-chemical and mechanical mechanisms responsible for powder densification and optimum product functionality. Atomic force microscopy (AFM) contact mode analysis was performed to measure nano-adhesion forces and surface energies between excipient-drug particles (6-10 different particles per each pair). Moreover, surface topography images (100 nm2–10 µm2) and roughness data were acquired from AFM tapping mode. AFM data were related to ODT macro/microscopic properties obtained from SEM, FTIR, XRD, thermal analysis using DSC and TGA, disintegration testing, Heckel and tabletability profiles. The study results showed a good association between the adhesive molecular and physical forces of paired particles and the resultant densification mechanisms responsible for mechanical strength of tablets. MCC micro roughness was 3 times that of D-mannitol which explains the high hardness of MCC ODTs due to mechanical interlocking. Hydrogen bonding between MCC particles could not be established from both AFM and FTIR solid state investigation. On the contrary, D-mannitol produced fragile ODTs due to fragmentation of surface crystallites during compression attained from its weak crystal structure. Furthermore, AFM analysis has shown the presence of extensive micro fibril structures inhabiting nano pores which further supports the use of MCC as a disintegrant. Overall, excipients (and model drugs) showed mechanistic behaviour on the nano/micro scale that could be related to the functionality of materials on the macro scale. PMID:25025427

Al-khattawi, Ali; Alyami, Hamad; Townsend, Bill; Ma, Xianghong; Mohammed, Afzal R.

2014-01-01

58

Evidence-based nanoscopic and molecular framework for excipient functionality in compressed orally disintegrating tablets.  

PubMed

The work investigates the adhesive/cohesive molecular and physical interactions together with nanoscopic features of commonly used orally disintegrating tablet (ODT) excipients microcrystalline cellulose (MCC) and D-mannitol. This helps to elucidate the underlying physico-chemical and mechanical mechanisms responsible for powder densification and optimum product functionality. Atomic force microscopy (AFM) contact mode analysis was performed to measure nano-adhesion forces and surface energies between excipient-drug particles (6-10 different particles per each pair). Moreover, surface topography images (100 nm2-10 µm2) and roughness data were acquired from AFM tapping mode. AFM data were related to ODT macro/microscopic properties obtained from SEM, FTIR, XRD, thermal analysis using DSC and TGA, disintegration testing, Heckel and tabletability profiles. The study results showed a good association between the adhesive molecular and physical forces of paired particles and the resultant densification mechanisms responsible for mechanical strength of tablets. MCC micro roughness was 3 times that of D-mannitol which explains the high hardness of MCC ODTs due to mechanical interlocking. Hydrogen bonding between MCC particles could not be established from both AFM and FTIR solid state investigation. On the contrary, D-mannitol produced fragile ODTs due to fragmentation of surface crystallites during compression attained from its weak crystal structure. Furthermore, AFM analysis has shown the presence of extensive micro fibril structures inhabiting nano pores which further supports the use of MCC as a disintegrant. Overall, excipients (and model drugs) showed mechanistic behaviour on the nano/micro scale that could be related to the functionality of materials on the macro scale. PMID:25025427

Al-Khattawi, Ali; Alyami, Hamad; Townsend, Bill; Ma, Xianghong; Mohammed, Afzal R

2014-01-01

59

Development of orally disintegrating tablets comprising controlled-release multiparticulate beads  

PubMed Central

Melperone is an atypical antipsychotic agent that has shown a wide spectrum of neuroleptic properties, particularly effective in the treatment of senile dementia and Parkinson’s-associated psychosis, and is marketed in Europe as an immediate-release (IR) tablet and syrup. An orally disintegrating tablet (ODT) dosage form would be advantageous for patients who experience difficulty in swallowing large tablets or capsules or those who experience dysphagia. Controlled-release (CR) capsule and ODT formulations containing melperone HCl were developed with target in vitro release profiles suitable for a once-daily dosing regimen. Both dosage forms allow for the convenient production of dose-proportional multiple strengths. Two ODT formulations exhibiting fast and medium release profiles and one medium release profile capsule formulation (each 50?mg) were tested in vivo using IR syrup as the reference. The two medium release formulations were shown to be bioequivalent to each other and are suitable for once-daily dosing. Based on the analytical and organoleptic test results, as well as the blend uniformity and in-process compression data at various compression forces using coated beads produced at one-tenth (1/10) commercial scale, both formulations in the form of CR capsules and CR ODTs have shown suitability for progression into further clinical development. PMID:22356215

2012-01-01

60

Preparation and evaluation of unpleasant taste-masked pioglitazone orally disintegrating tablets.  

PubMed

This study aimed to evaluate the taste and mouth feel of newly designed orally disintegrating tablets (ODTs) of pioglitazone, which is a typical type 2 diabetes medicine with an unpleasant taste, using a visual analog scale (VAS) analysis. The ODTs were subjected to either of these 2 taste-masking procedures: a physical masking procedure that included coating the inactive core granules with mixture of pioglitazone and Eudragit(®) E PO, followed by mixing the granules with aspartame and other excipients to form the tablet (physical masking ODT); or a gustatory masking procedure that involved blending pioglitazone with both sodium chloride and aspartame, followed by mixing the blend with other excipients to form the tablet (gustatory masking ODT). From the results of the VAS analysis, physical masking could suppress the bitterness but not the astringent; therefore, the overall palatability of the ODT was considered not improved. In contrast, gustatory masking significantly suppressed both the bitterness and astringent, and offered a slight sweetness; therefore, the overall palatability of the ODT was considered improved. In conclusion, VAS is a useful tool to evaluate the taste of ODTs and that gustatory masking can effectively mask the unpleasant taste of pioglitazone ODT. PMID:23419665

Nakano, Yoshinori; Maeda, Arisa; Uchida, Shinya; Namiki, Noriyuki

2013-03-25

61

Application of face centred central composite design to optimise compression force and tablet diameter for the formulation of mechanically strong and fast disintegrating orodispersible tablets.  

PubMed

A two factor, three level (3(2)) face centred, central composite design (CCD) was applied to investigate the main and interaction effects of tablet diameter and compression force (CF) on hardness, disintegration time (DT) and porosity of mannitol based orodispersible tablets (ODTs). Tablet diameters of 10, 13 and 15 mm, and CF of 10, 15 and 20 kN were studied. Results of multiple linear regression analysis show that both the tablet diameter and CF influence tablet characteristics. A negative value of regression coefficient for tablet diameter showed an inverse relationship with hardness and DT. A positive value of regression coefficient for CF indicated an increase in hardness and DT with increasing CF as a result of the decrease in tablet porosity. Interestingly, at the larger tablet diameter of 15 mm, while hardness increased and porosity decreased with an increase in CF, the DT was resistant to change. The optimised combination was a tablet of 15 mm diameter compressed at 15 kN showing a rapid DT of 37.7s and high hardness of 71.4N. Using these parameters, ODTs containing ibuprofen showed no significant change in DT (ANOVA; p>0.05) irrespective of the hydrophobicity of the ibuprofen. PMID:22465631

Pabari, Ritesh M; Ramtoola, Zebunnissa

2012-07-01

62

In vitro and in vivo correlation of disintegration and bitter taste masking using orally disintegrating tablet containing ion exchange resin-drug complex.  

PubMed

Although the taste-masking of bitter drug using ion exchange resin has been recognized, in vitro testing using an electronic tongue (e-Tongue) and in vivo bitterness test by human panel test was not fully understood. In case of orally disintegrating tablet (ODT) containing bitter medicine, in vitro and in vivo disintegration is also importance for dosage performance. Donepezil hydrochloride was chosen as a model drug due to its bitterness and requires rapid disintegration for the preparation of ODT. In this study, ion exchange resin drug complex (IRDC) at three different ratios (1:2, 1:1, 2:1) was prepared using a spray-drying method and then IRDC-loaded ODT containing superdisintegrants (crospovidone, croscarmellose sodium, and sodium starch glycolate) were prepared by the direct compression method. The physical properties and morphologies were then characterized by scanning electron microscopy (SEM), X-ray powder diffraction (PXRD) and electrophoretic laser scattering (ELS), respectively. The in vitro taste-masking efficiency was measured with an electronic tongue (e-Tongue). In vivo bitterness scale was also evaluated by human volunteers and then we defined new term, "bitterness index (BI)" to link in vitro e-Tongue. There was a good correlation of IRDC between in vitro e-Tongue values and in vivo BI. Furthermore, IRDC-loaded ODT showed good in vitro/in vivo correlation in the disintegration time. The optimal IRDC-loaded ODTs displayed similar drug release profiles to the reference tablet (Aricept(®) ODT) in release media of pH 1.2, pH 4.0, pH 6.8 and distilled water but had significantly better palatability in vivo taste-masking evaluation. The current IRDC-loaded ODT according to the in vitro and in vivo correlation of disintegration and bitter taste masking could provide platforms in ODT dosage formulations of donepezil hydrochloride for improved patient compliances. PMID:23933050

Kim, Jong-Il; Cho, Sang-Min; Cui, Jing-Hao; Cao, Qing-Ri; Oh, Euichaul; Lee, Beom-Jin

2013-10-15

63

Pharmacokinetic and bioequivalence comparison between orally disintegrating and conventional tablet formulations of flurbiprofen: A single-dose, randomized-sequence, open-label, two-period crossover study in healthy chinese male volunteers  

Microsoft Academic Search

Background: Flurbiprofen, an NSAID, is used for the treatment of inflammation and pain caused by rheumatoid arthritis and osteoarthritis as well as soft-tissue injuries. A new orally disintegrating tablet (ODT) of flurbiprofen has recently been developed; this study was conducted to provide support for this drug to obtain marketing authorization in China.Objective: The aim of the study was to compare

Yan-Mei Liu; Gang-Yi Liu; Yun Liu; Shui-Jun Li; Jing-Ying Jia; Meng-Qi Zhang; Chuan Lu; Yong-Mei Zhang; Xue-Ning Li; Chen Yu

2009-01-01

64

Formulation and evaluation of meloxicam oral disintegrating tablet with dissolution enhanced by combination of cyclodextrin and ion exchange resins.  

PubMed

Abstract Context: The bitter taste of drug is masked by the exchange of ionized drugs with counter ions of ion exchange resin, forming "resinate". Cyclodextrin reduces the unpleasant taste and enhances the drug solubility by encapsulating drug molecules into its central cavity. Objective: Oral disintegrating tablets (ODTs) using the combination of ion exchange resin and cyclodextrin was developed, to mask the bitter taste and enhance drug dissolution. Methods: Meloxicam (MX) was selected as a model drug. Formulations containing various forms of MX (free drug, MX-loaded resin or resinate, complexes of MX and 2-hydroxypropyl-?-cyclodextrin (HP?CD) or MX/HP?CD complexes, and a mixture of resinate and MX/HP?CD complexes) were made by direct compression. The ODTs were evaluated for weight variation, thickness, diameter, hardness, friability, disintegration time, wetting time, MX content, MX release, degree of bitter taste and stability. Results and discussion: The tablet hardness was ?3?kg/in(2), and the friability was <1%. Tablets formulated with resinate and the mixture of resinate and MX/HP?CD complexes disintegrated rapidly within 60?s, which is the acceptable limit for ODTs. These results were corresponded to the in vivo disintegration and wetting times. However, only tablets containing the mixture of resinate and MX/HP?CD complexes provided complete MX dissolution and successfully masked the bitter taste. In addition, this tablet was stable at least 6 months. Conclusions: The combination of ion exchange resin and cyclodextrin could be used in ODTs to mask the bitter taste and enhance the dissolution of drugs that are weakly soluble in water. PMID:24865111

Samprasit, Wipada; Akkaramongkolporn, Prasert; Ngawhirunpat, Tanasait; Rojanarata, Theerasak; Opanasopit, Praneet

2014-05-28

65

Taste-masked and affordable donepezil hydrochloride orally disintegrating tablet as promising solution for non-compliance in Alzheimer's disease patients.  

PubMed

Abstract Context: Manufacturing process and superdisintegrants used in orally disintegrating tablet (ODT) formulation are often time discussed. However, the effect of suitable filler for ODT formulation is not explored thoroughly. Objective: The aim of this study was to develop a novel taste masked and affordable donepezil hydrochloride ODT with fast disintegration time and stable to improve medication compliance of Alzheimer's disease patient. Methods and materials: The ODT was manufactured using simple wet-granulation method. Crospovidone XL-10 was used as superdisintegrant and optimization was done by comparing the effect of three grades of lactose monohydrate compound as filler: Starlac®, Flowlac® and Tablettose®. Results and discussion: Formulations containing higher amount of colloidal silicon dioxide showed increase in hardness, weight, disintegration time and wetting time after stability study. Formulation E which containing 50% of Starlac® was found with shortest in vitro disintegration time (21.7?±?1.67?s), in vivo disintegration time (24.0?±?1.05?s) and in vitro disintegration time in artificial salvia (22.5?±?1.67?s). Physical stability studies at 40?°C/75% RH for 6 months, Fourier transform infrared spectroscopy analysis and X-ray diffraction results showed that the formulation was stable. The drug-released profile showed that 80% of donepezil hydrochloride was released within 1?min. A single-dose, fasting, four-period, seven-treatment, double-blinded study involving 16 healthy human volunteers was performed to evaluate the palatability of ODT. Formulation VII containing 10?mg of ammonium glycyrrhizinate was able to mask the bitter taste of the drug. Conclusion: The product has the potential to be commercialized and it might serve as solution for non-compliance among the Alzheimer's disease patients. PMID:24495273

Liew, Kai Bin; Tan, Yvonne Tze Fung; Peh, Kok Khiang

2014-02-01

66

Orally disintegrating vardenafil tablets for the treatment of erectile dysfunction: efficacy, safety, and patient acceptability  

PubMed Central

Background: Erectile dysfunction (ED) is a well-documented medical condition that is expected to increase significantly over the next several decades, especially as men live longer and the prevalence of diabetes and cardiovascular diseases increase. Pharmacology agents are often the first line treatment approach. Newer solid dosage forms, known as orally disintegrating tablets (ODT), are now available as one treatment option. Objectives: To review the drug delivery mechanisms of ODTs in general and to review safety and efficacy of vardenafil ODT (a PDE-5 inhibitor) as a treatment option for management of ED. Method: Literature reviews were performed of pharmaceutical dosage forms and the POTENT I (n = 358 subjects) and POTENT II (n = 337 subjects) studies that investigated vardenafil ODT. Results: Vardenafil ODT has been successfully used in multiple age groups and in multiple settings with men from various ethnic backgrounds. Efficacy of vardenafil ODT, as measured using the International Index of Erectile Function (IIEF-EF) and from the Sexual Encounter Profile (SEP) was significantly greater than placebo (P < 0.0001) at 12 weeks. Safety profiles were similar to film-coated dosage forms with no patient deaths reported. Conclusion: Vardenafil ODT offers a convenient, ready-to-use approach for combating ED. Safety concerns are similar to other PDE-5 inhibitors and practitioners should counsel patients accordingly. PMID:21573049

Green, Roger; Hicks, Rodney W

2011-01-01

67

Effect of polacrilin potassium as disintegrant on bioavailability of diclofenac potassium in tablets : a technical note.  

PubMed

Polacrilin potassium is an ion exchange resin used in oral pharmaceutical formulations as a tablet disintegrant. It is a weakly acidic cation exchange resin. Chemically, it is a partial potassium salt of a copolymer of methacrylic acid with divinyl benzene. It ionizes to an anionic polymer chain and potassium cations. It was hypothesized that polacrilin potassium may be able to improve the permeability of anionic drugs according to the Donnan membrane phenomenon. The effect of polacrilin potassium on the permeability of diclofenac potassium, used as a model anionic drug, was tested in vitro using diffusion cells and in vivo by monitoring serum levels in rats. The amount of drug permeated across a dialysis membrane in vitro was significantly more in the presence of polacrilin potassium. Significant improvement was found in the extent of drug absorption in vivo. It could be concluded that polacrilin potassium may be used as a high-functionality excipient for improving the bioavailability of anionic drugs having poor gastrointestinal permeability. PMID:22585376

Bele, Mrudula H; Derle, Diliprao V

2012-09-01

68

Effects of pigeon pea and plantain starches on the compressional, mechanical, and disintegration properties of paracetamol tablets.  

PubMed

A study has been made of the effects of pigeon pea starch obtained from the plant Cajanus cajan (L) Millisp. (family Fabaceae) and plantain starch obtained from the unripe fruit of Musa paradisiaca L. (family Musaceae) on the compressional, mechanical, and disintegration properties of paracetamol tablets in comparison with official corn starch BP. Analysis of compressional properties was done by using density measurements, and the Heckel and Kawakita equations, whereas the mechanical properties of the tablets were evaluated by using tensile strength (T--a measure of bond strength) and brittle fracture index (BFI--a measure of lamination tendency). The ranking for the mean yield pressure, P(y), for the formulations containing the different starches was generally corn < pigeon pea < plantain starch while the ranking for P(k), an inverse measure of the amount of plasticity, was pigeon pea < plantain < corn starch, which indicated that formulations containing corn starch generally exhibited the fastest onset of plastic deformation, whereas those formulations containing pigeon pea starch exhibited the highest amount of plastic deformation during tableting. The tensile strength of the tablets increased with increase in concentration of the starches while the Brittle Fracture Index decreased. The ranking for T was pigeon pea > plantain > corn starch while the ranking for BFI was corn > plantain > pigeon pea starch. The bonding capacity of the formulations was in general agreement with the tensile strength results. The disintegration time (DT) of the formulation increased with concentration of plantain and corn starches but decreased with concentration of pigeon pea starch. The general ranking of DT values was plantain < pigeon pea < corn starch. Notably, formulations containing pigeon pea starch exhibited the highest bond strength and lowest brittleness, suggesting the usefulness of pigeon pea starch in producing strong tablets with minimal lamination tendency. Plantain starch, on the other hand, would be more useful where faster disintegration of tablet is desired. The results show that the starches could be useful in various formulations depending on the intended use of the tablets with the implication that the experimental starches can be developed for commercial purposes. PMID:16556540

Dare, Kunle; Akin-Ajani, Dorothy O; Odeku, Oluwatoyin A; Itiola, Oludele A; Odusote, Omotunde M

2006-03-01

69

RP-HPLC analytical method development and optimization for quantification of donepezil hydrochloride in orally disintegrating tablet.  

PubMed

An easy, fast and validated RV-HPLC method was invented to quantify donepezil hydrochloride in drug solution and orally disintegrating tablet. The separation was carried out using reversed phase C-18 column (Agilent Eclipse Plus C-18) with UV detection at 268 nm. Method optimization was tested using various composition of organic solvent. The mobile phase comprised of phosphate buffer (0.01M), methanol and acetonitrile (50:30:20, v/v) adjusted to pH 2.7 with phosphoric acid (80%) was found as the optimum mobile phase. The method showed intraday precision and accuracy in the range of 0.24% to -1.83% and -1.83% to 1.99% respectively, while interday precision and accuracy ranged between 1.41% to 1.81% and 0.11% to 1.90% respectively. The standard calibration curve was linear from 0.125 ?g/mL to 16 ?g/mL, with correlation coefficient of 0.9997±0.00016. The drug solution was stable under room temperature at least for 6 hours. System suitability studies were done. The average plate count was > 2000, tailing factor <1, and capacity factor of 3.30. The retention time was 5.6 min. The HPLC method was used to assay donepezil hydrochloride in tablet and dissolution study of in-house manufactured donepezil orally disintegrating tablet and original Aricept. PMID:24035953

Liew, Kai Bin; Peh, Kok Khiang; Fung Tan, Yvonne Tze

2013-09-01

70

Influence of non-water-soluble placebo pellets of different sizes on the characteristics of orally disintegrating tablets manufactured by freeze-drying.  

PubMed

The present study describes the development of an orally disintegrating tablet containing a non-water-soluble drug delivery system. A model system was applied to evaluate the effect of different-sized particles on tablet characteristics. Cellets were incorporated into tablets prepared by freeze-drying from a 100 mg/mL mannitol or sucrose solution. Particle size distributions were 200-355 µm for Cellets 200 (C200) and 500-710 µm for Cellets 500 (C500). An examination of the tablets revealed that the particles could not be sufficiently embedded in mannitol because of its crystalline nature. The tablet hardness was also inadequate. In contrast, the hardness of sucrose tablets was increased by the addition of Cellets 500. Therefore, the sucrose-based formulation was studied further. Binders [hydroxyethylstarch, sodium alginate, methylcellulose (MC), and gelatin] were added in different concentrations, and tablets were made either with or without placebo pellets. A positive effect of the Cellets on the hardness of tablets was identified. Furthermore, disintegration time could be clearly reduced by Cellets for tablets made from 100 mg/mL sucrose with addition of 10 mg/mL MC, 20 or 40 mg/mL gelatin. The freeze-dried tablet index revealed that the formulations of sucrose with 50 mg/mL hydroxyethylstarch or 20 mg/mL gelatin were particularly advantageous. PMID:23568590

Stange, Ulrike; Führling, Christian; Gieseler, Henning

2013-06-01

71

STUDIES ON AYURVEDIC TABLETS – PART I DISINTEGRATION TIME AS A PRELIMINARY TOOL FOR STANDARDISATION  

PubMed Central

The ayurvedic pharmacy needs to be established on the basis of modern quality standards. A study on ayurvedic Guti-Vati (tablets) was undertaken with this view, revealed that most of the tablets conform to the I P standards for hardness and DT. A few of the tablets showed curious responses similar to that of enteric coated and slow release tablets commonly used in modern medicine. A systematic supporting study is essential so as to establish relationship of such responses to the nature of ingredients and their relevance with the indications and therapeutic utility described in Ayurvedic texts. PMID:22556505

Patwardhan, Bhushan; Walimbe, V. V.; Palkar, Vijaya; Kulkarni, P.H.

1990-01-01

72

Assessment of disintegrant efficacy with fractal dimensions from real-time MRI.  

PubMed

An efficient disintegrant is capable of breaking up a tablet in the smallest possible particles in the shortest time. Until now, comparative data on the efficacy of different disintegrants is based on dissolution studies or the disintegration time. Extending these approaches, this study introduces a method, which defines the evolution of fractal dimensions of tablets as surrogate parameter for the available surface area. Fractal dimensions are a measure for the tortuosity of a line, in this case the upper surface of a disintegrating tablet. High-resolution real-time MRI was used to record videos of disintegrating tablets. The acquired video images were processed to depict the upper surface of the tablets and a box-counting algorithm was used to estimate the fractal dimensions. The influence of six different disintegrants, of different relative tablet density, and increasing disintegrant concentration was investigated to evaluate the performance of the novel method. Changing relative densities hardly affect the progression of fractal dimensions, whereas an increase in disintegrant concentration causes increasing fractal dimensions during disintegration, which are also reached quicker. Different disintegrants display only minor differences in the maximal fractal dimension, yet the kinetic in which the maximum is reached allows a differentiation and classification of disintegrants. PMID:25234864

Quodbach, Julian; Moussavi, Amir; Tammer, Roland; Frahm, Jens; Kleinebudde, Peter

2014-11-20

73

Novel sustained-release fast-disintegrating multi-unit compressed tablets of lornoxicam containing Eudragit RS coated chitosan-alginate beads.  

PubMed

Novel fast-disintegrating multi-unit tablets (FDMUTs) were prepared to modify the release of lornoxicam (a potent non-steroidal anti-inflammatory drug with a short half-life) as well as to combine the advantages of multi-unit systems with the cost-effectiveness of compressed tablets. The proposed FDMUTs consisted of sustained-release lornoxicam beads directly compressed with fast-disintegrating component, containing amorphous solid dispersion of lornoxicam, anticipating rapid drug release that starts in the stomach to rapidly alleviate the painful symptoms and continues in the intestine to maintain extended analgesic effect. Initially, calcium-alginate and chitosan-alginate beads containing lornoxicam were prepared. Then, the erosion of selected beads formulation was suppressed by treatment with Eudragit RS either through polymer-reinforcement or beads coating. The beads, which elicited appropriate sustainment of lornoxicam release, were directly compressed with fast-disintegrating components to form FDMUTs. The release characteristics of the original beads were maintained after compression which indicates that the adopted compression process did not induce mechanical damage to the beads or coating. All of the prepared FDMUTs demonstrated acceptable physical properties that complied with compendial requirements. Release studies, performed in simulated gastric and intestinal fluids used in sequence to mimic the gastrointestinal transit, illustrate that the FDMUTs containing 8?mg lornoxicam equally distributed between the sustained-release beads and the fast-release component, showed the desired release profile. PMID:20307250

Aburahma, Mona Hassan; Hamza, Yassin El-Said

2011-08-01

74

Evaluation of the disintegration properties of microcrystalline cellulose II and commercial disintegrants.  

PubMed

This study was conducted to assess the disintegration properties of cellulose II excipients named as spray-dried cellulose II (SDCII) and non spray-dried cellulose II (MCCII) in comparison with commercial disintegrants. Swelling and water sorption characteristics were determined by conventional methods. The swelling values, water uptake and percentage of compact volume expansion all suggested that SDCII and MCCII compacts disintegrate by a wicking mechanism similar to that of Polyplasdone-XL, whereas a swelling mechanism dominates for Primojel and Ac-Di-Sol. With commercial binders, SDCII, MCCII and Polyplasdone-XL produced strong, but fast disintegrating tablets. At high levels, their performance as a disintegrant was superior compared to Primojel and Ac-Di-Sol. Disintegration times of the pure excipients revealed SDCII and MCCII to be comparable to Polyplasdone-XL, but faster than Primojel and Ac-Di-Sol. Ibuprofen tablets prepared using disintegrants at all levels released 80% of the drug within 60 min. SDCII and MCCII offer potential for use as a disintegrant in the design and development of solid dosage forms. PMID:22822537

Rojas, J; Kumar, V

2012-06-01

75

The effects of screw configuration and polymeric carriers on hot-melt extruded taste-masked formulations incorporated into orally disintegrating tablets.  

PubMed

The primary aim of this research was to produce successfully taste masked formulations of Sildenafil Citrate (SC) using hot-melt extrusion (HME) technology. Multiple screw configurations and polymeric carriers were evaluated for their effects on taste masking efficiency, which was assessed by both E-tongue analysis and in vitro dissolution in simulated salivary fluid (SSF, pH 6.8 artificial saliva). The screw configurations were further assessed for their effects on the morphology of the API using PXRD, FT-IR and mid-infrared chemical imaging. It was determined that the screw configuration had a profound effect on the taste masking efficiency of the formulations as a result of altering the physical state of the API. Selected extruded formulations using ethylcellulose (EC) with a pore former were further formulated into orally disintegrating tablets (ODTs), which were optimized by varying the grade and percentage of the superdisintegrant used. An optimized disintegration time of approximately 8 seconds was achieved. The final ODT formulation exhibited excellent taste masking properties with over 85% drug release in gastric media as well as physical tablet properties. Interestingly, friability, which tends to be a common concern when formulating ODTs, was well within the acceptable limits (<1%) for common tablets. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 104:124-134, 2015. PMID:25410968

Morott, Joseph T; Pimparade, Manjeet; Park, Jun-Bom; Worley, Chelsea P; Majumdar, Soumyajit; Lian, Zhuoyang; Pinto, Elanor; Bi, Yunxia; Durig, Thomas; Repka, Michael A

2015-01-01

76

Preparation of Spherical Crystal Agglomerates of Naproxen Containing Disintegrant for Direct Tablet Making by Spherical Crystallization Technique  

Microsoft Academic Search

The purpose of this research was to obtain directly compressible agglomerates of naproxen containing disintegrant by spherical\\u000a crystallization technique. Acetone–water containing hydroxypropyl celloluse (HPC) and disintegrant was used as the crystallization\\u000a system. In this study croscarmellose sodium (Ac–Di–Sol) was employed as disintegrant. The agglomerates were characterized\\u000a by differential scanning calorimetry (DSC), powder X-ray diffraction (XRPD), and scanning electron microscopy and

A. Nokhodchi; M. Maghsoodi

2008-01-01

77

Effect of the mode of incorporation on the disintegrant properties of acid modified water and white yam starches  

PubMed Central

Acid modified starches obtained from two species of yam tubers namely white yam – Dioscorearotundata L. and water yam – D. alata L. DIAL2 have been investigated as intra- and extra-granular disintegrants in paracetamol tablet formulations. The native starches were modified by acid hydrolysis and employed as disintegrant at concentrations of 5 and 10% w/w and their disintegrant properties compared with those of corn starch BP. The tensile strength and drug release properties of the tablets, assessed using the disintegration and dissolution (t50 and t80 – time required for 50% and 80% of paracetamol to be released) times, were evaluated. The results showed that the tensile strength and the disintegration and dissolution times of the tablets decreased with increase in the concentration of the starch disintegrants. The acid modified yam starches showed better disintegrant efficiency than corn starch in the tablet formulations. Acid modification appeared to improve the disintegrant efficiency of the yam starches. Furthermore, tablets containing starches incorporated extragranularly showed faster disintegration but lower tensile strength than those containing starches incorporated intragranularly. This emphasizes the importance of the mode of incorporation of starch disintegrant. PMID:23960789

Odeku, Oluwatoyin A.; Akinwande, Babatunde L.

2011-01-01

78

Comparative evaluation of single and bilayered lamotrigine floating tablets  

PubMed Central

Aim: The purpose of this study was to prepare lamotrigine (LM) bilayered and single layered floating tablets and to compare their release profiles. Materials and Methods: LM floating tablets were prepared by direct compression method. Drug, hydroxy propyl methyl cellulose K4M, lactose monohydrate and polyvinylpyrrolidone K30 constitute controlled release layer components and floating layer components includes polymers and sodium bicarbonate. The prepared tablets were evaluated for physicochemical parameters such as hardness, friability, weight variation, thickness, floating lag time (FLT), floating time, in vitro buoyancy study, in vitro release studies. The drug-polymer interaction was studied by fourier transform infrared and differential scanning calorimetry. Results and Discussion: The FLT of all the formulations were within the prescribed limits (<3 min). When ethyl cellulose was used as floating layer component, tablets showed good buoyancy effect but eroded within 6-8 h. Hence it was replaced with hydroxypropyl cellulose -M hydrophilic polymer, which showed good FLT and floating duration for 16 h. Formulation LFC4 was found to be optimized with dissolution profile of zero order kinetics showing fickian diffusion. A comparative study of bilayered and single layered tablets of LM showed a highest similarity factor of 83.03, difference factor of 2.74 and t-test (P < 0.05) indicates that there is no significant difference between them. Conclusion: Though bilayered tablet possess many advantages, single layered tablet would be economical, cost-effective and reproducible for large scale production in the industry. However, the results of present study demonstrated that the in vitro development of bilayered gastro retentive floating tablets with controlled drug release profile for LM is feasible. PMID:24167788

Lakshmi, PK; Sridhar, M; Shruthi, B

2013-01-01

79

A Randomized, Multicenter Study Comparing the Safety and Efficacy of Sodium Phosphate Tablets With 2L Polyethylene Glycol Solution Plus Bisacodyl Tablets for Colon Cleansing  

Microsoft Academic Search

OBJECTIVE:The safety and efficacy of NaP tablets have not been compared with 2L PEG lavage solution. A multicenter, investigator-blinded study was conducted to compare the colon-cleansing efficacy of a new NaP tablet formulation with that of 2L PEG solution plus bisacodyl tablets in adults undergoing colonoscopy.METHODS:A total of 481 patients were randomized to receive either 32 tablets (48 g) of

John F. Johanson; John W. Popp; Lawrence B. Cohen; Sandra R. Lottes; William P. Forbes; Kelli Walker; Edwin Carter; Bing Zhang; Martin Rose

2007-01-01

80

Phase I trial of capecitabine rapidly disintegrating tablets and concomitant radiation therapy in children with newly diagnosed brainstem gliomas and high-grade gliomas  

PubMed Central

Background We conducted a phase I study to estimate the maximum tolerated dose and describe the dose-limiting toxicities and pharmacokinetics of oral capecitabine rapidly disintegrating tablets given concurrently with radiation therapy to children with newly diagnosed brainstem or high-grade gliomas. Methods Children 3–21 y with newly diagnosed intrinsic brainstem or high-grade gliomas were eligible for enrollment. The starting dose was 500 mg/m2, given twice daily, with subsequent cohorts enrolled at 650 mg/m2 and 850 mg/m2 using a 3 + 3 phase I design. Children received capecitabine at the assigned dose daily for 9 wks starting from the first day of radiation therapy (RT). Following a 2-wk break, patients received 3 courses of capecitabine 1250 mg/m2 twice daily for 14 days followed by a 7-day rest. Pharmacokinetic sampling was performed in consenting patients. Six additional patients with intrinsic brainstem gliomas were enrolled at the maximum tolerated dose to further characterize the pharmacokinetic and toxicity profiles. Results Twenty-four patients were enrolled. Twenty were fully assessable for toxicity. Dose-limiting toxicities were palmar plantar erythroderma (grades 2 and 3) and elevation of alanine aminotransferase (grades 2 and 3). Systemic exposure to capecitabine and metabolites was similar to or slightly lower than predicted based on adult data. Conclusions Capecitabine with concurrent RT was generally well tolerated. The recommended phase II capecitabine dose when given with concurrent RT is 650 mg/m2, administered twice daily. A phase II study to evaluate the efficacy of this regimen in children with intrinsic brainstem gliomas is in progress (PBTC-030). PMID:23592571

Kilburn, Lindsay B.; Kocak, Mehmet; Schaedeli Stark, Franziska; Meneses-Lorente, Georgina; Brownstein, Carrie; Hussain, Sazzad; Chintagumpala, Murali; Thompson, Patrick A.; Gururangan, Sri; Banerjee, Anuradha; Paulino, Arnold C.; Kun, Larry; Boyett, James M.; Blaney, Susan M.

2013-01-01

81

Utilization of date syrup as a tablet binder, comparative study  

PubMed Central

The aim of this study was to investigate the possibility of using dates syrup as a tablet binder. Dates syrup (40%, 50%, 60% w/w dates syrup:water) was utilized for the granulation of sodium bicarbonate and calcium carbonate as examples for water-soluble and water-insoluble materials; correspondingly. Those two materials represent examples of bulky drugs as well. Starch paste (10% w/w starch in water) and sucrose syrup (50% w/w sucrose in water), the well-known tablet binders, were used in the granulation of the same materials for the sake of comparison. The granulations were evaluated with regard to particle size and particle size distribution, granule strength, bulk density, flowability, moisture content and compression behavior. In addition, tablets prepared and evaluated from these granules. Taste and flavor of the prepared tablet have been tested by seven healthy volunteers. Within the scope of this work, dates syrup showed excellent properties as a tablet binder in comparison to starch paste or sucrose syrup for the granulation of both water-soluble and water-insoluble materials. Also, better flavoring and masking taste have been noticed from an evaluation by human volunteers demonstrating the usefulness of the date syrup as sweetener and flavoring the tablets in addition to its use as binder. PMID:23960724

Alanazi, Fars Kaed

2010-01-01

82

Isolation and Evaluation of Disintegrant Properties of Fenugreek Seed Mucilage  

Microsoft Academic Search

In the present study, Polysaccharide mucilage derived from the seeds of fenugreek, Trigonella foenum-graceum L (family Leguminosae) was investigated as disintegrant for use in mouth dissolving tablet formulations containing metformin hydrochloride. Mucilage extracted from fenugreek seeds were subjected to toxicity studies, it showed that extracted mucilage is devoid of toxicity. Fast disintegrating tablet (FDT) of metformin HCl was formulated using

Ravi Kumar; Swati Patil; M. B. Patil; Sachin R. Patil; Mahesh S. Paschapur; Mumbai Parade

83

Neem gum as a binder in a formulated paracetamol tablet with reference to Acacia gum BP.  

PubMed

This study determined the physical, compressional, and binding properties of neem gum (NMG) obtained from the trunk of Azadirachta indica (A Juss) in a paracetamol tablet formulation in comparison with official Acacia gum BP (ACA). The physical and flow properties were evaluated using density parameters: porosity, Carr's index, Hausner's ratio, and flow rate. Compressional properties were analyzed using Heckel and Kawakita equations. The tensile strength, brittle fracture index, and crushing strength-friability/disintegration time ratio were used to evaluate the mechanical properties of paracetamol tablets while the drug release properties of the tablets were assessed using disintegration time and dissolution times. Tablet formulations containing NMG exhibited faster onset and higher amount of plastic deformation during compression than those containing ACA. Neem gum produced paracetamol tablets with lower mechanical strength; however, the tendency of the tablets to cap or laminate was lower when compared to those containing ACA. Inclusion of NMG improved the balance between binding and disintegration properties of paracetamol tablets produced than those containing ACA. Neem gum produced paracetamol tablets with lower disintegration and dissolution times than those containing ACA. PMID:24500339

Ogunjimi, Abayomi Tolulope; Alebiowu, Gbenga

2014-04-01

84

Evaluation of named binders in Rauwolfia vomitoria root tablets.  

PubMed

Some physical properties of Rauwolfia vomitoria root tablets were studied. Tablet characteristics studied were: weight uniformity, tensile strength, friability, disintegration time and content uniformity. Tablet property varied depending on the type and concentration of the binder. The tablets had type and concentration of the binder. The tablets had acceptable hardness and friability profiles. Although tablets containing 150 mg R. vomitoria root had lower tensile strength values. All the tablets passed the B.P. disintegration time test of 15 min. Moreover tablets containing 150 mg R. vomitoria root disintegrated under 1 min. at 4% w/w binder concentration. PMID:10961024

Onunkwo, G C

2000-01-01

85

Evaluation of selected micronized poloxamers as tablet lubricants.  

PubMed

The primary objective of this study was to compare the lubrication properties of micronized poloxamer 188 (Lmicrotrol micro 68) and micronized poloxamer 407 (Lmicrotrol micro 127) with certain conventional lubricants such as magnesium stearate and stearic acid. The secondary objective was to use these micronized poloxamers as water-soluble tablet lubricants in preparation of effervecsent tablets. The results showed that these micronized poloxamers have superior lubrication properties compared with stearic acid, with no negative effect on tablet hardness, friability, disintegration, or dissolution. Moreover, lubricant mixing time had no significant effect on tablet properties when poloxamers were used as lubricants. Effervescent tablets also were produced successfully using micronized poloxamers as lubricants. The micronized poloxamers had a better lubrication effect in comparison with that of water-soluble lubricant l-leucine. PMID:17994358

Desai, D; Zia, H; Quadir, A

2007-10-01

86

A fixed-dose combination tablet of gemigliptin and metformin sustained release has comparable pharmacodynamic, pharmacokinetic, and tolerability profiles to separate tablets in healthy subjects  

PubMed Central

Background In type 2 diabetes mellitus, fixed-dose combination (FDC) can provide the complementary benefits of correction of multiple pathophysiologic defects such as dysfunctions in glycemic or metabolic control while improving compliance compared with separate tablets taken together. The objective of the study reported here was to compare the pharmacodynamic (PD), pharmacokinetic (PK), and tolerability profiles of gemigliptin and extended-release metformin (metformin XR) between FDC and separate tablets. Methods A randomized, open-label, single-dose, two-way, two-period, crossover study was conducted in 28 healthy male volunteers. Two FDC tablets of gemigliptin/metformin 25/500 mg or separate tablets of gemigliptin (50 mg ×1) and metformin XR (500 mg ×2) were orally administered in each period. Serial blood samples were collected up to 48 hours post-dose to determine dipeptidyl peptidase 4 (DPP-4) activity using spectrophotometric assay and concentrations of gemigliptin and metformin using tandem mass spectrometry. Geometric mean ratios (GMRs) of FDC to separate tablet formulations and their 90% confidence intervals (CIs) were calculated to compare the PD and PK parameters between the two formulations. Tolerability was assessed throughout the study. Results The plasma DPP-4 activity–time curves of the FDC and the separate tablets almost overlapped, leading to a GMR (90% CI) of the FDC to separate tablets for the plasma DPP-4 activity and its maximum inhibition of 1.00 (0.97–1.04) and 0.92 (0.82–1.05), respectively. Likewise, all of the GMRs (90% CIs) of FDC to separate tablets for the area under the plasma concentration–time curve and maximum plasma concentration of gemigliptin and metformin fell entirely within the conventional bioequivalence range of 0.80–1.25. Both the FDC and separate tablets were well tolerated. Conclusion The PD, PK, and tolerability profiles of gemigliptin and metformin XR in FDC and separate tablets were found to be comparable. The FDC tablet of gemigliptin and metformin sustained release can be a convenient therapeutic option in patients with type 2 diabetes mellitus requiring a combination approach.

Park, Sang-In; Lee, Howard; Oh, Jaeseong; Lim, Kyoung Soo; Jang, In-Jin; Kim, Jeong-Ae; Jung, Jong Hyuk; Yu, Kyung-Sang

2015-01-01

87

Comparative static curing versus dynamic curing on tablet coating structures.  

PubMed

Curing is generally required to stabilize film coating from aqueous polymer dispersion. This post-coating drying step is traditionally carried out in static conditions, requiring the transfer of solid dosage forms to an oven. But, curing operation performed directly inside the coating equipment stands for an attractive industrial application. Recently, the use of various advanced physico-chemical characterization techniques i.e., X-ray micro-computed tomography, vibrational spectroscopies (near infrared and Raman) and X-ray microdiffraction, allowed new insights into the film-coating structures of dynamically cured tablets. Dynamic curing end-point was efficiently determined after 4h. The aim of the present work was to elucidate the influence of curing conditions on film-coating structures. Results demonstrated that 24h of static curing and 4h of dynamic curing, both performed at 60°C and ambient relative humidity, led to similar coating layers in terms of drug release properties, porosity, water content, structural rearrangement of polymer chains and crystalline distribution. Furthermore, X-ray microdiffraction measurements pointed out different crystalline coating compositions depending on sample storage time. An aging mechanism might have occur during storage, resulting in the crystallization and the upward migration of cetyl alcohol, coupled to the downward migration of crystalline sodium lauryl sulfate within the coating layer. Interestingly, this new study clearly provided further knowledge into film-coating structures after a curing step and confirmed that curing operation could be performed in dynamic conditions. PMID:23792043

Gendre, Claire; Genty, Muriel; Fayard, Barbara; Tfayli, Ali; Boiret, Mathieu; Lecoq, Olivier; Baron, Michel; Chaminade, Pierre; Péan, Jean Manuel

2013-09-10

88

Effect of repeated compaction of tablets on tablet properties and work of compaction using an instrumented laboratory tablet press.  

PubMed

Abstract The repeated compaction of Avicel PH101, dicalcium phosphate dihydrate (DCP) powder, 50:50 DCP/Avicel PH101 and Starch 1500 was studied using an instrumented laboratory tablet press which measures upper punch force, punch displacement and ejection force and operates using a V-shaped compression profile. The measurement of work compaction was demonstrated, and the test materials were ranked in order of compaction behaviour Avicel PH101?>?DCP/Avicel PH101?>?Starch?>?DCP. The behaviour of the DCP/Avicel PH101 mixture was distinctly non-linear compared with the pure components. Repeated compaction and precompression had no effect on the tensile fracture strength of Avicel PH101 tablets, although small effects on friability and disintegration time were seen. Repeated compaction and precompression reduced the tensile strength and the increased disintegration time of the DCP tablets, but improved the strength and friability of Starch 1500 tablets. Based on the data reported, routine laboratory measurement of tablet work of compaction may have potential as a critical quality attribute of a powder blend for compression. The instrumented press was suitable for student use with minimal supervisor input. PMID:24171692

Gamlen, Michael John Desmond; Martini, Luigi G; Al Obaidy, Kais G

2015-01-01

89

Importance of excipient wettability on tablet characteristics prepared by moisture activated dry granulation (MADG).  

PubMed

For moisture activated dry granulation (MADG), microcrystalline cellulose (MCC) or silicon dioxide is recommended for the moisture absorption stage. The aim of this study was to assess the suitability of alternative excipients as moisture absorbents with regard to the disintegration mechanism of resulting lactose based placebo formulations. Beside high and low moisture MCC grades, the additions of magnesium aluminometasilicate (MAMS), pregelatinized starch (S1500), crospovidone (Kollidon CL) and carmellose calcium (ECG 505) were evaluated. High shear granulation (HSG) was conducted as a reference process. The overall disintegration time of all tablets produced by MADG was significantly faster whereas hardness yield and mass-variability were equal or superior compared to the HSG process. Powder wettability of the different moisture absorbents was identified to be a key driver for rapid disintegration, whereas tablet porosity had only a minor influence on the target hardness of the tablets. PMID:23994013

Takasaki, Hiroshi; Yonemochi, Etsuo; Messerschmid, Roman; Ito, Masanori; Wada, Koichi; Terada, Katsuhide

2013-11-01

90

Comparative release profile of sustained release matrix tablets of verapamil HCl  

PubMed Central

Introduction: Verapamil hydrochloride (VH) is a calcium channel blocking agent used in the treatment of hypertension, cardiac arrhythmia and angina pectoris. The short half-life and high frequency of administration of VH makes it a suitable candidate for designing sustained drug delivery system. The aim of the present investigation was to develop a sustained release matrix tablet of verapamil hydrochloride (VH) using ethyl cellulose, methyl cellulose, Eudragit RS 100, hydroxypropyl methylcellulose and carboxymethyl cellulose and to evaluate the drug release kinetics. Materials and Methods: In order to achieve the required sustained release profile, the tablets were prepared by a wet granulation method using avicel PH 101 and magnesium stearate as binder and lubricant, respectively. Results: The formulated tablets were characterized for pre-compression and post-compression parameters and they were in the acceptable limits. The drug release data obtained after an in vitro dissolution study was fitted to various release kinetic models in order to evaluate the release mechanism and kinetics. The criterion for selecting the best fit model was linearity (coefficient of correlation). Drug release mechanism was found to follow a complex mixture of diffusion, swelling and erosion. Furthermore, to minimize the initial burst drug release, batches were coated by using Eudragit RS100 polymer. After coating the tablets, a better release profile of the formulated tablets was expected and the release rate of the drug was compared with the marketed SR tablet of VH. Conclusion: The dosage form holds the potential to control the release rate of drug and extend the duration of action of a drug. PMID:23799207

Mathur, Vikas; Nagpal, Kalpana; Singh, Shailendra Kumar; Mishra, Dina Nath

2013-01-01

91

Disintegrating Mercuries  

NASA Astrophysics Data System (ADS)

Short-period exoplanets can have dayside surface temperatures surpassing 2000 K, hot enough to vaporize rock. Small enough planets can evaporate completely. We discuss the observations and theory underlying disintegrating planets such as KIC 12557548b --- which may have been stripped down to its iron core. Thermal evaporation models assert that the catastrophic disintegration phase lasts only a small fraction of a planet's life, and therefore predict that for every object like KIC 12557548b, there should be many near-quiescent progenitors with sub-day periods whose hard-surface transits may be detectable. Unresolved issues with the theory of mass loss will be highlighted, including the related inverse problem of in-situ formation of rocky bodies.

Chiang, Eugene

2015-01-01

92

Towards a real time release approach for manufacturing tablets using NIR spectroscopy.  

PubMed

The aim of this study was to use the near-infrared spectroscopy (NIRS) as a process analytical tool to evaluate the conformity of paracetamol tablets in terms of four Pharmacopoeia tests (content uniformity, hardness, disintegration time, friability) and to control in-line blend uniformity. Tablets were manufactured by direct compression. Three different active pharmaceutical ingredient (API) concentrations were manufactured and three different compaction pressures were used. Intact tablets were analysed by transmission mode with NIRS prior to European Pharmacopoeia tests that were used as reference methods. Partial least square (PLS) regression was selected to build the prediction NIR models for content uniformity, tablet hardness and disintegration time. The prediction of NIR content uniformity and tablet hardness methods were validated using the accuracy profile approach. The values of the root mean squared error of calibration (RMSEC) and the root mean squared error of prediction (RMSEP) for the disintegration time indicated the robustness and the global accuracy of the NIR model. Regarding the tablet friability test, the classification was based on K-nearest neighbours (KNN). Then tablet NIR analyses successfully allowed the prediction of their conformity. Compared to the time consuming Pharmacopoeia reference methods, the benefit of this nondestructive method is significant, especially for reducing batch release time. PMID:24880992

Pestieau, Aude; Krier, Fabrice; Thoorens, Grégory; Dupont, Anaïs; Chavez, Pierre-François; Ziemons, Eric; Hubert, Philippe; Evrard, Brigitte

2014-09-01

93

Formulation and evaluation of taste masked mouth dissolving tablets of levocetirizine hydrochloride.  

PubMed

Aim of this research work was to develop mouth dissolving tablet that disintegrates rapidly in mouth by using tasteless complex of Levocetirizine and Tulsion-335. Effect of different parameters such as swelling time, resin activation, drug resin ratio as well as stirring time was optimized by taste and percentage drug loading. Formulated DRC (Drug Resin Complex) was characterized by infrared spectroscopy, thermal analysis and X-ray diffraction pattern. Tablets were formulated by wet granulation with PVP as binder, Sodium Starch Glycolate (SSG) and Crospovidone as super disintegrants. In these batches optimum hardness was achieved but disintegration time was found to be very high as ? 70 second, so further trials were planned by using different superdisintegrants such as Croscarmellose sodium, Sodium Starch Glycolate (SSG) as well as Crospovidone by wet granulation method. Tablets formulated with 7.5% crospovidone showed comparatively low disintegration time (25 sec), wetting time (20 sec) and friability (0.60 %) than the other batches. In present study we optimized the conditions required for maximum drug loading of Levocetirizine with Tulsion-335. Among different superdisintergants, crospovidone was found suitable with drug-resin complex to get the low disintegration time, wetting time and friability of tablets. PMID:24250469

Sharma, Vijay; Chopra, Himansu

2012-01-01

94

Formulation and evaluation of aceclofenac mouth-dissolving tablet.  

PubMed

Aceclofenac has been shown to have potent analgesic and anti-inflammatory activities similar to indomethacin and diclofenac, and due to its preferential Cox-2 blockade, it has a better safety than conventional Non steroidal anti-inflammatory drug (NSAIDs) with respect to adverse effect on gastrointestinal and cardiovascular systems. Aceclofenac is superior from other NSAIDs as it has selectivity for Cox-2, a beneficial Cox inhibitor is well tolerated, has better Gastrointestinal (GI) tolerability and improved cardiovascular safety when compared with other selective Cox-2 inhibitor. To provide the patient with the most convenient mode of administration, there is need to develop a fast-disintegrating dosage form, particularly one that disintegrates and dissolves/disperses in saliva and can be administered without water, anywhere, any time. Such tablets are also called as "melt in mouth tablet." Direct compression, freeze drying, sublimation, spray drying, tablet molding, disintegrant addition, and use of sugar-based excipients are technologies available for mouth-dissolving tablet. Mouth-dissolving tablets of aceclofenac were prepared with two different techniques, wet granulation and direct compression, in which different formulations were prepared with varying concentration of excipients. These tablets were evaluated for their friability, hardness, wetting time, and disintegration time; the drug release profile was studied in buffer Phosphate buffered Saline (PBS) pH 7.4. Direct compression batch C3 gave far better dissolution than the wet granulation Batch F2, which released only 75.37% drug, and C3, which released 89.69% drug in 90 minutes. PMID:22171305

Solanki, Shailendra Singh; Dahima, Rashmi

2011-04-01

95

One-day treatment of vulvovaginal candidiasis with a 500-mg clotrimazole vaginal tablet compared with a three-day regimen of two 100-mg vaginal tablets daily.  

PubMed

In a randomized, double-blind trial, the efficacy and safety of a new single-dose clotrimazole vaginal tablet were compared with that of three-day clotrimazole therapy. Forty-two patients with clinically and mycologically confirmed vulvo-vaginal candidiasis received either one 500-mg clotrimazole tablet for one day or two 100-mg tablets daily for three days. Follow-up visits were performed approximately one week and one month after treatment. Thirty-six patients were evaluated for drug efficacy. There was no significant difference in clinical and mycological responses to the two regimens (P = 1.00, Fisher's exact test). At the final visit, 16 (89%) of the 18 patients receiving one-day treatment showed mycological and clinical clearance of infection, as compared to 15 (83%) of the 18 patients receiving three-day therapy. One patient in the three-day treatment group presented moderate edema of the vulva which was judged to be remotely related to treatment. The findings indicate that a single 500-mg tablet of clotrimazole is as effective and safe in the treatment of vulvovaginal candidiasis as a three-day course of 200 mg/day. PMID:3698065

Floyd, R; Hodgson, C

1986-01-01

96

Proniosomal Oral Tablets for Controlled Delivery and Enhanced Pharmacokinetic Properties of Acemetacin.  

PubMed

Free-flowing proniosomal powders of acemetacin (AC) were prepared using the slurry method and maltodextrin as carrier. Positively charged proniosomes composed of 70:20:10 of Span 60/cholesterol (Chol)/stearylamine (SA), respectively, were successively compressed into tablets using direct compression method. The tablets were characterized for weight variability, friability, hardness, drug content uniformity, and dissolution properties. The in vivo evaluation of the prepared proniosomes (powder or tablet forms) after oral administration was investigated by the determination of AC and its active metabolite indomethacin (IND) in the blood of albino rabbits. Results indicated that the increase of Chol from 10% to 20% markedly reduced the efflux of the drug. Further Chol addition from 30% to 50% led to increased AC release rates. The proniosome tablets of AC showed greater hardness and disintegration time and less friability than AC plain tablets. The dissolution of proniosomal tablets indicated a lower drug release percentage compared to powdered proniosomes and AC plain tablets. The mean pharmacokinetic parameters of AC and IND from different formulations indicated increased t 1/2 and area under the curve (AUC) of both AC and IND for proniosomal tablets compared with both proniosomal powders and AC plain tablets. This study suggested the formulation of AC proniosomal powder into tablets to control and extend its pharmacologic effects. PMID:25319057

Shehata, Tamer M; Abdallah, Marwa H; Ibrahim, Mahmoud Mokhtar

2014-10-16

97

Comprehensive review on oral disintegrating films.  

PubMed

Fast-dissolving drug-delivery systems were first developed in the late 1970s as an alternative to tablets, capsules, and syrups for pediatric and geriatric patients who experience difficulties swallowing traditional oral solid dosage forms. In response to this need, a variety of orally disintegrating tablet (ODT) formats were commercialized, which disintegrate within 1 min when placed in the mouth without drinking water or chewing. Oral drug delivery technology has improved from conventional dosage forms to modified release dosage forms to ODT to the recent oral disintegrating films (ODF). Oral disintegrating film or strip that employs a water dissolving polymer which allows the dosage form to quickly hydrate by saliva, adhere to mucosa, and disintegrate within a few seconds, dissolve and releases medication for oromucosal absorption when placed on the tongue or oral cavity. Oral strip technology provides an alternate route for drugs with first pass metabolism. This review give details of materials used in ODF, manufacturing aspects, technologies, evaluation tests and marketed products. PMID:22920576

Nagaraju, T; Gowthami, R; Rajashekar, M; Sandeep, S; Mallesham, M; Sathish, D; Kumar, Y Shravan

2013-02-01

98

Pharmaceutical and analytical evaluation of triphalaguggulkalpa tablets  

PubMed Central

Aim of the Study: Development of standardized, synergistic, safe and effective traditional herbal formulations with robust scientific evidence can offer faster and more economical alternatives for the treatment of disease. The main objective was to develop a method of preparation of guggulkalpa tablets so that the tablets meet the criteria of efficacy, stability, and safety. Materials and Methods: Triphalaguggulkalpa tablet, described in sharangdharsanhita and containing guggul and triphala powder, was used as a model drug. Preliminary experiments on marketed triphalaguggulkalpa tablets exhibited delayed in vitro disintegration that indicated probable delayed in vivo disintegration. The study involved preparation of triphalaguggulkalpa tablets by Ayurvedic text methods and by wet granulation, dry granulation, and direct compression method. The tablets were evaluated for loss on drying, volatile oil content, % solubility, and steroidal content. The tablets were evaluated for performance tests like weight variation, disintegration, and hardness. Results: It was observed that triphalaguggulkalpa tablets, prepared by direct compression method, complied with the hardness and disintegration tests, whereas tablets prepared by Ayurvedic text methods failed. Conclusion: Direct compression is the best method of preparing triphalaguggulkalpa tablets. PMID:21731383

Savarikar, Shreeram S.; Barbhind, Maneesha M.; Halde, Umakant K.; Kulkarni, Alpana P.

2011-01-01

99

[Calorimetric evaluation of directly compressed tablets].  

PubMed

The paper studies the effect of the type of the disintegrating substance and the lubricant on the destruction heat of tablet materials and tablets. Destruction heat was determined by means of isoperibolic calorimetry. Tablet materials and tablets contained Avicel PH 101 as the dry binder, 10% of Primojel, Ac-Di-Sol, or Polyplasdone XL as disintegrating substances, and 5% of magnesium strearate or sodium laurylsulfate as the lubricants. The sum of destruction heats of the individual auxiliary substances equalled the found values in tablet materials and tablets. In tablets, in contrast to tablet materials, values of destruction heat higher by 57.9% were found. In the disintegrating substances and lubricants tested, the found values of destruction heats were dependent on the values of destruction heats of the individual auxiliary substances. In the disintegrating substances, a linear dependence of the total destruction heat (CDT) on the destruction heat of the disintegrating substances (DTR) was found, given by the relationship CDT = 0.797.DTR + 17.666 with the correlation coefficient r = 0.986. PMID:11242832

Rehula, M; Lavická, J; Musilová, M

2001-01-01

100

Comparison of Echinacea alkylamide pharmacokinetics between liquid and tablet preparations.  

PubMed

The relative oral bioavailability of alkylamides from two different Echinacea dosage forms (liquid and tablet) were compared in a small two-way crossover study in humans (n=3). The liquid preparation investigated contained a mixture of Echinacea purpurea root (300 mg/ml) and Echinacea angustifolia root (200 mg/ml) extracted in 60% ethanol. The tablet preparation investigated was also a mixture of E. purpurea root (675 mg/tablet) and E. angustifolia root (600 mg/tablet), but was prepared from the dried 60% ethanolic extracts of these two Echinacea species. Alkylamides were found to be rapidly absorbed and measurable in plasma from both preparations. No significant differences in the tetraene alkylamide pharmacokinetic parameters for T(1/2), AUC(t-lin) and C(max) in the two different preparations were found. T(max) increased from 20 min for the liquid to 30 min for the tablet, which is not unexpected as the tablet required time for disintegration before absorption could occur. These results suggested that there was no significant difference in the bioavailability of alkylamides from the liquid and tablet Echinacea formulations. Furthermore, the results also indicated that the absorption site and any alkylamide loss due to digestive processes were similar in both preparations. PMID:17289362

Matthias, A; Addison, R S; Agnew, L L; Bone, K M; Watson, K; Lehmann, R P

2007-09-01

101

An easy-to-use approach for determining the disintegration ability of disintegrants by analysis of available surface area.  

PubMed

With the aim of directly predicting the functionality and mechanism of disintegrants during the disintegration and dissolution of tablets, we investigated an analysis method based on available surface area, which is the surface area of a drug in a formulation in direct contact with the external solvent during dissolution. We evaluated the following disintegrants in this study: sodium starch glycolate (Glycolys), crospovidone (Kollidon CL), carboxymethylcellulose calcium (CMC-Ca), low-substituted hydroxypropylcellulose (L-HPC), and croscarmellose sodium (Ac-Di-Sol). When disintegrant was added to a 50% ethenzamide tablet formulation, an increase in the dissolution rate dependent on disintegrant concentration was observed, according to the type of disintegrant. In addition, the available surface area also differed between disintegrants. For Glycolys, CMC-Ca, and Ac-Di-Sol, a rapid increase in available surface area and a large increase in maximum available surface area (Smax) were observed due to high swellability and wicking, even when the disintegrant concentration was only 1.0%. In contrast, for Kollidon CL and LH-21, a gradual increase in available surface area was observed, depending on the disintegrant concentration. To evaluate the disintegrant ability, ?tmax and ?Smax were calculated by subtracting peak time (tmax) at 5.0% from that at 1.0% and subtracting Smax at 1.0% from that at 5.0%, respectively, and it was found that the water absorption ratio had strong negative correlations with ?tmax and ?Smax. Therefore, this study demonstrates that analysis of only available surface area and parameters thereby obtained can directly provide useful information, especially about the disintegration ability of disintegrants. PMID:23518366

Iwao, Yasunori; Tanaka, Shoko; Uchimoto, Takeaki; Noguchi, Shuji; Itai, Shigeru

2013-05-01

102

Novel approach of aceclofenac fast dissolving tablet.  

PubMed

Fast disintegrating tablets (FDTs) have received ever increasing demand during the last decade, and the ?eld has become a hastily growing area in the pharmaceutical industry. Upon introduction into the mouth, these tablets dissolve or disintegrate in the mouth in the absence of additional water for easy administration of active pharmaceutical ingredients. Aceclofenac, an NSAID, has been recommended orally for the treatment of bone and connective tissue disorder and thus the formulation of the same resulted in development of several FDT technologies. The present aim is to formulate a tablet which disintegrate and dissolve rapidly and give its rapid onset of action: analgesic, antipyretic and anti-inflammatory action. Besides, the conventional tablets also show poor patient compliance an attempt had been made to formulate for FDT of aceclofenac by using various super disintegrants like sodium starch glycolate, croscarmellose sodium and crosspovidone (polyplasdone XL) and PEG 6000 followed by novel technique. The tablets were evaluated for friability, hardness, weight variation, disintegration time, wetting time, in vitro dissolution studies and drug content studies. It was concluded that the batch which was prepared by using combination of crosspovidone and sodium starch glycolate as a super disintegrant shows excellent disintegration time, enhance dissolution rate, taste masking and hence lead to improve efficacy and bioavailability of drug. PMID:25553683

Dave, Vivek; Yadav, Sachdev; Sharma, Swapnil; Vishwakarma, Pushpendra; Ali, Nasir

2015-01-01

103

In vitro--in vivo evaluation of tableted caseinchitosan microspheres containing diltiazem hydrochloride.  

PubMed

Casein-chitosan microspheres containing diltiazem hydrochloride (DTZ.HCL) were prepared using aqueous coacervation technique. The formed microspheres were not suitable for tableting by direct compression due to their poor binding properties. The effect of hydroxypropylmethylcellulose (HPMC), ethylcellulose (EC), carbopol 940 and egg albumin as dry binders at different concentrations on the properties of the tablets was studied. Each blend of microspheres with dry binder and 2% w/w magnesium stearate as glidant was hand-filled into the die cavity of a single punch tablet machine to ensure constant amount of drug (90 mg) in each tablet. The compression force was adjusted to produce tablets with hardness value about 7.73 +/- 0.79 Kp. The prepared tablets showed good appearance and low friability. The tested binders HPMC (10 and 30% w/w) and EC (20 and 30% w/w) gave fast tablet disintegration with high initial drug release (burst effect) while, carbopol 940 (5 and 10% w/w) and egg albumin (30% w/w) gave non-disintegrating tablets with low initial drug release. Tableted microspheres prepared with 30% egg albumin showed drug release profile similar to one of the commercial tablets (Dilzem retard, 90 mg) and was chosen for in-vivo study. Tableted microspheres and commercial tablets were administered orally in different occasions to six beagle dogs and diltiazem was assayed in dog plasma. The pharmacokinetic parameters including maximum drug concentration (Cmax) and time to reach that maximum (Tmax) were 106.24 +/- 17.96 ng.ml-1 and 5.8 +/- 2.04 hours, respectively, for the commercial sustained release DTZ tablets while, those were 107.9 +/- 12.89 ng.ml-1 and 3.6 +/- 1.36 hours, respectively for tableted microspheres. The elimination half-lives were nearly the same for the commercial and the formulated tablets (8.22 +/- 4.19 and 7.95 +/- 4.28 hours, respectively). No statistical differences (P > 0.05) were found between the two treatments for area under the plasma concentration curve (AUC0 infinity), mean residence time (MRT) and rate of drug absorption (Cmax/AUC0 infinity) indicating comparable extent and rate of drug absorption for both formulations. It was concluded that the formulated tableted microspheres provide an acceptable delivery for DTZ over an extended period of time. PMID:12680034

al-Suwayeh, Saleh A; el-Helw, Abdel-Rehim M; al-Mesned, Abdullah F; Bayomi, Mohsen A; el-Gorashi, Abobakr S

2003-01-01

104

Formulation and Characterization of Oral Mucoadhesive Chlorhexidine Tablets Using Cordia myxa Mucilage  

PubMed Central

Background The dilution and rapid elimination of topically applied drugs due to the flushing action of saliva is a major difficulty in the effort to eradicate infections of oral cavity. Utilization a proper delivery system for incorporation of drugs has a major impact on drug delivery and such a system should be formulated for prolonged drug retention in oral cavity. Objectives The aim of the present study was the use of mucilage of Cordia myxa as a mucoadhesive material in production of chlorhexidine buccal tablets and its substitution for synthetic polymers such as HPMC. Materials and Methods The influence of mucilage concentration on the physicochemical responses (hardness, friability, disintegration time, dissolution, swelling, and muco-adhesiveness strength) was studied and swelling of mucilage and HPMC were compared. The evaluated responses included pharmacopoeial characteristics of tablets, the force needed to separate tablets from mucosa, and the amount of water absorbed by tablets. Results In comparison to HPMC, the rise of mucilage concentration in the formulations increased disintegration time, drug dissolution rate, and reduced MDT. Also, compared to 30% HPMC, muco-adhesiveness strength of buccal tablets containing 20% mucilage was significantly higher. Conclusions It can be concluded that the presence of Cordia myxa powdered mucilage may significantly affect the tablet characteristics, and increasing in muco-adhesiveness may be achieved by using 20% w/w mucilage. PMID:24624170

Moghimipour, Eskandar; Aghel, Nasrin; Adelpour, Akram

2012-01-01

105

A new application of WT-ANN method to control the preparation process of metformin hydrochloride tablets by near infrared spectroscopy compared to PLS.  

PubMed

NIR spectroscopy was an effective expeditious and nondestructive technique to analyze various physical and chemical parameters of interest to the pharmaceutical industry. This paper proposed wavelet transform-artificial neural network (WT-ANN) to determinate mean particle size of metformin hydrochloride granulation process, tablet compression force, tablet hardness, tablet active content with two pretreatment method, standard normal variate (SNV) and multiplicative scatter correction (MSC). The proposed WT-ANN method which was applied to control the preparation process of metformin hydrochloride tablets was feasible and demonstrated more accurate as an available non-linear method compared to traditional methods such as partial least squares (PLS). PMID:23587532

Wu, Jia; Luo, Wei; Wang, Xuekai; Qiang cheng; Sun, Chaoguo; Li, Hui

2013-06-01

106

Comparison of properties of tablets and energy profile of compaction of two spray-dried lactoses.  

PubMed

The paper compared two spray-dried lactoses Flowlac 100 and SuperTab 14SD from the standpoint of tensile strength and disintegration time of tablets, the effect of an addition of the lubricant magnesium stearate and silicified microcrystalline cellulose on these properties, and also from the standpoint of the energy profile of compression. The comparison of the values was performed at the compression force of 15 kN. The strength of tablets was higher in the case of SuperTab 14SD, an increase in the concentration of magnesium stearate did not decrease tablet strength. Prosolv SMCC 90 increased the strength of tablets and made it equal for both lactoses, but it also increased the sensitivity to the added lubricant. The disintegration time of tablets was shorter in the case of SuperTab 14SD, an increased concentration of magnesium stearate prolonged it, and an addition of Prosolv SMCC 90 shortened it and made it equal for both lactoses. From the energy standpoint, the maximal energy was higher in the case of SuperTab 14SD, an addition of Prosolv SMCC 90 increased it and again made it equal for both lactoses. The differences in the values of the maximal energy were primarily due to the values of the energy for friction and the energy accumulated by the tablet after compression, and there was no marked difference in the values of the energy of decompression. SuperTab 14SD showed a higher plasticity than Flowlac 100. PMID:23610968

Muzíková, Jitka; Sináglová, Pavla

2013-01-01

107

Formulation and In Vitro Evaluation of Ofloxacin Tablets using Natural Gums as Binders.  

PubMed

Natural gums are economical, easily available, and useful as tablet binders. In the present investigation, an attempt was made to formulate Ofloxacin tablets using three natural binders, namely Acacia arabica, Hibiscus esculentus, and xanthan gum. Such six batches of Ofloxacin tablets were prepared by using different types and amounts of the natural binders by the wet granulation method. The tablets were analyzed for their hardness, friability, and weight variation, and in vitro release was performed in a phosphate buffer at pH 6.8. The prepared tablets were also evaluated for their various release kinetics and similarity factors f2. The physical properties of the tablets containing the natural binders showed sufficient hardness, desirable disintegration time, and low friability. Their better percentage of drug release was observed as compared to the marketed formulation showing more than 85% drug release within 45 minutes. The in vitro release data was well-fitted into zero-order and the values of release exponent 'n' were between 0.303 and 0.514. The high similarity factor f2 of 64.50 was achieved with the best batch in comparison to the marketed tablets. The results obtained indicated that the gum Acacia arabica performed as well as gelatin compared to the other binders for the Ofloxacin tablet formulation. PMID:24959411

Mistry, Amisha K; Nagda, Chirag D; Nagda, Dhruti C; Dixit, Bharat C; Dixit, Ritu B

2014-06-01

108

Formulation and In Vitro Evaluation of Ofloxacin Tablets using Natural Gums as Binders  

PubMed Central

Natural gums are economical, easily available, and useful as tablet binders. In the present investigation, an attempt was made to formulate Ofloxacin tablets using three natural binders, namely Acacia arabica, Hibiscus esculentus, and xanthan gum. Such six batches of Ofloxacin tablets were prepared by using different types and amounts of the natural binders by the wet granulation method. The tablets were analyzed for their hardness, friability, and weight variation, and in vitro release was performed in a phosphate buffer at pH 6.8. The prepared tablets were also evaluated for their various release kinetics and similarity factors f2. The physical properties of the tablets containing the natural binders showed sufficient hardness, desirable disintegration time, and low friability. Their better percentage of drug release was observed as compared to the marketed formulation showing more than 85% drug release within 45 minutes. The in vitro release data was well-fitted into zero-order and the values of release exponent ‘n’ were between 0.303 and 0.514. The high similarity factor f2 of 64.50 was achieved with the best batch in comparison to the marketed tablets. The results obtained indicated that the gum Acacia arabica performed as well as gelatin compared to the other binders for the Ofloxacin tablet formulation. PMID:24959411

Mistry, Amisha K.; Nagda, Chirag D.; Nagda, Dhruti C.; Dixit, Bharat C.; Dixit, Ritu B.

2014-01-01

109

Efficacy and safety of sodium phosphate tablets compared with PEG solution in colon cleansing: Two identically designed, randomized, controlled, parallel group, multicenter phase III trials  

Microsoft Academic Search

Background: Liquid purgatives for cleansing before colonoscopy often are poorly tolerated. A sodium phosphate tablet has been developed to provide equivalent efficacy with better patient tolerance. These 2 studies compare the safety, efficacy, and patient acceptance of the tablet (Visicol) to a polyethylene glycol (PEG) solution in adults undergoing colonoscopy. Methods: Two identically designed, randomized, investigator-blinded, multicenter trials were performed.

David Kastenberg; Richard Chasen; Cuckoo Choudhary; Dennis Riff; Stephen Steinberg; Eric Weiss; Lawrence Wruble

2001-01-01

110

Desktop 3D printing of controlled release pharmaceutical bilayer tablets.  

PubMed

Three dimensional (3D) printing was used as a novel medicine formulation technique for production of viable tablets capable of satisfying regulatory tests and matching the release of standard commercial tablets. Hydroxypropyl methylcellulose (HPMC 2208) (Methocel™ K100M Premium) and poly(acrylic acid) (PAA) (Carbopol(®) 974P NF) were used as a hydrophilic matrix for a sustained release (SR) layer. Hypromellose(®) (HPMC 2910) was used as a binder while microcrystalline cellulose (MCC) (Pharmacel(®) 102) and sodium starch glycolate (SSG) (Primojel(®)) were used as disintegrants for an immediate release (IR) layer. Commercial guaifenesin bi-layer tablets (GBT) were used as a model drug (Mucinex(®)) for this study. There was a favourable comparison of release of the active guaifenesin from the printed hydrophilic matrix compared with the commercially available GBT. The printed formulations were also evaluated for physical and mechanical properties such as weight variation, friability, hardness and thickness as a comparison to the commercial tablet and were within acceptable range as defined by the international standards stated in the United States Pharmacopoeia (USP). All formulations (standard tablets and 3D printed tablets) showed Korsmeyer-Peppas n values between 0.27 and 0.44 which indicates Fickian diffusion drug release through a hydrated HPMC gel layer. PMID:24280018

Khaled, Shaban A; Burley, Jonathan C; Alexander, Morgan R; Roberts, Clive J

2014-01-30

111

Childhood disintegrative disorder  

MedlinePLUS

... had already learned The condition is similar to autistic disorder ( autism ). ... such as childhood schizophrenia or pervasive developmental disorder (autism). The most important sign of childhood disintegrative disorder ...

112

[Tableting technology of a dry extract from Solidago virgaurea L. with the use of silicified microcrystalline cellulose (Prosolv) and other selected auxiliary substances].  

PubMed

Direct tableting is simpler and more cost-effective from the point of view of good manufacturing practice (GMP) than wet granulation or dry compacting. Moreover, the use of dry plant extracts in the process of direct tableting, omitting granulation, decreases the possibility of biological activity loss of active substances. Thus, pharmaceutical industry uses this particular process more and more frequently. Only few therapeutic substances form under compression tablets meeting current requirements. Very often addition of auxiliary substances appears to be indispensable. The aim of this study was to obtain uncoated tablets by the method of direct tableting with the use of selected auxiliary substances. Dry extract from Solidago virgaurea L. was the study material. Shrimp chitosan, silicified microcrystalline cellulose (Prosolv), polyvinylpyrrolidone, calcium carbonate and sodium stearyl fumarate were used as auxiliary substances. Eleven tablet batches were manufactured in a reciprocating instrumented tableting machine (Ewreka). The produced tablets were subjected to morphological tests comprising the tablet size, determination of batching accuracy (determination of mass uniformity of individual tablets), test of mechanical resistance (crushing strength), determination of disintegration time. The statistical hardness of the manufactured tablets was also estimated. Pharmaceutical availability tests were performed of the biologically active substances released from tablets to the acceptor fluid. The study was based on general and detailed regulations of Polish Pharmacopoeia VII (PP VII). The obtained results allow to conclude that the applied auxiliary substances appeared to be useful in adequate proportions in manufacturing tablets containing dry extract from Solidago virgaurea L. The properties of the obtained batches of tablets were in majority consistent with the current requirements. The applied method provides technological reproducibility and high durability of the drug. These tablets as compared to available herbal mixtures and aqueous extracts can be a more comfortable form of a drug. PMID:20099736

Marczyi?ski, Zbigniew

2009-01-01

113

Comparative bioavailability study of two controlled-release pentoxifylline tablet preparations.  

PubMed

The bioavailability of a generic preparation of pentoxifylline sustained-release (SR) tablet was evaluated in comparison with a proprietary product (Trental 400). For the study, 12 healthy male volunteers participated; the study was conducted according to a randomized, two-way crossover design. The bioavailability was compared using the parameters total area under the plasma level-time curve AUC0-infinity, peak plasma concentration Cmax, and time to reach peak plasma concentration Tmax. No statistically significant difference was observed between the values of the two products in all three parameters. The 90% confidence interval for the ratio of the logarithmic transformed AUC0-infinity values of the generic pentoxifylline over those of Trental 400 was found to lie between 0.83 and 1.00, while that of the parameter Cmax was between 0.91 and 1.29. In addition, elimination half-life t1/2 and apparent volume of distribution Vd were calculated. There was no statistically significant difference between the t1/2 Vd values obtained from the data of the two preparations. PMID:10872103

Yuen, K H; Wong, J W; Peh, K K; Julianto, T; Choy, W P

2000-07-01

114

A comparative study between conventional pan coater and quasi-continuous small batch coater on the stability of tablets containing acetylsalicylic acid.  

PubMed

The Supercell coater was developed as an in-line small batch tablet coater which uses air-fluidization for tablet coating. Coating time is very much reduced, with improved heat and mass transfer. It was hypothesized that the quasi-continuous Supercell coating process was more suitable for the aqueous coating of tablets containing moisture-sensitive drugs. Acetylsalicylic acid (ASA) was used as the model drug in this study. The extent of ASA degradation in Supercell coating was compared against that of tablets coated using the conventional pan coater. Less than 0.3% of ASA was degraded at the end of the coating process using either coater. The extent of ASA degradation was found to be more pronounced during storage. The Supercell coated tablets exhibited comparable or smaller percentage of ASA degradation than the pan coated tablets at the end of a storage period of 6months under accelerated stability conditions (40°C/75% RH) and 3years under ambient conditions (25°C/50% RH). The extent and rate of ASA degradation during storage were dependent on the processing conditions employed during Supercell coating. Increase in temperature generally led to a reduction in ASA degradation, while increase in spray rate and coating level caused more degradation. Greater extent of ASA degradation was observed on the surface of pan coated tablets compared with Supercell coated tablets due to greater moisture contact and the slower and wetter coating process. Changes to the processing conditions also influenced the residual moisture content (0.55-2.86%) of the tablets. However, no direct correlation between the residual moisture content of the tablets after coating and the extent of ASA degradation during storage was found. PMID:25448074

Cahyadi, Christine; Chan, Lai Wah; Heng, Paul Wan Sia

2014-11-15

115

Stability of freeze-dried tablets at different relative humidities.  

PubMed

The purpose of the study was to evaluate the stability of two different freeze-dried tablet formulations at different relative humidities (RHs). The tablets contained 25 mg hydrochlorothiazide (HCT) as a model drug and were prepared by freeze-drying a suspension and an oil-in-water (o/w) emulsion. Formulation A was a rapidly disintegrating tablet and consisted of 80 mg of maltodextrine DE38; 8 mg of polyethyleneglycol (PEG 6000), 8 mg of xanthan gum, and 25 mg of HCT. Formulation B was a lyophilized dry emulsion tablet that consisted of 160 mg of Miglyol 812, 80 mg of maltodextrin DE38, 16 mg of methylcellulose (Methocel) A15LV, and 25 mg of HCT. Tablets were packaged in different packing materials: polyvinylchloride (PVC)/aluminum blister packs, PVC-polyvinylidenechloride (PVDC)/aluminum blister packs, closed containers with a dessicant tablet, and open containers. The tablets were stored at three relative humidities (45%, 60%, and 85% RH) and were characterized on mechanical strength, residual moisture, porosity, content uniformity, and scanning electron microscopy (SEM) during a period of 6 months. After 1 month at 60% and 85% RH, a strong increase in moisture content (from 2.7% to 6.8%) was seen for the tablets packed in the open and closed containers and for the PVC/aluminum blistered tablets. This increase was higher for formulation A compared to formulation B since B contained 160 mg of triglycerides and was more hydrophobic. This increase in water content was correlated with a decrease in mechanical strength. The tablets also showed a change in microstructure and porosity. At a moisture content of 7.2%, formulation A showed a structural "collapse" since water acts as a plasticizer for the amorphous glass, lowering the glass transition temperature Tg. This phenomenon even occurred in PVC/aluminum blister packs at 85% RH. The structural collapse was associated with a complete loss of microstructure as detected by porosimetric analysis and SEM. For the PVC-PVDC/aluminum blistered tablets, the increase in moisture content and decrease in mechanical strength at 85% RH occurred much slower, and the water uptake and strength loss were less intensive. No significant breakdown of HCT could be observed in both formulations with all of the packing materials. Packaging of freeze-dried tablets with PVC/aluminum blister packs, PVC/PVDC/aluminum blister packs, or closed containers did not offer protection against moisture uptake, mechanical strength loss, and structural collapse. PMID:10518240

Corveleyn, S; Remon, J P

1999-09-01

116

[Applicability of a natural swelling matrix as the propellant of osmotic pump tablets].  

PubMed

The purpose of this study is to investigate the applicability of a natural swelling matrix derived from boat-fruited sterculia seed (SMS) as the propellant of osmotic pump tablets. The sugar components, static swelling, water uptake and viscosity of SMS were determined and compared with that of polythylene oxide (WSR-N10 and WSR-303). Both ribavirin and glipizide were used as water-soluble and water-insoluble model drugs. Then, the monolayer osmotic pump tablets of ribavirin and the bilayer osmotic pump tablets of glipizide were prepared using SMS as the osmotically active substance and propellant. SMS was mainly composed of rhamnose, arabinose, xylose and galactose and exhibited relatively high swelling ability. The area of the disintegrated matrix tablet was 20.1 times as that at initial after swelling for 600 s. SMS swelled rapidly and was fully swelled (0.5%) in aqueous solution with relative low viscosity (3.66 +/- 0.03) mPa x s at 25 degrees C. The monolayer osmotic pump tablets of ribavirin and the bilayer osmotic pump tablets of glipizide using SMS as propellant exhibited typical drug release features of osmotic pumps. In conclusion, the swelling matrix derived from boat-fruited sterculia seed, with low viscosity and high swelling, is a potential propellant in the application of osmotic pump tablets. PMID:24187843

Wu, Li; Li, Hai-Yan; Yin, Xian-Zhen; Li, Ying; Chen, Jian-Xiu; Hu, Rong-feng; Zhang, Ji-Wen

2013-08-01

117

A comparative clinical study of Shatapatrayadi churna tablet and Patoladi yoga in the management of Amlapitta  

PubMed Central

Amlapitta is a very common disease caused by Vidagdha Pitta with features such as Amlodgara, Hrid Kantha Daha, and Avipaka. This is a burning problem of the society. Irregular and improper food habits, and busy stressful lifestyle is one of the main culprit. Amlapitta is the GI disorder described in Ayurvedic texts that closely resembles with Gastritis in modern science. In chronic stage, it may lead to ulcerative conditions. In this study, total 41 patients were registered and were randomly divided into two groups. In group A, Shatapatrayadi churna tablet and in group B Patoladi Yoga tablet were given for 1 month. The Nidana, signs, and symptoms were observed carefully to get idea about the Samprapti of the disease. The effect of Patoladi Yoga on Roga Bala is 65.79%, 62.11% on Agni Bala, and 63.35% on Deha and Chetasa bala. The overall relief was 63.75%. The effect of Shatapatrayadi tablet on Roga Bala was 71.94%, 73.15% on Agni Bala, and 77.68% on Deha and Chetas Bala. The overall relief was 74.25%. PMID:22529651

Kumar, Jitendra; Dave, Alankruta R.; Vyas, Madhuri G.

2011-01-01

118

Development and Evaluation of Melt-in-Mouth Tablets of Metoclopramide Hydrochloride Using Novel Co-processed Superdisintegrants.  

PubMed

In the present investigation, a novel multifunctional co-processed superdisintegrants consisting of crospovidone and Kyron T-314 were fabricated by solvent evaporation method to develop melt-in-mouth tablets of metoclopramide hydrochloride with a view to enhance patient compliance by direct compression method. The simple physical blends and co-processed mixture of superdisintegrants were characterized for angle of repose, bulk density, tapped density, Carr's index, Hausner's ratio and compatibility studies by FTIR spectroscopy. Melt-in-mouth tablets of metoclopramide hydrochloride were prepared using the physical blends and co-processed mixture of superdisinterants and were evaluated for hardness, friability, in vitro disintegration time, in vitro dispersion time, wetting time, water absorption ratio, drug content, in vitro drug release and accelerated stability study at 40±2° temperature and 75±5% relative humidity. Among the tablets evaluated, formulation F-X prepared by adding co-processed superdisintegrants in ratio of 1:1 showed minimum in vitro dispersion time of 9.71±0.021 s, in vitro disintegration time of 5.70±0.117 s and higher amount of drug release of 99.695±0.29% at the end of 1 min. Formulation F-X was emerged as the overall best formulation based on drug release characteristics in pH 6.8 phosphate buffer compared with the tablets obtained from conventional method of manufacture as well as with marketed preparation. Analysis of drug release data indicated that formulation F-X followed first order kinetics. This study revealed that the co-processed mixture of superdisintegrants have excellent flow properties, high compressibility, render low disintegration time to tablets and have better binding properties as compared to physical blends of superdisintegrants. These materials can be a good substitute for inert superdisintegrants, which are normally used in tablet manufacturing. PMID:25425756

Ladola, M K; Gangurde, A B

2014-09-01

119

Hexagonal boron nitride as a tablet lubricant and a comparison with conventional lubricants.  

PubMed

The objective of this study was to investigate the lubrication properties of hexagonal boron nitride (HBN) as a new tablet lubricant and compare it with conventional lubricants such as magnesium stearate (MGST), stearic acid (STAC), and glyceryl behenate (COMP). Tablets were manufactured on an instrumented single-station tablet press to monitor lower punch ejection force (LPEF) containing varied lubricants in different ratio (0.5, 1, 2%). Tablet crushing strength, disintegration time and thickness were measured. Tensile strength of compacted tablets were measured by applying a diametrical load across the edge of tablets to determine mechanical strength. The deformation mechanism of tablets was studied during compression from the Heckel plots with or without lubricants. MGST was found to be the most effective lubricant based on LPEF-lubrication concentration profile and LPEF of HBN was found very close to that of MGST. HBN was better than both STAC and COMP. A good lubrication was obtained at 0.5% for MGST and HBN (189 and 195N, respectively). Where COMP and STAC showed 20 and 35% more LPEF compare to that of MGST (239 and 288N, respectively). Even at the concentration of 2% COMP and STAC did not decrease LPEF as much as 0.5% of MGST and HBN. Like all conventional lubricants the higher the concentration of HBN the lower the mechanical properties of tablets because of its hydrophobic character. However, this deterioration was not as pronounced as MGST. HBN had no significant effect on tablet properties. Based on the Heckel plots, it was observed that after the addition of 1% lubricant granules showed less plastic deformation. PMID:18160235

U?urlu, Timuçin; Turko?lu, Murat

2008-04-01

120

Formulation of fenofibrate liquisolid tablets using central composite design.  

PubMed

Liquisolid technique has been widely used to enhance the dissolution of poorly water soluble drugs. The present investigation is on formulation of liquisolid tablets of fenofibrate, a lipid lowering agent. Liquisolid formulation was prepared by applying central composite design (CCD) to optimize various formulation parameters. Amounts of PEG 600 (X1), Avicel PH 102 (X2), and Aerosil 200 (X3) were selected as independent variables while the angle of repose, hardness, disintegration time, and T90% (time required to release 90% drug) of liquisolid tablets were selected as dependent variables. Optimization of formulation was done by multiple linear regression analysis. The results indicated amounts of PEG 600 and Aviel PH 102 show greater effect on dependant variables. In vitro dissolution of fenofibrate in liquisolid formulations was enhanced compared to the pure form. To conclude, Liquisolid technique is a promising strategy in improving dissolution of poorly water soluble fenofibrate. PMID:24712439

Patel, Tejas; Patel, L D; Suhagia, B N; Soni, Tejal; Patel, Tushar

2014-01-01

121

Comparative effect of Navayasa Rasayana Leha and Medhya Rasayana tablet along with Dhatryadhyo Lepa in Ekkakushta (psoriasis)  

PubMed Central

All skin diseases can be included under the umbrella of Kushta Roga. Ekkakushta is a variety of Kshudra Kushtha with dominancy of Vata and Kapha Doshas. It is characterized by symptoms like- Aswedanam, Mahavastum, Matsyashakalopamam, etc., these characteristic features has a striking similarity with Psoriasis. It is a papulosqaumous disorder of the skin, characterized by sharply defined erythmatosqaumous lesion. Due to its chronic and recurrent nature, it has a great impact on the quality of life of the patients. The present study was aimed to compare the effect of Navayasa Rasayana Leha and Medhya Rasayana tablet along with Dhatryadhyo Lepa in patients of Ekkakushta (psoriasis). For this study, the selected patients were randomly divided into two groups. Koshtha Shuddhi was done by Eranda Bruhstha Haritaki (6 g-at night with Ushnodaka) in patients of both the groups for 3 days before starting the treatment. Total 111 patients were selected for present study. Patients of group A (45 patients) were given “Navayasa Rasayana Leha” and “Dhatryadhyo Lepa” for external application. Stress is a very well known precipitating factor of Psoriasis. Hence, to study the efficacy of Medhya Rasayana drugs, patients of group B (49 patients) were given Medhya Rasayana tablet along with the external application of Dhatryadhyo Lepa. The duration of the study was 3 months with follow up for one month. Both the groups showed highly significant results in all signs, symptoms and other parameters. Navayasa Rasayana Leha and Medhya Rasayana tablet along with Dhatryadhyo Lepa can be used effectively for the treatment of Ekkakushta. PMID:24501516

Mehta, Charmi S.; Dave, Alankruta R.; Shukla, V. D.

2013-01-01

122

Three-day therapy of vaginal candidiasis with clotrimazole vaginal tablets and econazole ovules: a multicenter comparative study.  

PubMed

The activity and tolerance of 200 mg clotrimazole vaginal tablets and 150 mg econazole vaginal ovules were compared in the treatment of vaginal candidiasis in a controlled multicenter (3 centers) study. Treatment was allocated according to a randomized list and each investigator treated 20 patients per group. Duration of therapy was 3 days. Follow-up investigations were carried out approximately 1 and 4 weeks after commencement of treatment. The results were analyzed for 54 patients treated with clotrimazole and 57 with econazole; 9 patients were excluded from the analysis because of insufficient data. At the first follow-up examination, 1 week after starting therapy, 93.7% of patients on clotrimazole and 83.7% of patients on econazole had negative cultures. The success of therapy, as judged by the clinicians, was 95.8% for clotrimazole and 88.0% for econazole. For the first and fourth week combined reviews, 86.0% of clotrimazole patients and 77.8% of econazole patients had negative cultures and the success of therapy was 88.4% for clotrimazole and 80.0% for econazole. These differences were not statistically significant but there was a clear numerical superiority for clotrimazole. Tolerance was good in all the patients and no side-effects were observed. One can conclude that the treatment of vaginal candidiasis with a 200-mg vaginal tablet of clotrimazole over 3 days is highly effective and comparable with other established treatment regimes. PMID:6761088

Stettendorf, S; Benijts, G; Vignali, M; Kreysing, W

1982-01-01

123

Childhood disintegrative disorder  

PubMed Central

We are presenting a case of a 10-year-old female child who presented with normal development till 5 years of age followed by deterioration in previously acquired language and social skills with stereotypic hand movements suggestive of childhood disintegrative disorder. This case is reported as this condition is very rare. PMID:22837782

Charan, Sri Hari

2012-01-01

124

Double-blind evaluation of miconazole tampons, compared with clotrimazole vaginal tablets, in vaginal candidiasis.  

PubMed

Fifty-one patients with vaginal candidiasis and positive cultures in Nickerson medium were treated either with two miconazole tampons daily for five days (26 patients, median age 28 years) or with one clotrimazole vaginal tablet daily for six days (25 patients, median age 36 years) in a randomized double-blind trial. Seven days after the end of the treatment, 24 (92%) patients in the miconazole group and 19 (76%) in the clotrimazole group had negative cultures. One month after the end of the treatment, the relapse rate was significantly (P less than 0.05) higher in the clotrimazole group. Symptoms subsided rapidly in both groups. No unwanted effects were reported. PMID:7307036

Lolis, D; Kanellopoulos, N; Liappas, I; Xyngakis, A; Zissis, N P

1981-01-01

125

Properties of Delonix regia seed gum as a novel tablet binder.  

PubMed

The mechanical and disintegration properties of paracetamol tablets formulated using Delonix regia seed gum (DRSG) as a binder have been studied in this work. Acacia BP (ACG) and tragacanth BP (TRG) were used as official gum standards. The mechanical properties, i.e. tensile strength (TS) and brittle fracture index (BFI), showed that with an increase in concentration of the gum binder, the tensile strength increased while the BFI was reduced. The crushing strength - friability/disintegration time ratio used to analyze the disintegration properties gave a rank order: tablets containing DRSG > tablets containing ACG > tablets containing TRG at 1%, w/w binder concentration while for higher binder concentrations, the rank order is: tablets containing ACG > tablets containing TRG > tablets containing DRSG. The results suggest that while Delonix regia seed gum may be useful as a binder, its use at a low concentration will improve the balance between the binding and disintegration properties of tablets when a faster disintegration is desired, while its use at a high concentration could serve the desire for a modified or sustained release tablet formulation. PMID:19702177

Adetogun, Gbadegesin E; Alebiowu, Gbenga

2009-01-01

126

Influence of Prosolv and Prosolv:Mannitol 200 direct compression fillers on the physicomechanical properties of atorvastatin oral dispersible tablets.  

PubMed

Abstract The objective of the present study was to evaluate the influence of Prosolv® and Prosolv®: Mannitol 200 direct compression (DC) fillers on the physicomechanical characteristics of oral dispersible tablets (ODTs) of crystalline atorvastatin calcium. ODTs were formulated by DC and were analyzed for weight uniformity, hardness, friability, drug content, disintegration and dissolution. Three disintegration time (DT) test methods; European Pharmacopoeia (EP) method for conventional tablets (Method 1), a modification of this method (Method 2) and the EP method for oral lyophilisates (Method 3) were compared as part of this study. All ODTs showed low weight variation of <2.5%. Prosolv® only ODTs showed the highest tablet hardness of ?73?N, hardness decreased with increasing mannitol content. Friability of all formulations was <1% although friability of Prosolv®:Mannitol ODTs was higher than for pure Prosolv®. DT of all ODTs was <30?s. Method 2 showed the fastest DT. Method 3 was non-discriminatory giving a DT of 13-15?s for all formulations. Atorvastatin dissolution from all ODTs was >60% within 5?min despite the drug being crystalline. Prosolv® and Prosolv®:Mannitol-based ODTs are suitable for ODT formulations by DC to give ODTs with high mechanical strength, rapid disintegration and dissolution. PMID:24397821

Gowda, Veeran; Pabari, Ritesh M; Kelly, John G; Ramtoola, Zebunnissa

2014-01-01

127

Pharmacokinetic profile and clinical efficacy of a once-daily ondansetron suppository in cyclophosphamide-induced emesis: a double blind comparative study with ondansetron tablets  

Microsoft Academic Search

We investigated the pharmacokinetic profile and the efficacy of ondansetron (day 1) given as 16 mg suppository once a day, as compared with ondansetron 8 mg tablets twice daily, in patients receiving moderately emetogenic chemotherapy. The study was primarily aimed at investigating the pharmacokinetics and was part of a large multinational, randomised, double-blind, double-dummy efficacy trial. Pharmacokinetic data were obtained

R de Wit; JH Beijnen; O van Tellingen; JHM Schellens; M de Boer-Dennert; J Verweij

1996-01-01

128

Comparing the Therapeutic Effects of Garlic Tablet and Oral Metronidazole on Bacterial Vaginosis: A Randomized Controlled Clinical Trial  

PubMed Central

Background: Bacterial vaginosis (BV) is one of the most common gynecological infections during reproductive age. Although metronidazole is one of the most effective medications recommended as the first-line treatment, it has various side effects. Because of the side effects and contraindications of some chemical medicines, using herbs has been investigated in treating BV. Objectives: The aim of this study was to compare the effect of garlic tablet (Garsin) and oral metronidazole in clinical treatment of the BV in women referred to Resalat Health Center, affiliated with Mazandaran University of Medical Sciences, in 2013. Patients and Methods: This randomized clinical trial was conducted on 120 married women aged 18 to 44 years who were diagnosed with BV by Amsel’s clinical criteria and Gram staining. Enrolled women were randomly allocated to two groups of 60 patients and were treated with either garlic tablet or oral metronidazole for seven days. Amsel’s criteria and Gram stain were assessed seven to ten days after beginning the treatment period and side effects were registered. Results: Amsel’s criteria were significantly decreased after treatment with garlic or metronidazole (70% and 48.3%, respectively; P < 0.001). Therapeutic effects of garlic on BV were similar to that of metronidazole (63.3% and 48.3%, respectively; P = 0.141). There were significant differences between the two treatment groups in terms of side effects; metronidazole was associated with more complications (P = 0.032). Conclusions: This study reveals that garlic could be a suitable alternative for metronidazole in treatment of BV in those interested in herbal medicines or those affected by side effects of metronidazole. PMID:25237588

Mohammadzadeh, Farnaz; Dolatian, Mahrokh; Jorjani, Masoome; Alavi Majd, Hamid; Borumandnia, Nasrin

2014-01-01

129

Technology of dispensing check based-on tablet features  

Microsoft Academic Search

This paper designs and realizes a bagged tablets checking system. First, according to tablet characteristics, color feature library and shape feature library are created. Second, the tablet image is clustered by K-means algorithm. And threshold segmentation for the tablet image use Ostu method. Finally, the recognition result of sorts of tablets in bag will compare with prescription in database written

Dong Yin; Jun Xu; Song Wang

2011-01-01

130

Lallemantia reylenne seeds as superdisintegrant: Formulation and evaluation of nimesulide orodispersible tablets  

PubMed Central

Aim: Orodispersible tablets also known as fast dissolving tablets disintegrate instantaneously within the mouth and thus can be consumed without water. The present study was aimed to formulate orodispersible tablets of nimesulide by using Lallemantia reylenne seeds as natural superdisintegrant. Materials and Methods: Powdered lallemantia seeds were characterized for powder flow properties (bulk density, tapped density, carr's consolidation index, hausner ratio, angle of repose), swelling index, viscosity, pH, and loss on drying. The prepared tablets were evaluated for different tablet parametric tests, wetting time, water absorption ratio, effective pore radius, porosity, packing fraction, in vitro and in vivo disintegration time, in vitro dissolution and stability studies. Results and Discussion: Increase in Lallementia reylenne concentration had an appreciable effect on tablet hardness and friability which clearly indicated binding potential of the seeds. Water absorption ratio increased with increase in Lallemantia reylenne concentration from batch A1 to A4. Water uptake coupled natural polymer swelling could be the most probable mechanism for concentration dependent reduction in disintegration time by the Lallemantia reylenne seeds. Porosity of the formulated tablets was found to increase from batch A1-A4. The in vitro disintegration results were in line with in vivo disintegration results. Conclusion: It could be concluded that Lallemantia reylenne seeds could be used as natural superdisintegrant in the formulation of orodispersible tablets. PMID:23071942

Malik, Karan; Arora, Gurpreet; Singh, Inderbir; Arora, Sandeep

2011-01-01

131

Satellite disintegration dynamics  

NASA Technical Reports Server (NTRS)

The subject of satellite disintegration is examined in detail. Elements of the orbits of individual fragments, determined by DOD space surveillance systems, are used to accurately predict the time and place of fragmentation. Dual time independent and time dependent analyses are performed for simulated and real breakups. Methods of statistical mechanics are used to study the evolution of the fragment clouds. The fragments are treated as an ensemble of non-interacting particles. A solution of Liouville's equation is obtained which enables the spatial density to be calculated as a function of position, time and initial velocity distribution.

Dasenbrock, R. R.; Kaufman, B.; Heard, W. B.

1975-01-01

132

Phase transformation in thiamine hydrochloride tablets: Influence on tablet microstructure, physical properties, and performance.  

PubMed

The objective of this article was to monitor phase transformation in thiamine hydrochloride, from a nonstoichiometric hydrate (NSH) to a hemihydrate (HH), in stored tablets, prepared both by direct compression and wet granulation, and to relate the storage-induced phase transformation with changes in tablet microstructure, physical properties, and performance. Raman spectroscopy revealed complete NSH ? HH transformation in tablets, within 30 h of storage at 40°C/75% relative humidity. When the tablets were prepared by wet granulation of NSH alone, there was a marked increase in both tablet volume and hardness on storage. However, when microcrystalline cellulose (MCC) was included in granulation, the resulting stored tablets also exhibited a pronounced increase in disintegration time. In contrast, tablets prepared by dry processing via compression of a NSH-MCC physical mixture did not exhibit any changes in properties, despite the in situ solid form conversion. Scanning electron microscopy revealed growth of needle-like HH crystals in all stored tablets and mercury porosimetry revealed considerable changes in the pore size distribution during storage. Longer storage led to crystal growth (Ostwald ripening), causing further gradual but less dramatic changes in properties. The phase transformation and the complex interparticulate associations in the tablet influenced the changes in tablet microstructure, compact physical properties, and product behavior. PMID:22213350

Chakravarty, Paroma; Suryanarayanan, Raj; Govindarajan, Ramprakash

2012-04-01

133

Effect of silicification on the tableting performance of cellulose ii: a novel multifunctional excipient.  

PubMed

The effect of silicification on the tableting performance of microcrystalline cellulose II (MCCII) was assessed through coprocessing with fumed silica via spray drying and wet granulation at the 98:2, 95:5, 90:10 and 80:20 ratios. Compacts produced by spray drying and wet granulation rendered better tensile strength than MCCII. The Kawakita and Heckel models implied that silicification increased compressibility and decreased the plastic deforming behavior and densification by die filling at the early stage of compression for MCCII. It also decreased the sensitivity to hydrophobic lubricants such as magnesium stearate, especially for the spray-dried products due to the competing effect with magnesium stearate. Further, silicification decreased the high elastic recovery typical of MCCII due to the increase in specific surface area and fragmenting behavior which contributed to the formation of stronger compacts. Moreover, silicification did not affect the fast disintegrating properties and release rates of poorly soluble drugs such as griseofulvin formulated in tablets compared to those of Prosolv® SMCC 50 and Prosolv® SMCC 90. The new silicified materials are appropriate to formulate fast disintegrating tablets by direct compression. PMID:22689398

Rojas, John; Kumar, Vijay

2012-01-01

134

Disintegration of a Liquid Jet  

NASA Technical Reports Server (NTRS)

This report presents an experimental determination of the process of disintegration and atomization in its simplest form, and the influence of the physical properties of the liquid to be atomized on the disintegration of the jet. Particular attention was paid to the investigation of the process of atomization.

Haenlein, A

1932-01-01

135

Single-dose 500-mg clotrimazole vaginal tablets compared with placebo in the treatment of Candida vaginitis.  

PubMed

In a double-blind controlled clinical trial, 29 practitioners randomized 55 women with culture-proven Candida vaginitis to treatment with single-dose 500-mg clotrimazole vaginal tablets, and 40 to placebo. At a follow-up visit 7 to 10 days after treatment, Candida was present in 21 (38%) of those treated with clotrimazole and in 30 (75%) in the placebo group (P less than .05). Symptoms had improved or disappeared in 38 (69%) treated with clotrimazole, compared with 22 (55%) in the placebo group (P greater than .05). In 10 (23%) of the mycologically cured women, symptoms were unchanged or worse, whereas symptoms had improved or disappeared in 26 (51%) in whom Candida was isolated at the follow-up visit (P = .015). Questionnaires sent to the 95 women 4 weeks after the follow-up visit were returned by 62. Vaginal symptoms were reported by 50% in both groups. Further clinical trials including placebo are needed in general practice in the evaluation of the treatment of Candida vaginitis. PMID:2199599

Bro, F

1990-08-01

136

Three-day therapy of vaginal candidiasis with clotrimazole vaginal tablets and econazole ovules: a multicentre comparative study.  

PubMed

The activity and tolerance of 200 mg clotrimazole vaginal tablets and 150 mg econazole vaginal ovules were compared in the treatment of vaginal candidiasis in a controlled multicentre (3 centres) study. Treatment was allocated according to a randomized list and each investigator treated 20 patients per group. The duration of therapy was 3 days. Follow-up investigations were carried out approximately 1 week and 4 weeks after commencement of treatment. The results were analyzed for 54 patients treated with clotrimazole and 57 with econazole: 9 patients were excluded from the analysis because of insufficient data. At the first follow-up examination, 1 week after starting therapy, 93.7% of patients on clotrimazole and 83.7% of patients on econazole had negative cultures. The success of therapy, as judged by the clinicians, was 95.8% for clotrimazole and 88.0% for econazole. For the first and fourth week combined reviews, 86.0% of clotrimazole patients and 77.8% of econazole patients had negative cultures and the success of therapy was 88.4% for clotrimazole and 80.0% for econazole. These differences were not statistically significant but there was a clear numerical superiority for clotrimazole. Tolerance was good in all the patients and no side-effects were observed. PMID:7428415

Benijts, G; Vignalli, M; Kreysing, W; Stettendorf, S

1980-01-01

137

Comparative Studies on the Dissolution Profiles of Oral Ibuprofen Suspension and Commercial Tablets using Biopharmaceutical Classification System Criteria  

PubMed Central

In vitro dissolution studies for solid oral dosage forms have recently widened the scope to a variety of special dosage forms such as suspensions. For class II drugs, like Ibuprofen, it is very important to have discriminative methods for different formulations in physiological conditions of the gastrointestinal tract, which will identify different problems that compromise the drug bioavailability. In the present work, two agitation speeds have been performed in order to study ibuprofen suspension dissolution. The suspensions have been characterised relatively to particle size, density and solubility. The dissolution study was conducted using the following media: buffer pH 7.2, pH 6.8, 4.5 and 0.1 M HCl. For quantitative analysis, the UV/Vis spectrophotometry was used because this methodology had been adequately validated. The results show that 50 rpm was the adequate condition to discriminate the dissolution profile. The suspension kinetic release was found to be dependent on pH and was different compared to tablet release profile at the same experimental conditions. The ibuprofen release at pH 1.0 was the slowest. PMID:23626386

Rivera-Leyva, J. C.; García-Flores, M.; Valladares-Méndez, A.; Orozco-Castellanos, L. M.; Martínez-Alfaro, M.

2012-01-01

138

Disintegration of liquid sheets  

NASA Technical Reports Server (NTRS)

The development, stability, and disintegration of liquid sheets issuing from a two-dimensional air-assisted nozzle is studied. Detailed measurements of mean drop size and velocity are made using a phase Doppler particle analyzer. Without air flow the liquid sheet converges toward the axis as a result of surface tension forces. With airflow a quasi-two-dimensional expanding spray is formed. The air flow causes small variations in sheet thickness to develop into major disturbances with the result that disruption starts before the formation of the main break-up region. In the two-dimensional variable geometry air-blast atomizer, it is shown that the air flow is responsible for the formation of large, ordered, and small chaotic 'cell' structures.

Mansour, Adel; Chigier, Norman

1990-01-01

139

Comparative evaluation of drug release from aged prolonged polyethylene oxide tablet matrices: effect of excipient and drug type.  

PubMed

Abstract Polyethylene oxide (PEO) undergoes structural adjustments caused by elevated temperatures, which results in loss of its stability within direct compression tablets. The aim of this study was to evaluate the influence of filler solubility on the drug delivery process of matrix tablets containing drugs with different water-solubility properties and stored at elevated temperature. The results demonstrated that in the case of propranolol HCl (highly water-soluble) tablet matrices, soluble lactose promoted drug release, whereas, a stable release of drug was observed with insoluble DCP. A drug release pattern similar to the propranolol HCl formulation containing DCP was obtained for hydrophilic matrix tablets containing either lactose or DCP for the less water-soluble drug, zonisamide. In the case of the partially water-soluble drug, theophylline, formulated with lower molecular weight PEO 750, drug release increased considerably in the presence of both fillers with increasing storage time, however a stable release rate (similar to fresh samples) was observed in the case of higher molecular weight PEO 303 tablet matrices containing theophylline with either lactose or DCP. The hydration properties (e.g. solubility) of the diluents had a considerable effect on drug release behavior from various model matrices; this effect was dependent on both molecular weight of PEO and solubility of drug. PMID:25410967

Shojaee, Saeed; Kaialy, Waseem; Cumming, Kenneth Iain; Nokhodchi, Ali

2014-11-20

140

Isolation and characterization of jackfruit mucilage and its comparative evaluation as a mucoadhesive and controlled release component in buccal tablets  

PubMed Central

Background: The purpose of the present research work was to extract jackfruit mucilage, use it as a mucoadhesive agent, and to develop extended release buccoadhesive tablets with an intention to avoid hepatic first-pass metabolism, by enhancing residence time in the buccal cavity. Materials and Methods: The mucilage was isolated from the jackfruit pulp by the aqueous extraction method and characterized for various physiochemical parameters as well as for its adhesive properties. Three batches of tablets were prepared (wet granulation method) and evaluated containing three mucoadhesive components: Methocel K4M, Carbopol 974P, and isolated jackfruit mucilage using chlorpheniramine maleate (CPM) as a model drug and changing the proportion of the mucoadhesive component (1:2:3), resulting in nine different formulations. Results: The results of the study indicate that the isolated mucilage had good physicochemical and morphological characteristics, granules and tablets conformed to the Pharmacopoeial specifications, and in vitro release studies showed the sustained action of drug with increasing concentration of the isolated natural mucoadhesive agent in the formulations. Permeability studies indicated that changing the mucoadhesive component, permeability behavior was not statistically different (P > 0.05). FTIR and UV spectroscopy studies between mucilage and CPM suggested the absence of a chemical interaction between CPM and jackfruit mucilage. Conclusion: The developed mucoadhesive tablets for buccal administration containing natural mucilage (MF3) have a potential for the sustained action of drug release. Thus, mucoadhesive tablets for controlled release were successfully developed using natural jackfruit mucilage. PMID:23119234

Sabale, Vidya; Patel, Vandana; Paranjape, Archana

2012-01-01

141

In vitro determination of aceclofenac Mouth Dissolving Tablets.  

PubMed

In the present study, Mouth Dissolving Tablets (MDTs) of aceclofenac were formulated by direct compression technique. Sodium starch glycolate and crospovidone were employed as superdisintegrants in various concentrations like 2%, 3% and 4% w/w. All prepared tablets were evaluated for weight variation, hardness, drug content, friability, disintegration time, in vitro wetting time and percent drug release. MDTs containing 4% w/w concentration of crospovidone give best results and is therefore considered as the best formula. It has shown 30 s disintegration time, 25 s wetting time and 79.34% in vitro release of drug in 25 min. PMID:24596037

Shobhit, Shobhit; Gupta, Satish Kumar

2013-01-01

142

Comparative Effectiveness of Di'ao Xin Xue Kang Capsule and Compound Danshen Tablet in Patients With Symptomatic Chronic Stable Angina  

PubMed Central

A high proportion of patients with stable angina remains symptomatic despite multiple treatment options. Di'ao Xinxuekang (XXK) capsule and Compound Danshen (CDS) tablet have been approved for treating angina pectoris for more than 20 years in China. We compare the anti-anginal effectiveness of XXK capsule and CDS tablet in patients with symptomatic chronic stable angina. A randomized, multicenter, double-blind, parallel-group, superiority trial was conducted in 4 study sites. 733 patients with symptomatic chronic stable angina were included in the full analysis set. The primary outcomes were the proportion of patients who were angina-free and the proportion of patients with normal electrocardiogram (ECG) recordings during 20 weeks treatment. Compared with CDS, XXK significantly increased the proportion of angina-free patients, but no significant difference was noted in the proportion of patients with normal ECG recordings. Weekly angina frequency and nitroglycerin use were significantly reduced with XXK versus CDS at week 20. Moreover, XXK also improved the quality of life of angina patients as measured by the SAQ score and Xueyu Zheng (a type of TCM syndrome) score. We demonstrate that XXK capsule is more effective for attenuating anginal symptoms and improving quality of life in patients with symptomatic chronic stable angina, compared with CDS tablet. PMID:25394847

Yu, Yanan; Hu, Siyuan; Li, Guoxin; Xue, Jie; Li, Zhuoming; Liu, Xiangling; Yang, Xiyan; Dong, Bo; Wang, Donghai; Wang, Xiaofeng; Liu, Shurong; Liu, Jun; Chen, Bingwei; Wang, Liying; Liu, Songshan; Chen, Qiguang; Shen, Chunti; Wang, Zhong; Wang, Yongyan

2014-01-01

143

Single dose therapy of vaginal candidiasis: a comparative trial of fenticonazole vaginal ovules versus clotrimazole vaginal tablets.  

PubMed

An open, randomized comparative clinical trial was performed in 153 patients suffering from symptomatic vaginal candidiasis confirmed by mycological tests. Patients were allocated at random into two groups: the first group (consisting of 75 subjects) was treated with a single vaginal ovule of fenticonazole (600 mg) and the second group (consisting of 78 subjects) was treated with a single vaginal tablet of clotrimazole (500 mg). Therapeutic efficacy was assessed by microbiological and clinical criteria 7 days and 1 month (when possible) after the single dose treatment. At the first follow-up visit, complete disappearance of the signs and symptoms or a highly significant reduction of their intensity was observed in both treatment groups. No significant difference was evident between the two drugs. At 7 days, the mycological tests gave negative results in 92% of the patients in the fenticonazole group and in 88.5% of the patients in the clotrimazole group. The difference between the two treatment groups was again not statistically significant. The second follow-up visit was performed in 55 (73.3%) patients of the fenticonazole group and in 52 (66.7%) patients of the clotrimazole group. The results indicate that 83.6% of patients in the fenticonazole group and 69.2% of patients in the clotrimazole group were still disease free at the time of this visit. Both drugs were well tolerated. Mild, local and short lasting side-effects were reported in only 5 cases of the group treated with fenticonazole.(ABSTRACT TRUNCATED AT 250 WORDS) PMID:2202548

Lawrence, A G; Houang, E T; Hiscock, E; Wells, M B; Colli, E; Scatigna, M

1990-01-01

144

Formulation and evaluation of fast dissolving tablet containing domperidone ternary solid dispersion  

PubMed Central

Introduction: Fast dissolving tablet containing domperidone ternary solid dispersion was developed to improve the dissolution of drug and stability of solid dispersion. Materials and Methods: Binary and ternary solid dispersions were prepared by fusion method. They were characterized by solubility study, in vitro dissolution, dissolution efficiency, and stability study. The solid state properties of solid dispersions were characterized by differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), and X-ray diffraction (XRD). Ternary solid dispersion was successfully incorporated into fast dissolving tablet by direct compression method. Tablets were characterized for pre-compression parameters, post-compression parameters, and stability study. Results: Optimized ternary solid dispersion containing ratio 1:2:1.5 of drug: Gelucire 50/13: Poloxamer 188 gave maximum dissolution. The FTIR, DSC, and XRD studies of solid dispersions were confirmed the formation of solid dispersion. Ternary solid dispersion was more stable compared to binary solid dispersion at accelerated environment conditions for one month as confirmed by DSC study. Crospovidone as a superdisintegrant (4%) showed good result with disintegration time of 19 s and dissolution near to 100% in 0.1N HCL at 30 min. Conclusion: The studies indicated that the dissolution of drug and stability of solid dispersion was improved in the presence of ternary agent (surfactant) as compared to binary solid dispersion. It was concluded that fast dissolving tablet containing ternary solid dispersion was stable at accelerated environmental conditions for 1 month. PMID:25426438

Patel, Dasharath M.; Patel, Sweeti P.; Patel, Chhagan N.

2014-01-01

145

Formulation and Evaluation of Alstonia boonei Stem Bark Powder Tablets.  

PubMed

The aim of this work was to formulate Alstonia boonei dried stem bark powder into tablets by wet granulation method using acacia, gelatine and sodium carboxymethyl cellulose as binders at concentrations of 1, 2, 4 and 8% w/w. The phytochemistry of the stem bark of Alstonia boonei was evaluated. The micromeritic properties of the granules prepared were studied. The tablets were evaluated using the necessary official and unofficial tests. The results of the phytochemical analysis showed that alkaloids, tannins, steroids, saponins, glycosides, flavonoids and terpenoids were present while anthroquinones and acidcompounds were absent. Micromeritic studies showed that Alstonia boonei granules had good flowability. The formulated tablets complied with British Pharmacopoeial specification for weight uniformity, hardness (?5 kgf) and tablet friability (<1%). For disintegration test, tablets formulated with gelatine and acacia at concentrations of 1, 2 and 4% w/w complied with Pharmacopoeial specification. However, tablets formulated with SCMC (1-8% w/w) and 8% w/w of acacia and gelatine failed the disintegration tests (Disintegration time more than 15 min). PMID:24019574

Chime, Salome A; Ugwuoke, E C; Onyishi, I V; Brown, S A; Onunkwo, G C

2013-03-01

146

Formulation and Evaluation of Alstonia boonei Stem Bark Powder Tablets  

PubMed Central

The aim of this work was to formulate Alstonia boonei dried stem bark powder into tablets by wet granulation method using acacia, gelatine and sodium carboxymethyl cellulose as binders at concentrations of 1, 2, 4 and 8% w/w. The phytochemistry of the stem bark of Alstonia boonei was evaluated. The micromeritic properties of the granules prepared were studied. The tablets were evaluated using the necessary official and unofficial tests. The results of the phytochemical analysis showed that alkaloids, tannins, steroids, saponins, glycosides, flavonoids and terpenoids were present while anthroquinones and acidcompounds were absent. Micromeritic studies showed that Alstonia boonei granules had good flowability. The formulated tablets complied with British Pharmacopoeial specification for weight uniformity, hardness (?5 kgf) and tablet friability (<1%). For disintegration test, tablets formulated with gelatine and acacia at concentrations of 1, 2 and 4% w/w complied with Pharmacopoeial specification. However, tablets formulated with SCMC (1-8% w/w) and 8% w/w of acacia and gelatine failed the disintegration tests (Disintegration time more than 15 min). PMID:24019574

Chime, Salome A.; Ugwuoke, E. C.; Onyishi, I. V.; Brown, S. A.; Onunkwo, G. C.

2013-01-01

147

Relative bioavailability of iron and folic acid from a new powdered supplement compared to a traditional tablet in pregnant women  

PubMed Central

Background Deficiencies of iron and folic acid during pregnancy can lead to adverse outcomes for the fetus, thus supplements are recommended. Adherence to current tablet-based supplements is documented to be poor. Recently a powdered form of micronutrients has been developed which may decrease side-effects and thus improve adherence. However, before testing the efficacy of the supplement as an alternate choice for supplementation during pregnancy, the bioavailability of the iron needs to be determined. Our objective was to measure the relative bioavailability of iron and folic acid from a powdered supplement that can be sprinkled on semi-solid foods or beverages versus a traditional tablet supplement in pregnant women. Methods Eighteen healthy pregnant women (24 – 32 weeks gestation) were randomized to receive the supplements in a crossover design. Following ingestion of each supplement, the changes (over baseline) in serum iron and folate over 8 hours were determined. The powdered supplement contained 30 mg of iron as micronized dispersible ferric pyrophosphate with an emulsifier coating and 600 ?g folic acid; the tablet contained 27 mg iron from ferrous fumarate and 1000 ?g folic acid. Results Overall absorption of iron from the powdered supplement was significantly lower than the tablet (p = 0.003). There was no difference in the overall absorption of folic acid between supplements. Based on the differences in the area under the curve and doses, the relative bioavailability of iron from powdered supplement was lower than from the tablet (0.22). Conclusion The unexpected lower bioavailability of iron from the powdered supplement is contrary to previously published reports. However, since pills and capsules are known to be poorly accepted by some women during pregnancy, it is reasonable to continue to explore alternative micronutrient delivery systems and forms of iron for this purpose. Trial Registration ClinicalTrials.gov NCT00789490 PMID:19635145

Hartman-Craven, Brenda; Christofides, Anna; O'Connor, Deborah L; Zlotkin, Stanley

2009-01-01

148

A comparative study of calcium absorption following a single serving administration of calcium carbonate powder versus calcium citrate tablets in healthy premenopausal women  

PubMed Central

Background Calcium is an essential mineral often taken as a daily, long-term nutritional supplement. Data suggests that once-daily dosing is important with regard to long-term compliance of both drugs and nutritional supplements. Objective This study was undertaken to compare the bioavailability of a single serving of two calcium supplements in healthy, premenopausal women. Design A two-period, crossover bioavailability study of a single serving of calcium citrate tablets (two tablets=500 mg calcium) versus a single serving of calcium carbonate powder (one packet of powder=1,000 mg calcium) was performed in healthy women aged between 25 and 45. All subjects were on a calcium-restricted diet 7 days prior to testing and fasted for 12 h before being evaluated at 0, 1, 2, and 4 h after oral administration of the test agents. Blood measurements for total and ionized calcium and parathyroid hormone were performed and adverse events were monitored. Results Twenty-three women were evaluable with a mean age of 33.2±8.71. Results showed that administration of a single serving of a calcium carbonate powder resulted in greater absorption in total and ionized calcium versus a single serving of calcium citrate tablets at 4 h (4.25±0.21 vs. 4.16±0.16, p=0.001). There were minimal side effects and no reported serious adverse events. Conclusions This study shows that a single serving of a calcium carbonate powder is more bioavailable than a single serving of calcium citrate tablets. This may be beneficial for long-term compliance. PMID:24772062

Wang, Haiyuan; Bua, Peter; Capodice, Jillian

2014-01-01

149

Taste Masked Microspheres of Ofloxacin: Formulation and Evaluation of Orodispersible Tablets  

PubMed Central

Ofloxacin is a synthetic chemotherapeutic antibiotic used for treatment of a variety of bacterial infections, but therapy suffers from low patients’ compliance due to its unpleasant taste. This study was aimed to develop taste masked microspheres of ofloxacin using Eudragit and to prepare orodispersible tablets of the formulated microspheres using natural superdisintegrant. Taste masking Eudragit E100 microspheres were prepared by solvent evaporation technique with an entrapment efficiency ranging from 69.54 ± 1.98 to 86.52 ± 2.25%. DSC revealed no interaction between the drug and polymer. Microspheres prepared at a drug/polymer ratio of 1:4 and 1:5 revealed sufficient flow properties and better taste masking as compared to other ratios. Drug loaded microspheres were formulated as orodispersible tablets using locust bean gum as a natural superdisintegrant offering the advatages of biocompatibility and biodegrad-ability. The wetting time, water absorption ratio and in-vitro disintegration time of the tablets were found to range between 19 ± 2 to 10 ± 3 seconds, 59.11 ± 0.65 to 85.76 ± 0.96 and 22 ± 2 to 10 ± 2 seconds, respectively. The in-vitro ofloxacin release was about 97.25% within 2h. The results obtained from the study suggested the use of eudragit polymer for preparing ofloxacin loaded microspheres with an aim to mask the bitter taste of the drug and furthermore orodispersible tablets could be formulated using locust bean gum as a natural superdisintegrant. PMID:21886910

Malik, Karan; Arora, Gurpreet; Singh, Inderbir

2011-01-01

150

Taste masked microspheres of ofloxacin: formulation and evaluation of orodispersible tablets.  

PubMed

Ofloxacin is a synthetic chemotherapeutic antibiotic used for treatment of a variety of bacterial infections, but therapy suffers from low patients' compliance due to its unpleasant taste. This study was aimed to develop taste masked microspheres of ofloxacin using Eudragit and to prepare orodispersible tablets of the formulated microspheres using natural superdisintegrant. Taste masking Eudragit E100 microspheres were prepared by solvent evaporation technique with an entrapment efficiency ranging from 69.54 ± 1.98 to 86.52 ± 2.25%. DSC revealed no interaction between the drug and polymer. Microspheres prepared at a drug/polymer ratio of 1:4 and 1:5 revealed sufficient flow properties and better taste masking as compared to other ratios. Drug loaded microspheres were formulated as orodispersible tablets using locust bean gum as a natural superdisintegrant offering the advatages of biocompatibility and biodegrad-ability. The wetting time, water absorption ratio and in-vitro disintegration time of the tablets were found to range between 19 ± 2 to 10 ± 3 seconds, 59.11 ± 0.65 to 85.76 ± 0.96 and 22 ± 2 to 10 ± 2 seconds, respectively. The in-vitro ofloxacin release was about 97.25% within 2h. The results obtained from the study suggested the use of eudragit polymer for preparing ofloxacin loaded microspheres with an aim to mask the bitter taste of the drug and furthermore orodispersible tablets could be formulated using locust bean gum as a natural superdisintegrant. PMID:21886910

Malik, Karan; Arora, Gurpreet; Singh, Inderbir

2011-09-01

151

Tablet Weaving  

ERIC Educational Resources Information Center

Article described a weaving technique called tablet weaving, an ancient textile process that provides opportunity for making a variety of items, such as guitar straps, belts, and decorative bands. (Author/RK)

Kren, Margo

1976-01-01

152

Comparative Bioavailability and Tolerability of Single and Multiple Doses of 2 Diclofenac Sodium Sustained-Release Tablet Formulations in Fasting, Healthy Chinese Male Volunteers?  

PubMed Central

Background Diclofenac is a nonsteroidal anti-inflammatory drug used for the treatment of patients with osteoarthritis. Objectives Our primary objective was to compare bioavailability and tolerability of a generic sustained-release tablet with the established reference sustained-release tablet of diclofenac sodium in a fasting, healthy Chinese male population. Methods A randomized, open-label, single- and multiple-dose study design was used. After the single dose, volunteers received diclofenac sodium sustained-release tablet once daily for 5 days. In the single-dose phase, blood samples were collected from 0 to 36 hours after drug administration. In the multiple-dose phase, samples were obtained before drug administration at 8:00 am on Days 3 and 4 to determine Cmin,ss of diclofenac sodium; on Day 5, samples were collected from 0 to 36 hours. Adverse events were monitored via subject interview, vital signs, and blood sampling. Results Twenty-four Chinese male volunteers were enrolled. The pharmacokinetic parameters (mean [SD]) for diclofenac after single dose of 75 and 100 mg were: Cmax 473.5 [179.5] and 546.6 [154.9] ng/mL; AUC0–? 3841.2 [1402.3], and 5019.1 [2,314.0] ng·h/mL; Tmax 4.9 [2.4], and 4.3 [2.2] hours; t1/2 5.9 [2.5], and 6.0 [2.2] hours. Mean [SD] values after multiple doses of 75 and 100 mg were: Cmax,ss 525.6 [127.4] and 650.5 [167.0] ng/mL, Cmin,ss 33.9 [20.9] and 62.9 [34.9] ng/mL, AUCss 4316.3 [633.0] and 5335.1 [1291.9] ng·h/mL, Cav,ss 179.8 [26.4] and 222.3 [53.8] ng/mL, Tmax 5.1 [1.8] and 4.5 [0.9] hours and t1/2 5.2 [2.9] and 5.5 [2.8] hours, respectively. Conclusions This diclofenac sodium 75 mg tablet has features compatible with the 100 mg sustained-release tablet and appeared to be well tolerated. ClinicalTrials.gov identifier: 2010L01969 PMID:24465044

Zhai, Xue-Jia; Yu, Ye; Chen, Fen; Lu, Yong-Ning

2013-01-01

153

Preparation and evaluation of sublingual tablets of zolmitriptan  

PubMed Central

Aim: Zolmitriptan is a 5-HT receptor agonist (1B/1D). It is used in the acute treatment of migraine having low bioavailability about 40% orally due to hepatic first pass metabolism. The purpose of the present research was to formulate fast acting sublingual tablets of zolmitriptan. Materials and Methods: Sublingual tablets were prepared using ispaghula husk powder, gellan gum, sodium alginate as super disintegrating polymers and citric acid, tartaric acid and camphor as permeation enhancers by direct compressible technique and evaluated for weight variation, thickness, friability, content uniformity, hardness, disintegration time, wetting time, in-vitro drug release, in-vitro and ex-vivo permeation study. Stability study of optimized formulation was performed as per ICH (International Conference on Harmonisation) guideline. Results: The in-vitro disintegration time of the optimized formulation (D5) was 9 ± 2 s and all formulations showed 100% of dissolution within 6 ± 2 min. Formulation containing 4% of gellan gum (D5) showed highest disintegration and 2% of citric acid formulation (P3) showed highest permeation 88% within 30 min and ex-vivo permeation was 52% within 30 min. Optimized formulation was stable for 1 month during stability study as per ICH guideline. Conclusion: The sublingual tablet formulation gives better results using natural super disintegrant for fast onset of action. PMID:24678459

Prajapati, Shailesh T; Patel, Manoj V; Patel, Chhaganbhai N

2014-01-01

154

Evaluation of hexagonal boron nitride as a new tablet lubricant.  

PubMed

In this study, hexagonal boron nitride (HBN) was evaluated as a new lubricant for pharmaceutical tablet manufacturing. The other conventional lubricants such as magnesium stearate (MGST), stearic acid (STAC), and glyceryl behenate (COMP) were also tested along with HBN. Tablets were manufactured on an instrumented single-station tablet press to monitor and quantify the lower punch ejection force (LPEF). The force ratio, tablet crushing strength, disintegration time, and thickness were measured. The lubricant film formation and lubricant distribution in tablets were studied using the scanning electron microscopy (SEM) and electron probe micro analyzer (EPMA). Based on the force ratio, a good lubrication was obtained at 1% for MGST and HBN; in contrast, STAC and COMP did not show a good lubrication. After 1%, all lubricants performed well. MGST was found to be the most effective lubricant based on LPEF-lubricant concentration profile. HBN provided a 50% decrease in LPEF at 2% lubricant concentration and was rated as an effective tablet lubricant. HBN was better than either STAC or COMP. Unlike MGST, HBN had no significant prolongation effect on tablet disintegration times. PMID:16176018

Turkoglu, Murat; Sahin, Inan; San, Tangul

2005-01-01

155

Optimization of an effervescent tablet formulation using a central composite design optimization of an effervescent tablet formulation containing spray dried l-leucine and polyethylene glycol 6000 as lubricants using a central composite design  

Microsoft Academic Search

A rotatable central composite design is used to evaluate the effects of lubricants and compression force on the physical characteristics of effervescent tablets. Effervescent tablets lubricated with a combination of spray dried l-leucine and polyethylene glycol 6000 are prepared by direct compression and examined. Residual force, crushing strength and disintegration time are considered as response variables and related to the

Bärbel Rotthäuser; Gerolf Kraus; Peter C Schmidt

1998-01-01

156

Formulation and optimization of potassium iodide tablets  

PubMed Central

The use of potassium iodide (KI) as a protective agent against accidental radioactive exposure is well established. In this study, we aimed to prepare a KI tablet formulation using a direct compression method. We utilized Design of Experiment (DoE)/mixture design to define the best formulation with predetermined physical qualities as to its dissolution, hardness, assay, disintegration, and angle of repose. Based on the results from the DoE, the formulation had the following components (%w/w): Avicel 48.70%, silicon dioxide 0.27%, stearic acid (1.00%), magnesium stearate 2.45%, and dicalcium phosphate 18.69%, in addition to potassium iodide 28.89% (130 mg/tablet). This formulation was scaled-up using two tablet presses, a single-punch press and a rotary mini tablet press. The final scaled-up formulation was subjected to a variety of quality control tests, including photo-stability testing. The results indicate that potassium iodide tablets prepared by a rotary mini tablet press had good pharmaceutical characteristics and a shelf-life of 25 days when stored at room temperature protected from light.

Al-Achi, Antoine; Patel, Binit

2014-01-01

157

A multicentric, open label, randomised, postmarketing efficacy study comparing multidose of lincomycin hydrochloride capsule 500 mg with multidose cefpodoxime proxetil tablet 200 mg in patients with tonsillitis, sinusitis.  

PubMed

Tonsillitis causes considerable short and medium term morbidity, and can be recurrent. Sinusitis can be acute (less than 4 weeks), subacute (4-8 weeks) or chronic (8 weeks or more). To study the comparative efficacy and safety of multidose treatments of lincomycin hydrochloride 500 mg capsules against cefpodoxime proxetil 200 mg tablets on its outcome in the Indian scenario are the aims and objective of the study. A total of 41 tonsillitis, sinusitis cases of either gender aged above 18 years were enrolled in the study. The diagnosis of sonsillitis, sinusitis was made based on examination of symptoms and throat swab. A randomised treatment of either lincomycin hydrochloride 500 mg capsules or cefpodoxime proxetil 200 mg tablets twice daily for five days alongwith other concomitant medications depending on related symptoms was given to 40 patients. At the end of study, all patients were re-evaluated and the response rate was assessed. The most common clinical symptoms were body temperature, headache, throat pain, postnasal discharge, mucopus, odynophagia, sinus tenderness, nasal congestion, pharyngeal congestion and tonsillar congestion. The overall response rate of lincomycin hydrochloride in all the symptoms except headache was more effective than cefpodoxime proxetil. Out of 100% (n = 20) patients in each group, 67.89% in lincomycin and 52.27% in cefpodoxime patients achieved complete relief, in all the clinical symptoms. The study suggests that lincomycin hydrochloride capsules, a conventional antibiotic indicates effective treatment for relief from tonsillitis and sinusitis, as compared to new third generation antibiotic. PMID:23741829

Kothadiya, Ajay

2012-08-01

158

Prevalence of Childhood Disintegrative Disorder.  

ERIC Educational Resources Information Center

A review of 32 epidemiological surveys of autism and pervasive developmental disorders found four surveys yielded estimates for childhood disintegrative disorder (CDD) ranging from 1.1 to 6.4 per 100,000. It is concluded that CDD is very rare and its prevalence is 60 times less than that of autistic disorder. (Contains references.) (Author/CR)

Fombonne, Eric

2002-01-01

159

A quality-by-design study for an immediate-release tablet platform: examining the relative impact of active pharmaceutical ingredient properties, processing methods, and excipient variability on drug product quality attributes.  

PubMed

The impact of filler-lubricant particle size ratio variation (3.4-41.6) on the attributes of an immediate-release tablet was compared with the impacts of the manufacturing method used (direct compression or dry granulation) and drug loading (1%, 5%, and 25%), particle size (D[4,3]: 8-114 ?m), and drug type (theophylline or ibuprofen). All batches were successfully manufactured, except for direct compression of 25% drug loading of 8 ?m (D[4,3]) drug, which exhibited very poor flow properties. All manufactured tablets possessed adequate quality attributes: tablet weight uniformity <4% RSD, tablet potency: 94%-105%, content uniformity <6% RSD, acceptance value ? 15, solid fraction: 0.82-0.86, tensile strength >1 MPa, friability ? 0.2% weight loss, and disintegration time < 4 min. The filler-lubricant particle size ratio exhibited the greatest impact on blend and granulation particle size and granulation flow, whereas drug property variation dominated blend flow, ribbon solid fraction, and tablet quality attributes. Although statistically significant effects were observed, the results of this study suggest that the manufacturability and performance of this immediate-release tablet formulation is robust to a broad range of variation in drug properties, both within-grade and extra-grade excipient particle size variations, and the choice of manufacturing method. PMID:24375069

Kushner, Joseph; Langdon, Beth A; Hicks, Ian; Song, Daniel; Li, Fasheng; Kathiria, Lalji; Kane, Anil; Ranade, Gautam; Agarwal, Kam

2014-02-01

160

Drawbacks of Surfactant Presence on the Dissolution and Mechanical Properties of Detergent Tablets: How to Control Interfaces by Surfactant Localization  

Microsoft Academic Search

The aim of this study is to limit the hurdles generated by the presence of a surfactant, i.e., sodium dodecyl sulfate (SDS),\\u000a in effervescent detergent tablets containing a chlorine provider. The results are highlighted by investigating the tablet’s\\u000a functional characteristics (mechanical strength, disintegration time). A second objective is to increase the surfactant content\\u000a of the tablet in order to improve

Florence Chantraine; Marylène Viana; Christelle Pouget; Nelly Brielles; Olivier Mondain-Monval; Paul Branlard; Gilles Rubinstenn; Dominique Chulia

2009-01-01

161

Self-organizing map analysis using multivariate data from theophylline tablets predicted by a thin-plate spline interpolation.  

PubMed

The "quality by design" concept in pharmaceutical formulation development requires the establishment of a science-based rationale and a design space. We integrated thin-plate spline (TPS) interpolation and Kohonen's self-organizing map (SOM) to visualize the latent structure underlying causal factors and pharmaceutical responses. As a model pharmaceutical product, theophylline tablets were prepared based on a standard formulation. The tensile strength, disintegration time, and stability of these variables were measured as response variables. These responses were predicted quantitatively based on nonlinear TPS. A large amount of data on these tablets was generated and classified into several clusters using an SOM. The experimental values of the responses were predicted with high accuracy, and the data generated for the tablets were classified into several distinct clusters. The SOM feature map allowed us to analyze the global and local correlations between causal factors and tablet characteristics. The results of this study suggest that increasing the proportion of microcrystalline cellulose (MCC) improved the tensile strength and the stability of tensile strength of these theophylline tablets. In addition, the proportion of MCC has an optimum value for disintegration time and stability of disintegration. Increasing the proportion of magnesium stearate extended disintegration time. Increasing the compression force improved tensile strength, but degraded the stability of disintegration. This technique provides a better understanding of the relationships between causal factors and pharmaceutical responses in theophylline tablet formulations. PMID:23449198

Yasuda, Akihito; Onuki, Yoshinori; Obata, Yasuko; Yamamoto, Rie; Takayama, Kozo

2013-01-01

162

Evaluation of citrus fibers as a tablet excipient.  

PubMed

The consumption of fibers is associated with many health benefits, such as a reduction of cardiovascular and gastrointestinal diseases, control of body weight, and prevention of diabetes. Despite the widespread use of fiber supplements such as capsules or tablets, there is an almost complete lack of information concerning the technological properties of functional fibers used in nutraceutical formulations. The aim of this work was to characterize the technological properties of citrus fibers necessary for their use as a processing aid in tableting. The results obtained showed that citrus fibers share many properties of other polysaccharides used as tableting excipients, such as thermal behavior and compaction mechanism, together with an appreciable tabletability. However, the most interesting properties resulted from their disintegration power. Citrus fibers behaved in a similar manner to the well-known super disintegrant croscarmellose sodium and resulted to be little susceptible to their concentration, to lubricant type, and lubricant concentration. Thus, this work supports the idea of a potential use of citrus fibers as "active" substances and processing aid in the tableting of nutraceutical products and also as functional excipient in pharmaceutical tablets formulation. PMID:24306677

Cespi, Marco; Bonacucina, Giulia; Roberts, Matthew; Hanson, Samuel; Jones, Stephen; Makevica, Elina; Casettari, Luca; Palmieri, Giovanni Filippo

2014-04-01

163

Formulation and optimization of orodispersible tablets of flutamide.  

PubMed

The present study aimed to formulate orodispersible tablets of flutamide (FTM) to increase its bioavailability. Orodispersible tablets were prepared by direct compression technique using three different approaches namely; super-disintegration, effervescence and sublimation. Different combined approaches were proposed and evaluated to optimize tablet characteristics. Sodium starch glycolate (SSG) was used as the superdisintegrant. The prepared powder mixtures were subjected to both pre and post compression evaluation parameters including; IR spectroscopy, micromeritics properties, tablet hardness, friability, wetting time, disintegration time and in-vitro drug release. IR studies indicated that there was no interaction between the drug and the excipients used except Ludipress. The results of micromeritics studies revealed that all formulations were of acceptable to good flowability. Tablet hardness and friability indicated good mechanical strength. Wetting and dispersion times decreased from 46 to 38 s by increasing the SSG concentration from 3.33 to 6.66% w/w in tablets prepared by superdisintegration method. The F8 formulation which was prepared by combined approaches of effervescence and superdisintegrant addition gave promising results for tablet disintegration and wetting times but failed to give faster dissolution rate. The incorporation of 1:5 solid dispersion of FTM: PEG 6000 instead of the pure drug in the same formulation increased the drug release rate from 73.12 to 96.99% after 15 min. This increase in the dissolution rate may be due to the amorphization of the drug during the solid dispersion preparation. The presence of the amorphous form of the drug was shown in the IR spectra. PMID:24493974

Elkhodairy, Kadria A; Hassan, Maha A; Afifi, Samar A

2014-01-01

164

Numerical simulation on zonal disintegration in deep surrounding rock mass.  

PubMed

Zonal disintegration have been discovered in many underground tunnels with the increasing of embedded depth. The formation mechanism of such phenomenon is difficult to explain under the framework of traditional rock mechanics, and the fractured shape and forming conditions are unclear. The numerical simulation was carried out to research the generating condition and forming process of zonal disintegration. Via comparing the results with the geomechanical model test, the zonal disintegration phenomenon was confirmed and its mechanism is revealed. It is found to be the result of circular fracture which develops within surrounding rock mass under the high geostress. The fractured shape of zonal disintegration was determined, and the radii of the fractured zones were found to fulfill the relationship of geometric progression. The numerical results were in accordance with the model test findings. The mechanism of the zonal disintegration was revealed by theoretical analysis based on fracture mechanics. The fractured zones are reportedly circular and concentric to the cavern. Each fracture zone ruptured at the elastic-plastic boundary of the surrounding rocks and then coalesced into the circular form. The geometric progression ratio was found to be related to the mechanical parameters and the ground stress of the surrounding rocks. PMID:24592166

Chen, Xuguang; Wang, Yuan; Mei, Yu; Zhang, Xin

2014-01-01

165

Preparation of multiparticulate vaginal tablet using glyceryl monooleate for sustained progesterone delivery.  

PubMed

Most of the sustained release vaginal formulations are in the form of bioadhesive gels and tablets. Though proved efficient, their presence in the vagina for a longer time as a bulk produces discomfort and interference with body functioning including sexual activities. Hence, they lack complete patient compliance. In this study, multiparticulate vaginal tablets were prepared by utilizing progesterone (PRO) loaded dry powder precursor of cubic phase (DPPCP) of glyceryl monooleate (GMO). DPPCP were obtained by spray drying GMO with magnesium trisilicate (MTS) and have presented PRO sustained release in simulated vaginal fluid (SVF) for 14 hours. The effect of hydrophilic and hydrophobic tableting excipients on compression, phase, bioadhesion and drug release properties of prepared tablets was evaluated. The effervescent hydrophilic tablet (EHT) prepared with hydrophilic excipients showed rapid disintegration but, diminished sustaining ability owing to transformation into lamellar phase whereas the multiparticulate hydrophobic tablet (MHT) obtained from hydrophobic excipients presented both rapid disintegration and sustained release in SVF by virtue of cubic phase retention. During bioadhesivity testing, fast disintegration of MHT with formation of uniform and viscous bioadhesive layer on cow mucosa was observed even with a small volume of SVF. As MHT may not produce discomfort and interference, it will be preferred over bioadhesive gel or tablet. PMID:18802845

Biradar, Shailesh V; Dhumal, Ravindra S; Shah, Manish H; Paradkar, Anant R; Yamamura, Shigeo

2009-01-01

166

A Combined-Formulation Tablet of Lamivudine\\/Nevirapine\\/Stavudine: Bioequivalence Compared With Concurrent Administration of Lamivudine, Nevirapine, and Stavudine in Healthy Indian Subjects  

Microsoft Academic Search

Generic fixed-dose combinations of antiretrovirals are frequently prescribed for the treatment of human immunodeficiency virus infection. A randomized, 2-way study was conducted in 24 fasting, healthy, Indian male subjects to assess bioequivalence between a single combination tablet containing lamivudine, stavudine, and nevirapine (treatment A) with respect to separate marketed tablets administered simultaneously (treatment B). Each subject received treatments A and

Vishal S. Narang; Amar Lulla; Geena Malhotra; Shrinivas Purandare

2005-01-01

167

Sufentanil Sublingual Tablet System vs. Intravenous Patient-Controlled Analgesia with Morphine for Postoperative Pain Control: A Randomized, Active-Comparator Trial  

PubMed Central

Background Problems with intravenous patient-controlled analgesia (IV PCA) are well known, including invasive route of delivery and pump programming errors. The primary objective of this study was to evaluate patient satisfaction with a novel sublingual sufentanil PCA system (sufentanil sublingual tablet system 15 mcg with a 20-minute lockout interval; SSTS) to IV PCA morphine sulfate 1 mg with a 6-minute lockout interval (IV PCA MS) for the management of acute postoperative pain. Methods This was a randomized, open-label, 48-hour non-inferiority study with optional extension to 72 hours at 26 U.S. sites enrolling patients scheduled for elective major open abdominal or orthopedic (hip or knee replacement) surgery. The primary outcome measure was the proportion of patients who responded “good” or “excellent” (collectively “success”) at the 48-hour timepoint on the Patient Global Assessment of method of pain control (PGA48). Results A total of 357 patients received study drug and 78.5% vs. 65.6% of patients achieved PGA48 “success” for SSTS vs. IV PCA MS, respectively, demonstrating non-inferiority (P < 0.001 using the one-side Z-test against the non-inferiority margin) as well as statistical superiority for treatment effect (P = 0.007). Patients using SSTS reported more rapid onset of analgesia and patient and nurse ease of care and satisfaction scores were higher than IV PCA MS. Adverse events were similar between the 2 groups; however, SSTS had fewer patients experiencing oxygen desaturations below 95% compared to IV PCA MS (P = 0.028). Conclusions Sufentanil sublingual tablet system is a promising new analgesic technology that may address some of the concerns with IV PCA. PMID:25155134

Melson, Timothy I; Boyer, David L; Minkowitz, Harold S; Turan, Alparslan; Chiang, Yu-Kun; Evashenk, Mark A; Palmer, Pamela P

2014-01-01

168

Interplanetary dust particles - Disintegration and orbital motion  

NASA Astrophysics Data System (ADS)

Abrupt or gradual disintegration of the interplanetary dust particle causes increase of its distance from the sun due to the solar radiation pressure. The problem of the orbital evolution of the interplanetary dust particles under such disintegration processes is discussed. The process of gradual disintegration due to the solar wind particles is calculated in detail. Obtained results represent corrections to the changes of orbital elements for the Poynting-Robertson effect and effect of the solar wind.

Klacka, J.

1993-01-01

169

Prediction of tablet characteristics from residual stress distribution estimated by the finite element method.  

PubMed

Tablet characteristics of tensile strength and disintegration time were predicted using residual stress distribution, simulated by the finite element method (FEM). The Drucker-Prager Cap (DPC) model was selected as the method for modeling the mechanical behavior of pharmaceutical powders composed of lactose (LAC), cornstarch (CS), and microcrystalline cellulose (MCC). The DPC model was calibrated using a direct shear test and analysis of the hardening law of the powder. The constructed DPC model was fed into the analysis using the FEM, and the mechanical behavior of pharmaceutical powders during compaction was analyzed using the FEM. The results revealed that the residual stress distribution of the tablets was uniform when the compression force increased. In particular, the residual stress distribution of tablets composed of equal amounts of LAC, CS, and MCC was more uniform than the tablets composed of 67% LAC and 33% CS, with no MCC. The tensile strength and disintegration time were predicted accurately from the residual stress distribution of tablets using multiple linear regression analysis and partial least squares regression analysis. This suggests that the residual stress distribution of tablets is related closely to the tensile strength and disintegration time. PMID:23897300

Hayashi, Yoshihiro; Miura, Takahiro; Shimada, Takuya; Onuki, Yoshinori; Obata, Yasuko; Takayama, Kozo

2013-10-01

170

Comparative clinical trial of fenticonazole ovule (600 mg) versus clotrimazole vaginal tablet (500 mg) in the treatment of symptomatic vaginal candidiasis.  

PubMed

A multi-centre, randomized, single-blind, parallel-group clinical trial was undertaken in 50 patients (26 fenticonazole, 24 clotrimazole) with symptomatic vaginal candidiasis to compare the antifungal efficacy and tolerability of single-dose intra-vaginal treatment with a fenticonazole ovule (600 mg) or a clotrimazole vaginal tablet (500 mg). Assessment was by laboratory mycological investigation and symptomatic assessments for a period of 3 weeks from the day of treatment. Of the 50 patients, 43 (23 fenticonazole, 20 clotrimazole) returned for assessment 1 week after drug administration and 32 (17 fenticonazole, 15 clotrimazole) were re-assessed 3 weeks after drug administration. Both treatments resulted in very similar and highly significant improvements in symptoms, associated with disappearance of detectable Candida in approximately 70% of patients. There were no significant differences between treatments and no appreciable incidence of relapse during the 3-week period of observation. At the end of this period, 10 (59%) of 17 fenticonazole patients were totally disease-free, as compared with 10 (67%) of 15 patients after clotrimazole treatment. The cure rate observed was somewhat less than that previously seen when intra-vaginal cream formulations of the same two drugs were given on a multiple-dose basis. Both drugs were very well tolerated, with no reports of appreciable local or systemic adverse reactions to either drug. PMID:2680285

Studd, J W; Dooley, M M; Welch, C C; Vijayakanthan, K; Mowat, J M; Wade, A; Newell, M

1989-01-01

171

Internal solitary waves: propagation, deformation and disintegration  

E-print Network

Internal solitary waves: propagation, deformation and disintegration Roger Grimshaw1 , Tatiana-amplitude, horizontally propagating internal solitary waves. Typically these waves occur in regions of variable bottom the propagation, deformation and disintegration of internal solitary waves as they propagate over the continental

172

Apparatus for disintegrating kidney stones  

NASA Technical Reports Server (NTRS)

The useful life of the wire probe in an ultrasonic kidney stone disintegration instrument is enhanced and prolonged by attaching the wire of the wire probe to the tip of an ultrasonic transducer by means of a clamping arrangement. Additionally, damping material is applied to the wire probe in the form of a damper tube through which the wire probe passes in the region adjacent the transducer tip. The damper tube extends outwardly from the transducer tip a predetermined distance, terminating in a resilient soft rubber joint. Also, the damper tube is supported intermediate its length by a support member. The damper system thus acts to inhibit lateral vibrations of the wire in the region of the transducer tip while providing little or no damping to the linear vibrations imparted to the wire by the transducer.

Angulo, E. D. (inventor)

1984-01-01

173

Improving biodegradation behavior of calcium sulfate bone graft tablet by using water vapor treatment.  

PubMed

The biodegradation rate of calcium sulfate hemihydrate (CSH) tablets is extremely rapid. This study adopts a water vapor treatment to modify the surface structure of a CSH tablet. After the treatment, a small amount of calcium sulfate dihydrate (CSD) forms on the surface; the porosity near the surface region decreases, consequently enhancing tablet strength and surface hardness. Because of the decrease in porosity at the surface, the time for complete disintegration increases from 1.2 h to 7.2 h; the time for complete dissolution increases from 7 days to 25 days. PMID:25428052

Tsai, Yu-Yu; Wang, Sea-Fue; Kuo, Shu-Ting; Tuan, Wei-Hsing

2013-01-01

174

Contribution of the physicochemical properties of active pharmaceutical ingredients to tablet properties identified by ensemble artificial neural networks and Kohonen's self-organizing maps.  

PubMed

The aim of this study was to create a tablet database for use in designing tablet formulations. We focused on the contribution of active pharmaceutical ingredients (APIs) to tablet properties such as hardness and disintegration time (DT). Before we investigated the effects of the APIs, we optimized the tablet base formulation (placebo tablet) according to an expanded simplex search. The optimal placebo tablet showed sufficient hardness and rapid disintegration. We then tested 14 kinds of compounds as the model APIs. The APIs were characterized in terms of their physicochemical properties using Kohonen's self-organizing maps. We also prepared model tablets by incorporating the APIs into the optimal placebo tablet, and then examined the tablet properties, including tensile strength and DT. On the basis of the experimental data, an ensemble artificial neural network incorporating general regression analysis was conducted. A reliable model of the correlation between the physicochemical properties of the APIs and the tablet properties was thus constructed. From the correlation model, we clarified the detailed contributions of each physicochemical property to the tablet attributes. PMID:22473528

Onuki, Yoshinori; Kawai, Shota; Arai, Hiroaki; Maeda, Jin; Takagaki, Keisuke; Takayama, Kozo

2012-07-01

175

Pharmacokinetics of metformin gastric-retentive tablets in healthy volunteers.  

PubMed

The single-dose pharmacokinetics of two gastric-retentive, extended-release tablet formulations of metformin hydrochloride in fed, healthy volunteers were compared with those of the currently marketed immediate-release metformin hydrochloride product. The plasma concentration-time profiles demonstrated extended-release characteristics from the gastric-retentive tablets. The mean bioavailability from each gastric-retentive tablet was approximately 115%, relative to the immediate-release (IR) product. Cmax values were lower and tmax values were greater for the gastric-retentive tablets compared with the IR product. In contrast to conventional extended-release metformin tablets reported in the literature, these gastric-retentive tablets showed extended-release plasma concentration profiles of metformin hydrochloride and increased bioavailability compared with the immediate-release tablet. PMID:11402634

Gusler, G; Gorsline, J; Levy, G; Zhang, S Z; Weston, I E; Naret, D; Berner, B

2001-06-01

176

Evaluation of starches obtained from four Dioscorea species as binding agent in chloroquine phosphate tablet formulations  

PubMed Central

Starches obtained from four Dioscorea species namely Dioscorea dumetorum (Bitter), Dioscorea oppositifolia (Chinese), Dioscorea alata (Water), and Dioscorea rotundata (White) have been evaluated as binding agents in chloroquine phosphate tablet formulations in comparison with official corn starch. The compressional properties of the formulations were analyzed using density measurements and the Heckel and Kawakita equations. The mechanical properties of the tablets were assessed using tensile strength, brittle fracture index (BFI), and friability tests while the drug release properties of the tablets were assessed using disintegration and dissolution times. The results indicate that the four starches vary considerably in their physicochemical properties. The ranking for the tensile strength and the disintegration and dissolution times for the formulations was Chinese > Bitter > Corn > White > Water while the ranking was reversed for BFI and friability. The results suggest that Water, White, and Corn could be useful when faster disintegration time of tablets is desired while Chinese and Bitter could be more useful when bond strength is of concern and in minimizing the problems of lamination and capping in tablet formulation. PMID:23960747

Okunlola, Adenike; Odeku, Oluwatoyin A.

2011-01-01

177

Evaluation of starches obtained from four Dioscorea species as binding agent in chloroquine phosphate tablet formulations.  

PubMed

Starches obtained from four Dioscorea species namely Dioscorea dumetorum (Bitter), Dioscorea oppositifolia (Chinese), Dioscorea alata (Water), and Dioscorea rotundata (White) have been evaluated as binding agents in chloroquine phosphate tablet formulations in comparison with official corn starch. The compressional properties of the formulations were analyzed using density measurements and the Heckel and Kawakita equations. The mechanical properties of the tablets were assessed using tensile strength, brittle fracture index (BFI), and friability tests while the drug release properties of the tablets were assessed using disintegration and dissolution times. The results indicate that the four starches vary considerably in their physicochemical properties. The ranking for the tensile strength and the disintegration and dissolution times for the formulations was Chinese > Bitter > Corn > White > Water while the ranking was reversed for BFI and friability. The results suggest that Water, White, and Corn could be useful when faster disintegration time of tablets is desired while Chinese and Bitter could be more useful when bond strength is of concern and in minimizing the problems of lamination and capping in tablet formulation. PMID:23960747

Okunlola, Adenike; Odeku, Oluwatoyin A

2011-04-01

178

Development Strategies for Herbal Products Reducing the Influence of Natural Variance in Dry Mass on Tableting Properties and Tablet Characteristics  

PubMed Central

One “Quality by Design” approach is the focus on the variability of the properties of the active substance. This is crucially important for active substances that are obtained from natural resources such as herbal plant material and extracts. In this paper, we present various strategies for the development of herbal products especially taking into account the natural batch-to-batch variability (mainly of the dry mass) of tablets that contain a fixed amount of tincture. The following steps in the development have been evaluated for the outcome of the physico-chemical properties of the resulting tablets and intermediates: concentration of the tincture extracted from Echinacea fresh plant, loading of the concentrate onto an inert carrier, the respective wet granulation and drying step, including milling, and the adjuvant excipients for the tablet compression step. The responses that were investigated are the mean particle size of the dried and milled granulates, compaction properties and disintegration time of the tablets. Increased particle size showed a significant increase of the disintegration time and a decrease of the compaction properties. In addition, our results showed that the particle size has a great dependency on the ratio of liquid to carrier during the wet granulation process. Thus, the variability of the respective parameters tested was influenced by the performed strategies, which is how the tincture correlated to its dry mass and the relation of the amount of carrier used. In order to optimize these parameters, a strategy considering the above-mentioned points has to be chosen. PMID:24300367

Qusaj, Ylber; Leng, Andreas; Alshihabi, Firas; Krasniqi, Blerim; Vandamme, Thierry

2012-01-01

179

Formulation, release characteristics and bioavailability of novel monolithic hydroxypropylmethylcellulose matrix tablets containing acetaminophen  

Microsoft Academic Search

Effect of incorporating pharmaceutical excipients on the in vitro release profiles and the release mechanism of monolithic hydroxypropylmethylcellulose (4000 cps) matrix tablets (m-HPMC tablets) in terms of mimicking the dual drug release character of bi-layered Tylenol® ER tablets was studied. We also compared the in vitro release profiles of optimized m-HPMC matrix tablet and Tylenol® ER tablet in water, pH

Qing-Ri Cao; Yun-Woong Choi; Jing-Hao Cui; Beom-Jin Lee

2005-01-01

180

Modifying drug release and tablet properties of starch acetate tablets by dry powder agglomeration.  

PubMed

In this study three model drugs (N-acetyl-D-glucosamine (NAG), anhydrous caffeine, and propranolol hydrochloride) were agglomerated with starch acetate (SA) by mixing the binary powders on a stainless steel (SS) plate. Agglomeration was induced by triboelectrification of the particles during mixing, and it was evaluated as a method to achieve controlled drug release rate. These agglomerates, mixed with different amounts of a disintegrant, were compressed into tablets whose dissolution characteristics were determined. Triboelectric measurements showed that when the drugs were in contact with SS, charges of the opposite polarity were generated to SA (+) and caffeine and NAG (-) promoting adhesion. Instead, propranolol HCl was charged with the same polarity as SA. SEM micrographs showed that smaller caffeine particles, in spite of their larger negative charge, agglomerated less efficiently with SA than larger NAG particles. This emphasizes the importance of particle size in the agglomeration process. Propranolol HCl did not form agglomerates with SA since their particle sizes and charges were identical. As a result, agglomeration of powders prior to tablet compression allows for modification and control of the release rate of the drugs from the SA matrix tablets as well as the tensile strength of the tablets. PMID:17075868

Mäki, Riikka; Suihko, Eero; Rost, Susanne; Heiskanen, Minna; Murtomaa, Matti; Lehto, Vesa-Pekka; Ketolainen, Jarkko

2007-02-01

181

Randomized clinical trial comparing the pharmacokinetics of standard- and increased-dosage lopinavir-ritonavir coformulation tablets in HIV-positive pregnant women.  

PubMed

A lopinavir-ritonavir (LPV/r)-based regimen is recommended during pregnancy to reduce the risk of HIV mother-to-child transmission, but the appropriate dose is controversial. We compared the pharmacokinetics of standard and increased LPV/r doses during pregnancy. This randomized, open-label prospective study enrolled 60 pregnant women between gestational weeks 14 and 30. The participants received either the standard dose (400/100 mg twice a day [BID]) or increased dose (600/150 mg BID) of LPV/r tablets during pregnancy and the standard dose for 6 weeks after childbirth. Pharmacokinetics analysis was performed using a high-performance liquid chromatography-tandem mass spectrometry method. Adherent participants who received the standard dose presented minimum LPV concentrations of 4.4, 4.3, and 6.1 ?g/ml in the second and third trimesters and postpartum, respectively. The increased-dose group exhibited values of 7.9, 6.9, and 9.2 ?g/ml at the same three time points. Although LPV exposure was significantly higher in the increased-dose group, the standard dose produced therapeutic levels of LPV against wild-type virus in all adherent participants, except one patient in the third trimester; 50%, 37.5%, and 25%, and 0%, 15%, and 0% of the participants in the standard- and increased-dose groups failed to achieve therapeutic levels against resistant viruses during the second and third trimesters and after childbirth, respectively. After 12 weeks of treatment and after childbirth, all adherent participants achieved undetectable HIV viral loads, and their babies (49/54) were uninfected. No serious drug-related adverse events were observed. We conclude that the standard dose is appropriate for use during pregnancy and that an increased dose may be necessary for women harboring resistant HIV. (This study has been registered at ClinicalTrials.gov under registration no. NCT00605098.). PMID:24614377

Santini-Oliveira, Marilia; Estrela, Rita de Cássia Elias; Veloso, Valdiléa Gonçalves; Cattani, Vitória Berg; Yanavich, Carolyn; Velasque, Luciane; Torres, Thiago Silva; Marins, Luana Monteiro Spindola; Pilotto, José Henrique; João, Esaú Custódio; Gonçalves, José Carlos Saraiva; Grinsztejn, Beatriz

2014-05-01

182

Potential of carnuba wax in ameliorating brittle fracture during tableting.  

PubMed

Carnuba wax (as binder) forms hard tablets even at low compression load attributable to its high plasticity. The aim of the present study is to investigate its potential in ameliorating brittle fracture (i.e., lamination and capping) a problem often encountered during tableting. Granules of paracetamol (test drug) were made by triturating the drug powder with the melted wax or starch mucilage (20%w/v). Resulting granules were separated into different size fractions which were separately compressed into tablets with and without a centre hole (as in- built defect) using different compression loads. The tablets were evaluated for tensile strength and the data used to calculate the brittle fracture index (BFI), using the expression: BFI = 0.5(T/T(0)-1) where T0 and T are the tensile strength of tablets with and without a centre hole respectively. The BFI values were significantly lower (p<0.05) in tablets made with carnuba wax compared with tablets made with maize starch as binders. Increase in particle size of the granules or lowering of the compression load further ameliorated the brittle fracture tendency of the tablets. Using granules with the larger particle size (850microm) and applying the lowest unit of load (6 arbitrary unit on the load scale of the tableting machine) the BFI values were 0.03 (carnuba wax tablets) and 0.11 (maize starch tablets). When the conditions were reversed (i.e., a highest load, 8 units and the smallest particle size, 212microm) the BFI values now became 0.17 (carnuba wax tablets) and 0.26 (maize starch tablets). The indication is that the use of large granules and low compression loads to form tablets can further enhance the potential of carnuba wax in ameliorating brittle fracture tendency of tablets during their manufacture. PMID:19168422

Uhumwangho, M U; Okor, R S; Adogah, J T

2009-01-01

183

Evaluation and comparison of different brands of domperidone tablets available in Karachi, Pakistan.  

PubMed

Domperidone is an anti-dopaminergic drug used for the treatment of nausea, vomiting and dyspepsia. It has also been used in Parkinson's disease. In this study, five different brands of Domeperidone tablets were selected from the local market for evaluation of their quality as the local market is occupied of many competitors for a single generic. The evaluation of Domperidone tablets was done using various pharmacopoeial and non-pharmacopoeial tests. All the test results fell within BP specified limits for all the selected brands i.e. the results for Brands A to E for weight variation, thickness and diameter were satisfactory and within limits. For Brands A to E, the results for hardness and friability were also satisfactory i.e. 4-10kg/cm2and 0.1-0.6% respectively. The results for Brands A to E for disintegration were 2-6 minutes; for dissolution and assay, the results were 89-92% and 95-99% respectively. The results of similarity factor (f2) also showed that all brands of Domperidone have comparative dissolution profiles. PMID:25015463

Khan, Muhammad Qamar; Razvi, Nighat; Anjum, Fakhsheena; Ghazal, Lubna; Siddiqui, Saeed Ahmed; Shoaib, Muhammad Harris

2014-07-01

184

Development and characterization of buccoadhesive nifedipine tablets  

Microsoft Academic Search

The buccoadhesive controlled-release tablets for delivery of nifedipine were prepared by direct compression of carboxymethyl cellulose (CMC) with carbomer (CP), which showed superior bioadhesion properties compared to polyvinylpyrrolidone (PVP), polyvinyl alcohol (PVA), hydroxypropylmethyl cellulose (HPMC), and acacia in a modified tensiometry method in vitro. The tablets containing 30mg of nifedipine and various amounts of CMC and CP showed a zero-order

J. Varshosaz; Z. Dehghan

2002-01-01

185

Preparation of controlled release tablets of TA-5707F with wax matrix type and their in vivo evaluation in beagle dogs.  

PubMed

Studies on controlled release dosage forms were conducted by using waxy materials for a newly developed anti-allergy drug, 6-methyl-N-(1H-tetrazol-5-yl)-2-pyridinecarboxamide (TA-5707F), which is not maintained at an effective level in blood for a long duration. Four kinds of tablets were prepared by changing the amount of hydrogenated oil (K3 wax) and polyethyleneglycol-6000 in the tablets. Then, they were administered orally to beagle dogs, and the TA-5707F concentration in the plasma was determined by a HPLC method. The pharmacokinetic parameters were estimated and compared with the results of the in vitro dissolution test determined by the JP paddle method and by the disintegration method. The linearity between the in vivo mean dissolution time (MDT) and in vitro MDT was good in both in vitro dissolution methods. However, the MDTs obtained by the disintegration method were one-third of the in vivo MDT, while those obtained by the paddle methods were 3 times higher. This suggests that both the diffusion of TA-5707F through the waxy matrix and the erosion of the wax matrix caused by the gastrointestinal (GI) tract mobility contributed to the in vivo dissolution mechanism. The blood levels were very low when the tablet was administered after giving food. The prolongation of resident time in the stomach and the low solubility of TA-5707F in an acidic medium seemed to be related to the phenomena. By the depression of GI motility using propantheline bromide, the blood levels could be markedly prolonged and the area under the plasma concentration-time curve (AUC) increased 1.3 times. PMID:7581255

Yamakita, H; Maejima, T; Osawa, T

1995-07-01

186

A randomized clinical trial comparing doses and efficacy of lormetazepam tablets or oral solution for insomnia in a general practice setting.  

PubMed

Lormetazepam is a short-acting benzodiazepine hypnotic which is beneficial in shortening the time to onset of sleep. The aim of the study was to assess a new formulation of lormetazepam (oral solution) in comparison with lormetazepam tablets in out-patients with insomnia. This trial was an open randomized parallel group study conducted by 30 general practitioners. One hundred and eight patients took 0.5 mg on the first night and were allowed to increase their dosage by 0.25 mg (for oral solution) and 0.5 mg (for tablets), respectively, each day and every 2 days. The patients assessed the efficacy, acceptability and tolerance of lormetazepam using a diary card and a set of visual analogue scales assessing their sleep. Over 14 days of treatment, the mean daily dose of lormetazepam was lower in the oral solution group than in the tablets group (0.78 mg versus 0.97 mg). The cumulated dose of lormetazepam was lower with the oral solution (18% reduction). No significant difference between the two groups was found in the assessment of sleep characteristics. The occurrence of side effects did not differ between the two groups. These results suggest that a unitary dose as achieved by an oral solution of lormetazepam allows easier determination of the minimal individual effective dose. PMID:14994324

Ancolio, C; Tardieu, S; Soubrouillard, C; Alquier, C; Pradel, V; Micallef, J; Blin, O

2004-03-01

187

Formulation and evaluation of fast dissolving tablets of cinnarizine using superdisintegrant blends and subliming material  

PubMed Central

The aim of this investigation was to develop fast dissolving tablet of cinnarizine. A combination of super disintegrants, i.e., sodium starch glycolate (SSG) and crosscarmellose sodium (CCS) were used along with camphor as a subliming material. An optimized concentration of camphor was added to aid the porosity of the tablet. A 32 full factorial design was applied to investigate the combined effect of two formulation variables: Amount of SSG and CCS. Infrared (IR) spectroscopy was performed to identify the physicochemical interaction between drug and polymer. IR spectroscopy showed that there is no interaction of drug with polymer. In the present study, direct compression was used to prepare the tablets. The powder mixtures were compressed into tablet using flat face multi punch tablet machine. Camphor was sublimed from the tablet by exposing the tablet to vacuum drier at 60°C for 12 hours. All the formulations were evaluated for their characteristics such as average weight, hardness, wetting time, friability, content uniformity, dispersion time (DT), and dissolution rate. An optimized tablet formulation (F 9) was found to have good hardness of 3.30 ± 0.10 kg/cm2, wetting time of 42.33 ± 4.04 seconds, DT of 34.67 ± 1.53 seconds, and cumulative drug release of not less than 99% in 16 minutes. PMID:22247895

Basu, Biswajit; Bagadiya, Abhishek; Makwana, Sagar; Vipul, Vora; Batt, Devraj; Dharamsi, Abhay

2011-01-01

188

The physical characteristics of lyophilized tablets containing a model drug in different chemical forms and concentrations.  

PubMed

Orodispersible tablets, usually prepared using freeze-drying method, are becoming a popular drug formulation for patients who have difficulties swallowing solid dosage forms. The influence of drug solubility and concentration on the physical characteristics of lyophilized tablets composed of mannitol and gelatin was investigated. Phenobarbital and phenobarbital sodium were studied as model drugs. The tablets were analyzed for mechanical strength using a new method employing Instron, a material testing apparatus. For tablets containing phenobarbital in the form of sodium salt, better mechanical strength was demonstrated than for tablets prepared with water insoluble phenobarbital--acid form. Besides, the mechanical characteristics of the tablets indicate that plasticity and porosity were reduced when sodium phenobarbital was incorporated at a higher dose. Lyophilized tablets were not hygroscopic and only a small increase of tablet mass by 1% and 3% was observed after 4 weeks of storage at 40% and 60% RH, respectively. All formulations disintegrated in seconds in water, at a temperature of 37 degrees C. PMID:16022490

Sznitowska, Ma?gorzata; P?aczek, Marcin; Klunder, Ma?gorzata

2005-01-01

189

Inulin as filler-binder for tablets prepared by direct compaction.  

PubMed

The tabletting properties of a number of different amorphous inulin types were investigated. The types varied with respect to chain length, particle size and amount of included air in the particles. Powder flow properties and densities of the different types were investigated. Just as expected, it was found that the flow properties improved with increased particle size of the material. Compactibility was investigated by compression of tablets on a compaction simulator, simulating the compression on high-speed tabletting machines. The bonding capacity of all inulins was high. However, the lubricant sensitivity strongly varied among the different types of inulin. Generally, amorphous materials such as starches are highly lubricant sensitive, because they show ductile behaviour upon compaction. On the other hand, crystalline materials such as dicalcium phosphate dihydrate have a low lubricant sensitivity, because they fragment during compaction. A high lubricant sensitivity was indeed found for amorphous inulins with a low amount of entrapped air. In contrast, the lubricant sensitivity of the amorphous inulin was low when particles containing large amounts of air were compressed. Obviously entrapped air induces fragmentation of the powder particles by which the lubricant film, covering the particles, was destroyed. Tablets prepared from inulin did not disintegrate but they dissolved when incubated in water. The disintegration/dissolution time increased with decreasing chain length of the inulin. The addition of a disintegrant reduced the disintegration time. The somewhat slower dissolution of the longer chain inulin can be an advantage for chewable tablets or lozenges. It was concluded that inulin with large amounts of entrapped air is a good filler-binder and an attractive alternative to commonly used filler-binders. PMID:11803129

Eissens, Anko C; Bolhuis, Gerad K; Hinrichs, Wouter L J; Frijlink, Henderik W

2002-02-01

190

Application and Characterization of Gum from Bombax buonopozense Calyxesas an Excipient in Tablet Formulation  

PubMed Central

This study was undertaken to explore gum from Bombax buonopozense calyxes as a binding agent in formulation of immediate release dosage forms using wet granulation method. The granules were characterized to assess the flow and compression properties and when compressed, non-compendial and compendial tests were undertaken to assess the tablet properties for tablets prepared with bombax gum in comparison with those prepared with tragacanth and acacia gums. Granules prepared with bombax exhibited good flow and compressible properties with angle of repose 28.60°, Carr’s compressibility of 21.30% and Hausner’s quotient of 1.27. The tablets were hard, but did not disintegrate after one hour. Furthermore, only 52.5% of paracetamol was released after one hour. The drug release profile followed zero order kinetics. Tablets prepared with bombax gum have the potential to deliver drugs in a controlled manner over a prolonged period at a constant rate. PMID:24300296

Ngwuluka, Ndidi C.; Kyari, Jehu; Taplong, John; Uwaezuoke, Onyinye J.

2012-01-01

191

Tableting lipid-based formulations for oral drug delivery: a case study with silica nanoparticle-lipid-mannitol hybrid microparticles.  

PubMed

Silica-lipid-mannitol hybrid (SLMH) microparticles have been developed that were compressible into high quality tablets suitable for oral dosing and delivery of poorly soluble drugs. SLMH tablets enable high lipid-loading levels (>40%) and retain the immediate release, enhanced lipase digestion and drug solubilisation performance. Specifically, we report formulation optimisation of SLMH microparticles and tablets using coumarin 102 (log P = 4.09) as a model Biopharmaceutics Classification System class II drug. SLMH tablets were acceptable according to standard British Pharmacopoeia friability, hardness and disintegration tests; this is not the case for conventional dry emulsions. Furthermore, in vitro dissolution and pancreatic-lipase-induced lipolysis studies under simulated intestinal conditions have demonstrated enzymatic-digestion-mediated drug solubilisation. SLMH microparticles and tablets are suitable as liquid lipid containing solid dosage forms for enhancing and controlling oral absorption of poorly soluble drugs. PMID:23242712

Bremmell, Kristen E; Tan, Angel; Martin, Amanda; Prestidge, Clive A

2013-02-01

192

Finitely Additive Conditional Probabilities, Conglomerability and Disintegrations  

Microsoft Academic Search

For any finitely additive probability measure to be disintegrable, that is, to be an average with respect to some marginal distribution of a system of finitely additive conditional probabilities, it suffices, and is plainly necessary, that the measure be conglomerative, that is, that there be a conditional expectation such that the expectation of no random variable can be negative if

Lester E. Dubins

1975-01-01

193

Pharmaceutical quality of seven generic Levodopa/Benserazide products compared with original Madopar® / Prolopa®  

PubMed Central

Background By definition, a generic product is considered interchangeable with the innovator brand product. Controversy exists about interchangeability, and attention is predominantly directed to contaminants. In particular for chronic, degenerative conditions such as in Parkinson’s disease (PD) generic substitution remains debated among physicians, patients and pharmacists. The objective of this study was to compare the pharmaceutical quality of seven generic levodopa/benserazide hydrochloride combination products marketed in Germany with the original product (Madopar® / Prolopa® 125, Roche, Switzerland) in order to evaluate the potential impact of Madopar® generics versus branded products for PD patients and clinicians. Methods Madopar® / Prolopa® 125 tablets and capsules were used as reference material. The generic products tested (all 100 mg/25 mg formulations) included four tablet and three capsule formulations. Colour, appearance of powder (capsules), disintegration and dissolution, mass of tablets and fill mass of capsules, content, identity and amounts of impurities were assessed along with standard physical and chemical laboratory tests developed and routinely practiced at Roche facilities. Results were compared to the original “shelf-life” specifications in use by Roche. Results Each of the seven generic products had one or two parameters outside the specifications. Deviations for the active ingredients ranged from +8.4% (benserazide) to ?7.6% (levodopa) in two tablet formulations. Degradation products were measured in marked excess (+26.5%) in one capsule formulation. Disintegration time and dissolution for levodopa and benserazide hydrochloride at 30 min were within specifications for all seven generic samples analysed, however with some outliers. Conclusions Deviations for the active ingredients may go unnoticed by a new user of the generic product, but may entail clinical consequences when switching from original to generic during a long-term therapy. Degradation products may pose a safety concern. Our results should prompt caution when prescribing a generic of Madopar®/Prolopa®, and also invite to further investigations in view of a more comprehensive approach, both pharmaceutical and clinical. PMID:23617953

2013-01-01

194

Enantioselective HPLC-DAD method for the determination of etodolac enantiomers in tablets, human plasma and application to comparative pharmacokinetic study of both enantiomers after a single oral dose to twelve healthy volunteers.  

PubMed

An enantioselective high performance liquid chromatographic method with diode array detection (HPLC-DAD) was developed and validated for the determination of etodolac enantiomers in tablets and human plasma. Enantiomeric separation was achieved on a Kromasil Cellucoat chiral column (250 mm × 4.6mm i.d., 5 µm particle size) using a mobile phase consisting of hexane: isopropanol: triflouroacetic acid (90:10:0.1 v/v/v) at a flow rate of 1.0 mL min(-1). The chromatographic system enables the separation of the two enantiomers and the internal standard within a cycle time of 8 min. The resolution between the two enantiomers was 4.25 and the resolution between each enantiomer and the internal standard was more than 2.0. Detection was carried out at 274 nm, and the purity assessment was performed using a photodiode array detector. Solid phase extraction technique using C-18 cartridge was applied to extract the analytes from the plasma samples, and the percentage recovery was more than 95% for the lower quantification limit. The method has been validated with respect to selectivity, linearity, accuracy and precision, robustness, limit of detection and limit of quantification. The validation acceptance criteria were met in all cases. The linearity range for the determination of each enantiomer in human plasma was 0.4-30.0 µg mL(-1) and the limits of quantification of R-etodolac and S-etodolac were 0.20 and 0.19 µg mL(-1), respectively. The validated method was successfully applied to the determination of etodolac enantiomers in tablets and to a comparative pharmacokinetic study of the two enantiomers after the administration of 300 mg single oral dose etodolac racemate tablets to twelve healthy volunteers. PMID:25159440

Hewala, Ismail I; Moneeb, Marwa S; Elmongy, Hatem A; Wahbi, Abdel-Aziz M

2014-12-01

195

Effect of hydrophilic diluents on the release profile of griseofulvin from tablet formulations.  

PubMed

Studies have shown that when compressing drugs with low aqueous solubility, the solubility of diluents selected is very crucial as it influences the disintegration, dissolution and bioavailability of such drugs. Based on these reports, the present study was undertaken to investigate the effect of some commonly used hydrophilic tablet diluents (lactose, sucrose, mannitol and dextrose) on the in vitro release properties of griseofulvin from compressed tablets. Griseofulvin granules and tablets were prepared using the wet granulation method. Tablet properties evaluated as a function of the diluents used include, hardness, friability, dissolution profile and dissolution efficiency at 60 min. Results obtained indicated variability in griseofulvin release in the presence of the diluents. The relative enhanced dissolution effects of the four hydrophilic diluents is in the order of dextrose>sucrose>lactose>mannitol. All the griseofulvin tablet batches produced exhibited a better drug release (in terms of rate and extent of release) than a commercially available tablet sample of griseofulvin (Fulcin(®)). The results of the dissolution efficiency (DE60min) are 91.7, 83.5, 48.7, 35.3 and 15.6% for dextrose, sucrose, lactose, mannitol and fulcin(®), respectively. The overall results indicated that dextrose or sucrose can be utilised to improve the in vitro release profile and hence in vivo bioavailability of griseofulvin from compressed tablets. PMID:24591749

Umeh, O N C; Azegba, J C; Ofoefule, S I

2013-11-01

196

Material and tableting properties of Azadirachta indica gum with reference to official acacia gum.  

PubMed

This study determined the material and tableting properties of Azadirachta indica gum (NMG) relative to acacia gum (ACA). The morphological properties were assessed with size and shape factors of aspect ratio, roundness, irregularity and equivalent-circle-diameter. The tableting properties of the gums were determined using compressional characteristics, tensile strength (TS), brittle fracture index (BFI) and crushing-strength-friability/disintegration-time ratio (CSFR/DT). The results suggest that NMG possesses larger, irregular and more elongated particles than ACA. The onset and amount of plastic deformation occurring in NMG was faster and higher, respectively, than in ACA. The result shows that, although ACA tablets were stronger, their tendency to cap/laminate was higher than in NMG tablets. The NMG tablets possess lower DT than those of ACA, while the CSFR/DT result suggests that a better balance exists between the strength and weakness of NMG tablets. The study concluded that NMG can be a useful excipient in tablet formulation. PMID:24779199

Ogunjimi, Abayomi T; Alebiowu, Gbenga

2014-01-01

197

Effect of Hydrophilic Diluents on the Release Profile of Griseofulvin from Tablet Formulations  

PubMed Central

Studies have shown that when compressing drugs with low aqueous solubility, the solubility of diluents selected is very crucial as it influences the disintegration, dissolution and bioavailability of such drugs. Based on these reports, the present study was undertaken to investigate the effect of some commonly used hydrophilic tablet diluents (lactose, sucrose, mannitol and dextrose) on the in vitro release properties of griseofulvin from compressed tablets. Griseofulvin granules and tablets were prepared using the wet granulation method. Tablet properties evaluated as a function of the diluents used include, hardness, friability, dissolution profile and dissolution efficiency at 60 min. Results obtained indicated variability in griseofulvin release in the presence of the diluents. The relative enhanced dissolution effects of the four hydrophilic diluents is in the order of dextrose>sucrose>lactose>mannitol. All the griseofulvin tablet batches produced exhibited a better drug release (in terms of rate and extent of release) than a commercially available tablet sample of griseofulvin (Fulcin®). The results of the dissolution efficiency (DE60min) are 91.7, 83.5, 48.7, 35.3 and 15.6% for dextrose, sucrose, lactose, mannitol and fulcin®, respectively. The overall results indicated that dextrose or sucrose can be utilised to improve the in vitro release profile and hence in vivo bioavailability of griseofulvin from compressed tablets. PMID:24591749

Umeh, O. N. C.; Azegba, J. C.; Ofoefule, S. I.

2013-01-01

198

Optimization of disintegration behavior of biodegradable poly (hydroxy butanoic acid) copolymer mulch films in soil environment  

NASA Astrophysics Data System (ADS)

Biodegradation of polymeric films used for mulch film applications in agriculture not only eliminates problems of sorting out and disposal of plastics films, but also ensures increased yields in crop growth and cost reduction. One such polymer which is completely biodegradable in the soil is poly 3-hydroxy butanoic acid copolymer, which is a promising alternative to non-biodegradable incumbent polyethylene mulch films. The purpose of mulch film made of poly 3-hydroxy butanoic acid copolymers is to sustain itself during the crop growth and disintegrate and eventually biodegrade back to nature after the crop cycle is over. The disintegration phase of the biodegradation process was evaluated for poly 3-hydroxy butanoic acid copolymer incorporated with no additive, antimicrobial additives, varying amount of crystallinities, another biodegradable polymer, and in different soils, with or without varying soil moisture content. The tools used for quantification were weight loss and visual observation. The test method was standardized using repeatability tests. The onset of disintegration was optimized with addition of right anti-microbial additives, higher crystallinity of film, blending with other biodegradable polymers, compared to virgin poly 3-hydroxy butanoic acid copolymer film. The onset of disintegration time was reduced when soil moisture content was reduced. After the onset of disintegration, the polymer film was physically and mechanically deteriorated, withering away in soil, which is possible to tailor with the crop growth cycle.

Mahajan, Viabhav

199

Pharmacokinetic Comparative Study of Gastrodin and Rhynchophylline after Oral Administration of Different Prescriptions of Yizhi Tablets in Rats by an HPLC-ESI/MS Method  

PubMed Central

Pharmacokinetic characters of rhynchophylline (RIN), gastrodin (GAS), and gastrodigenin (p-hydroxybenzyl alcohol, HBA) were investigated after oral administration of different prescriptions of Yizhi: Yizhi tablets or effective parts of tianma (total saponins from Gastrodiae, EPT) and gouteng (rhynchophylla alkaloids, EPG). At different predetermined time points after administration, the concentrations of GAS, HBA, and RIN in rat plasma were determined by an HPLC-ESI/MS method, and the main pharmacokinetic parameters were investigated. The results showed that the pharmacokinetic parameters Cmax and AUC0–? (P < 0.05) were dramatically different after oral administration of different prescriptions of Yizhi. The data indicated that the pharmacokinetic processes of GAS, HBA, and RIN in rats would interact with each other or be affected by other components in Yizhi. The rationality of the compatibility of Uncaria and Gastrodia elata as a classic “herb pair” has been verified from the pharmacokinetic viewpoint. PMID:25610474

Ge, Zhaohui; Liang, Qionglin; Wang, Yiming; Luo, Guoan

2014-01-01

200

Pharmacokinetic Comparative Study of Gastrodin and Rhynchophylline after Oral Administration of Different Prescriptions of Yizhi Tablets in Rats by an HPLC-ESI/MS Method.  

PubMed

Pharmacokinetic characters of rhynchophylline (RIN), gastrodin (GAS), and gastrodigenin (p-hydroxybenzyl alcohol, HBA) were investigated after oral administration of different prescriptions of Yizhi: Yizhi tablets or effective parts of tianma (total saponins from Gastrodiae, EPT) and gouteng (rhynchophylla alkaloids, EPG). At different predetermined time points after administration, the concentrations of GAS, HBA, and RIN in rat plasma were determined by an HPLC-ESI/MS method, and the main pharmacokinetic parameters were investigated. The results showed that the pharmacokinetic parameters C max and AUC0-? (P < 0.05) were dramatically different after oral administration of different prescriptions of Yizhi. The data indicated that the pharmacokinetic processes of GAS, HBA, and RIN in rats would interact with each other or be affected by other components in Yizhi. The rationality of the compatibility of Uncaria and Gastrodia elata as a classic "herb pair" has been verified from the pharmacokinetic viewpoint. PMID:25610474

Ge, Zhaohui; Xie, Yuanyuan; Liang, Qionglin; Wang, Yiming; Luo, Guoan

2014-01-01

201

Pulse release of doxazosin from hydroxyethylcellulose compression coated tablet: Mechanistic and in vivo study.  

PubMed

Chronotherapeutically programmed hydroxyethylcellulose (HEC) based compression coated doxazosin tablets were prepared and the influence of disintegrants croscarmellose sodium, l-hydroxypropylcellulose (l-HPC), gellan gum on drug release and in vivo performance were investigated. Infrared spectroscopy and differential scanning calorimetric studies did not indicate any excipient incompatibility in the tablets. The disintegrants induced a continuous water influx resulting in a rapid expansion of the membrane. The subsequent formation of fractures into the coats leads to a fast drug release after an initial lag time. Release rates indicated that croscarmellose sodium and l-HPC were directly proportional to their concentration in the formulations. In vitro optimized croscarmellose sodium-HEC matrix showed significantly faster (p<0.05) drug release (t90%=46min) after an initial lag of 243min. Disintegrant-HEC blended matrices were found significantly superior (p<0.05) in terms of in vitro release and bioavailability in comparison to plain HEC matrices. Drug release kinetics followed modified power law and Weibull model (r>0.99). The mechanism involved in release was anomalous transport and super case II transport with matrix swelling. The pulsatile tablets showed no changes either in physicochemical appearance, drug content or in dissolution pattern during its accelerated stability studies. PMID:25179280

Biswas, Nikhil; Guha, Arijit; Sahoo, Ranjan Kumar; Kuotsu, Ketousetuo

2015-01-01

202

Evaluation of the material and tablet formation properties of modified forms of Dioscorea starches.  

PubMed

Starches obtained from four different Dioscorea species-namely, White yam (Dioscorea rotundata), Bitter yam (Dioscorea dumetorum), Chinese yam (Dioscorea oppositifolia), and Water yam (Dioscorea alata)-were modified by cross-linking, hydroxypropylation, and dual modification-cross-linking followed by hydroxypropylation. The physicochemical, material, and tablet properties of the modified starches were investigated with the aim of understanding their properties to determine their potential use for different applications. The tablet formation properties were assessed using 3D modeling, the Heckel equation, and force-displacement profiles. The analyzed tablet properties were elastic recovery, compactibility, and disintegration. The result indicates that the modifications generally increased the swelling power for all the starches in the rank order hydroxypropyl > hydroxypropylated cross-linked > cross-linked (CL) while the solubility did not show a clear-cut pattern. This indicates that hydroxypropylation generally showed the strongest effects on swelling. Furthermore, hydroxypropylation improved the hot water swelling of the CL starches. The modifications did not cause any detectable morphological change in the starch granules shape or size although slight rupture was observed in some granules. CL starch had the lowest water sorption capacity and hydroxypropylation increased the sorption capacity of the CL starches. The material property results indicate that hydroxypropylation and cross-linking did not significantly improve the flowability and compressibility but improved bonding, which resulted in an increased compaction and higher tablet crushing force even though they all disintegrated rapidly. Thus, the modified Dioscorea starches showed potentials for development as new excipients in solid dosage form design, and they could be useful as disintegrants or for Soft tableting. PMID:19832640

Odeku, Oluwatoyin A; Picker-Freyer, Katharina M

2009-11-01

203

Integration of Trade and Disintegration of Production in the Global Economy  

Microsoft Academic Search

The last few decades have seen a spectacular integration of the global economy through trade. The rising integration of world markets has brought with it a disintegration of the production process, however, in which manufacturing or services activities done abroad are combined with those performed at home. The author compares several different measures of foreign outsourcing and argues that they

Robert C. Feenstra

1998-01-01

204

Microstructural investigation of tablet compaction and tablet pharmacological properties  

E-print Network

In current tablet manufacturing processes, there is a knowledge gap concerning material transformation and the subsequent impact on tablet properties; this gap presents a barrier to rational formulation / process design. ...

Mao, Kangyi

2010-01-01

205

The use of inorganic salts to improve the dissolution characteristics of tablets containing Soluplus®-based solid dispersions.  

PubMed

The dissolution enhancement advantages inherent to amorphous solid dispersions systems are often not fully realized once they are formulated into a solid dosage form. The objective of this study was to investigate the ability of inorganic salts to improve the dissolution rate of carbamazepine (CBZ) from tablets containing a high loading of a Soluplus®-based solid dispersion. Cloud point and viscometric studies were conducted on Soluplus® solutions to understand the effect of temperature, salt type and salt concentration on the aqueous solubility and gelling tendencies of Soluplus®, properties that can significantly impact dissolution performance. Studies indicated that Soluplus® exhibited a cloud point that was strongly dependent on the salt type and salt concentration present in the dissolving medium. The presence of kosmotropic salts dehydrated the polymer, effectively lowering the cloud point and facilitating formation of a thermoreversible hydrogel. The ability of ions to impact the cloud point and gel strength generally followed the rank order of the Hofmeister series. Solid dispersions of CBZ and Soluplus® were prepared by KinetiSol® Dispersing, characterized to confirm an amorphous composition was formed and incorporated into tablets at very high levels (70% w/w). Dissolution studies demonstrated the utility of including salts in tablets to improve dissolution properties. Tablets that did not contain a salt or those that included a chaotropic salt hydrated at the tablet surface and did not allow for sufficient moisture ingress into the tablet. Conversely, the inclusion of kosmotropic salts allowed for rapid hydration of the entire tablet and the formation of a gel structure with strength dependent on the type of salt utilized. Studies also showed that, in addition to allowing tablet hydration, potassium bicarbonate and potassium carbonate provided effervescence which effectively destroyed the gel network and allowed for rapid dissolution of CBZ. Subsequent dissolution studies in 0.1 N HCl showed that potassium bicarbonate was an effective tablet disintegrant at levels as low as 1% and provided for tablets that rapidly disintegrated over a wide range of applied compression forces, presumably due to synergy between the ability to form a weak hydrogel structure and carbon dioxide liberation. Similar dissolution performance was measured in pH 4.5 acetate buffer, despite reduced polymer solubility caused by kosmotropic salts in solution, demonstrating robustness. With the use of inorganic salts such as potassium bicarbonate, it may be possible to substantially improve disintegration and dissolution characteristics of tablets containing Soluplus®. PMID:23348153

Hughey, Justin R; Keen, Justin M; Miller, Dave A; Kolter, Karl; Langley, Nigel; McGinity, James W

2013-03-12

206

Organic-aqueous crossover coating process for the desmopressin orally disintegrating microparticles.  

PubMed

Abstract The purpose of the present study was to prepare desmopressin orally disintegrating microparticles (ODMs) using organic-aqueous crossover coating process which featured an organic sub-coating followed by an aqueous active coating. Sucrose beads and hydroxypropyl cellulose (HPC) were used as inert cores and a coating material, respectively. Characterizations including size distribution analysis, in-vitro release studies and in-vitro disintegration studies were performed. A pharmacokinetic study of the ODMs was also conducted in eight beagle dogs. It was found that sucrose beads should be coated using organic solvents to preserve their original morphology. For the active coating, the aqueous coating solution should be used for drug stability. When sucrose beads were coated using organic-aqueous crossover coating process, double-layer ODMs with round shapes were produced with detectable impurities below limit of US Pharmacopeia. The median size of ODMs was 195.6??m, which was considered small enough for a good mouthfeel. The ODMs dissolved in artificial saliva within 15?s because of hydrophilic materials including sucrose and HPC in the ODMs. Because of its fast-dissolving properties, 100% release of the drug was reached within 5?min. Pharmacokinetic parameters including Cmax and AUC24 indicated bioequivalence of the ODMs and the conventional immediate release tablets. Therefore, by using the organic-aqueous crossover coating process, double-layer ODMs were successively prepared with small size, round shapes and good drug stability. PMID:24252109

Kim, Ju-Young; Hwang, Kyu-Mok; Park, Chun-Woong; Rhee, Yun-Seok; Park, Eun-Seok

2015-02-01

207

Effects of various excipients on tizanidine hydrochloride tablets prepared by direct compression.  

PubMed

This study was conducted to assess the effects of various excipients in 10 different Tizanidine hydrochloride tablet dosage forms that were prepared by direct compression method (DC). Various excipients are available for DC method; we selected those excipients that are used commonly in tablet manufacturing. The excipients used included lactose anhydrous, di-basic calcium phosphate anhydrous, starch, talc, sodium carboxy methyl cellulose, polyvinyl pyrrolidone (PVP), silicon dioxide (Aerosil), stearic acid, magnesium stearate and microcrystalline cellulose (Avicel). These tablets were then evaluated by performing different pharmacopoeial and non-pharmacopoeial tests (i.e. diameter, hardness, thickness, weight variation, disintegration and assay). It was observed that Formulations B, D and H of Tizanidine hydrochloride gave best results within USP specified limits for the tests employed among all the formulations whereas Formulations F and G showed poor friability, disintegration and dissolution profiles rendering starch in combination of talc and sodium carboxy-methyl cellulose unsuitable for Tizanidine hydrochloride tablet formulations. With the present approach, more studies can be designed using other active ingredients and excipients to get an optimal and cost effective product. PMID:25176379

Khan, Lubna Ghazal; Razvi, Nighat; Anjum, Fakhsheena; Siddiqui, Saeed Ahmed; Ghayas, Sana

2014-09-01

208

Effects of ultrasonic disintegration on sludge microbial activity and dewaterability.  

PubMed

Ultrasonic treatment can disintegrate sludge, enhance microbial activity and improve sludge dewaterability at different energy inputs. To find their relationship, the three phenomena during ultrasonic treatment were investigated synchronously, and an experimental model was established to describe the process of ultrasonic sludge disintegration. Analysis results showed that the changes of sludge microbial activity and dewaterability were dependent on sludge disintegration degree during ultrasonic treatment. When sludge disintegration degree was lower than 20%, sludge flocs were disintegrated into micro-floc aggregates and the microbial activity increased over 20%. When sludge disintegration degree was over 40%, most cells were destroyed at different degree, and sludge activity decreased drastically. Only when sludge disintegration degree was 2-5%, sludge dewaterability was improved with the conditioning of FeCl(3). It was also found that the sonication with low density and long duration was more efficient than sonication with high density and short duration at the same energy input for sludge disintegration, and a transmutative power function model can be used to describe the process of ultrasonic disintegration. PMID:18547717

Huan, Li; Yiying, Jin; Mahar, Rasool Bux; Zhiyu, Wang; Yongfeng, Nie

2009-01-30

209

In vitro and in vivo evaluation of fast-dissolving tablets containing solid dispersion of lamotrigine  

PubMed Central

Aim: Investigation of in vitro/in vivo behavior of fast-dissolving tablets containing solid dispersions (SDs) of lamotrigine (LM) was the aim and focus of the present research work. Material and Methods: The effect of various hydrophilic polymers on the aqueous solubility of LM was studied. Polyethylene glycol (PEG 6000) was selected as the vehicle and SDs were prepared by melting and solvent evaporation method (SEM). Evaluation of SD for dissolution indicated SVM was more appropriate as seen from an enhancement in drug dissolution. Infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffraction studies indicated a lack of physicochemical interaction between the drug and the carrier. A total of nine formulations were compressed into fast-dissolving tablets using Avicel pH 102 as a directly compressible filler and ac-di-sol, sodium starch glycolate and crospovidone as super disintegrates and evaluated for pre- and post-compression parameters and in vitro drug release. Results: Mathematical analysis of in vitro data suggested that first order was most suitable mathematical model for describing the optimized formulation. Stability studies indicated that the effect of storage was insignificant at 5% level of confidence. In vivo studies of pure drug, selected formulation and marketed product were carried out in male Wistar rats and pharmacokinetic (PK) parameters were calculated using PK function for Microsoft Excel. The best formulation has shown Tmax of 0.5 h which was highly significant (P < 0.05) when compared with pure drug and marketed formulation. The statistical significance was assessed by one way analysis of variance. Conclusion: Therefore, the SDs prepared by SEM using PEG 6000 as hydrophilic carrier can be successfully used for improvement of dissolution of LM and resulted in faster onset of action as indicated by in vivo studies. PMID:25599034

Mohan, Arti; Gundamaraju, Rohit

2015-01-01

210

Research studies on the quality of bio-mucoadhesive tablets containing miconazole nitrate.  

PubMed

Biomucoadhesive tablets are widely used to formulate topical antifungal drugs for treating acute oral candidiasis. The research focuses on the pharmaco-technological control of certain bio-mucoadhesive tablets containing miconazole nitrate, formulas developed and prepared by the authors based on the original formulas. The analyzed parameters were: macroscopic aspect, physical-chemical (pH) and pharmacotechnical properties (hardness, friability, mass uniformity, in vitro disintegration).The used methods are described in literature, most of them included in the Romanian and European Pharmacopoeia. The obtained results allow us to conclude that of the five original formulas, two (formulas IV and V) meet the criteria for oral mucosa drug by their tolerance (pH 5.77 to 5.84) and retention time (65-90 min.), the intimate contact of the tablet with the oral mucosa determining a high concentration of active substance. PMID:24505925

Birsan, Magdalena; Popovici, Iuliana; Palade, Laura; Cojocaru, Ileana

2013-01-01

211

Taste-masked orodispersible tablets of cyclosporine self-nanoemulsion lyophilized with dry silica.  

PubMed

Abstract The aim of the current study was to investigate the effects of formulation parameters on the disintegration, water absorption and dissolution characteristics of cyclosporine A (CyA) loaded self-emulsifying drug delivery system (SEDDS) in an orodispersible compacts. Its taste masking efficiency was also attempted using an electronic tongue. ODTs were prepared by freeze-drying liquid SEDDS and synthetic amorphous silica suspension followed by direct compression. The influences of the compression forces and super-disintegrant were evaluated to optimize tablet characteristics. The liquid SEDDS was characterized by vesicular size of 48.5?nm, polydispersity index of 0.95, turbidity of 40.7?NTU and rapid CyA dissolution and emulsification rate. The results of micrometric studies demonstrated an acceptable flow, hardness and friability to indicate good mechanical strength of ODTs. The interaction and Pareto charts demonstrated a greater effect of low compression force to increase the porosity and facilitate the disintegration rather than the deformation action of the super-disintegrant. Super-disintegrant level was the most important factor affecting the dissolution parameter followed by the compression force then their interaction effect. Moreover, as indicated by Euclidean distance values and discrimination indices, the unpalatable taste and aversion taste of CyA to stimuli were masked in its optimized SEDDS incorporated ODTs. PMID:25069592

Zidan, Ahmed S; Aljaeid, Bader M; Mokhtar, Mahmoud; Shehata, Tamer M

2014-07-29

212

Suitability of ?-carrageenan pellets for the formulation of multiparticulate tablets with modified release.  

PubMed

?-Carrageenan is a novel pelletisation aid with high formulation robustness and quick disintegration leading to fast drug release unlike the matrix-like release from non-disintegrating microcrystalline cellulose pellets. Compression of pellets into tablets is cost effective. The feasibility of formulating multiparticulate tablets with coated ?-carrageenan pellets was investigated. Pellets containing a highly soluble drug in acid, namely bisacodyl and ?-carrageenan or MCC as pelletisation aid were prepared, enteric coated with a mixture of Kollicoat(®) MAE 30 DP and Eudragit(®) NE 30 D and compressed using silicified microcrystalline cellulose as embedding powder. The effect of coating level, type of pellet core, compression force and punch configurations on drug release were studied. A sufficient coating thickness for ?-carrageenan pellets was necessary to obtain multiparticulate tablets with adequate resistance in the acid stage regardless of the compression pressure used. While ?-carrageenan pellets and their tablets released over 80% of the drug during the neutral stage only about 20-24% was released from MCC pellets and their tablets. The type of punches used (oblong or round) did not significantly influence the drug release from the prepared tablets. Moreover, sufficient prolonged release properties were obtained with ?-carrageenan pellets containing theophylline as a model drug and coated with Kollicoat(®) SR 30 D using Kollicoat(®) IR as pore former. A lower coating level and higher amount of pore former were needed in case of theophylline pellets formulated with MCC as pelletisation aid. The sustained release properties of both coated pellet formulations were maintained after compression at different compression pressures. PMID:21335073

Ghanam, Dima; Kleinebudde, Peter

2011-05-16

213

Evaluating the effect of coating equipment on tablet film quality using terahertz pulsed imaging.  

PubMed

In this study, terahertz pulsed imaging (TPI) was employed to investigate the effect of the coating equipment (fluid bed and drum coater) on the structure of the applied film coating and subsequent dissolution behaviour. Six tablets from every batch coated with the same delayed release coating formulation under recommended process conditions (provided by the coating polymer supplier) were mapped individually to evaluate the effect of coating device on critical coating characteristics (coating thickness, surface morphology and density). Although the traditional coating quality parameter (weight gain) indicated no differences between both batches, TPI analysis revealed a lower mean coating thickness (CT) for tablets coated in the drum coater compared to fluid bed coated tablets (p<0.05). Moreover, drum coated tablets showed a more pronounced CT variation between the two sides and the centre band of the biconvex tablets, with the CT around the centre band being 22.5% thinner than the top and bottom sides for the drum coated tablets and 12.5% thinner for fluid bed coated tablets. The TPI analysis suggested a denser coating for the drum coated tablets. Dissolution testing confirmed that the film coating density was the drug release governing factor, with faster drug release for tablets coated in the fluid bed coater (98 ± 4% after 6h) compared to drum coated tablets (72 ± 6% after 6h). Overall, TPI investigation revealed substantial differences in the applied film coating quality between tablets coated in the two coaters, which in turn correlated with the subsequent dissolution performance. PMID:23563103

Haaser, Miriam; Naelapää, Kaisa; Gordon, Keith C; Pepper, Michael; Rantanen, Jukka; Strachan, Clare J; Taday, Philip F; Zeitler, J Axel; Rades, Thomas

2013-11-01

214

Novel mechanism for J /? disintegration in relativistic heavy ion collisions  

NASA Astrophysics Data System (ADS)

In this paper we discuss the possibility of J /? disintegration due to Z (3) domain walls that are expected to form in a QGP medium. These domain walls give rise to a localized color electric field, which disintegrates J /?, on interaction, by changing its color composition and simultaneously exciting it to higher states of cc ¯ system.

Atreya, Abhishek; Bagchi, Partha; Srivastava, Ajit M.

2014-09-01

215

Nonlinear disintegration of the internal tide Karl R. Helfrich1  

E-print Network

Nonlinear disintegration of the internal tide Karl R. Helfrich1 and Roger H. J. Grimshaw2 1 The disintegration of a first-mode internal tide into shorter solitary-like waves is considered. Because observations frequently show both tides and waves with amplitudes beyond the re- strictions of weakly nonlinear theory

216

Disintegration of Water Drops in an Electric Field  

Microsoft Academic Search

The disintegration of drops in strong electric fields is believed to play an important part in the formation of thunderstorms, at least in those parts of them where no ice crystals are present. Zeleny showed experimentally that disintegration begins as a hydrodynamical instability, but his ideas about the mechanics of the situation rest on the implicit assumption that instability occurs

Geoffrey Taylor

1964-01-01

217

Development and evaluation of fixed dose bi therapy sublingual tablets for treatment stress hypertension and anxiety  

PubMed Central

Objective: A stress induced rise in the blood pressure. Some believe that patients with hypertension are characterized by a generalized state of increased anxiety. Aim: The purpose of this study is to prepare a fixed dose bi therapy using bisoprolol hemifumarate (BH) as antihypertensive drug and buspirone hydrochloride (BuHCl) as anxiolytic drug, which can be used to treat both diseases concomitantly. Using sublingual tablets is hopeful to improve the BuHCl poor oral bioavailability and to facilitate administration to patients experiencing problems with swallowing. Materials and Methods: A total of 5mg BH and 10mg BuHCl were selected based on compatibility study. A 3×22 full factorial design was adopted for the optimization of the tablets prepared by direct compression method. The effects of the filler type, the binder molecular weight, and the binder type were studied. The prepared formulae were evaluated according to their physical characters as hardness, friability, disintegration time (new modified method and in vivo disintegration time) and wetting properties. In vitro drugs dissolute, permeation through the buccal mucosa and the effect of storage were analyzed by a new valid high pressure liquid chromatography (HPLC) method. Bioavailability study of the selected formula study was carried out and followed by the clinical. Results: The optimized tablet formulation showed accepted average weight, hardness, wetting time, friability, content uniformity, disintegration time (less than 3 min). Maximum drug release could be achieved with in 10 min. In addition enhancing drug permeation through the buccal mucosa and, the maximum concentration of the drug that reached the blood was in the first 10 min which means a rapid onset of action and improved the extent of both drug's absorption. Conclusion: The results revealed that sublingual (F6) tablets containing both drugs would maintain rapid onset of action, and increase bioavailability. BuHCl with BH can be attributed to the marked decline in DBP and SBP. That led to a reduction in the MAP. PMID:24082695

El-Nabarawi, Mohamed A.; Tayel, Saadia A.; Soliman, Nadia A.; Abo Enin, Hadel A.

2013-01-01

218

CES 2011: Tablet Crazy  

ERIC Educational Resources Information Center

Ereaders are so last year. Tablets were the watchword at this year's annual Consumer Electronics Show (CES) in Las Vegas, January 6-9. This year, the show set new records, with some 2700 companies from around the world exhibiting at the multiple exhibition halls and 30,000 attendees gawking at the products. What did they see? There were still some…

Rapp, David

2011-01-01

219

Evaluation of Three Chitin Metal Silicate Co-Precipitates as a Potential Multifunctional Single Excipient in Tablet Formulations  

PubMed Central

The performance of the novel chitin metal silicate (CMS) co-precipitates as a single multifunctional excipient in tablet formulation using direct compression and wet granulation methods is evaluated. The neutral, acidic, and basic drugs Spironolactone (SPL), ibuprofen (IBU) and metronidazole (MET), respectively, were used as model drugs. Commercial Aldactone®, Fleximex® and Dumazole® tablets containing SPL, IBU and MET, respectively, and tablets made using Avicel® 200, were used in the study for comparison purposes. Tablets of acceptable crushing strength (>40 N) were obtained using CMS. The friability values for all tablets were well below the maximum 1% USP tolerance limit. CMS produced superdisintegrating tablets (disintegration time < 1 min) with the three model drugs. Regarding the dissolution rate, the sequence was as follow: CMS > Fleximex® > Avicel® 200, CMS > Avicel® 200 > Dumazole® and Aldactone® > Avicel® 200 > CMS for IBU, MET and SPL, respectively. Compressional properties of formulations were analyzed using density measurements and the compression Kawakita equation as assessment parameters. On the basis of DSC results, CMS co precipitates were found to be compatible with the tested drugs. Conclusively, the CMS co-precipitates have the potential to be used as filler, binder, and superdisintegrant, all-in-one, in the design of tablets by the direct compression as well as wet granulation methods. PMID:20559493

Hamid, Rana Al-Shaikh; Al-Akayleh, Faisal; Shubair, Mohammad; Rashid, Iyad; Remawi, Mayyas Al; Badwan, Adnan

2010-01-01

220

Preparation and characterization of tablet formulation based on solid dispersion of glimepiride and poly(ester amide) hyperbranched polymer.  

PubMed

The feasibility of incorporating a solid dispersion containing poorly soluble antidiabetic drug glimepiride and poly(ester amide) hyperbranched polymer into a tablet using a direct-compression tabletting technique was investigated. Tablet cores were additionally coated with hydroxypropyl methylcellulose phthalate in order to protect the extremely hygroscopic solid dispersion from atmospheric moisture. Preliminary stability studies show that glimepiride, which is in amorphous form within solid dispersion, is chemically stable, even if tablets are exposed to elevated temperature and/or moisture. In-vitro dissolution studies show some impact of storage conditions on the tablet cores disintegration time and, consequently, drug release rate. Glimepiride solubility also deteriorates somewhat, most probably due to its partial recrystallization. Storage conditions much less affect the physical stability of coated tablets, which was ascribed to reduced tablet hygroscopicity due to the presence of protecting coating. The hyperbranched polymers are rather new and complex macromolecules. Therefore, we addressed also the biocompatibility of hyperbranched polymer, i.e., its impact on haemolysis of the red blood cells. The concentration required for the haemolytic effect on the red blood cells is around 100-times higher than its expected gastrointestinal luminal concentration, which makes the occurrence of hyperbranched polymer mediated cytotoxicity very unlikely. PMID:21812524

Reven, Sebastjan; Homar, Miha; Peternel, Luka; Kristl, Julijana; Žagar, Ema

2013-01-01

221

Comparison of the Rates of Disintegration, Gastric Emptying, and Drug Absorption Following Administration of a New and a Conventional Paracetamol Formulation, Using ? Scintigraphy  

Microsoft Academic Search

Purpose. To investigate the hypothesis that faster drug absorption from a new paracetamol formulation containing sodium bicarbonate compared to that from a conventional formulation results from a combination of enhanced gastric emptying and disintegration\\/dissolution.

Kilian Kelly; Bridget O'Mahony; Blythe Lindsay; Tamara Jones; Tim J. Grattan; Amin Rostami-Hodjegan; Howard N. E. Stevens; Clive G. Wilson

2003-01-01

222

Validation of standard manufacturing procedure of Gu??c? sattva (aqueous extract of Tinospora cordifolia (Willd.) Miers) and its tablets  

PubMed Central

Introduction: Gu??ci Sattva is a highly valued formulation among ayurvedic physicians, commonly recommended in conditions such as Jvara (fever), D?ha (burning sensation) and other conditions of Pitta predominance. In spite of its numerous medicinal attributes, no published work is available until date on manufacturing guidelines along with its quality control parameters. Aims and Objectives: The aim of this study is to develop the standard manufacturing procedure for preparation of Gu??ci Sattva and its tablets. Materials and Methods: A total of 15 batches of Gu??ci Sattva were prepared in the laboratory. During its preparation, pharmaceutical findings and observations were systematically recorded. To maintain quality control, Gu??ci Sattva tablets were further subjected to analysis such as shape, diameter, width, hardness, weight variation, disintegration time (DT) and friability. Qualitative analysis to detect the presence of various functional groups and high performance thin layer chromatography (HPTLC) profile were also carried out. Results and Conclusion: The average percentage of dried Sattva obtained was 3.8%. The tablets were prepared by direct compression method as per pharmacopoeal specifications. Optimum hardness, weight of tablets, DT and friability of Gu??ci Sattva tablets were found complying with official standards. Alkaloids, carbohydrates and starch were found present in Sattva tablets. Number of peaks obtained in HPTLC also corresponds to this finding. Data obtained by present study may be considered as standard for future studies. Conclusion: The average percentage of dried Sattva obtained was 3.8%. The tablets were prepared by direct compression method as per pharmacopoeal specifications. Optimum hardness, weight of tablets, DT and friability of Gu??ci Sattva tablets were found complying with official standards. Alkaloids, carbohydrates and starch were found present in Sattva tablets. Number of peaks obtained in HPTLC also corresponds to this finding. Data obtained by present study may be considered as standard for future studies. PMID:25161327

Sharma, Rohit; Amin, Hetal; Galib; Prajapati, P. K.

2013-01-01

223

Randomized, double-blind, placebo-controlled and active-controlled study to assess the relative abuse potential of oxycodone HCl-niacin tablets compared with oxycodone alone in nondependent, recreational opioid users  

PubMed Central

Background Abuse-deterrent formulations attempt to address public health and societal concerns regarding opioid abuse. Oxycodone HCl-niacin tablets combine oxycodone HCl with niacin and functional inactive excipients to create potential barriers to oral, intranasal, and intravenous abuse. This study compared the relative abuse potential of oral immediate-release oxycodone HCl-niacin with that of oral immediate-release oxycodone HCl and placebo in nondependent, recreational opioid users. Methods Forty-nine participants received oxycodone HCl-niacin 40/240 mg and 80/480 mg, oxycodone 40 mg and 80 mg, and placebo in a randomized, double-blind, placebo-controlled and active-controlled, five-way crossover study. Primary endpoints based on a bipolar 100 mm visual analog scale for drug liking were area under effect curve (AUE0–1h, AUE0–2h, AUE0–3h), peak disliking, and effect at 0.5 hours post-dose (E0.5h). Other endpoints included take drug again assessment, overall drug liking, and pupillometry. Results There were statistically significant differences between oxycodone HCl-niacin and oxycodone HCl doses for all primary endpoints (P < 0.0001, all comparisons), suggesting reduced abuse potential with oxycodone HCl-niacin. Take drug again and overall drug liking showed greater liking of oxycodone alone. Oxycodone HCl-niacin 80/480 mg had consistently lower liking assessments than oxycodone HCl-niacin 40/240 mg, suggesting a dose-response to the aversive effects of niacin. Opioid-related adverse events were similar for equivalent oxycodone doses. The treatment-emergent adverse events most specifically associated with oxycodone HCl-niacin (ie, skin-burning sensation, warmth, and flushing) were consistent with the expected vasocutaneous effects of niacin. No serious adverse events were reported. Conclusion Oxycodone HCl-niacin tablets may, in a dose-dependent manner, decrease the potential for oral abuse of oxycodone without unexpected adverse events or clinically signifi-cant differences in safety parameters compared with oxycodone alone. Although statistically powered, the small size of the study sample and the characteristics of its participants may not be generalizable to the population that abuses prescription opioid medications. PMID:24474870

Webster, Lynn R; Rolleri, Robert L; Pixton, Glenn C; Sommerville, Kenneth W

2012-01-01

224

Design and Optimization of Domperidone Fast Dissolving Tablet Using Central Composite Design.  

PubMed

The main aim of this work was to optimize fast dissolving tablet (FDT) formulation using response surface approach. The variables studied were sodium bicarbonate (X1), citric acid (X2), and superdisintegrant, Ac-Di-Sol (X3). The main aspect of present work was to develop FDT of Domperidone with fast disintegration and high mechanical strength. It was found that the response was affected by all the three factors studied. The statistical models were successfully used to prepare FDT of Domperidone with fast disintegration (31.08 seconds) and adequate hardness (4.1 kg/cm2). Pharmacokinetic studies in rats showed statistically insignificant difference (p>0.05) between Domperidone fast dissolving tablet (DFDT) and marketed product, concluded that optimized FDT was found to be bioequivalent with the marketed formulation. The values of Tmax were found to be 0.5 h and 0.75 h for DFDT and reference product, respectively. Conditioned place aversion study was performed on Swiss Albino mice and the study showed the better anti emetic potency of optimized FDT in nauseated condition over market product (p<0.05). Thus, the present investigation conclusively demonstrates the potential role in terms of rapid disintegration and high mechanical strength. PMID:25335985

Shailendra, Bhatt; Shailendra, Mandge; Manish, Jaimini; Singh, Tanwar Yuvraj; Priti, Trivedi

2014-10-21

225

New Dissolution Method for Mesalamine Tablets and Capsules  

Microsoft Academic Search

Dissolution methods are different for extended-release mesalamine capsules (pH 7.5 only) and delayed-release tablets (pH 1.4, 6.0, and 7.2). Mesalamine is used for the treatment of ulcerative colitis. The USP methods have several drawbacks in that they do not mimic gastrointestinal tract environments; tablets are removed from vessels to change dissolution medium; and neither method has been adopted to compare

Monica C. Chuong; J. Mark Christensen; James W. Ayres

226

Bioavailability of syrup and tablet formulations of cefetamet pivoxil.  

PubMed Central

Two studies examining the bioavailability of cefetamet pivoxil in healthy male subjects were conducted. In the first, the bioavailabilities of the 250-mg (M250) and M500 tablet formulations of cefetamet pivoxil to be marketed were compared with that of a tablet used in clinical trials. All products were given with food at a dose of 500 mg. In the second study, the bioavailability of the syrup formulation was evaluated under both fasting and nonfasting conditions and compared with that of the M500 tablet formulation given with food. The absolute bioavailabilities of the M500 and M250 tablets (55.0% +/- 8.0% and 55.7% +/- 7.0%, respectively) were not significantly different from that of the clinical-trial formulation (49.8% +/- 8.5%). The newer tablet formulations exhibited faster absorption as evidenced by higher peak concentrations (3.8 [M500] and 3.9 [M250] mg/liter compared with 3.2 mg/liter for the clinical-trial formulation), a shorter time to peak concentration, and a shorter mean absorption time. The syrup formulation was found to have significantly lower absolute bioavailability (37.9% +/- 6.0%) compared with that of the M500 tablet (58.4% +/- 9.0%) when both were given with food. Food had no significant effect on the bioavailability of the syrup, which averaged 34.0% +/- 8.6% under fasting conditions, although absorption was delayed by food (mean absorption time increased from 2.2 to 3.9 h). This contrasts with the results of previous studies documenting significant increases in tablet bioavailability with food. Despite the lower bioavailability of the syrup, unbound-cefetamet concentrations are expected to remain above the MICs for 90% of the strains tested for susceptible organisms for approximately 10 h of the usual 12-h dosing interval with both syrup and tablet formulations of cefetamet pivoxil given with food. PMID:8109939

Ducharme, M P; Edwards, D J; McNamara, P J; Stoeckel, K

1993-01-01

227

21 CFR 520.581 - Dichlorophene tablets.  

Code of Federal Regulations, 2010 CFR

... § 520.581 Dichlorophene tablets. (a) Specifications. Each tablet contains 1 gram of dichlorophene...Amount. Single dose of 1 tablet (1 gram of dichlorophene...foods and milk for at least 12 hours prior to medication...

2010-04-01

228

21 CFR 520.812 - Enrofloxacin tablets.  

Code of Federal Regulations, 2010 CFR

...2010-04-01 false Enrofloxacin tablets. 520.812 Section 520... § 520.812 Enrofloxacin tablets. (a) Specifications. Each tablet contains either 22.7, 68...divided into 2 equal doses at 12 hour intervals,...

2010-04-01

229

21 CFR 520.455 - Clomipramine tablets.  

Code of Federal Regulations, 2010 CFR

...2010-04-01 false Clomipramine tablets. 520.455 Section 520... § 520.455 Clomipramine tablets. (a) Specifications. Each tablet contains 5, 20, 40, or 80...veterinarian. [64 FR 1762, Jan. 12, 1999, as amended at 72...

2010-04-01

230

DC calcium lactate, a new filler-binder for direct compaction of tablets.  

PubMed

In this paper, a directly compressible form of calcium lactate is introduced as a filler-binder for direct compaction of tablets. Calcium lactate is one of the most important calcium sources and has, in comparison with other organic calcium salts, a good solubility and bioavailability. Two different modifications, calcium lactate trihydrate and calcium lactate pentahydrate are described in the main pharmacopoeias. This paper describes that the compaction properties of calcium lactate pentahydrate (Puracal DC) are much better than those of the calcium lactate trihydrate (Puracal TP). Calcium lactate pentahydrate has better compaction properties than dicalcium phosphate dihydrate, even if lubricated with magnesium stearate. Moreover, as a consequence of its crystalline structure, calcium lactate pentahydrate has a low compaction speed sensitivity. This means that, in combination with its excellent flow properties, calcium lactate pentahydrate is a suitable filler-binder in tablets prepared by high-speed compaction. In a number of formulation examples it will be illustrated that tablets containing calcium lactate pentahydrate as main or additional filler-binder have a short disintegration time and a fast drug release. Directly compressible calcium lactate can be considered as a promising excipient in both pharmaceutical tablets and tablets for the nutraceutical market. PMID:11397569

Bolhuis, G K; Eissens, A C; Zoestbergen, E

2001-06-19

231

Hard Photo-disintegration of proton pairs in ^3He  

NASA Astrophysics Data System (ADS)

Hard deuteron photo-disintegration has been investigated for 20 years, as its cross sections follow the constituent counting rules and it provides insight into the interplay between hadronic and quark-gluon degrees of freedom in high-momentum transfer exclusive reactions. We have now measured for the first time hard pp-pair disintegration in the reaction ?,3 He ->pp + n, using kinematics corresponding to a spectator neutron. Clues to the underlying physics can be found in the comparison of our measurements with deuteron photo-disintegration, the energy dependence of the cross sections at 90^o c.m., the ?n distribution, and the angular distribution.

Gilman, Ronald; Piasetzky, Eli; Pomerantz, Ishay

2007-10-01

232

Comparative study of the continuous wavelet transform, derivative and partial least squares methods applied to the overlapping spectra for the simultaneous quantitative resolution of ascorbic acid and acetylsalicylic acid in effervescent tablets.  

PubMed

The simultaneous spectrophotometric determination of ascorbic acid (AA) and acetylsalicylic acid (ASA) in effervescent tablets in the presence of the overlapping spectra was accomplished by the continuous wavelet transform (CWT), derivative spectrophotometry (DS) and partial least squares (PLS) approaches without using any chemical pre-treatment. CWT and DS calibration equations for AA and ASA were obtained by measuring the CWT and DS amplitudes corresponding to zero-crossing points of spectra obtained by plotting continuous wavelet coefficients and first-derivative absorbance values versus the wavelengths, respectively. The PLS calibration was constructed by using the concentration set and its full absorbance data consisting of 850 points from 220 to 305 nm in the range of 210-310 nm. These three methods were tested by analyzing the synthetic mixtures of the above drugs and they were applied to the real samples containing two commercial pharmaceutical preparations of subjected drugs. A comparative study was carried out by using the experimental results obtained from three analytical methodologies and precise and accurate results were obtained. PMID:15740918

Dinç, Erdal; Ozdemir, Abdil; Baleanu, Dumitru

2005-03-01

233

Formulation, development, and performance evaluation of metoclopramide HCl oro-dispersible sustained release tablet.  

PubMed

The present study was undertaken to develop and evaluate an oro-dispersible, sustained release tablet of metoclopramide HCl. The technology was comprised of developing sustained release microparticles, and compression of resultant microspheres into a fast dispersible tablet by direct compression. The microspheres of metoclopramide HCl were prepared by an emulsification-solvent evaporation method using ethylcellulose as the matrix polymer. The prepared microspheres were evaluated for morphology, particle size, entrapment efficiency, and in vitro drug release characteristics. Scanning electron microscopy demonstrated spherical particles with a mean diameter of 81.27 ± 5.87 ?m and the drug encapsulation efficiency was found to be 70.15 ± 3.06%. The process and formulation variables such as rotation speed, polymer concentration, and drug concentration influenced the drug encapsulation efficiency and in vitro drug release. Optimized microspheres were compressed into tablets which were comprised of metoclopramide HCl microspheres, 53% (w/v) of D-mannitol granules, 7% (w/w) of Polyplasdone XL 10, and 0.5% (w/w) of calcium stearate. The tablets demonstrated a hardness of 59 ± 3 N, friability of 0.21% and disintegration time of 27 ± 3 sec. The formulations were subjected to stability studies as per ICH guidelines and were found to be stable after a 6 month study. In vivo experiments conducted in rats demonstrated that a constant level of metoclopramide HCl in plasma could be maintained for up to 20 h at a suitable concentration for antiemetic activity. An appropriate combination of excipients made it possible to obtain orally disintegrating sustained release tablets of metoclopramide HCl using simple and conventional techniques. PMID:22076769

Kasliwal, Nikhil; Negi, Jeetendra Singh; Jugran, Vandana; Jain, Rahul

2011-10-01

234

Developing a mapping tool for tablets  

NASA Astrophysics Data System (ADS)

Digital field mapping offers significant benefits when compared with traditional paper mapping techniques in that it provides closer integration with downstream geological modelling and analysis. It also provides the mapper with the ability to rapidly integrate new data with existing databases without the potential degradation caused by repeated manual transcription of numeric, graphical and meta-data. In order to achieve these benefits, a number of PC-based digital mapping tools are available which have been developed for specific communities, eg the BGS•SIGMA project, Midland Valley's FieldMove®, and a range of solutions based on ArcGIS® software, which can be combined with either traditional or digital orientation and data collection tools. However, with the now widespread availability of inexpensive tablets and smart phones, a user led demand for a fully integrated tablet mapping tool has arisen. This poster describes the development of a tablet-based mapping environment specifically designed for geologists. The challenge was to deliver a system that would feel sufficiently close to the flexibility of paper-based geological mapping while being implemented on a consumer communication and entertainment device. The first release of a tablet-based geological mapping system from this project is illustrated and will be shown as implemented on an iPad during the poster session. Midland Valley is pioneering tablet-based mapping and, along with its industrial and academic partners, will be using the application in field based projects throughout this year and will be integrating feedback in further developments of this technology.

Vaughan, Alan; Collins, Nathan; Krus, Mike

2014-05-01

235

Use of Propranolol-Magnesium Aluminium Silicate Intercalated Complexes as Drug Reservoirs in Polymeric Matrix Tablets  

PubMed Central

The objective of the present study was to investigate the use of propranolol–magnesium aluminium silicate intercalated complexes as drug reservoirs in hydroxypropylmethylcellulose tablets. The matrix tablets containing the complexes were prepared and characterised with respect to propranolol release and were subsequently compared with those loading propranolol or a propranolol–magnesium aluminium silicate physical mixture. Additionally, the effects of varying viscosity grades of hydroxypropyl methylcellulose, compression pressures and calcium acetate incorporation on the drug release characteristics of the complex-loaded tablets were also examined. The results showed that the complex-loaded tablets have higher tablet hardness than those containing propranolol or a physical mixture. The drug release from the complex-loaded tablets followed a zero-order release kinetic, whereas an anomalous transport was found in the propranolol or physical mixture tablets. The drug release rate of the complex tablet significantly decreased with increasing hydroxypropylmethylcellulose viscosity grade. Increase in the compression pressure caused a decrease in the drug release rate of the tablets. Furthermore, the incorporation of calcium ions could accelerate propranolol release, particularly in acidic medium, because calcium ions could be exchanged with propranolol molecules intercalated in the silicate layers of magnesium aluminium silicate. These findings suggest that propranolol-magnesium aluminium silicate intercalated complexes show strong potential for use as drug reservoirs in matrix tablets intended for modifying drug release. PMID:23626384

Pongjanyakul, T.; Rojtanatanya, S.

2012-01-01

236

Isoniazid, Pyrazinamide and Rifampicin Content Variation in Split Fixed-Dose Combination Tablets  

PubMed Central

Setting In most developing countries, paediatric tuberculosis is treated with split tablets leading to potential inaccuracy in the dose delivery and drug exposure. There is no data on the quality of first-line drugs content in split fixed-dose combination tablets. Objective To determine Isoniazid, Pyrazinamide and Rifampicin content uniformity in split FDC tablets used in the treatment of childhood tuberculosis. Design Drug contents of 15 whole tablets, 30 half tablets and 36 third tablets were analysed by high performance liquid chromatography. The content uniformity was assessed by comparing drug content measured in split portions with their expected amounts and the quality of split portions was assessed applying qualitative specifications for whole tablets. Results All whole tablets measurements fell into the USP proxy for the three drugs. But a significant number of half and third portions was found outside the tolerated variation range and the split formulation failed the requirements for content uniformity. To correct for the inaccuracy of splitting the tablets into equal portions, a weight-adjustment strategy was used but this did not improve the findings. Conclusion In split tablets the content of the three drugs is non-uniform and exceeded the USP recommendations. There is an absolute need to make child-friendly formulations available for the treatment of childhood tuberculosis. PMID:25004128

Pouplin, Thomas; Phuong, Pham Nguyen; Toi, Pham Van; Nguyen Pouplin, Julie; Farrar, Jeremy

2014-01-01

237

ON IMPROVING THE DISINTEGRATION OF AYURVEDIC PILLS CONTAINING GUGGULU  

PubMed Central

An attempt is made in this communication to report a better way of preparing guggulu – containing pills. This technique improves the disintegration time of the preparation, thus enhancing its therapeutic value. PMID:22556694

Chaube, Anjana; Dixit, S.K.; Sharma, P.V.

1995-01-01

238

Separation of the Components of a Commercial Analgesic Tablet: A Two-Week Sequence Comparing Purification by Two-Base Extraction and Column Chromatography  

ERIC Educational Resources Information Center

A new laboratory experiment is described in which students compare two benchtop separation methods to isolate the three active components of the commercial analgesic Excedrin. In the two-week sequence, aspirin, acetaminophen, and caffeine are separated using either a two-base liquid-liquid extraction or silica column chromatography. Students then…

Revell, Kevin D.

2011-01-01

239

Evaluation of Gum of Moringa oleifera as a Binder and Release Retardant in Tablet Formulation.  

PubMed

The present study was undertaken to find out the potential of gum from Moringa oleifera to act as a binder and release retardant in tablet formulations. The effect of calcium sulphate dihydrate (water insoluble) and lactose (water soluble) diluent on the release of propranolol hydrochloride was studied. The DSC thermograms of drug, gum and mixture of gum/drug indicated no chemical interaction. Tablets (F1, F2, F3, and F4) were prepared containing calcium sulphate dihydrate as diluent, propranolol hydrochloride as model drug using 10%, 8%, 6% and 4% w/v of gum solution as binder. Magnesium stearate was used as lubricant. Physical and technological properties of granules and tablets like flow rate, Carr index, Hausner ratio, angle of repose, hardness, friability and disintegration time were determined and found to be satisfactory. Tablets were prepared by wet granulation method containing calcium sulphate dihydrate as excipient, propranolol hydrochloride as model drug using 10%, 20% and 30% of gum as release retardant, magnesium stearate was used as lubricant. Similarly tablets were prepared replacing lactose with calcium sulphate dihydrate. Despite of the widely varying physico-chemical characteristics of the excipients, the drug release profiles were found to be similar. The drug release increased with increasing proportions of the excipient and decreased proportion of the gum irrespective of the solubility characteristics of the excipient. The values of release exponent 'n' are between 0.37 and 0.54. This implies that the release mechanism is Fickian. There is no evidence that the dissolution or erosion of the excipient has got any effect on the release of the drug. The t(50%) values for tablets containing calcium sulphate dihydrate were on an average 10%-15% longer than the tablets containing lactose as excipient. These relatively small differences in t(50%) values suggest that the nature of excipient used appeared to play a minor role in regulating the release, while the gum content was a major factor. PMID:21394258

Panda, D S; Choudhury, N S K; Yedukondalu, M; Si, S; Gupta, R

2008-09-01

240

Characterization of oral disintegrating film containing donepezil for Alzheimer disease.  

PubMed

The aim of this study was to develop a taste-masked oral disintegrating film (ODF) containing donepezil, with fast disintegration time and suitable mechanical strength, for the treatment of Alzheimer's disease. Hydroxypropyl methylcellulose, corn starch, polyethylene glycol, lactose monohydrate and crosspovidone served as the hydrophilic polymeric bases of the ODF. The uniformity, in vitro disintegration time, drug release and the folding endurance of the ODF were examined. The in vitro results showed that 80% of donepezil hydrochloride was released within 5 minutes with mean disintegration time of 44 seconds. The result of the film flexibility test showed that the number of folding time to crack the film was 40 times, an indication of sufficient mechanical property for patient use. A single-dose, fasting, four-period, eight-treatment, double-blind study involving 16 healthy adult volunteers was performed to evaluate the in situ disintegration time and palatability of ODF. Five parameters, namely taste, aftertaste, mouthfeel, ease of handling and acceptance were evaluated. The mean in situ disintegration time of ODF was 49 seconds. ODF containing 7 mg of sucralose were more superior than saccharin and aspartame in terms of taste, aftertaste, mouthfeel and acceptance. Furthermore, the ODF was stable for at least 6 months when stored at 40°C and 75% relative humidity. PMID:22167416

Liew, Kai Bin; Tan, Yvonne Tze Fung; Peh, Kok Khiang

2012-03-01

241

Characterization of physical mixtures and directly compressed tablets of sulfamerazine polymorphs: implications on in vitro release characteristics.  

PubMed

The present study evaluates the effects of excipients, compression pressure, and relative humidity (RH) on the stability of sulfamerazine polymorphs (referred here as SMZ I and SMZ II) and their release from directly compressed tablets using differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and dissolution analysis. SMZ I and SMZ II tablets were compressed with magnesium stearate (MGST), and microcrystalline cellulose (MCC) at 5000, 7500, and 10,000 lbs. pressures and stored at 40, 75, 95, and 100% RH conditions for 5 weeks. There were indications of possible drug-excipient interaction in the binary mixtures under different relative humidity conditions from the DSC data, but they could not be confirmed by PXRD because the crystal structures of the drug and excipients remained unaltered. The crystal structures of the polymorphs in the tablet also remained unaltered under the above conditions. There were, however, significant differences observed in the drug release properties of the two polymorphs. SMZ II was found in general to have a higher rate of drug release than SMZ I. Extensive gelation of MCC under higher moisture conditions, compression pressure during tableting, and inherent tabletability of the sulfamerazine crystals were factors that affected drug release. All these factors contributed towards prolonging the disintegration and deaggregation of the tablet particles and were therefore concluded to be the rate limiting steps for the dissolution process. PMID:12661061

Roy, Shouvik; Alexander, Kenneth S; Riga, Alan T; Chatterjee, Koustuv

2003-04-01

242

Tablet PCs: The Write Approach  

ERIC Educational Resources Information Center

This article discusses the transforming effects of tablet PCs in the classroom. As 1-to-1 computing becomes the goal on K-12 campuses, school districts are turning to this newer, pen-based technology. Saint Mary's School's new Lenovo ThinkPad X41 tablet PCs had transformed the way Saint Mary's teachers did their jobs. Teachers created outlines for…

Milner, Jacob

2006-01-01

243

MTN-001: Randomized Pharmacokinetic Cross-Over Study Comparing Tenofovir Vaginal Gel and Oral Tablets in Vaginal Tissue and Other Compartments  

PubMed Central

Background Oral and vaginal preparations of tenofovir as pre-exposure prophylaxis (PrEP) for human immunodeficiency virus (HIV) infection have demonstrated variable efficacy in men and women prompting assessment of variation in drug concentration as an explanation. Knowledge of tenofovir concentration and its active form, tenofovir diphosphate, at the putative vaginal and rectal site of action and its relationship to concentrations at multiple other anatomic locations may provide key information for both interpreting PrEP study outcomes and planning future PrEP drug development. Objective MTN-001 was designed to directly compare oral to vaginal steady-state tenofovir pharmacokinetics in blood, vaginal tissue, and vaginal and rectal fluid in a paired cross-over design. Methods and Findings We enrolled 144 HIV-uninfected women at 4 US and 3 African clinical research sites in an open label, 3-period crossover study of three different daily tenofovir regimens, each for 6 weeks (oral 300 mg tenofovir disoproxil fumarate, vaginal 1% tenofovir gel [40 mg], or both). Serum concentrations after vaginal dosing were 56-fold lower than after oral dosing (p<0.001). Vaginal tissue tenofovir diphosphate was quantifiable in ?90% of women with vaginal dosing and only 19% of women with oral dosing. Vaginal tissue tenofovir diphosphate was ?130-fold higher with vaginal compared to oral dosing (p<0.001). Rectal fluid tenofovir concentrations in vaginal dosing periods were higher than concentrations measured in the oral only dosing period (p<0.03). Conclusions Compared to oral dosing, vaginal dosing achieved much lower serum concentrations and much higher vaginal tissue concentrations. Even allowing for 100-fold concentration differences due to poor adherence or less frequent prescribed dosing, vaginal dosing of tenofovir should provide higher active site concentrations and theoretically greater PrEP efficacy than oral dosing; randomized topical dosing PrEP trials to the contrary indicates that factors beyond tenofovir’s antiviral effect substantially influence PrEP efficacy. Trial Registration ClinicalTrials.gov NCT00592124 PMID:23383037

Hendrix, Craig W.; Chen, Beatrice A.; Guddera, Vijayanand; Hoesley, Craig; Justman, Jessica; Nakabiito, Clemensia; Salata, Robert; Soto-Torres, Lydia; Patterson, Karen; Minnis, Alexandra M.; Gandham, Sharavi; Gomez, Kailazarid; Richardson, Barbra A.; Bumpus, Namandje N.

2013-01-01

244

Imperatorin sustained-release tablets: In vitro and pharmacokinetic studies.  

PubMed

We prepared and evaluated imperatorin (IMP) sustained-release tablets. IMP is an active compound in Angelica dahuricae, a Chinese herbal medicine. We used different polymers, such as hydroxypropyl methylcellulose (HPMC K4M, K15M, and K100M), carbopol 934P, sodium carboxymethyl cellulose (CMC-Na), and their combinations to prepare the matrix tablets and achieve the desired sustained release profile. The in vitro release profiles of these formulations were examined and fit to various kinetic release models. We also tested the effects of polymer combination ratios on the in vitro release rate. In vivo studies were performed for the optimized formulation in six beagle dogs, and pharmacokinetic parameters were compared with plain IMP tablets. IMP sustained-release tablets exhibited a more sustained plasma concentration than the plain tablets, with a relative bioavailability of 127.25%. The in vitro releases rates and in vivo absorption correlated for the initial 8 hours. These results demonstrate that the sustained-release tablet system can effectively control the release of IMP. PMID:20803124

Pan, Jingjing; Lu, Wen; Li, Changhui; Wang, Sicen; He, Langchong

2010-08-01

245

A phytosterol enriched refined extract of Brassica campestris L. pollen significantly improves benign prostatic hyperplasia (BPH) in a rat model as compared to the classical TCM pollen preparation Qianlie Kang Pule'an Tablets.  

PubMed

In Qinghai Province, the Brassica campestris L. pollen preparation Qianlie Kang Pule'an Tablet (QKPT) is traditionally used for BPH therapy. However, in QKPT the content of supposedly active phytosterols is relatively low at 2.59%, necessitating high doses for successful therapy. Therefore, a phytosterol enriched (4.54%) refined extract of B. campestris pollen (PE) was developed and compared with QKPT in a BPH rat model. Six groups of rats (n=8 each), namely sham-operated distilled water control, castrated distilled water control, castrated QKPT 2.0g/kg, castrated PE 0.1g/kg, castrated PE 0.2g/kg, and castrated PE 0.4g/kg, were intragastrically treated with the respective daily doses. Testosterone propionate (0.3mg/day) was administered to all castrated rats, while the sham-operated group received placebo injections. After 30 days, the animals were sacrificed and prostates as well as seminal vesicles excised and weighted in order to calculate prostate volume index (PVI) as well as prostate index (PI) and seminal vesicle index (SVI), defined as organ weight in g per 100g body weight. Compared with sham-operated controls, PI (p<0.01), PVI (p<0.01), and SVI (p<0.01) were all significantly increased in all castrated, testosterone treated rats. After treatment with PE at 0.4 and 0.2g/kg or QKPT at 2.0g/kg per day, both indices were significantly reduced (p<0.01) as compared to the castrated distilled water control. For PE at 0.1g/kg per day only PI was significantly reduced (p<0.05). At the highest PE concentration of 0.4g/kg per day both PI and SVI were also significantly reduced when compared to the QKPT group (p<0.05). Both PE and QKPT demonstrated curative effects against BPH in the applied animal model. In its highest dose at 0.4g/kg per day, PE was clearly superior to QKPT. PMID:25636883

Wang, Ruwei; Kobayashi, Yuta; Lin, Yu; Rauwald, Hans Wilhelm; Fang, Ling; Qiao, Hongxiang; Kuchta, Kenny

2015-01-15

246

Vardenafil orodispersible tablet.  

PubMed

Vardenafil orodispersible tablet (ODT) is a supralingual formulation of vardenafil that is available for the on-demand treatment of erectile dysfunction. The pharmacokinetics of vardenafil ODT are not equivalent to those of the vardenafil film-coated tablet in that the ODT formulation provides consistently greater vardenafil systemic exposure. Therefore, the two formulations are not interchangeable. The efficacy of on-demand vardenafil ODT 10 mg was established in the POTENT I and II studies, which were 6-week, randomized, double-blind, multinational trials in men with erectile dysfunction of at least 6 months duration. In both trials, vardenafil ODT improved erectile function significantly more than placebo, as indicated by International Index of Erectile Function-Erectile Function subscale scores at week 12 and overall erection success rates during treatment according to responses to questions 2 and 3 of the Sexual Encounter Profile (coprimary endpoints). In a pooled analysis of both trials, vardenafil ODT improved erectile function regardless of age, severity of erectile dysfunction at baseline or the presence or absence of underlying medical conditions. Vardenafil ODT was generally well tolerated in clinical trials, including in men aged ?65 years, and adverse events were mostly mild or moderate in severity. PMID:22191797

Sanford, Mark

2012-01-01

247

Formulation and stability evaluation of extemporaneously prepared atenolol capsules from crushed atenolol tablets.  

PubMed

The purpose of this study was to formulate a 25-mg atenolol capsule starting from a commercial 100-mg atenolol tablet, given the fact that this strength is not available in Palestine and also because 50-mg atenolol tablets failed the splitting uniformity test of the European Pharmacopoeia, and to evaluate the chemical stability and dissolution behavior of the obtained capsules so as to ensure a high-quality product. A high-performance liquid chromatographic system was used for the analysis and quantification of atenolol in the samples studied. Samples of atenoIol for analysis were prepared as reported by the United States Pharmacopeia monograph. Disintegration and dissolution tests were performed according to the United States Pharmacopeia. The high-performance liquid chromatography assay indicated that the 25-mg atenolol capsules were stable for four months when stored at ambient temperature conditions. The disintegration time for all atenolol capsules was within the United States Pharmacopeia limits of 15 minutes. Atenolol release profile showed that approximately 90% of atenolol dissolved after 10 minutes. This study is important for patients who need to take one half of a 50-mg tablet, but for whom the splitting process doesn't give equal halves, and also for modifying the dose for patients with renal or hepatic problems. Therefore, it is possible for the community pharmacist to crush atenolol 100-mg tablets and refill them in new capsules with each containing a precise amount of atenolol, calculated according to body surface area and kidney and liver functions without affecting the chemical stability of the active ingredient nor its dissolution profile and also have a cost effective dosage form. PMID:23050394

Zaid, Abdel Naser; Malkieh, Numan; Kharoaf, Maher; Abu Ghoush, Abeer; Al-Ramahi, Rowa'

2012-01-01

248

[Ultrasonic sludge disintegration and its influence on sludge microbial activity].  

PubMed

The changes of sludge disintegration degree, microbial activity and particle size were examined synchronously, and the relationships between the changes and the effect of ultrasonic parameters on microbial activity were also analyzed. The results show that the process of ultrasonic sludge treatment can be divided into two stages: at the first stage, sludge flocs are disrupted into small micro-floc aggregates with the diameter of 10-20 microm, the extracellular organic substances are dissolved, bacteria are dissociated from flocs, and the microbial activity is enhanced; at the second stage, the micro-floc aggregates are disintegrated further into bacteria bodies with the diameter less than 10 microm, the intracellular organic substances are released, and the microbial activity are decreased. The two stages are not entirely separated because sludge is inhomogeneity. When sludge disintegration degree is lower than 20%, sludge floc disruption is the main effect and the microbial activity can increase over 20%; when sludge disintegration degree is between 20%-40%, some bacteria are hurt and the microbial activity can increase by less than 20%; when sludge disintegration degree is over 40%, most bacteria are damaged and sludge activity would decrease quickly. Because low energy ultrasonic can disrupt sludge floc with no damage to microorganism in a long treatment duration time, it is suitable to stimulate sludge microbial activity. PMID:19927824

Li, Huan; Jin, Yi-Ying; Nie, Yong-Feng

2009-09-15

249

Development and evaluation of acid-buffering bioadhesive vaginal tablet for mixed vaginal infections.  

PubMed

An acid-buffering bioadhesive vaginal tablet was developed for the treatment of genitourinary tract infections. From the bioadhesion experiment and release studies it was found that polycarbophil and sodium carboxymethylcellulose is a good combination for an acid-buffering bioadhesive vaginal tablet. Sodium monocitrate was used as a buffering agent to provide acidic pH (4.4), which is an attribute of a healthy vagina. The effervescent mixture (citric acid and sodium bicarbonate) along with a superdisintegrant (Ac-Di-sol) was used to enhance the swellability of the bioadhesive tablet. The drugs clotrimazole (antifungal) and metronidazole (antiprotozoal as well as an antibacterial) were used in the formulation along with Lactobacillus acidophilus spores to treat mixed vaginal infections. From the ex vivo retention study it was found that the bioadhesive polymers hold the tablet for more than 24 hours inside the vaginal tube. The hardness of the acid-buffering bioadhesive vaginal tablet was optimized, at 4 to 5 kg hardness the swelling was found to be good and the cumulative release profile of the developed tablet was matched with a marketed conventional tablet (Infa-V). The in vitro spreadability of the swelled tablet was comparable to the marketed gel. In the in vitro antimicrobial study it was found that the acid-buffering bioadhesive tablet produces better antimicrobial action than marketed intravaginal drug delivery systems (Infa-V, Candid-V and Canesten 1). PMID:18181530

Alam, Mohd Aftab; Ahmad, Farhan Jalees; Khan, Zeenat Iqbal; Khar, Roop Krishen; Ali, Mushir

2007-01-01

250

Optimization of matrix tablets controlled drug release using Elman dynamic neural networks and decision trees.  

PubMed

The main objective of the study was to develop artificial intelligence methods for optimization of drug release from matrix tablets regardless of the matrix type. Static and dynamic artificial neural networks of the same topology were developed to model dissolution profiles of different matrix tablets types (hydrophilic/lipid) using formulation composition, compression force used for tableting and tablets porosity and tensile strength as input data. Potential application of decision trees in discovering knowledge from experimental data was also investigated. Polyethylene oxide polymer and glyceryl palmitostearate were used as matrix forming materials for hydrophilic and lipid matrix tablets, respectively whereas selected model drugs were diclofenac sodium and caffeine. Matrix tablets were prepared by direct compression method and tested for in vitro dissolution profiles. Optimization of static and dynamic neural networks used for modeling of drug release was performed using Monte Carlo simulations or genetic algorithms optimizer. Decision trees were constructed following discretization of data. Calculated difference (f(1)) and similarity (f(2)) factors for predicted and experimentally obtained dissolution profiles of test matrix tablets formulations indicate that Elman dynamic neural networks as well as decision trees are capable of accurate predictions of both hydrophilic and lipid matrix tablets dissolution profiles. Elman neural networks were compared to most frequently used static network, Multi-layered perceptron, and superiority of Elman networks have been demonstrated. Developed methods allow simple, yet very precise way of drug release predictions for both hydrophilic and lipid matrix tablets having controlled drug release. PMID:22402474

Petrovi?, Jelena; Ibri?, Svetlana; Betz, Gabriele; ?uri?, Zorica

2012-05-30

251

Analysis of fatty acids in ecstasy tablets.  

PubMed

Fatty acids are the basis of so-called stearates which are frequently used as lubricants in the production of ecstasy tablets. Being a product added at the initial tablet production step its composition does not change once the compression is performed. The analysis of fatty acids can therefore provide useful information for a drug intelligence purpose. In this context an appropriate analytical method was developed to improve results already obtained by routine analyses. Considering the small quantity of such fatty acids in ecstasy tablets (approximately 3%) the research focussed on their extraction and concentration. Two different procedures were tested: (1) liquid/liquid extraction using dichloromethane followed by derivatisation and (2) in situ transesterification using bortrifluoride. Analyses were performed by GC-MS. The two procedures were optimized and applied to eight ecstasy seizures, in order to choose one of the procedures for its application to a large ecstasy sample set. They were compared by considering the number of peaks detected and sample amount needed, reproducibility and other technical aspects. PMID:19395206

Baer, Ines; Margot, Pierre

2009-07-01

252

A novel approach to sustained pseudoephedrine release: differentially coated mini-tablets in HPMC capsules.  

PubMed

We developed and optimized a novel pseudoephedrine hydrochloride (PSE) sustained-release dosage form. The system comprises immediate-release mini-tablets (IRMT) and sustained-release mini-tablets (SRMT) contained in a hydroxypropyl methylcellulose (HPMC) capsule. The IRMT contained PSE, excipients and low-substituted hydroxypropyl cellulose (a disintegrant), and the tablets were coated with HPMC, a water-soluble polymer. IRMT prepared with varying amounts of low-substituted hydroxypropyl cellulose all dissolved completely within the first 60min, so low-substituted hydroxypropyl cellulose content does not greatly influence PSE release. The SRMT contained only PSE and excipients, and were coated with a mixture of HPMC and the water-insoluble polymer ethylcellulose. The PSE release profile for the SRMT could be controlled by varying the thickness of the coat, and the lag time could be controlled by varying the amount of ethylcellulose present in the polymer coat. PSE was released immediately from our encapsulated mini-tablet system and release was sustained over an extended period of time: the PSE in the IRMT dissolved within 60min, whereas the PSE in the SRMT was released over 8-10h. This system can be modified to yield various extended drug-release profiles, thereby harnessing the benefits of both SRMT and IRMT. PMID:18467046

Ishida, Makoto; Abe, Kenichi; Hashizume, Minoru; Kawamura, Masao

2008-07-01

253

Development of a chewable tablet from Dugdh?malaky?di Yoga: An Ayurvedic preparation  

PubMed Central

Background: ?malaki (Embelica officinalis Gaertn.) is one of the most celebrated herbs in the Indian system of traditional medicine. It is one of the best Ras?yana-s (health promoting) drug. In Dugdh?malaky?di yoga, ?malaki (Embelica officinalis Gaertn.) powder is administered along with milk in case of svarabha?ga (hoarseness of voice). Here an attempt is made to convert this formulation into chewable tablet without altering its property to improve its palatability, shelf life and fixation of proper therapeutic dose. Methodology: Chewable tablets were prepared by wet granulation method. Here, ?malaki powder was prepared initially and it was mixed with additives and preservatives. Granules were prepared from this mixture by adding binding agent, finally compressed in to tablets. Results and Conclusion: The physico-chemical analysis of ?malaki standard are: Foreign Matter-Nil, Acid insoluble Ash-0.51%w/w, Water soluble Ash-2.01% w/w, Alcoholic Extractives-44.48%, Aqueous Extractives 67.52%, pH-3.1, Moisture content-8.19%. Quality control test for chewable tablet was carried out and found satisfactory with general characteristics of tablet viz. hardness 1.8, disintegration time 15-20 min, friability 0.5%, weight variation +/- 3%. The TLC of ?malaki powder showed 3 spots with Rf value 0.14, 0.4, and 0.73 and the chewable tablets showed 2 spots with Rf value 0.31 and 0.89 under 254 nm. The adaptation of modern techniques or methods to convert the Ayurvedic formulations without altering its therapeutic property is necessary to made them suitable for the present trends of newer drug delivery dosage forms. PMID:23929992

Santhosh, S. B.; Ambi, Arun B.; Hiremath, R. R.; Mannur, V. S.

2012-01-01

254

Combined effects of wetting, drying, and microcrystalline cellulose type on the mechanical strength and disintegration of pellets.  

PubMed

Effects of wetting and drying conditions on micromeritic, mechanical and disintegration properties of microcrystalline cellulose (MCC) pellets were evaluated. Extrusion/spheronization and three drying methods (fluidized bed, microwaves, and freeze drying) were applied using two wetting liquids (water or water-isopropanol 60:40 w/w) and three MCC types: (standard, silicified, and modified). Additionally, the effects of drying method were compared on highly porous pellets prepared by the incorporation and extraction of pore former (NaCl). It was found that the drying method has the greatest effect on the pellet size and porosity followed by the wetting liquid. The modification of MCC resulted in reduced water retention ability, implying hornification, increased porosity, reduced resistance to deformation and tensile strength of pellets. The disintegration time also decreased markedly due to the modification but only in the low porosity range <37%. Silicification increased greatly the disintegration time of the low porosity pellets (<14%). Combination of water-isopropanol, freeze drying and modified MCC gave the greatest increase in pellet size and porosity. The increase in pellet porosity caused exponential reduction in the resistance to deformation, tensile strength and disintegration time, as expected. Compared to fluidized bed, the freeze drying resulted in 20-30% higher porosity for pellets prepared without pore former and 6% for those with pore former, indicating the possibility of preparing highly porous pellets by employing freeze drying. PMID:18548618

Balaxi, Maria; Nikolakakis, Ioannis; Kachrimanis, Kyriakos; Malamataris, Stavros

2009-02-01

255

Hard Photo-disintegration of proton pairs in ^3He  

NASA Astrophysics Data System (ADS)

Hard deuteron photo-disintegration has been investigated for 20 years, as its cross sections follow the constituent counting rules and it provides insight into the interplay between hadronic and quark-gluon degrees of freedom in high-momentum transfer exclusive reactions. During the summer of 2007, at Jefferson lab, Hall A, we measured for the first time hard pp-pair disintegration in the reaction ?,3 He ->pp + n, using kinematics corresponding to a spectator neutron. The current state of the analysis and preliminary results will be shown. Clues to the underlying physics can be found in the comparison of our measurements with deuteron photo-disintegration, the energy dependence of the cross sections at 90^o c.m., and the ?n distribution.

Pomerantz, Ishay; Piasetzky, Eli; Gilman, Ronald

2008-10-01

256

Hard Photo-disintegration of proton pairs in ^3He  

NASA Astrophysics Data System (ADS)

Hard deuteron photo-disintegration has been investigated for 20 years, as its cross sections follow the constituent counting rules and it provides insight into the interplay between hadronic and quark-gluon degrees of freedom in high-momentum transfer exclusive reactions. We have now measured for the first time hard pp-pair disintegration in the reaction ?,3 He ->pp + n, using kinematics corresponding to a spectator neutron. The current state of the analysis will be shown. Clues to the underlying physics can be found in the comparison of our measurements with deuteron photo-disintegration, the energy dependence of the cross sections at 90^o c.m., and the ?n distribution.

Gilman, Ronald; Piasetzky, Eli; Pomerantz, Ishay

2008-04-01

257

Oral bioavailability of mesna tablets  

Microsoft Academic Search

To test the feasibility of uroprotection with sodium 2-mercaptoethane-sulfonate (mesna) in tablet form the bioavailability of mesna tablets was determined in healthy volunteers by HPLC. The area under the plasma concentration-time curve (AUC) of free mesna was significantly lower following oral (110 µmol.l-1.h-1; 95% CI 98–122) than following i.v. administration of 1.2 g of mesna (201 µmol.l-1.h-1; 95% CI 158–244).

Brigitte Stofer-Vogell; Thomas Cerny; Markus Borner; Bernhard H. Lauterburgl

1993-01-01

258

The effect of chitosan on the stability and morphological parameters of tablets with Epilobium parviflorum Schreb. extract.  

PubMed

The study is a continuation of research on manufacturing oral solid drug form containing extract from Epilobium parviflorum Schreb. This study aims at investigating the usefulness of selected high-molecular substances with particular consideration of chitosan (Ch), silicified microcrystalline cellulose (Prosolv) and croscarmellose sodium (Vivasol) as a carrier of E. parviflorum Schreb. extract in oral solid drug form in the process of direct tableting. In one series the alternative technological process (with initial granulation) was applied. The polymer carriers of extract were selected so as to obtain shorter disintegration time in relation to the earlier published studies and stability after longer time of storage. The effect of chitosan was estimated on selected morphological parameters of practical relevance during storage. The obtained results allow to state that the applied high-molecular adjuvant substances proved to be useful in adequate proportions in the production of tablets from dry extract from Epilobium parviflorum Schreb. through direct pressing of the tablet mass. The tablet properties in all series were in accordance with obligatory standards also after longer time of storage (12-month). The tablets formed from E. parviflorum Schreb. extract with chitosan can be included into preparations of sustained release time of the biologically active substances. PMID:18251200

Marczy?ski, Zbigniew; Bodek, Kazimiera Henryka

2007-01-01

259

Design of bilayer tablets using modified Dioscorea starches as novel excipients for immediate and sustained release of aceclofenac sodium  

PubMed Central

Bilayer tablets of aceclofenac sodium were developed using carboxymethylated white yam (Dioscorea rotundata) starch (CWY) for a fast release layer (2.5, 5.0, and 7.5% w/w), and acid-hydrolyzed bitter yam (Dioscorea dumetorum) starch (ABY) for a sustaining layer (27% w/w). Sodium starch glycolate (SSG) and hydroxypropyl methyl cellulose (HPMC) were used as standards. The starches were characterized using Fourier Transform Infrared spectroscopy (FT-IR), particle size, swelling power, densities and flow analyses. Mechanical properties of the tablets were evaluated using crushing strength and friability while release properties were evaluated using disintegration and dissolution times. Distinctive fingerprint differences between the native and modified starches were revealed by FT-IR. Carboxymethylation produced starches of significantly (p < 0.05) higher swelling and flow properties while acid-modification produced starches of higher compressibility. Bilayer tablets containing ABY had significantly higher crushing strength and lower friability values (p < 0.05) than those containing HPMC. Crushing strength increased while friability values decreased with increase in CWY. Generally tablets containing the modified Dioscorea starches gave faster (p < 0.05) disintegration times and produced an initial burst release to provide the loading dose of the drug from the immediate-release layer followed by sustained release (300 ± 7.56–450 ± 11.55 min). The correlation coefficient (R2) and chi-square (?2) test were employed as error analysis methods to determine the best-fitting drug release kinetic equations. In vitro dissolution kinetics generally followed the Higuchi and Hixson-Crowell models via a non-Fickian diffusion-controlled release. Carboxymethylated white yam starch and acid-modified bitter yam starch could serve as cheaper alternative excipients in bilayer tablet formulations for immediate and sustained release of drugs respectively, particularly where high mechanical strength is required.

Okunlola, Adenike

2015-01-01

260

Design of bilayer tablets using modified Dioscorea starches as novel excipients for immediate and sustained release of aceclofenac sodium.  

PubMed

Bilayer tablets of aceclofenac sodium were developed using carboxymethylated white yam (Dioscorea rotundata) starch (CWY) for a fast release layer (2.5, 5.0, and 7.5% w/w), and acid-hydrolyzed bitter yam (Dioscorea dumetorum) starch (ABY) for a sustaining layer (27% w/w). Sodium starch glycolate (SSG) and hydroxypropyl methyl cellulose (HPMC) were used as standards. The starches were characterized using Fourier Transform Infrared spectroscopy (FT-IR), particle size, swelling power, densities and flow analyses. Mechanical properties of the tablets were evaluated using crushing strength and friability while release properties were evaluated using disintegration and dissolution times. Distinctive fingerprint differences between the native and modified starches were revealed by FT-IR. Carboxymethylation produced starches of significantly (p < 0.05) higher swelling and flow properties while acid-modification produced starches of higher compressibility. Bilayer tablets containing ABY had significantly higher crushing strength and lower friability values (p < 0.05) than those containing HPMC. Crushing strength increased while friability values decreased with increase in CWY. Generally tablets containing the modified Dioscorea starches gave faster (p < 0.05) disintegration times and produced an initial burst release to provide the loading dose of the drug from the immediate-release layer followed by sustained release (300 ± 7.56-450 ± 11.55 min). The correlation coefficient (R (2)) and chi-square (?(2)) test were employed as error analysis methods to determine the best-fitting drug release kinetic equations. In vitro dissolution kinetics generally followed the Higuchi and Hixson-Crowell models via a non-Fickian diffusion-controlled release. Carboxymethylated white yam starch and acid-modified bitter yam starch could serve as cheaper alternative excipients in bilayer tablet formulations for immediate and sustained release of drugs respectively, particularly where high mechanical strength is required. PMID:25628566

Okunlola, Adenike

2014-01-01

261

Accelerating the sludge disintegration potential of a novel bacterial strain Planococcus jake 01 by CaCl2 induced deflocculation.  

PubMed

The present study investigates the impacts of phase separated disintegration through CaCl2 (calcium chloride) mediated biosurfactant producing bacterial pretreatment. In the initial phase of the study, the flocs were disintegrated (deflocculation) with 0.06g/gSS of CaCl2. In the subsequent phase, the sludge biomass was disintegrated (cell disintegration) through potent biosurfactant producing new novel bacteria, Planococcus jake 01. The pretreatment showed that suspended solids reduction and chemical oxygen demand solubilization for deflocculated - bacterially pretreated sludge was found to be 17.14% and 14.14% which were comparatively higher than flocculated sludge (treated with bacteria alone). The biogas yield potential of deflocculated - bacterially pretreated, flocculated, and control sludges were observed to be 0.322(L/gVS), 0.225(L/gVS) and 0.145(L/gVS) respectively. To our knowledge, this is the first study to present the thorough knowledge of biogas production potential through a novel phase separated biosurfactant bacterial pretreatment. PMID:25459848

Kavitha, S; Saranya, T; Kaliappan, S; Adish Kumar, S; Yeom, Ick Tae; Rajesh Banu, J

2014-10-31

262

Design of Controlled Release Non-erodible Polymeric Matrix Tablet Using Microwave Oven-assisted Sintering Technique.  

PubMed

The objective of the present study was to evaluate the effect of sintering condition on matrix formation and subsequent drug release from polymer matrix tablet for controlled release. The present study highlights the use of a microwave oven for the sintering process in order to achieve more uniform heat distribution with reduction in time required for sintering. We could achieve effective sintering within 8 min which is very less compared to conventional hot air oven sintering. The tablets containing the drug (propranolol hydrochloride) and sintering polymer (eudragit S-100) were prepared and kept in a microwave oven at 540 watt, 720 watt and 900 watt power for different time periods for sintering. The sintered tablets were evaluated for various tablet characteristics including dissolution study. Tablets sintered at 900 watt power for 8 min gave better dissolution profile compared to others. We conclude that microwave oven sintering is better than conventional hot air oven sintering process in preparation of controlled release tablets. PMID:21897655

Patel, Dm; Patel, Bk; Patel, Ha; Patel, Cn

2011-07-01

263

An evaluation of butoconazole nitrate 2% site release vaginal cream (Gynazole-1) compared to fluconazole 150 mg tablets (Diflucan) in the time to relief of symptoms in patients with vulvovaginal candidiasis.  

PubMed Central

BACKGROUND: It is estimated that as many as 13 million cases of vulvovaginal infection occur in the United States annually, the majority of which are the result of Candida albicans infection. The symptoms of vulvovaginal infections are often painful and distressing to the patient. The objective of this study was to compare the time to symptomatic relief of vulvovaginal candidiasis (VVC) with butoconazole nitrate 2% Site Release vaginal cream (Gynazole-1) and oral fluconazole 150 mg tablets (Diflucan). METHODS: This randomized, open-label, parallel study evaluated 181 female patients with moderate to severe symptoms of VVC. Patients were randomized to single-dose therapy with either butoconazole nitrate 2% Site Release vaginal cream or fluconazole. The primary outcome measure was the time to onset of first relief of symptoms. Secondary measures included the time to overall relief of symptoms and the reinfection rate over the first 30 days following treatment. The overall safety of both products was investigated through the collection of adverse event reports. RESULTS: The median time to first relief of symptoms occurred at 17.5 h for butoconazole patients as compared to 22.9 h for fluconazole patients (p < 0.001). The time at which 75% of patients experienced first relief of symptoms was 24.5 h versus 46.3 h for butoconazole and fluconazole, respectively (p < 0.001). By 12- and 24-h post-treatment, 44.4% and 72.8% of patients in the butoconazole treatment group reported first relief of symptoms versus 29.1% and 55.7% of patients in the fluconazole group (p = 0.044 and p = 0.024 respectively). In patients experiencing first relief of symptoms within 48 h of dosing, the median time to first relief of symptoms in the butoconazole treatment group was significantly shorter at 12.9 h compared to 20.7 h for the fluconazole treatment group (p = 0.048). There were no significant differences between the two groups with respect to time to total relief of symptoms or reoccurrence of infection within 30 days of treatment. Butoconazole therapy was shown to have fewer reported adverse events, including drug-related adverse events, than fluconazole therapy. Vulvovaginal pruritis and vulvovaginal burning were the most common drug-related adverse events attributed to butoconazole. Headache, diarrhea, nausea, upset stomach and skin sensitivity were the most common drug-related adverse events attributable to fluconazole. CONCLUSIONS: Single-dose butoconazole nitrate 2% Site Release vaginal cream provides statistically significant improvement in time to first relief of symptoms in the treatment of VVC compared to fluconazole. There is no difference between these two treatments with respect to total relief of symptoms or reinfection rate. Although there was no significant difference in the incidence of adverse events judged by the investigator to be treatment-related, butoconazole treatment did result in fewer patients experiencing adverse events than fluconazole. PMID:16338779

Seidman, Larry S; Skokos, Campbell K

2005-01-01

264

Evaluation of surface and bulk characteristics of cellulose I powders in relation to compaction behavior and tablet properties.  

PubMed

The particle properties and solid-state characteristics of two celluloses, Avicel PH101 and cellulose obtained from the alga Cladophora sp., were evaluated and related to the compaction behavior and the properties of the tablets made from them. The surface area of the celluloses was measured at different levels of penetration capacity, ranging from external surface area of particles to molecular texture with Blaine permeametry, Kr-gasadsorption, and solid-state NMR. The important cellulose fibril surface area was best reflected by solid-state NMR, although for the Cladophora cellulose, Kr-gas adsorption also resulted in a surface area of the order of what has been suggested earlier on the basis of the cellulose fibril dimensions. The difference in fibril dimension and, thereby, the fibril surface area of the two celluloses was shown to be the primary factor in determining their properties and behavior. Properties such as the crystallinity and the tablet disintegration could be related to the fibril dimensions. The Cladophora cellulose resulted in rather strong compacts that still disintegrated rapidly. The irregular surface morphology of the particles and the fragmenting behavior of Cladophora probably contributed to the strength of the tablets. PMID:14677770

Gustafsson, Christina; Lennholm, Helena; Iversen, Tommy; Nyström, Christer

2003-11-01

265

Formulation development and optimization of fast dissolving tablets of aceclofenac using natural superdisintegrant.  

PubMed

The current research work involves preparation of fast dissolving tablets of Aceclofenac by direct compression method using different concentrations of Lepidium sativum mucilage as natural superdisintegrant. A two-factor three-level (3(2)) factorial design is being used to optimize the formulation. Nine formulation batches (D1-D9) were prepared accordingly. Two factors as independent variables (X 1-amount of ?-cyclodextrin and X 2-amount of Lepidium sativum mucilage) were taken with three levels (+1, 0, -1). The levels of two factors were selected on the basis of preliminary experiments conducted and their effect on three dependent variables (disintegration time, wetting time, and in vitro drug release) was studied along with their % prediction error. All the active blends were evaluated for postcompression parameters (angle of repose, Carr's index, Hausner ratio, etc.) and the tablets were evaluated for postcompression parameters (weight variation, hardness, and friability, wetting time, disintegration time, water absorption ratio, and in vitro drug release studies). The optimum batch was further used for SEM and stability studies. Formulation D5 was selected by the Design-Expert software which exhibited DT (15.5?sec), WT (18.94?sec), and in vitro drug release (100%) within 15 minutes. PMID:24944837

Kaur, Lovleen; Bala, Rajni; Kanojia, Neha; Nagpal, Manju; Dhingra, Gitika Arora

2014-01-01

266

Hard pion exchange currents and the backward deuteron disintegration  

NASA Astrophysics Data System (ADS)

Relation between exchange currents and a potential is discussed in the framework of the Schroedinger-like scheme. Backward deuteron disintegration is studied using the Paris and Reid soft-core potentials and the static hard pion exchange currents up to the order ?

Truhlik, E.; Adam, J.

267

Larsen Iceshelf: Iceshelf Partial Disintegration and Iceberg Calving  

NSDL National Science Digital Library

Visitors can study this account of the calving of the Larsen ice shelf and the disintegration of the ice shelf around James Ross Island that occured in Austral Summer of 1994-95. The account is in chronolgical order and is accompanied by photographs. Follow-up examinations from 1996-2002 and links to related material are provided.

268

Nucleation, aggregation, annealing, and disintegration of granular clusters  

NASA Astrophysics Data System (ADS)

The processes of nucleation, aggregation, annealing, and disintegration of clusters of non-Brownian paramagnetic beads in a vibrofluidized system are experimentally investigated. The interaction among the beads is induced by a magnetic seed composed of two dipoles allocated outside the container cell. We observe a clearly differentiated nucleation stage, whose evolution (nucleation time versus acceleration strength) follows a power law. Thereafter, the beads aggregate forming 2D disordered clusters around the nucleus. Both processes (nucleation and aggregation) are determined by the competition between magnetic forces and the drag produced by a thermal bath created by glass particles. Once the agglomerates reach a final state (shape and length), they are annealed by increasing and decreasing the granular temperature. We found that the fractal dimension and the lacunarity index clearly describe the structural variations of the clusters. Our discussion on this phenomenon is addressed, making a rough analogy with the glass transition in a super-cooled liquid. Finally, we study the disintegration of the clusters as a function of time and the density of the surrounding gas. The question is not if, but how they disintegrate upon removing the external field; we find that the disintegration follows an exponential decay.

González-Gutiérrez, Jorge; Carrillo-Estrada, J. L.; Ruiz-Suárez, J. C.

2014-05-01

269

Spatial Ice Rigidity Distribution of Larsen B Before its Disintegration  

Microsoft Academic Search

The disintegration of 3250 square kilometers of Larsen B Ice Shelf in the Antarctic Peninsula within 5 weeks in 2002 provided the opportunity to establish a clear connection between the removal of ice shelves and the acceleration of their ice streams. Radar interferometry observations analyzed by Rignot et al. [2004] revealed that glaciers flowed up to eight times faster after

A. Khazendar; E. Rignot

2006-01-01

270

Spatial Ice Rigidity Distribution Of Larsen B Before Its Disintegration  

Microsoft Academic Search

The disintegration of 3250 square kilometers of Larsen B Ice Shelf in the Antarctic Peninsula within 5 weeks in 2002 provided the opportunity to establish a clear connection between the removal of ice shelves and the acceleration of their ice streams. Radar interferometry observations analyzed by Rignot et al. [2004] revealed that glaciers flowed up to eight times faster after

A. Khazendar; E. Rignot

2005-01-01

271

Cultural Disintegration Perpetuated through Substance Abuse among American Indians.  

ERIC Educational Resources Information Center

Alcohol, perhaps more than any other factor, symbolizes the degree of cultural disintegration experienced by American Indians today. It has been recognized as a symptom of the numerous cultural adjustments forced upon American Indians since white contact. Indeed, alcohol among Indian groups was prohibited for a far longer period than the…

French, Laurence Armand

272

Disintegration of fluids under supercritical conditions from mixing layer studies  

NASA Technical Reports Server (NTRS)

Databases of transitional states obtained from Direct Numerical simulations (DNS) of temporal, supercritical mixing layers for two species systems, O2/H2 and C7H16/N2, are analyzed to elucidate species-specific turbulence aspects and features of fluid disintegration.

Okong'o, N.; Bellan, J.

2003-01-01

273

Safety and Colon-Cleansing Efficacy of a New Residue-Free Formulation of Sodium Phosphate Tablets  

Microsoft Academic Search

OBJECTIVE:A residue-free sodium phosphate tablet (RF-NaP) was formulated that lacks microcrystalline cellulose, which can appear as a whitish residue in the colon. A multicenter, randomized, investigator-blinded study was conducted to compare the colon-cleansing efficacy of 40 or 32 tablets of RF-NaP with the marketed 40-tablet NaP treatment regimen.METHODS:Eight hundred sixteen patients were randomized prior to colonoscopy to receive either 40

Douglas K. Rex; Howard Schwartz; Michael Goldstein; John Popp; Seymour Katz; Charles Barish; Robyn G. Karlstadt; Martin Rose; Kelli Walker; Sandra Lottes; Nancy Ettinger; Bing Zhang

2006-01-01

274

Automated shape annotation for illicit tablet preparations: a contour angle based classification from digital images.  

PubMed

In order to facilitate forensic intelligence efforts in managing large collections of physical feature data pertaining to illicit tablets, we have developed an automated shape classification method. This approach performs categorical shape annotation for the domain of illicit tablets. It is invariant to scale, rotation and translation and operates on digital images of seized tablets. The approach employs two processing levels. The first (coarse) level is being based on comparing the contour curvature space of tablet pairs. The second (fine) level is a rule based approach, implemented as a classification tree, that exploits characteristic similarities of shape categories. Annotation is demonstrated over a collection of 169 tablets selected for their diverse shapes with an accuracy of 97.6% when 19 shape categories are defined. PMID:23380064

Lopatka, Martin; van Houten, Wiger

2013-03-01

275

Detailed calculation of K- and L-Auger electron emission intensities following radioactive disintegration.  

PubMed

A program has been set up to calculate the K- and L-Auger electron emissions resulting from the radioactive disintegration process, and to study all the possible emissions in detail. Due to the fact that only a small number of experimental results are available in the measurements of K- and L-Auger electrons, the calculated values obtained in this work were compared with the other calculated values available. Good agreement was found between the values. Some of the results are given as examples. PMID:16569503

Bé, Marie-Martine; Chisté, Vanessa; Dulieu, Christophe

2006-01-01

276

Effect of X-ray exposure on the pharmaceutical quality of drug tablets using X-ray inspection equipment.  

PubMed

Abstract Context: X-ray inspection equipment is widely used to detect missing materials and defective goods in opaque containers. Its application has been expanded to the pharmaceutical industry to detect the presence of drug tablets in aluminum foil press-through packaging. However, the effect of X-rays on the pharmaceutical quality of drug tablets is not well known. Objective: In this study, the effect of X-rays on the pharmaceutical quality of drug tablets was investigated. Methods: Exposure of acetaminophen, loxoprofen and mefenamic acid tablets to X-ray doses of 0.34?mGy (thrice the dose by X-ray scanning) to 300?Gy (maximum dose from our X-ray equipment) was demonstrated, and the samples were evaluated by formulation tests. Results: Exposure to X-rays did not affect the pharmaceutical quality of the drug content. The samples exposed to X-rays exhibited almost the same profile in formulation tests (dissolution test, disintegrating test and hardness test) as control samples (0?Gy). The combination of X-ray exposure with accelerated temperature and humidity tests (six months) also did not affect the pharmaceutical quality. The color change of light-sensitive drugs (nifedipine and furosemide tablets) after X-ray exposure was negligible (tablet color was remarkably changed by light from a D65 lamp. Conclusion: The X-ray scanning and X-ray exposure under our experimental conditions did not affect the pharmaceutical quality of drug tablets. PMID:24842380

Uehara, Kazuaki; Tagami, Tatsuaki; Miyazaki, Itaru; Murata, Norikazu; Takahashi, Yoshifumi; Ohkubo, Hiroshi; Ozeki, Tetsuya

2014-05-19

277

E-Books and the Tablet PC.  

ERIC Educational Resources Information Center

Highlights the emerging technologies of e-books, electronic versions of texts, and the Tablet PC, a new hybrid laptop computer and personal digital assistant that features a writing tablet and stylus-based input/navigation. (Author/VWL)

Goodwin-Jones, Bob

2003-01-01

278

21 CFR 520.1310 - Marbofloxacin tablets.  

Code of Federal Regulations, 2010 CFR

...2010-04-01 2010-04-01 false Marbofloxacin tablets. 520.1310 Section 520...FORM NEW ANIMAL DRUGS § 520.1310 Marbofloxacin tablets. (a) Specifications ...50, 100, or 200 milligrams (mg) marbofloxacin. (b) Sponsor. See No....

2010-04-01

279

21 CFR 520.1380 - Methocarbamol tablets.  

Code of Federal Regulations, 2014 CFR

...DRUGS § 520.1380 Methocarbamol tablets. (a) Chemical name. 3-(O-Methoxyphenoxy)-1,2-propanediol 1-carbamate. (b) Specifications. Each tablet contains 500 milligrams of methocarbamol. (c) Sponsor. See No. 000856...

2014-04-01

280

21 CFR 520.1380 - Methocarbamol tablets.  

Code of Federal Regulations, 2010 CFR

...DRUGS § 520.1380 Methocarbamol tablets. (a) Chemical name. 3-(O-Methoxyphenoxy)-1,2-propanediol 1-carbamate. (b) Specifications. Each tablet contains 500 milligrams of methocarbamol. (c) Sponsor. See No. 000856...

2010-04-01

281

21 CFR 520.1380 - Methocarbamol tablets.  

Code of Federal Regulations, 2013 CFR

...DRUGS § 520.1380 Methocarbamol tablets. (a) Chemical name. 3-(O-Methoxyphenoxy)-1,2-propanediol 1-carbamate. (b) Specifications. Each tablet contains 500 milligrams of methocarbamol. (c) Sponsor. See No. 000856...

2013-04-01

282

21 CFR 520.1380 - Methocarbamol tablets.  

Code of Federal Regulations, 2011 CFR

...DRUGS § 520.1380 Methocarbamol tablets. (a) Chemical name. 3-(O-Methoxyphenoxy)-1,2-propanediol 1-carbamate. (b) Specifications. Each tablet contains 500 milligrams of methocarbamol. (c) Sponsor. See No. 000856...

2011-04-01

283

21 CFR 520.1380 - Methocarbamol tablets.  

Code of Federal Regulations, 2012 CFR

...DRUGS § 520.1380 Methocarbamol tablets. (a) Chemical name. 3-(O-Methoxyphenoxy)-1,2-propanediol 1-carbamate. (b) Specifications. Each tablet contains 500 milligrams of methocarbamol. (c) Sponsor. See No. 000856...

2012-04-01

284

21 CFR 520.312 - Carnidazole tablets.  

Code of Federal Regulations, 2010 CFR

...Conditions of use —(1) Amount. Adult pigeons: 1 tablet (10 milligrams); newly weaned pigeons: 1/2 tablet (5 milligrams). (2...trichomoniasis (canker) in ornamental and homing pigeons. (3) Limitations. Not for...

2010-04-01

285

21 CFR 520.312 - Carnidazole tablets.  

Code of Federal Regulations, 2011 CFR

...Conditions of use —(1) Amount. Adult pigeons: 1 tablet (10 milligrams); newly weaned pigeons: 1/2 tablet (5 milligrams). (2...trichomoniasis (canker) in ornamental and homing pigeons. (3) Limitations. Not for...

2011-04-01

286

21 CFR 520.2088 - Roxarsone tablets.  

Code of Federal Regulations, 2012 CFR

...Conditions of use —(i) Growing chickens and growing turkeys—(a ) Amount. Dissolve 2 tablets in each gallon of... (4) Conditions of use in growing chickens and growing turkeys —(i) Amount . 1 tablet in each gallon of drinking...

2012-04-01

287

21 CFR 520.2088 - Roxarsone tablets.  

Code of Federal Regulations, 2010 CFR

...Conditions of use —(i) Growing chickens and growing turkeys—(a ) Amount. Dissolve 2 tablets in each gallon of... (4) Conditions of use in growing chickens and growing turkeys —(i) Amount . 1 tablet in each gallon of drinking...

2010-04-01

288

21 CFR 520.2088 - Roxarsone tablets.  

Code of Federal Regulations, 2013 CFR

...Conditions of use —(i) Growing chickens and growing turkeys—(a ) Amount. Dissolve 2 tablets in each gallon of... (4) Conditions of use in growing chickens and growing turkeys —(i) Amount . 1 tablet in each gallon of drinking...

2013-04-01

289

21 CFR 520.2088 - Roxarsone tablets.  

Code of Federal Regulations, 2011 CFR

...Conditions of use —(i) Growing chickens and growing turkeys—(a ) Amount. Dissolve 2 tablets in each gallon of... (4) Conditions of use in growing chickens and growing turkeys —(i) Amount . 1 tablet in each gallon of drinking...

2011-04-01

290

Spectrophotometric methods for the determination of Ibuprofen in tablets.  

PubMed

Ibuprofen in film coated tablets of different strengths has been determined using different spectrophotometric methods. These are: (i) the compensation method, (ii) a two wavelengths method, (iii) second-order and (iv) fourth-order derivative methods, and (v) a curve fitting method based upon computing the quadratic coefficient of the orthogonal polynomials expansion of its benzenoid absorption characteristics. All results were compared with the HPLC method of the B.P. 2003 using paired comparison. Developed methods have been validated and applied to different tablet formulations. Mean differences from the B.P. method were found to be -0.10, -0.30, -0.10, -0.16, -0.34%, respectively. In view of the relatively low specific absorbance of ibuprofen in the ultraviolet region [A (1%, 1 cm) =18.5 at 264 nm] its accurate and precise determination in different tablet formulations is challenging due to the presence of interferences from excipients. PMID:16380350

Wahbi, Abdel Aziz; Hassan, Ekram; Hamdy, Dalia; Khamis, Essam; Barary, Magda

2005-10-01

291

Comparison of extraction techniques for spray dried dispersion tablet formulations.  

PubMed

Non-traditional sample preparation/extraction techniques that utilized the Caliper Life Sciences Tablet Processing Workstation II (TPW II), Microwave Assisted Extraction (MAE), and Accelerated Solvent Extraction (ASE) were evaluated for the extraction of Compound A from a 50 mgA, 15% Spray Dried Dispersion (SDD) immediate released (IR) tablet formulation. The TPW II consistently provided complete recoveries with very short preparation/extraction times (approximately 30 min). MAE also provided complete recovery of the API from the tablet formulation, but required approximately twice the extraction time, while ASE provided the lowest recovery of the three non-traditional techniques. The sample preparation/extraction efficiencies of the three non-traditional techniques were compared to that of the 5.5 h long manual method. PMID:17888606

Lee, Carlos; Gallo, Jenny; Arikpo, William; Bobin, Vincent

2007-11-30

292

Preparation, evaluation and need of spherical crystallization in case of high speed direct tabletting.  

PubMed

In direct compression (DC), the significance of usual flow properties of powder from the hopper to the dies of the tablet machine cannot be overstressed. Ensuring the free flow of powder presents a number of challenges to the pharmaceutical formulator in case of high speed tabletting. This research work was conceived to obtain directly compressible agglomerates by spherical crystallization technique and were comparatively evaluated for physicochemical properties as well as tableting properties of agglomerates and unprocessed aceclofenac. Agglomerates of aceclofenac were developed via spherical crystallization method by a solvent arrangement containing dichloromethane (DCM) as a good solvent, water as a bad solvent and acetone as a bridging liquid. Hydroxypropyl cellulose (HPC) in variable quantity was implemented as hydrophilic polymer. The agglomerates were evaluated for yield, solubility, drug content, FTIR spectroscopy, porosity, particle size, micromeritic properties, differential scanning calorimetry (DSC), X-ray diffraction studies (XRD), scanning electron microscopy (SEM), and dissolution studies. The agglomerates expressed improved micromeritic and dissolution properties, in equivalence to pure drug. Formulation F3 (optimized agglomerates) exposed estimable rotundity, better drug release, and easily compression into tablets by high speed DC Technique. The tablets showed acceptable physicochemical properties and complied with the pharmacopoeial specifications. The dissolution rate of prepared tablets from agglomerates was better than the tablets of pure drug. The F3 agglomerates show splendid physicochemical and micromeritic properties. Agglomerated compression mix also showed good tableting properties as needed for high speed compression and enough stability under accelerated conditions at least for 1 month. PMID:23848355

Pandey, Suneel; Patil, Arun T

2014-01-01

293

Biopharmaceutical evaluation of new slow release tablets obtained by hot tableting of coated pellets with tramadol hydrochloride.  

PubMed

This study was aimed at a biopharmaceutical evaluation of a new oral dosage form of tramadol hydrochloride (TH)--slow release tablets obtained by hot tableting of coated pellets, 100 mg (TP), compared to the conventional slow release tablets, Tramal Retard, 100 mg (TR). Both TP and TR formulations showed a similar release profile of TH (f2 was 71) in in vitro release studies. The in vivo study was a two-treatment, two-period, two-sequence, single-oral dose 100 mg, crossover design using rabbit model with the phases separated by a washout period of 14 days. It was shown that the amount of TH absorbed into the systemic circulation is similar for TP and TR (the 90% confidence intervals for the AUC(0-1), AUC(0-infinity) and ratios were 85-122 and 92-107%, respectively). However, after administration of slow release tablets obtained by hot tableting of coated pellets, a prolonged absorption and elimination processes and a smoother and more extended plasma profile of TH were observed. It can be assumed that the use of a new oral dosage form of TH in patients affects the extension of analgesia after single administration of the drug, with its gradual absorption into the systemic circulation. PMID:25362810

Szkutnik-Fiedler, Danuta; Sawicki, Wies?aw; Balcerkiewicz, Monika; Mazgalski, Jaros?aw; Grabowski, Tomasz; Grze?kowiak, Edmund

2014-01-01

294

Preparation and Evaluation of Microencapsulated Fast Melt Tablets of Ambroxol Hydrochloride  

PubMed Central

Natural resources in general and plant materials in particular are receiving more attention due to their safety as pharmaceutical excipients. Present work assessed the potential of a natural polysaccharide, pectin to mask the bitter taste of ambroxol hydrochloride, by microencapsulation technique, and its possibility to formulate as a fast disintegrating dosage form. Taste masking is an important developmental challenge in fast dissolving drug delivery system since it dissolves or disintegrates in the patient's mouth in close proximity to the taste buds. The prepared microspheres by emulsion solvent evaporation technique possessed good sphericity, smooth surface morphology, uniform and narrow size distribution (10-90 ?m), when analyzed by scanning electron microscopy, laser diffraction and optical microscopy. Method of preparation has influenced the particle size and drug loading efficiency. Drug-polymer compatibility was confirmed by Fourier transform infrared spectroscopy and thin layer chromatography. DSC and X-ray diffraction studies revealed that the drug was dispersed inside the microspheres in the form of an insoluble matrix. The formation of microspheres was affected by glass transition temperature of the polymer, surfactant, type of plasticizers, volume of internal phase, stirrer speed etc. Fast dissolving tablets were prepared by the modification of melt granulation technique. The resulting granules were found to melt fast at body temperature, have smooth mouth feel and good physical stability. This study demonstrated that pectin could be a right choice in developing patient favored formulations for bitter drugs and can be utilized in fast disintegrating dosage forms as well. PMID:20490294

Jacob, S.; Shirwaikar, A.

2009-01-01

295

Instability of Misoprostol Tablets Stored Outside the Blister: A Potential Serious Concern for Clinical Outcome in Medical Abortion  

PubMed Central

Introduction Misoprostol (Cytotec) is recognised to be effective for many gynaecological indications including termination of pregnancy, management of miscarriage and postpartum haemorrhage. Although not licensed for such indications, it has been used for these purposes by millions of women throughout the world. Misoprostol tablets are most often packaged as multiple tablets within an aluminium strip, each within an individual alveolus. When an alveolus is opened, tablets will be exposed to atmospheric conditions. Objective To compare the pharmaco technical characteristics (weight, friability), water content, misoprostol content and decomposition product content (type A misoprostol, type B misoprostol and 8-epi misoprostol) of misoprostol tablets Cytotec (Pfizer) exposed to air for periods of 1 hour to 720 hours (30 days), to those of identical non exposed tablets. Methods Four hundred and twenty (420) tablets of Cytotec (Pfizer) were removed from their alveoli blister and stored at 25°C/60% relative humidity. Water content, and misoprostol degradation products were assayed in tablets exposed from 1 to 720 hours (30 days). Comparison was made with control tablets (N?=?60) from the same batch stored in non-damaged blisters. Statistical analyses were carried out using Fisher’s exact test for small sample sizes. Results By 48 hours, exposed tablets demonstrated increased weight (+4.5%), friability (+1 300%), and water content (+80%) compared to controls. Exposed tablets also exhibited a decrease in Cytotec active ingredient dosage (?5.1% after 48 hours) and an increase in the inactive degradation products (+25% for type B, +50% for type A and +11% for 8-epi misoprostol after 48 hours) compared to controls. Conclusion Exposure of Cytotec tablets to ‘typical’ European levels of air and humidity results in significant time-dependent changes in physical and biological composition that could impact adversely upon clinical efficacy. Health professionals should be made aware of the degradation of misoprostol with inappropriate storage of misoprostol tablets. PMID:25502819

Berard, Veronique; Fiala, Christian; Cameron, Sharon; Bombas, Teresa; Parachini, Mirella; Gemzell-Danielsson, Kristina

2014-01-01

296

Graft copolymers of ethyl methacrylate on waxy maize starch derivatives as novel excipients for matrix tablets: drug release and fronts movement kinetics.  

PubMed

A previous paper deals with the physicochemical and technological characterization of novel graft copolymers of ethyl methacrylate (EMA) on waxy maize starch (MS) and hydroxypropylstarch (MHS). The results obtained suggested the potential application of these copolymers as excipients for compressed non-disintegrating matrix tablets. Therefore, the purpose of the present study was to investigate the mechanism governing drug release from matrix systems prepared with the new copolymers and anhydrous theophylline or diltiazem HCl as model drugs with different solubility. The influence of the carbohydrate nature, drying procedure and initial pore network on drug release kinetics was also evaluated. Drug release experiments were performed from free tablets. Radial drug release and fronts movement kinetics were also analysed, and several mathematical models were employed to ascertain the drug release mechanisms. The drug release markedly depends on the drug solubility and the carbohydrate nature but is practically not affected by the drying process and the initial matrix porosity. A faster drug release is observed for matrices containing diltiazem HCl compared with those containing anhydrous theophylline, in accordance with the higher drug solubility and the higher friability of diltiazem matrices. In fact, although diffusion is the prevailing drug release mechanism for all matrices, the erosion mechanism seems to have some contribution in several formulations containing diltiazem. A reduction in the surface exposed to the dissolution medium (radial release studies) leads to a decrease in the drug release rate, but the release mechanism is not essentially modified. The nearly constant erosion front movement confirms the behaviour of these systems as inert matrices where the drugs are released mainly by diffusion through the porous structure. PMID:22210473

Marinich, J A; Ferrero, C; Jiménez-Castellanos, M R

2012-04-01

297

Double-Layered Mucoadhesive Tablets Containing Nystatin  

Microsoft Academic Search

The objective of this work was to design a mucoadhesive tablet with a potential use in the treatment of oral candidosis. A 2-layered tablet containing nystatin was formulated. Lactose CD (direct compression), carbomer (CB), and hydroxypropylmethylcellulose (HPMC) were used as excipients. Tablets were obtained through direct compression. Properties such as in vitro mucoadhesion, water uptake, front movements, and drug release

Juan Manuel Llabot; Ruben Hilario Manzo; Alberto allemandi

2002-01-01

298

21 CFR 520.816 - Epsiprantel tablets.  

Code of Federal Regulations, 2010 CFR

...2010-04-01 2010-04-01 false Epsiprantel tablets. 520.816 Section 520.816 Food...ANIMAL DRUGS § 520.816 Epsiprantel tablets. (a) Specifications . Each tablet contains either 12.5, 25, 50, or 100 milligrams of...

2010-04-01

299

Scaffolding Equals Success in Teaching Tablet PCs  

ERIC Educational Resources Information Center

After many years of using the mouse and keyboard as the primary means of computer input, people are seeing a strong surge into a new generation of input technologies such as tablet PCs. As more professionals adopt tablet PCs for use in the workplace, there is a subsequent increased demand for tablet PC instruction in the classroom. Examples of…

Dickerson, Jeremy; Williams, Scott; Browning, J. B.

2009-01-01

300

Onsite Wastewater Treatment Systems: Tablet Chlorination  

E-print Network

the basin. As that tablet dissolves and/or erodes, the tablet above it falls by gravity to replace it. A tablet can dissolve quickly or slowly, depending on the amount of wastewater coming into contact Richard Weaver and Bruce Lesikar Professor in Soil...

Lesikar, Bruce J.

2008-10-23

301

Disintegration of rocks based on magnetically isolated high voltage discharge  

NASA Astrophysics Data System (ADS)

Recently, a method utilizing pulsed power technology for disintegration of rocks arouses great interest of many researchers. In this paper, an improved method based on magnetic switch and the results shown that the uniform dielectrics like plastic can be broken down in water is presented, and the feasible mechanism explaining the breakdown of solid is proposed and proved experimentally. A high voltage pulse of 120 kV, rise time 0.2 ?s was used to ignite the discharging channel in solids. When the plasma channel is formed in the solid, the resistance of the channel is quiet small; even if a relatively low voltage is applied on the channel on this occasion, it will produce high current to heat the plasma channel rapidly, and eventually disintegrate the solids. The feasibility of promising industrial application in the drilling and demolition of natural and artificial solid materials by the method we presented is verified by the experiment result in the paper.

He, Mengbing; Jiang, Jinbo; Huang, Guoliang; Liu, Jun; Li, Chengzu

2013-02-01

302

Real-time microradiology of disintegration of iron ore sinteres  

NASA Astrophysics Data System (ADS)

We first present real-time microradiology of disintegration of self-fluxing iron ore sinters in low temperature reduction using highly collimated synchrotron source. The experiments were performed on the 5C1 beamline at PLS (Pohang Light Source, Pohang, Korea), operating at 2.5 GeV. We used unmonochromatized ("white") light with no optical elements except beryllium windows. The images of the crack superimpose, on the two-dimensional projection of a three-dimensional phenomenon, suggest that cracks are always initiated from pores in the sinters and propagate along neighboring pores. Interestingly, cracking occurs mostly on macropores (>800 ?m), preferentially initiated from stress concentrated sites on pore surfaces. This dynamic study of the disintegration of sinters clearly shows that the crack initiation temperature is as low as 450 °C.

Kim, Jong Ryun; Kang, H. S.; Lee, Ho Jun; Je, Jung Ho; Jeong, S. K.; Tsai, W.-L.; Hsu, P. C.; Hwu, Y.

2003-01-01

303

Experimental analysis of tablet properties for discrete element modeling of an active coating process.  

PubMed

Coating of solid dosage forms is an important unit operation in the pharmaceutical industry. In recent years, numerical simulations of drug manufacturing processes have been gaining interest as process analytical technology tools. The discrete element method (DEM) in particular is suitable to model tablet-coating processes. For the development of accurate simulations, information on the material properties of the tablets is required. In this study, the mechanical parameters Young's modulus, coefficient of restitution (CoR), and coefficients of friction (CoF) of gastrointestinal therapeutic systems (GITS) and of active-coated GITS were measured experimentally. The dynamic angle of repose of these tablets in a drum coater was investigated to revise the CoF. The resulting values were used as input data in DEM simulations to compare simulation and experiment. A mean value of Young's modulus of 31.9 MPa was determined by the uniaxial compression test. The CoR was found to be 0.78. For both tablet-steel and tablet-tablet friction, active-coated GITS showed a higher CoF compared with GITS. According to the values of the dynamic angle of repose, the CoF was adjusted to obtain consistent tablet motion in the simulation and in the experiment. On the basis of this experimental characterization, mechanical parameters are integrated into DEM simulation programs to perform numerical analysis of coating processes. PMID:23354469

Just, Sarah; Toschkoff, Gregor; Funke, Adrian; Djuric, Dejan; Scharrer, Georg; Khinast, Johannes; Knop, Klaus; Kleinebudde, Peter

2013-03-01

304

Hard Photo-disintegration of proton pairs in ^3He  

NASA Astrophysics Data System (ADS)

Hard deuteron photo-disintegration has been investigated for 20 years [1], as its cross sections follow the constituent counting rules and it provides insight into the interplay between hadronic and quark-gluon degrees of freedom in high-momentum transfer exclusive reactions [2]. During the summer of 2007, we measured in Jefferson Lab Hall A [3] hard pp-pair disintegration for the first time, in the reaction ?,3 He ->pp + n, using kinematics corresponding to a spectator neutron. The current state of the analysis and preliminary results will be shown. Clues to the underlying physics can be found in the comparison of our measurements with deuteron photo-disintegration, the energy dependence of the cross sections at 90^o c.m., and the ?n distribution. References: [1] R. Gilman and F. Gross, J. Phys. G 28, R37 (2002). [2] S. J. Brodsky et al., Phys. Lett. B 578, 69 (2004). [3] http://hallaweb.jlab.org/experiment/E03-101/

Piasetzky, E.; Pomerantz, I.; Gilman, R.

2009-05-01

305

Crystallization of excipients in tablets.  

PubMed

Whisker-like crystals appeared on the surface of tablets that contained lactose or mannitol, a hygroscopic material such as docusate sodium, magnesium chloride, or potassium acetate, and other ingredients stored in an atmosphere of high relative humidity. The crystals were observed under a scanning electron microscope and were measured using differential scanning calorimetry and TLC. The crystals contained lactose or mannitol. PMID:3921688

Ando, H; Watanabe, S; Ohwaki, T; Miyake, Y

1985-02-01

306

Real-time monitoring of changes of adsorbed and crystalline water contents in tablet formulation powder containing theophylline anhydrate at various temperatures during agitated granulation by near-infrared spectroscopy.  

PubMed

Real-time monitoring of adsorbed water content (FW) and hydrate formation of theophylline anhydrate (THA) in tablet formulation during agitated granulation was investigated by near-infrared (NIR) spectroscopy. As the wet-granulation process of THA tablet formulation involves change in pseudo-polymorphs between THA and theophylline monohydrate (THM), the pharmaceutical properties of THA tablet depend on the degree of hydration during granulation. After mixing of the powder materials (4 g) containing THA, and excipients and the addition of 600 ?L of binding water, the powder was kneaded at 27°C, 40°C, and 50°C and then dried. The mixing, granulating, and drying processes were monitored using NIR. The calibration models to predict THM and total water contents during granulation in THA tablet formulation were obtained by partial least-squares regression. The FW in the formulation was determined by subtracting THM from the water content. The results of the THA formulation powder bed during granulation by NIR monitoring indicated that the transformation pathway of the THA powder was THA ? THM ? THA at 27°C and 40°C, but that at 50°C was THA ? THA ? THA. The pharmaceutical properties, such as tablet porosity, hardness, tablet disintegration time, and dissolution rate of the final THA tablet products, were affected by the degree of crystalline transformation during granulation. PMID:24832393

Otsuka, Makoto; Kanai, Yoshinori; Hattori, Yusuke

2014-09-01

307

Validity of childhood disintegrative disorder apart from autistic disorder with speech loss.  

PubMed

In order to test clinical validity of DSM-IV childhood disintegrative disorder (CDD), 10 CDD children (mean age = 8.2 years, SD = 3.8; 7 male and 3 female) and 30 age- and gender-matched children with DSM-IV autistic disorder (AD) with speech loss (SL) (ADSL) were compared on 24 variables not directly related to CDD criteria. Compared with the ADSL children, the CDD children showed fearfulness significantly more frequently during the period of SL; displayed epilepsy significantly more frequently and stereotypy significantly more prominently at first visit on average about 6 years after SL; and had significantly less uneven intellectual profile at first visit to support the validity of CDD to a certain extent. No significant difference in the retardation level at first visit between the two groups suggested no worse short-term outcome in CDD than ADSL, although a long-term prospective study to compare them from infancy is needed. PMID:15365892

Kurita, Hiroshi; Koyama, Tomonori; Setoya, Yutaro; Shimizu, Kaoru; Osada, Hirokazu

2004-08-01

308

Latent structure modeling underlying theophylline tablet formulations using a Bayesian network based on a self-organizing map clustering.  

PubMed

Abstract The "quality by design" concept in pharmaceutical formulation development requires the establishment of a science-based rationale and design space. In this article, we integrate thin-plate spline (TPS) interpolation, Kohonen's self-organizing map (SOM) and a Bayesian network (BN) to visualize the latent structure underlying causal factors and pharmaceutical responses. As a model pharmaceutical product, theophylline tablets were prepared using a standard formulation. We measured the tensile strength and disintegration time as response variables and the compressibility, cohesion and dispersibility of the pretableting blend as latent variables. We predicted these variables quantitatively using nonlinear TPS, generated a large amount of data on pretableting blends and tablets and clustered these data into several clusters using a SOM. Our results show that we are able to predict the experimental values of the latent and response variables with a high degree of accuracy and are able to classify the tablet data into several distinct clusters. In addition, to visualize the latent structure between the causal and latent factors and the response variables, we applied a BN method to the SOM clustering results. We found that despite having inserted latent variables between the causal factors and response variables, their relation is equivalent to the results for the SOM clustering, and thus we are able to explain the underlying latent structure. Consequently, this technique provides a better understanding of the relationships between causal factors and pharmaceutical responses in theophylline tablet formulation. PMID:24994002

Yasuda, Akihito; Onuki, Yoshinori; Obata, Yasuko; Takayama, Kozo

2014-07-01

309

Influence of enzymes and surfactants on the disintegration behavior of cross-linked hard gelatin capsules during dissolution.  

PubMed

Gelatin exhibits cross-linking upon storage at stress conditions. Capsules stored at these conditions fail to show appropriate in vitro dissolution. The aim of this study is to show the effect of surfactants in the medium on the disintegration of the gelatin capsule. This is demonstrated in the presence and absence of the enzymes pancreatin and pepsin, the function of which is to improve the dissolution. Sodium lauryl sulfate (SLS) and Tween 80 are tested as surfactants. When SLS is used in the medium, dissolution is significantly hampered due to the formation of a less soluble precipitate of gelatin. Compared to SLS, Tween 80 shows far better disintegration and solubility results in dissolution media with neutral or low pH. Therefore, it is concluded in this study that Tween 80 is preferred when a surfactant is necessary to comply with sink condition requirements. PMID:16455602

Pennings, F H; Kwee, B L S; Vromans, H

2006-01-01

310

Influence of in vitro test conditions on release of aspirin from commercial tablets.  

PubMed

The influence of in vitro test conditions on the release of aspirin from commercial tablets was assessed with a USP rotating-basket dissolution apparatus. Three types of aspirin tablets were evaluated: plain, buffered, and microencapsulated. The variables investigated were stirring speed, pH, and volume and temperature of the dissolution medium. Plain tablets gave the best dissolution profiles under all experimental conditions, except at pH 3. Microencapsulated tablets showed sustained release. For all three types of tablets, faster dissolution was observed at pH 4.5 compared with that in artificial gastric juices. Increasing the stirring rate increased the dissolution rate, an effect most pronounced for plain tablets. Very similar dissolution curves were obtained when the dissolution test was conducted in 500 and 900 mL of dissolution media regardless of the pH of the media. No significant difference in dissolution profiles was observed when the effect of temperature was investigated. The dissolution data were evaluated on the basis of theoretical dissolution equations and by linear transformation of dissolution curves. Highly significant linear correlation coefficients revealed that the cube root equation could be used to describe drug release in artificial gastric juices, regardless of tablet type. When pH 4.5 buffer solution was used as the dissolution medium, different kinetic models were applicable. PMID:1501078

Nikoli?, L; Djuri?, Z; Jovanovi?, M

1992-04-01

311

Cost evaluation of alternative pharmaceutical tableting processes by simulation.  

PubMed

A simulation model and a subsequent computer program were developed as experimentation methods for evaluating tableting processes with respect to cost. These methods also allow estimation of the various times involved in a tableting operation (e.g., the processing time). The model was programmed in FORTRAN using the GASP IV simulation language. After verification of the program, experiments were run that involved comparing different levels of specific input variables to determine which variable had an effect on the cost-time relationships of a particular processing method. Among the possible input variables chosen for evaluation were the drying method, the type of tableting machine, the batch size, the labor rate, and the operation of the equipment in the process. An analysis of variance was made, and three separate regression equations were developed that described the relationship between the input variables and the dependent variables of processing cost and time. Graphs were developed from the regression equations by manipulating them through series of different independent variables. These graphs then were used in determining minimum costs and times, breakeven points, and rates of change, as well as in simple evaluation of processes through graphic representation. By using the simulation program to run experiments and then by analyzing them, results can be obtained to help in making intelligent decisions about the cost-time relationships of a particular tableting procedure before it is implemented. PMID:7205569

Franz, R M; Banker, G S; Buck, J R; Peck, G E

1980-06-01

312

Quantitative determination of captopril and prednisolone in tablets by FT-Raman spectroscopy  

Microsoft Academic Search

A procedure for the quantitative determination of captopril and prednisolone in commercial tablets based on partial least squares (PLS) and principal component regression (PCR) treatment of FT-Raman spectroscopic data is described. In the studied medicines active pharmaceutical ingredients (APIs) constitute 4.2–16.7% of the tablet mass. Results obtained from calibration models built using unnormalised spectra were compared with the values found

Sylwester Mazurek; Roman Szostak

2006-01-01

313

The content of ecstasy tablets: implications for the study of their long-term effects  

Microsoft Academic Search

Aims To examine the variation in the content of ecstasy tablets seized in the north-west of England during 2001 and to compare it to the UK average from 1991 to 2001. Measurements All tablets submitted to the Forensic Science Service in the north-west of England during 2001 were analysed by high performance liquid chromatography with diode array detection (HPLC-DAD). The

Jon C. Cole; Mike Bailey; Harry R. Sumnall; Graham F. Wagstaff; Les A. King

2002-01-01

314

21 CFR 520.2158b - Dihydrostreptomycin tablets.  

Code of Federal Regulations, 2010 CFR

...false Dihydrostreptomycin tablets. 520.2158b Section...AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.2158b Dihydrostreptomycin tablets. (a) Specifications. Each tablet contains 37.5...

2010-04-01

315

21 CFR 520.1696d - Penicillin V potassium tablets.  

Code of Federal Regulations, 2011 CFR

...2011-04-01 2011-04-01 false Penicillin V potassium tablets. 520.1696d...ANIMAL DRUGS § 520.1696d Penicillin V potassium tablets. (a) Specifications. Each tablet contains penicillin V potassium equivalent to...

2011-04-01

316

21 CFR 520.1696d - Penicillin V potassium tablets.  

Code of Federal Regulations, 2012 CFR

...2012-04-01 2012-04-01 false Penicillin V potassium tablets. 520.1696d...ANIMAL DRUGS § 520.1696d Penicillin V potassium tablets. (a) Specifications. Each tablet contains penicillin V potassium equivalent to...

2012-04-01

317

21 CFR 520.1696d - Penicillin V tablets.  

Code of Federal Regulations, 2013 CFR

...2013-04-01 2013-04-01 false Penicillin V tablets. 520.1696d Section...NEW ANIMAL DRUGS § 520.1696d Penicillin V tablets. (a) Specifications. Each tablet contains penicillin V potassium equivalent to 125...

2013-04-01

318

21 CFR 520.1696d - Penicillin V tablets.  

Code of Federal Regulations, 2014 CFR

...2014-04-01 2014-04-01 false Penicillin V tablets. 520.1696d Section...NEW ANIMAL DRUGS § 520.1696d Penicillin V tablets. (a) Specifications. Each tablet contains penicillin V potassium equivalent to 125...

2014-04-01

319

21 CFR 520.1696d - Penicillin V potassium tablets.  

Code of Federal Regulations, 2010 CFR

...2010-04-01 2010-04-01 false Penicillin V potassium tablets. 520.1696d...ANIMAL DRUGS § 520.1696d Penicillin V potassium tablets. (a) Specifications. Each tablet contains penicillin V potassium equivalent to...

2010-04-01

320

21 CFR 520.82a - Aminopropazine fumarate tablets.  

Code of Federal Regulations, 2010 CFR

... § 520.82a Aminopropazine fumarate tablets. (a) Specifications. The drug is in tablet form. Each tablet contains aminopropazine fumarate equivalent...weight. The dosage can be repeated every 12 hours, as indicated.1 (3)...

2010-04-01

321

21 CFR 520.1284 - Sodium liothyronine tablets.  

Code of Federal Regulations, 2010 CFR

...Specifications. Sodium liothyronine tablets consist of tablets intended for oral administration...liothyronine at 60 or 120 micrograms per tablet, as the sodium salt. (b...orally to dogs at levels up to 12.8 micrograms per...

2010-04-01

322

21 CFR 520.434 - Chlorphenesin carbamate tablets.  

Code of Federal Regulations, 2012 CFR

...2012-04-01 2012-04-01 false Chlorphenesin carbamate tablets. 520.434 ...FORM NEW ANIMAL DRUGS § 520.434 Chlorphenesin carbamate tablets. (a) Specifications...Each tablet contains 400 milligrams of chlorphenesin carbamate. (b) Sponsor....

2012-04-01

323

21 CFR 520.434 - Chlorphenesin carbamate tablets.  

Code of Federal Regulations, 2011 CFR

...2011-04-01 2011-04-01 false Chlorphenesin carbamate tablets. 520.434 ...FORM NEW ANIMAL DRUGS § 520.434 Chlorphenesin carbamate tablets. (a) Specifications...Each tablet contains 400 milligrams of chlorphenesin carbamate. (b) Sponsor....

2011-04-01

324

21 CFR 520.434 - Chlorphenesin carbamate tablets.  

Code of Federal Regulations, 2013 CFR

...2013-04-01 2013-04-01 false Chlorphenesin carbamate tablets. 520.434 ...FORM NEW ANIMAL DRUGS § 520.434 Chlorphenesin carbamate tablets. (a) Specifications...Each tablet contains 400 milligrams of chlorphenesin carbamate. (b) Sponsor....

2013-04-01

325

21 CFR 520.434 - Chlorphenesin carbamate tablets.  

Code of Federal Regulations, 2010 CFR

...2010-04-01 2010-04-01 false Chlorphenesin carbamate tablets. 520.434 ...FORM NEW ANIMAL DRUGS § 520.434 Chlorphenesin carbamate tablets. (a) Specifications...Each tablet contains 400 milligrams of chlorphenesin carbamate. (b) Sponsor....

2010-04-01

326

21 CFR 520.434 - Chlorphenesin carbamate tablets.  

Code of Federal Regulations, 2014 CFR

...2014-04-01 2014-04-01 false Chlorphenesin carbamate tablets. 520.434 ...FORM NEW ANIMAL DRUGS § 520.434 Chlorphenesin carbamate tablets. (a) Specifications...Each tablet contains 400 milligrams of chlorphenesin carbamate. (b) Sponsor....

2014-04-01

327

Effect of turbulence on the disintegration rate of flushable consumer products.  

PubMed

A previously developed model for the physical disintegration of flushable consumer products is expanded by investigating the effects of turbulence on the rate of physical disintegration. Disintegration experiments were conducted with cardboard tampon applicators at 100, 150, and 200 rotations per minute, corresponding to Reynold's numbers of 25,900, 39,400, and 52,900, respectively, which were estimated by using computational fluid dynamics modeling. The experiments were simulated with the disintegration model to obtain best-fit values of the kinetic and distribution parameters. Computed rate coefficients (ki) for all solid sizes (i.e., greater than 8, 4 to 8, 2 to 4, and 1 to 2 mm) increased strongly with Reynold's number or rotational speed. Thus, turbulence strongly affected the disintegration rate of flushable products, and the relationship of the ki values to Reynold's number can be included in mathematical representations of physical disintegration. PMID:22852428

Karadagli, Fatih; Rittmann, Bruce E; McAvoy, Drew C; Richardson, John E

2012-05-01

328

A study on maize proteins as a potential new tablet excipient.  

PubMed

This investigation has examined the use of zein proteins from maize as the major component in oral controlled-release tablets, such formulations often being required to improve patient compliance. Tablets containing ground zein proteins, calcium hydrogen orthophosphate, polyvinyl pyrrolidone, theophylline and magnesium stearate were produced by wet granulation and compression on a single station tablet press and were compared to directly compressed tablets based on zein proteins, calcium hydrogen orthophosphate and theophylline. Non invasive techniques such as Fourier Transform infrared spectroscopy and Fourier Transform Raman spectroscopy were employed to investigate any changes in the secondary structure of zein proteins during tablet production. Random coils, alpha helices and beta sheets predominated and their relative content remained unaffected during grinding, wet granulation and compression, indicating that formulations based on zeins will be robust, i.e. insensitive to minor changes in the production conditions. Drug release from the tablets was studied using a standard pharmacopoeial dissolution test. Dissolution profiles in water, 0.1M HCl (pH=1) and phosphate buffer (pH=6.8) show that only a limited amount of theophylline was released after 4.5h, suggesting that zein proteins could act as a potential vehicle for oral controlled drug release. Analysis of the theophylline release profiles using the Peppas and Sahlin model reveals that diffusion and polymer relaxation occurred in acidic (pH=1) and buffered (pH=6.8) conditions for wet granulated tablets, whereas diffusion was predominant in directly compressed tablets. In conclusion, the present study has shown that zeins can be successfully used as a pharmaceutical excipient, and in particular as a matrix in monolithic controlled release tablets. PMID:18294824

Georget, Dominique M R; Barker, Susan A; Belton, Peter S

2008-06-01

329

Quality-by-Design III: Application of Near-Infrared Spectroscopy to Monitor Roller Compaction In-process and Product Quality Attributes of Immediate Release Tablets.  

PubMed

The objective of this study is to use near-infrared spectroscopy (NIRS) coupled with multivariate chemometric models to monitor granule and tablet quality attributes in the formulation development and manufacturing of ciprofloxacin hydrochloride (CIP) immediate release tablets. Critical roller compaction process parameters, compression force (CFt), and formulation variables identified from our earlier studies were evaluated in more detail. Multivariate principal component analysis (PCA) and partial least square (PLS) models were developed during the development stage and used as a control tool to predict the quality of granules and tablets. Validated models were used to monitor and control batches manufactured at different sites to assess their robustness to change. The results showed that roll pressure (RP) and CFt played a critical role in the quality of the granules and the finished product within the range tested. Replacing binder source did not statistically influence the quality attributes of the granules and tablets. However, lubricant type has significantly impacted the granule size. Blend uniformity, crushing force, disintegration time during the manufacturing was predicted using validated PLS regression models with acceptable standard error of prediction (SEP) values, whereas the models resulted in higher SEP for batches obtained from different manufacturing site. From this study, we were able to identify critical factors which could impact the quality attributes of the CIP IR tablets. In summary, we demonstrated the ability of near-infrared spectroscopy coupled with chemometrics as a powerful tool to monitor critical quality attributes (CQA) identified during formulation development. PMID:25319052

Kona, Ravikanth; Fahmy, Raafat M; Claycamp, Gregg; Polli, James E; Martinez, Marilyn; Hoag, Stephen W

2015-02-01

330

Theoretical investigations into the influence of the position of a breaking line on the tensile failure of flat, round, bevel-edged tablets using finite element methodology (FEM) and its practical relevance for industrial tablet strength testing.  

PubMed

Flat, round tablets may have a breaking ("score") line. Pharmacopoeial tablet breaking load tests are diametral in their design, and industrially used breaking load testers often have automatic tablet feeding systems, which position the tablets between the loading platens of the machine with the breaking lines in random orientation to the applied load. The aim of this work was to ascertain the influence of the position of the breaking line in a diametral compression test using finite element methodology (FEM) and to compare the theoretical results with practical findings using commercially produced bevel-edged, scored tablets. Breaking line test positions at an angle of 0°, 22.5°, 45°, 67.5° and 90° relative to the loading plane were studied. FEM results obtained for fully elastic and elasto-plastic tablets were fairly similar, but they highlighted large differences in stress distributions depending on the position of the breaking line. The stress values at failure were predicted to be similar for tablets tested at an angle of 45° or above, whereas at lower test angles the predicted breaking loads were up to three times larger. The stress distributions suggested that not all breaking line angles would result in clean tensile failure. Practical results, however, did not confirm the differences in the predicted breaking loads, but they confirmed differences in the way tablets broke. The results suggest that it is not advisable to convert breaking loads obtained on scored tablets into tablet tensile strength values, and comparisons between different tablets or batches should carefully consider the orientation of the breaking line with respect to the loading plane, as the failure mechanisms appear to vary. PMID:25455775

Podczeck, Fridrun; Newton, J Michael; Fromme, Paul

2014-12-30

331

Design and optimization of bilayered tablet of Hydrochlorothiazide using the Quality-by-Design approach  

PubMed Central

Aim: The aim of the present study is to develop an optimize bilayered tablet using Hydrochlorothiazide (HCTZ) as a model drug candidate using quality by design (QbD) approach. Introduction and Method: The bilayered tablet gives biphasic drug release through loading dose; prepared using croscarmellose sodium a superdisintegrant and maintenance dose using several viscosity grades of hydrophilic polymers. The fundamental principle of QbD is to demonstrate understanding and control of pharmaceutical processes so as to deliver high quality pharmaceutical products with wide opportunities for continuous improvement. Risk assessment was carried out and subsequently 22 factorial designs in duplicate was selected to carry out design of experimentation (DOE) for evaluating the interactions and effects of the design factors on critical quality attribute. The design space was obtained by applying DOE and multivariate analysis, so as to ensure desired disintegration time (DT) and drug release is achieved. Bilayered tablet were evaluated for hardness, thickness, friability, drug content uniformity and in vitro drug dissolution. Result: Optimized formulation obtained from the design space exhibits DT of around 70 s, while DR T95% (time required to release 95% of the drug) was about 720 min. Kinetic studies of formulations revealed that erosion is the predominant mechanism for drug release. Conclusion: From the obtained results; it was concluded that independent variables have a significant effect over the dependent responses, which can be deduced from half normal plots, pareto charts and surface response graphs. The predicted values matched well with the experimental values and the result demonstrates the feasibility of the design model in the development and optimization of HCTZ bilayered tablet. PMID:25006554

Dholariya, Yatin N; Bansod, Yogesh B; Vora, Rahul M; Mittal, Sandeep S; Shirsat, Ajinath Eknath; Bhingare, Chandrashekhar L

2014-01-01

332

Double-layered mucoadhesive tablets containing nystatin  

Microsoft Academic Search

The objective of this work was to design a mucoadhesive tablet with a potential use in the treatment of oral candidosis. A\\u000a 2-layered tablet containing nystain was formulated. Lactose CD (direct compression), carbomer (CB), and hydroxypropylmethylcellulose\\u000a (HPMC) were used as excipients. Tablets were obtained through direct compression. Properties such as in vitro mucoadhesion,\\u000a water uptake, front movements, and drug release

Juan Manuel Llabot; Ruben Hilario Manzo; Alberto allemandi

2002-01-01

333

Measurement of Disintegration Rates and Absolute {gamma}-ray Intensities  

SciTech Connect

The majority of practical radioactive materials decay by modes that include {gamma}-ray emission. For questions of 'how much' or 'how pure', one must know the absolute intensities of the major radiations. We are using liquid scintillation counting (LSC) to measurements of disintegration rates, coupled with {gamma}-ray spectroscopy to measure absolute {gamma}-ray emission probabilities. Described is a study of the 227Th chain yielding absolute {gamma}-ray intensities with {approx}0.5% accuracy and information on LSC efficiencies.

DeVries, Daniel J.; Griffin, Henry C. [Department of Chemistry, University of Michigan, Ann Arbor, MI 48109 (United States)

2006-03-13

334

1H-NMR microscopy of tablets.  

PubMed

A 1H-nuclear magnetic resonance (NMR) microscopy method was utilized for the first time to determine the porosity distribution of physically intact tablets. The main advantage of this newly developed method was that porosity cross sections through whole tablets or specific locations could be obtained without mechanically destroying the tested tablet. This was achieved by filling tablet cavities with silicone oil under vacuum. The amount of silicone oil locally within the tablet was then determined by 1H-NMR microscopy, revealing the inverse inner structure. To reduce the measuring time, a paramagnetic gadolinium complex was added to the silicone oil. The cross sectional signals produced by 1H-NMR microscopy through the tablet were transformed into a color image by a specially designed computer graphic program. To improve the signal-noise ratio an algorithm of 3D-filtering was introduced. The maximal spatial resolution achieved with this method was about 95 microns for a cube's edge length corresponding to some 380,000 positions in a 9-mm-diameter compression-coated tablet. Uneven porosity distributions within tablets, cracks, or cavities could be visualized with this newly developed method. Different compaction mechanisms were observed with plastic- or brittle-type tablets. The different states of densification during compaction of powders could be detected. The integrity of compression coatings was determined to be dependent on the pressure load and the location of the core within the coat. PMID:7616364

Nebgen, G; Gross, D; Lehmann, V; Müller, F

1995-03-01

335

SEM/EDX and confocal Raman microscopy as complementary tools for the characterization of pharmaceutical tablets.  

PubMed

The drug distribution on the surface of hot-melt extruded, pre-mixed hot-melt extruded and direct compressed tablet formulations was characterized by using scanning electron microscopy, energy dispersive X-ray spectroscopy (EDX) and confocal Raman spectroscopy. Formulations of paracetamol (PMOL) and Compritol(®) (C-888) were extruded using hot-melt extrusion at different processing temperatures and formulation compositions before being compressed into tablets. EDX and confocal Raman spectroscopy were employed to map the drug and excipient distribution, both qualitatively and quantitatively, on the surface of the tablets. The results from EDX and confocal Raman studies confirmed better uniformity and distribution of PMOL in the pre-mixed extruded formulations compared to both hot-melt extruded formulations and those obtained by means of direct compression. The quantification of the drug composition on the surface of the tablets by both EDX and confocal Raman was in good agreement with the theoretically expected values. PMID:24836664

Scoutaris, Nikolaos; Vithani, Kapilkumar; Slipper, Ian; Chowdhry, Babur; Douroumis, Dennis

2014-08-15

336

The forensic aspects of contemporary disintegrating rifle bullets.  

PubMed

A relatively new type of rifle bullet has appeared in the last few years that contains no lead and rapidly disintegrates into very small particles and jacket fragments immediately upon entry into soft tissue. These bullets are intended for use by 'varmint' hunters in high-velocity centerfire rifles where the effect on such animals as prairie dogs, gophers, ground hogs, and other similarly sized animals is nothing short of explosive. The shooting of much larger animals to include human beings will typically result in nonperforating wounds with short wound paths. X-ray views of a decedent or gunshot victim will lack any recognizable bullet or projectile. Only 1 jacket fragment among the many present in the wound tract is suitable for subsequent firearms identification purposes, namely, the small copper disc that represents the base or heel of the bullet jacket. This small circular fragment bears vestiges of the rifling marks of the responsible firearm.This article will aid the forensic pathologist in recognizing gunshot wounds produced by these atypical bullets and the importance of recovering the base portion of the disintegrated bullet jacket. PMID:23361072

Haag, Lucien C

2013-03-01

337

Formulation and characterization of acetaminophen nanoparticles in orally disintegrating films.  

PubMed

Abstract The purpose of this study was to prepare orally disintegrating films containing nanoparticles loaded with acetaminophen. Nanoparticles were prepared by the emulsion-solvent evaporation method where acetone phase containing acetaminophen and poly(lactide-co-glycolide acid) (PLGA) was added to water phase containing hydroxypropyl methyl cellulose, poly ethylene glycol, polyvinyl alcohol (PVA) and aspartame in a rate of 1.5 drop?s(-1) and agitated at 1200?rpm. The size, polydispersity index (PI) and drug entrapment (DE) were measured. The emulsions were cast to form films, which were evaluated physico-mechanically. The effect of different degrees of hydrolization of PVA and polymerization of PLGA and the effect of different ratios of PVA to PLGA was studied. Films with acceptable physico-mechanical properties were further studied. The size and PI of the nanoparticles was dependent on PVA hydrolization, PLGA polymerization and the ratio of PVA to PLGA. All films disintegrated in less than one minute, but acetaminophen was not free in the dissolution media even after six days. These results may indicate that although the nanoparticles released from the films immediately when impressed in solution the drug is sustained in the nanoparticles for longer time, which is to be clarified in future work. PMID:25013958

Al-Nemrawi, Nusaiba K; Dave, Rutesh H

2014-07-11

338

Novel tablet formulation of amorphous candesartan cilexetil solid dispersions involving P-gp inhibition for optimal drug delivery: in vitro and in vivo evaluation.  

PubMed

Abstract Objective: The aim of this study was to develop a novel tablet formulation of amorphous candesartan cilexetil (CAN) solid dispersion involving effective P-gp inhibition for optimal drug delivery by direct compression (DC) method. Methods: To accomplish DC, formulation blends were evaluated for micromeritic properties. The Carr index, Hausner ratio, flow rate and cotangent of the angle ? were determined. The tablets with and without naringin prepared by DC technique were evaluated for average weight, hardness, disintegration time and friability assessments. The drug release profiles were determined to study the dissolution kinetics. In vivo pharmacokinetic studies were conducted in rabbits. Accelerated stability studies were performed for tablets at 40?±?2?°C/75% RH?±?5% for 6 months. Results: FTIR studies confirmed no discoloration, liquefaction and physical interaction between naringin and drug. The results indicated that tablets prepared from naringin presented a dramatic release (82%) in 30?min with a similarity factor (76.18), which is most likely due to the amorphous nature of drug and the higher micromeritic properties of blends. Our findings noticed 1.7-fold increase in oral bioavailability of tablet prepared from naringin with mean Cmax and AUC0-12?h values as 35.81?±?0.13??g/mL and 0.14?±?0.09??g h/mL, respectively. The tablets with and without naringin prepared by DC technique were physically and chemically stable under accelerated stability conditions upon storage for 6 months. Conclusion: These results are attractive for further development of an oral tablet formulation of CAN through P-gp inhibition using naringin, a natural flavonoid as a pharmaceutical excipient. PMID:25080228

Surampalli, Gurunath; Nanjwade, Basavaraj K; Patil, P A; Chilla, Rakesh

2014-07-31

339

Bioequivalence study of 400 and 100 mg imatinib film-coated tablets in healthy volunteers.  

PubMed

The aim of the study was to investigate the bioavailability of a generic product of 100 mg and 400 mg imatinib film-coated tablets (test) as compared to that of a branded product (reference) at the same strength to determine bioequivalence. The secondary objective of the study was to evaluate tolerability of both products. An open-label, randomized, crossover, two-period, single-dose, comparative study was conducted in 43 (Imatynib-Biofarm 100 mg film-coated tablet) and in 42 (Imatynib-Biofarm 400 mg film-coated tablet), brand name Imatenil, Caucasian healthy volunteers in fed conditions. A single oral dose administration of the test or reference product was separated by 14-day washout period. The imatinib and its metabolite N-desmethyl imatinib concentrations were determined using a validated LC MS/MS method. The results of the single-dose study in healthy volunteers indicated that the film-coated tablets of Imatynib-Biofarm 100 mg and 400 mg film-coated tablets manufactured by Biofarm Sp. z o.o. (test products) are bioequivalent to those of Glivec 100 mg and 400 mg film-coated tablets manufactured by Novartis Pharma GmbH (reference products). Both products in the two doses of imatinib were well tolerated. PMID:25362813

Ostrowicz, Andrzej; Miko?ajczak, Przemys?aw L; Wierzbicka, Marzena; Boguradzki, Piotr

2014-01-01

340

Smartphones and tablets: Reshaping radiation oncologists’ lives  

PubMed Central

Background Smartphones and tablets are new handheld devices always connected to an information source and capable of providing instant updates, they allow doctors to access the most updated information and provide decision support at the point of care. Aim The practice of radiation oncology has always been a discipline that relies on advanced technology. Smartphones provide substantial processing power, incorporating innovative user interfaces and applications. Materials and methods The most popular smartphone and tablet app stores were searched for “radiation oncology” and “oncology” related apps. A web search was also performed searching for smartphones, tablets, oncology, radiology and radiation oncology. Results Smartphones and tablets allow rapid access to information in the form of podcasts, apps, protocols, reference texts, recent research and more. Conclusion With the rapidly changing advances in radiation oncology, the trend toward accessing resources via smartphones and tablets will only increase, future will show if this technology will improve clinical care. PMID:24669308

Gomez-Iturriaga, Alfonso; Bilbao, Pedro; Casquero, Francisco; Cacicedo, Jon; Crook, Juanita

2012-01-01

341

Universal scaling laws for the disintegration of electrified drops  

PubMed Central

Drops subjected to strong electric fields emit charged jets from their pointed tips. The disintegration of such jets into a spray consisting of charged droplets is common to electrospray ionization mass spectrometry, printing and coating processes, and raindrops in thunderclouds. Currently, there exist conflicting theories and measurements on the size and charge of these small electrospray droplets. We use theory and simulation to show that conductivity can be tuned to yield three scaling regimes for droplet radius and charge, a finding missed by previous studies. The amount of charge that electrospray droplets carry determines whether they are coulombically stable and charged below the Rayleigh limit of stability or are unstable and hence prone to further explosions once they are formed. Previous experiments reported droplet charge values ranging from 10% to in excess of . Simulations unequivocally show that electrospray droplets are coulombically stable at the instant they are created and that there exists a universal scaling law for droplet charge, . PMID:23487744

Collins, Robert T.; Sambath, Krishnaraj; Harris, Michael T.; Basaran, Osman A.

2013-01-01

342

Effect of magnesium stearate concentration on dissolution properties of ranitidine hydrochloride coated tablets.  

PubMed

Most pharmaceutical formulations also include a certain amount of lubricant to improve their flowability and prevent their adhesion to the surfaces of processing equipment. Magnesium stearate is an additive that is most frequently used as a lubricant. Magnesium stearate is capable of forming films on other tablet excipients during prolonged mixing, leading to a prolonged drug liberation time, a decrease in hardness, and an increase in disintegration time. It is hydrophobic, and there are many reports in the literature concerning its adverse effect on dissolution rates. The objective of this study was to evaluate the effects of two different concentrations of magnesium stearate on dissolution properties of ranitidine hydrochloride coated tablet formulations labeled to contain 150 mg. The uniformity content was also checked. During the drug formulation development, several samples were designed for choice of the formulation. For this study, two formulations containing 0,77 and 1,1% of magnesium stearate added in the manufacture of cores were chosen. Fraction of ranitidine hydrochloride released in dissolution medium was calculated from calibration curves. The data were analyzed using pharmacopeial test for similarity of dissolution profiles ( f2 equation), previously proposed by Moore and Flanner. Application of f2 equation showed differences in time-course of ranitidine hydrochloride dissolution properties. The obtained values indicate differences in drug release from analyzed ranitidine hydrochloride formulations and could cause differences in therapeutic response. PMID:17848158

Uzunovi?, Alija; Vrani?, Edina

2007-08-01

343

Fundamental mechanisms for tablet dissolution: simulation of particle deaggregation via Brownian dynamics.  

PubMed

For disintegrating tablet formulations, deaggregation of small particles is sometimes one of the rate-limiting processes for drug release. Because the tablets contain particles that are in the colloidal size range, it may be assumed that the deaggregation process, at least qualitatively, is governed by Brownian motion and electrostatic and van der Waals interactions, where the latter two can be described by a Derjaguin-Landau-Verwey-Overbeek interaction potential. On the basis of this hypothesis, the present work investigates the applicability of Brownian dynamics (BD) simulations as a tool to understand the deaggregation mechanism on a fundamental level. BD simulations are therefore carried out to determine important deaggregation characteristics such as the so-called mean first passage time (MFPT) and first passage time distribution (FPTD) for various two-, three-, and four-particle aggregates. The BD algorithm is first validated and tuned by comparison with analytical expressions for the MFPT and FPTD in the two-particle case. It is then shown that the same algorithm can also be used for the three-particle case. Lastly, the simulations of three- and four-particle aggregates show that the initial shape of the aggregates may significantly affect the deaggregation time. PMID:23508875

Kaunisto, Erik; Rasmuson, Anders; Bergenholtz, Johan; Remmelgas, Johan; Lindfors, Lennart; Folestad, Staffan

2013-05-01

344

Terahertz Technology: A Boon to Tablet Analysis  

PubMed Central

The terahertz gap has a frequency ranges from ?0.3 THz to ?10 THz in the electromagnetic spectrum which is in between microwave and infrared. The terahertz radiations are invisible to naked eye. In comparison with x-ray they are intrinsically safe, non-destructive and non-invasive. Terahertz spectroscopy enables 3D imaging of structures and materials, and the measurement of the unique spectral fingerprints of chemical and physical forms. Terahertz radiations are produced by a dendrimer based high power terahertz source and spectroscopy technologies. It resolves many of the questions left unanswered by complementary techniques, such as optical imaging, Raman and infrared spectra. In the pharmaceutical industries it enables nondestructive, internal, chemical analysis of tablets, capsules, and other dosage forms. Tablet coatings are a major factor in drug bioavailability. Therefore tablet coatings integrity and uniformity are of crucial importance to quality. Terahertz imaging gives an unparalleled certainty about the integrity of tablet coatings and the matrix performance of tablet cores. This article demonstrates the potential of terahertz pulse imaging for the analysis of tablet coating thickness by illustrating the technique on tablets. PMID:20490288

Wagh, M. P.; Sonawane, Y. H.; Joshi, O. U.

2009-01-01

345

Evaluation of the binder effects of the gum mucilages of Cissus populnea and Acassia senegal on the mechanical properties of paracetamol tablets  

Microsoft Academic Search

A comparative study has been carried out to investigate the binder effects of the gums of Cissus populnea and Accasia senegal on the mechanical properties of paracetamol tablets. Tablet mechanical properties evaluated include the packing fraction (Pf), the tensile strength (T) and the brittle fracture tendency (BFI). Varying concentrations of the gum mucilage ranging from 1 - 15% (w\\/v) was

F. E. Eichie

2007-01-01

346

Comparison of cefpodoxime proxetil release and antimicrobial activity from tablet formulations: complexation with hydroxypropyl-?-cyclodextrin in the presence of water soluble polymer.  

PubMed

This study aims to prove the complexation of cefpodoxime proxetil (CP) by hydroxypropyl-?-cyclodextrin (HP-?-CD) in the presence of sodium carboxymethyl cellulose (Na CMC), and makes a comparison of commercial tablets by dissolution and antimicrobial activity studies. The CP--HP-?-CD complex was prepared by kneading method and characterized by SEM, FTIR and DSC. The solubility method was used to investigate the effect of HP-?-CD and Na CMC on the solubility of CP. The complex tablets were prepared using direct compression method. Dissolution studies were performed with complex tablets and commercial tablets in pH 1.2, 4.5, 6.8 and 7.4 buffer solutions. It was observed that complexation occurred in all formulations, and HP-?-CD is able to increase CP solubility and dissolution rate of CP was improved from complex tablets, when compared with commercial tablets. Furthermore, the antimicrobial activity studies revealed that the CP--HP-?-CD complex and complex tablets were shown to have more effective antimicrobial activity than commercial tablets. It is evident from the results that complexation with HP-?-CD in the presence of Na CMC is feasible way to prepare a more efficient tablet formulation with improved dissolution and antimicrobial activity. PMID:22010782

Gundogdu, Evren; Koksal, Cinel; Karasulu, Ercument

2012-06-01

347

Exploring the potential of a highly compressible microcrystalline cellulose as novel tabletting excipient in the compaction of extended-release coated pellets containing an extremely water-soluble model drug.  

PubMed

Compaction of controlled-release coated pellets into tablets is challenging because of the fusion of pellets and the rupturing of coated film. The difficulty in compaction intensifies with the use of extremely water-soluble drugs. Therefore, the present study was conducted to prepare and compact pellets containing pseudoephedrine hydrochloride as an extremely water-soluble model drug. The pellets were produced using an extrusion-spheronization technique. The drug-loaded pellets were coated to extend the drug release up to 12-h employing various polymers, and then they were compressed into tablets using microcrystalline cellulose Ceolus KG-801 as a novel tabletting excipient. The in vitro drug release studies of coated pellets and tablets were undertaken using the USP basket method in dissolution test apparatus I. The amount of drug released was analyzed at a wavelength of 215 nm. The combined coatings of hydroxypropyl methylcellulose and Kollicoat SR-30D yielded 12-h extended-release pellets with drug release independent of pH of dissolution medium following zero-order kinetics. The drug release from the tablets prepared using inert Celous KG-801 granules as tabletting excipient was found faster than that of coated pellets. However, a modification in drug release rate occurred with the incorporation of inert Ceolus KG-801 pellets. The drug dissolution profile from tablets containing 40% w/w each of coated pellets and inert granules along with 20% w/w inert pellets was found to be closely similar to that of coated pellets. Furthermore, the friability, tensile strength, and disintegration time of the tablets were within the USP specifications. PMID:19554454

Zeeshan, F; Peh, K K; Tan, Y T F

2009-01-01

348

Difference in the lubrication efficiency of bovine and vegetable-derived magnesium stearate during tabletting.  

PubMed

The purpose of this work was to evaluate and compare the functionality of bovine fatty acids-derived (MgSt-B) and vegetable fatty acids-derived (MgSt-V) magnesium stearate powders when used for the lubrication of granules prepared by high-shear (HSG) and fluid bed (FBG) wet granulation methods. The work included evaluation of tablet compression and ejection forces during tabletting and dissolution testing of the compressed tablets. Granules prepared by both granulation methods required significantly lower ejection force (p < 0.01) when lubricated with the MgSt-V powder as compared to those lubricated with the MgSt-B powder. Granules prepared by the HSG method and lubricated with the MgSt-V powder also required significantly lower compression force (p < 0.01) to produce tablets of similar weight and hardness as compared to those lubricated with the MgSt-B powder. The dissolution profiles were not affected by these differences and were the same for tablets prepared by same granulation method and lubricated with either magnesium stearate powder. The results indicate significant differences (p < 0.01) between lubrication efficiency of the MgSt-B and the MgSt-V powders and emphasize the importance of functionality testing of the MgSt powders to understand the impact of these differences. PMID:19390976

Gupta, Abhay; Hamad, Mazen L; Tawakkul, Mobin; Sayeed, Vilayat A; Khan, Mansoor A

2009-01-01

349

An open-label, randomized bioavailability study with alternative methods of administration of crushed ticagrelor tablets in healthy volunteers  

PubMed Central

Objective: To compare the bioavailability and safety profile of crushed ticagrelor tablets suspended in water and administered orally or via nasogastric tube, with that of whole tablets administered orally. Methods: In this single-center, open-label, randomized, three-treatment crossover study, 36 healthy volunteers were randomized to receive a single 90-mg dose of ticagrelor administered orally as a whole tablet or as crushed tablets suspended in water and given orally or via a nasogastric tube into the stomach, with a minimum 7-day wash-out between treatments. Plasma concentrations of ticagrelor and AR-C124910XX were assessed at 0, 0.5, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 36, and 48 hours post-ticagrelor dose for pharmacokinetic analyses. Safety and tolerability was assessed throughout the study. Results: At 0.5 hours postdose, plasma concentrations of ticagrelor and AR-C124910XX were higher with crushed tablets administered orally (148.6 ng/mL and 13.0 ng/mL, respectively) or via nasogastric tube (264.6 ng/mL and 28.6 ng/mL, respectively) compared with whole-tablet administration (33.3 ng/mL and 5.2 ng/mL, respectively). A similar trend was observed at 1 hour postdose. Ticagrelor tmax was shorter following crushed vs. whole-tablet administration (1 vs. 2 hours, respectively). Geometric mean ratios between treatments for AUC and Cmax were contained within the bioequivalence limits of 80 – 125% for ticagrelor and AR-C124910XX. All treatments were generally well tolerated. Conclusions: Ticagrelor administered as a crushed tablet is bioequivalent to whole-tablet administration, independent of mode of administration (oral or via nasogastric tube), and resulted in increased plasma concentrations of ticagrelor and AR-C124910XX at early timepoints. PMID:25500486

Teng, Renli; Carlson, Glenn; Hsia, Judith

2015-01-01

350

Early clinical development of artemether-lumefantrine dispersible tablet: palatability of three flavours and bioavailability in healthy subjects  

PubMed Central

Background Efforts to ease administration and enhance acceptability of the oral anti-malarial artemether-lumefantrine (A-L) crushed tablet to infants and children triggered the development of a novel dispersible tablet of A-L. During early development of this new formulation, two studies were performed in healthy subjects, one to evaluate the palatability of three flavours of A-L, and a second one to compare the bioavailability of active principles between the dispersible tablet and the tablet (administered crushed and intact). Methods Study 1 was performed in 48 healthy schoolchildren in Tanzania. Within 1 day, all subjects tasted a strawberry-, orange- and cherry-flavoured oral A-L suspension for 10 seconds (without swallowing) in a randomized, single-blind, crossover fashion. The palatability of each formulation was rated using a visual analogue scale (VAS). Study 2 was an open, randomized crossover trial in 48 healthy adults given single doses of A-L (80 mg artemether + 480 mg lumefantrine) with food. The objectives were to compare the bioavailability of artemether, dihydroartemisinin (DHA) and lumefantrine between the dispersible tablet and the tablet administered crushed (primary objective) and intact (secondary objective). Results Study 1 showed no statistically significant difference in VAS scores between the three flavours but cherry had the highest score in several ratings (particularly for overall liking). Study 2 demonstrated that the dispersible and crushed tablets delivered bioequivalent artemether, DHA and lumefantrine systemic exposure (area under the curve [AUC]); mean ± SD AUC0-tlast were 208 ± 113 vs 195 ± 93 h.ng/ml for artemether, 206 ± 81 vs 199 ± 84 h.ng/ml for DHA and 262 ± 107 vs 291 ± 106 h.?g/ml for lumefantrine. Bioequivalence was also shown for peak plasma concentrations (Cmax) of DHA and lumefantrine. Compared with the intact tablet, the dispersible tablet resulted in bioequivalent lumefantrine exposure, but AUC and Cmax values of artemether and DHA were 20-35% lower. Conclusions Considering that cherry was the preferred flavour, and that the novel A-L dispersible tablet demonstrated similar pharmacokinetic performances to the tablet administered crushed, a cherry-flavoured A-L dispersible tablet formulation was selected for further development and testing in a large efficacy and safety study in African children with malaria. PMID:20815879

2010-01-01

351

Ice dynamics preceding catastrophic disintegration of the floating part of Jakobshavn Isbræ, Greenland  

NASA Astrophysics Data System (ADS)

The floating terminal of Jakobshavn Isbræ, the fastest Greenland ice stream, has disintegrated since 2002, resulting in a doubling of ice velocity and rapidly lowering inland ice elevations. Conditions prior to disintegration were modeled using control theory in a plane-stress solution, and the Missoula model of ice-shelf flow. Both approaches pointed to a mechanism that inhibits ice flow and that is not captured by either approach. Jamming of flow, an inherent property of granular materials passing through a constriction (Jakobshavn Isfjord), is postulated as the mechanism. Rapid disintegration of heavily crevassed floating ice accompanies break-up of the ice jam.

Johnson, Jesse V.; Prescott, Paul R.; Hughes, Terence J.

352

21 CFR 520.1310 - Marbofloxacin tablets.  

Code of Federal Regulations, 2012 CFR

...CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1310 Marbofloxacin tablets...Indications for use . For the treatment of infections in dogs and cats associated with bacteria susceptible to marbofloxacin....

2012-04-01

353

Pharmaceutical tablet compaction : product and process design  

E-print Network

This thesis explores how tablet performance is affected by microstructure, and how microstructure can be controlled by selection of excipients and compaction parameters. A systematic strategy for formulation and process ...

Pore, Mridula

2009-01-01

354

Development of novel fast-dissolving tacrolimus solid dispersion-loaded prolonged release tablet.  

PubMed

The goal of this research was to develop a novel prolonged release tablet bioequivalent to the commercial sustained release capsule. A number of tacrolimus-loaded fast-dissolving solid dispersions containing various amounts of DOSS were prepared using the spray drying technique. Their solubility, dissolution and pharmacokinetics in rats were studied. DOSS increased drug solubility and dissolution in the solid dispersions. Compared with the drug powder, the solubility, dissolution and bioavailability of tacrolimus with the fast-dissolving solid dispersion containing tacrolimus/HP-?-CD/DOSS in the weight ratio of 5:40:4 were boosted by approximately 700-, 30- and 2-fold, respectively. Several tablet formulations were accomplished with this solid dispersion in combination with various ratios of HPMC/ethylcellulose. The release behaviour and pharmacokinetic studies in beagle dogs were assessed compared with the commercial prolonged release capsule. A decrease in HPMC/ethylcellulose ratios reduced the dissolution of tacrolimus from the tablets. Particularly, the tacrolimus-loaded prolonged release tablet consisting of fast-dissolving tacrolimus solid dispersion, HPMC, ethylcellulose and talc at the weight ratio of 20:66:112:2 exhibited a dissolution profile similar to that produced by the commercial prolonged release capsule. Furthermore, there were no significant differences in the AUC, Cmax, Tmax and MRT values between them in beagle dogs. Consequently, this tacrolimus-loaded prolonged release tablet might be bioequivalent to the tacrolimus-loaded commercial capsule. PMID:24388864

Cho, Jung Hyun; Kim, Yong-Il; Kim, Dong-Wuk; Yousaf, Abid Mehmood; Kim, Jong Oh; Woo, Jong Soo; Yong, Chul Soon; Choi, Han-Gon

2014-04-11

355

Tablets for Timely Design Documentation  

NSDL National Science Digital Library

One of the biggest challenges we have experienced in supervising digital systems senior design projects is the quality and completeness of the individual lab notebooks. Of the five outcomes we continuously track for this capstone course, the lab notebooks have consistently received the lowest quantitative scores. A significant improvement was achieved three years ago when we transitioned from carbon paper and pen notebooks to on-line (HTML) notebooks. Many teams took advantage of (and put to good use) the ability to post digital pictures of prototyping setups, provide hyperlinks to all their device datasheets, post their latest schematics and software listings for evaluation, and post video clips of their project in action (as verification of their project success criteria). The primary drawback has been the need for students to be in front of a networked computer to make lab notebook entries; consequently, the notebook updates still tended to be done in spurts (typically after the fact) rather than in real time. Project work (and inspiration), in fact, does not always occur in a lab setting, where networked computers are readily available, nor does it occur when all team members are working in the same physical location. Our hypothesis is that equipping each project team with wireless Tablet PCs should not only significantly improve the spontaneity (and regularity) with which the on-line lab notebooks are updated, but also facilitate collaboration among team members working on the design project at different locations. An HP Technology for Teaching Grant has provided a critical mass of Tablet PCs to test this hypothesis. A description of how the equipment provided is being utilized, along with a discussion of the preliminary results obtained, is presented in this paper.

Brown, Cordelia; Johnson, Mark; Meyer, David

2009-08-25

356

Comparative evaluation of silicified microcrystalline cellulose II as a direct compression vehicle.  

PubMed

The powder flow and tableting properties of novel silicified microcrystalline cellulose II (SMCCII) were evaluated and compared with current silicified cellulosic I excipients such as ProSolv(®) SMCC50 and ProSolv(®) SMCC90. This excipient was prepared by coprocessing cellulose II and silicon dioxide (SiO(2)) at a 95:5 ratio by spray drying. The novel SMCCII yielded more benefits in terms of functionality as compared with the parent cellulose II material. SMCCII had higher bulk and tap densities, better powder packing ability, reduced porosity, increased surface area, and increased flowability. This silicified excipient had the highest brittleness behavior as given by the Heckel, Leuenberger and brittle fracture index analyses. The mechanical properties of SMCCII, such as toughness and Young's modulus were comparable to those of commercial products. SMCCII was the least sensitive material to magnesium stearate, and blending time or reprocessing did not affect its compactibility. It also provided for the fastest compact disintegration and release of griseofulvin. This new material has the potential for use as a direct compression excipient. PMID:21708237

Rojas, John; Kumar, Vijay

2011-09-15

357

Investigation of excipient type and level on drug release from controlled release tablets containing HPMC.  

PubMed

The purpose of this study was to investigate the influence of excipient type and level on the release of alprazolam formulated in controlled release matrix tablets containing hydroxypropyl methylcellulose (HPMC). Each tablet formulation contained alprazolam, HPMC (Methocel K4MP), excipients, and magnesium stearate. The soluble excipients investigated were lactose monohydrate, sucrose, and dextrose, and the insoluble excipients included dicalcium phosphate dihydrate, dicalcium phosphate anhydrous, and calcium sulfate dihydrate. The similarity factor (f2 factor) was used to compare the dissolution profile of each formulation. The insoluble excipients, especially dicalcium phosphate dihydrate, caused the drug to be released at a slower rate and to a lesser extent than the soluble excipients. Soluble excipients created a more permeable hydrated gel layer for drug release, increased the porosity resulting in faster diffusion of drug, and increased the rate of tablet erosion. Use of binary mixtures of lactose monohydrate and dicalcium phosphate dihydrate produced release profiles of intermediate duration. Rapid drug dissolution was obtained when only 9.1% w/w of lactose monohydrate was present in the tablet formulation. Only when the dicalcium phosphate dihydrate level was sufficiently high (36.5% w/w) was the release rate and extent decreased. It was demonstrated that the type and level of excipient influenced the rate and extent of drug release from controlled release tablets containing HPMC. The release mechanism of alprazolam from each tablet formulation was described by either the Hixson-Crowell cube root kinetics equation or Peppas's equation. However, the different excipient types investigated did not influence the release mechanism of alprazolam from the final tablets. PMID:12066573

Williams, Robert O; Reynolds, Thomas D; Cabelka, Tim D; Sykora, Matthew A; Mahaguna, Vorapann

2002-05-01

358

Tablet formulation studies on an oxcarbazepine-beta cyclodextrin binary system.  

PubMed

Oxcarbazepine is a poorly water-soluble (0.083 mg/ml) anti-epileptic drug according to the BCS system (class II) and its dissolution is rate-limiting step for its absorption. The objective of this work was to develop tablet formulations of oxcarbazepine-beta-cyclodextrin (OX-beta-CD) binary systems. Three types of binary systems--physical mixtures, kneaded systems, and coevaporated systems--were studied. Phase solubility studies indicated 1:1 M complexation of oxcarbazepine with beta-cyclodextrin. Drug-beta-CD binary systems were prepared at 1:1 molar ratios and used in formulation studies. The dissolution properties of OX-beta-CD KS (kneaded system, 100.10% drug release in 15 min) were superior than those of the other binary system and pure oxcarbazepine. The tablet formulations containing drug-beta-CD binary systems prepared by wet granulation and direct compression showed superior dissolution properties when compared with the formulations of the corresponding pure drug formulations. Tablet formulations containing drug-beta-CD binary systems prepared by the kneading method showed good dissolution properties (100% drug release in 15 min in direct compression method and 99.9% drug release in 20 min in wet granulation method). Overall, the dissolution properties of tablet formulations prepared by the direct compression method were superior to those of tablets prepared by the wet granulation method. Accelerated stability studies on some selected tablet formulations were also conducted by keeping the samples at 40 +/- 2 degrees C and 75% relative humidity. There were no statistical differences in the percentage of drug dissolved at 15 and 20 min between fresh and stored samples at the different time points (P < 0.05). Drug content also remained within acceptable limits. Thus, drug-beta-CD binary systems are useful in developing tablet formulations of oxcarbazepine with improved dissolution properties. PMID:18468386

Patel, N V; Chotai, N P; Patel, M P

2008-04-01

359

A new brittleness index for compacted tablets.  

PubMed

A dimensionless index that quantifies the brittle or ductile character of tablets is presented. The work of failure (WOF) of crushed or broken flat tablets is calculated by numerical integration of the force-displacement measurement in a flexure tester. The ratio between WOF and the crushing force (F) corrected for the diameter of the tablet (D) is proposed to express the brittle/ductile index (BDI). [Formula: see text] This dimensionless index quantitatively denotes the brittle/ductile character of the compacted material as the normalized deformation in percentage of a cylindrical tablet at the breaking point. For ideal brittle materials, the BDI value will be 0 and for complete plastic deformation, that is, a total compression of the tablet without fracture, BDI will be 100. The validity and discriminative power is demonstrated on mixtures of microcrystalline cellulose and lactose. The robust measure of brittleness with an acceptable accuracy is obtained with only a minor influence of the tablet diameter and the speed of platen. PMID:24258281

Sonnergaard, Jørn M

2013-12-01

360

Producing Magnesium Metallic Glass By Disintegrated Melt Deposition  

NASA Astrophysics Data System (ADS)

Bulk metallic glasses are new class of engineering materials that exhibit high resistance to crystallization in the under cooled liquid state. The development of bulk metallic glasses of thickness 1cm or less has opened new doors for fundamental studies of both liquid state and glass transition previously not feasible in metallic materials. Moreover, bulk metallic glasses exhibit superior hardness, strength, specific strength, and elastic strain limit, along with good corrosion and wear resistance. Thus they are potential candidates in various sports, structural, engineering and medical applications. Among several BMGs investigated, magnesium-based BMGs have attracted considerable attention because of their low density and superior mechanical properties. The major drawback of this magnesium based BMGs is poor ductility. This can be overcome by the addition of ductile particles/reinforcement to the matrix. In this study, a new technique named disintegrated melt deposition technique was used to synthesize magnesium based BMGs. Rods of different sizes are cast using the current method. Mechanical characterization studies revealed that the amorphous rods produced by the current technique showed superior mechanical properties.

Shanthi, M.; Gupta, M.; Jarfors, A. E. W.; Tan, M. J.

2011-01-01

361

Muon induced deuteron disintegration in three-dimensions  

NASA Astrophysics Data System (ADS)

We present a three-dimensional (3D) description of muon induced deuteron disintegration. This reaction is treated as the decay of the muonic atom with the muon initially on the lowest K shell. Our aim is to calculate the total and differential decay rates. We work in momentum space and use 3D momentum eigenstates directly. This approach allowed us to calculate the appropriate nuclear matrix elements, necessary building blocks for the differential decay rate, in a single step. For contrast - in classical calculations many partial-waves have to be taken into account. We achieved a very good agreement between the 3D and partial-wave methods for calculations that involve single-nucleon currents. Our result for the total decay rate is also in agreement with experimental values, though these are not very precise. This success motivates us to also include two-nucleon current contributions that include the meson exchange currents. Additionally, our formalism can also be applied to other, so far poorly described, processes like: ? +3 He? ? + n + d or ? +3 He ? ? + n + n + p.

Topolnicki, Kacper; Golak, Jacek; Skibi?ski, Roman; Marcucci, Laura Elisa; Wita?a, Henryk; Eldeen Elmeshneb, Alaa

2014-11-01

362

Identity, Rationality, and Emotion in the Processes of State Disintegration and Reconstruction  

E-print Network

I wish to address both a substantive and a methodological issue in this chapter. Substantively, I will discuss the process of state disintegration and reconstruction. Here, I will draw on the experience of Eastern Europe ...

Petersen, Roger D.

363

Evidence for Sub-Glacial Particle Deformation Capable of Inducing Accelerated Glacial Disintegration  

E-print Network

Disintegration by Jamie Beaulieu Credit: Untipografico #12;Background · The Laurentide Ice Sheet ­ Covered 16 in an attempt to reduce the influence of differing material hardness. ­ Granite Heights and Bald Mountain

Jackson, Daniel R.

364

Visual deficits in a patient with `kaleidoscopic disintegration of the visual world'  

E-print Network

Visual deficits in a patient with `kaleidoscopic disintegration of the visual world' L. M. Vainaa and a failure to `pull objects together into a whole.' She described her condition as a `kaleidoscopic disinteg

Vaina, Lucia M.

365

Functional disintegration in paranoid schizophrenia using resting-state fMRI  

Microsoft Academic Search

Functional disintegration has been observed in schizophrenia during task performance. We sought to investigate functional disintegration during rest because an intrinsic functional brain organization, including both “task-negative” (i.e., “default mode”) and “task-positive” networks, has been suggested to play an important role in integrating ongoing information processing. Additionally, the brain regions that are involved in the intrinsic organization are believed to

Yuan Zhou; Meng Liang; Lixia Tian; Kun Wang; Yihui Hao; Haihong Liu; Zhening Liu; Tianzi Jiang

2007-01-01

366

Effects of chemical sludge disintegration on the performances of wastewater treatment by membrane bioreactor.  

PubMed

A new wastewater treatment process combining a membrane bioreactor (MBR) with chemical sludge disintegration was tested in bench scale experiments. In particular, the effects of the disintegration treatment on the excess sludge production in MBR were investigated. Two MBRs were operated. In one reactor, a part of the mixed liquor was treated with NaOH and ozone gas consecutively and was returned to the bioreactor. The flow rate of the sludge disintegration stream was 1.5% of the influent flow rate. During the 200 days of operation, the MLSS level in the bioreactor with the disintegration treatment was maintained relatively constant at the range of 10,000-11,000 mg/L while it increased steadily up to 25,000 mg/L in the absence of the treatment. In the MBR with the sludge disintegration, relatively constant transmembrane pressures (TMPs) could be maintained for more than 6 months while the MBR without disintegration showed an abrupt increase of TMP in the later phase of the operation. In conclusion, a complete control of excess sludge production in the membrane-coupled bioreactor was possible without significant deterioration of the treated water quality and membrane performances. PMID:17451782

Oh, Young-Khee; Lee, Ki-Ryong; Ko, Kwang-Baik; Yeom, Ick-Tae

2007-06-01

367

Evaluation of monolithic osmotic tablet system for nifedipine delivery in vitro and in vivo.  

PubMed

The aim of this study was to evaluate the monolithic osmotic tablet system (MOTS) containing a solid dispersion with the practically water-insoluble drug nifedipine in vitro and in vivo. In the drug release study in vitro, the release profiles of this system had almost zero-order kinetics. The influences of tablet formulation variables, sizes of the delivery orifice, membrane variables, and values of pH in the dissolution medium on nifedipine release from MOTS have been investigated. The results provided evidence that the tablet core played an important role in MOTS. While orifice sizes and membrane variables affected the nifedipine release rate, MOTS was independent of the dissolution medium. The appropriate orifice size was found to be in the range of 0.5-1.0 mm. The coating membrane incorporating hydrophilic polyethylene glycol (PEG) formed a porous structure. The human pharmacokinetics and relative bioavailability of MOTS containing nifedipine were compared with a commercial Adalat osmotic tablet system containing an equivalent dose of nifedipine following an oral single dose of 30 mg given to each of 11 healthy volunteers in an open, randomized crossover study in vivo. The relative bioavailability for MOTS was 112%. There was no statistically significant difference in the pharmacokinetic parameters between two dosage forms. It is concluded that the monolithic osmotic tablet controlled release system is feasible for a long-acting preparation as a once-daily treatment. PMID:12906339

Liu, Xing; Chen, Dawei; Zhang, Ruhua

2003-08-01

368

Formulation and optimisation of raft-forming chewable tablets containing H2 antagonist  

PubMed Central

Purpose: The purpose of this research work was to formulate raft-forming chewable tablets of H2 antagonist (Famotidine) using a raft-forming agent along with an antacid- and gas-generating agent. Materials and Methods: Tablets were prepared by wet granulation and evaluated for raft strength, acid neutralisation capacity, weight variation, % drug content, thickness, hardness, friability and in vitro drug release. Various raft-forming agents were used in preliminary screening. A 23 full-factorial design was used in the present study for optimisation. The amount of sodium alginate, amount of calcium carbonate and amount sodium bicarbonate were selected as independent variables. Raft strength, acid neutralisation capacity and drug release at 30 min were selected as responses. Results: Tablets containing sodium alginate were having maximum raft strength as compared with other raft-forming agents. Acid neutralisation capacity and in vitro drug release of all factorial batches were found to be satisfactory. The F5 batch was optimised based on maximum raft strength and good acid neutralisation capacity. Drug–excipient compatibility study showed no interaction between the drug and excipients. Stability study of the optimised formulation showed that the tablets were stable at accelerated environmental conditions. Conclusion: It was concluded that raft-forming chewable tablets prepared using an optimum amount of sodium alginate, calcium carbonate and sodium bicarbonate could be an efficient dosage form in the treatment of gastro oesophageal reflux disease. PMID:23580933

Prajapati, Shailesh T; Mehta, Anant P; Modhia, Ishan P; Patel, Chhagan N

2012-01-01

369

Formulation and evaluation of sustained release matrix tablet of rabeprazole using wet granulation technique  

PubMed Central

Introduction: Rabeprazole, a member of substituted benzimidazoles, inhibits the final step in gastric acid secretions. This drug claims to cause fastest acid separation (due to higher pKa), and more rapidly converts to the active species to aid gastric mucin synthesis. The most significant pharmacological action of Rabeprazole is dose dependent suppression of gastric acid secretion; without anticholinergic or H2-blocking action. It completely abolishes the hydrochloric acid secretion as it is powerful inhibitor of gastric acid. Rabeprazole is acid labile and hence commonly formulated as an enteric coated tablet. The absorption of rabeprazole occurs rapidly as soon as tablet leaves the stomach. Aim: In the present study an attempt was made to formulate and evaluate Rabeprazole sustained release matrix tablet using wet granulation technique incorporating various polymers like HPMC-E15, Carbopol934, and sodium carboxymethyl cellulose (CMC). Materials and Methods: The Formulated tablets were evaluated for different physicochemical properties like rheological properties, weight variation, thickness, hardness, % friability, in vitro release studies and drug content. Results: Studies revealed that all the physicochemical parameters comply with the official standards. The in vitro release studies exhibits the release up to 90%, over a prolonged period of time which confirms the extended release profile of formulation, having better bioavailability as well as decreased dosing frequency with reduced doses. Conclusion: The sustained release matrix tablets of rabiprazole shown better bioavailability, efficacy and potency, when compared with official standards. PMID:25035637

Khan, Ruqaiyah; Ashraf, Md Shamim; Afzal, Muhammad; Kazmi, Imran; Jahangir, Mohammed Asadullah; Singh, Rajbala; Chandra, Ramesh; Anwar, Firoz

2014-01-01

370

Angular circulation speed of tablets in a vibratory tablet coating pan.  

PubMed

In this work, a single tablet model and a discrete element method (DEM) computer simulation are developed to obtain the angular circulation speed of tablets in a vibratory tablet coating pan for range of vibration frequencies and amplitudes. The models identify three important dimensionless parameters that influence the speed of the tablets: the dimensionless amplitude ratio (a/R), the Froude number (a?2/g), and the tablet-wall friction coefficient, where a is the peak vibration amplitude at the drum center, ? is the vibration angular frequency, R is the drum radius, and g is the acceleration due to gravity. The models predict that the angular circulation speed of tablets increases with an increase in each of these parameters. The rate of increase in the angular circulation speed is observed to decrease for larger values of a/R. The angular circulation speed reaches an asymptote beyond a tablet-wall friction coefficient value of about 0.4. Furthermore, it is found that the Froude number should be greater than one for the tablets to start circulating. The angular circulation speed increases as Froude number increases but then does not change significantly at larger values of the Froude number. Period doubling, where the motion of the bed is repeated every two cycles, occurs at a Froude number larger than five. The single tablet model, although much simpler than the DEM model, is able to predict the maximum circulation speed (the limiting case for a large value of tablet-wall friction coefficient) as well as the transition to period doubling. PMID:23325382

Kumar, Rahul; Wassgren, Carl

2013-03-01

371

Perivascular microglia promote blood vessel disintegration in the ischemic penumbra.  

PubMed

The contribution of microglia to ischemic cortical stroke is of particular therapeutic interest because of the impact on the survival of brain tissue in the ischemic penumbra, a region that is potentially salvable upon a brain infarct. Whether or not tissue in the penumbra survives critically depends on blood flow and vessel perfusion. To study the role of microglia in cortical stroke and blood vessel stability, CX3CR1(+/GFP) mice were subjected to transient middle cerebral artery occlusion and then microglia were investigated using time-lapse two-photon microscopy in vivo. Soon after reperfusion, microglia became activated in the stroke penumbra and started to expand cellular protrusions towards adjacent blood vessels. All microglia in the penumbra were found associated with blood vessels within 24 h post reperfusion and partially fully engulfed them. In the same time frame blood vessels became permissive for blood serum components. Migration assays in vitro showed that blood serum proteins leaking into the tissue provided molecular cues leading to the recruitment of microglia to blood vessels and to their activation. Subsequently, these perivascular microglia started to eat up endothelial cells by phagocytosis, which caused an activation of the local endothelium and contributed to the disintegration of blood vessels with an eventual break down of the blood brain barrier. Loss-of-microglia-function studies using CX3CR1(GFP/GFP) mice displayed a decrease in stroke size and a reduction in the extravasation of contrast agent into the brain penumbra as measured by MRI. Potentially, medication directed at inhibiting microglia activation within the first day after stroke could stabilize blood vessels in the penumbra, increase blood flow, and serve as a valuable treatment for patients suffering from ischemic stroke. PMID:25500713

Jolivel, Valérie; Bicker, Frank; Binamé, Fabien; Ploen, Robert; Keller, Stefanie; Gollan, René; Jurek, Betty; Birkenstock, Jérôme; Poisa-Beiro, Laura; Bruttger, Julia; Opitz, Verena; Thal, Serge C; Waisman, Ari; Bäuerle, Tobias; Schäfer, Michael K; Zipp, Frauke; Schmidt, Mirko H H

2015-02-01

372

Tablets and E-Readers May Disrupt Your Sleep  

MedlinePLUS

... on this page, please enable JavaScript. Tablets and E-readers May Disrupt Your Sleep Light from these ... HealthDay News) -- People who receive a tablet or e-book reader for the holidays might wind up ...

373

21 CFR 529.400 - Chlorhexidine tablets and suspension.  

Code of Federal Regulations, 2014 CFR

... —(1) Amount. Place 1 or 2 tablets deep in each uterine horn; or infuse a solution of 1 tablet disolved in an appropriate amount of clean boiled water; or infuse one syringe of suspension into the uterus. (2) Indications for...

2014-04-01

374

SANCTUARY : asymmetric interfaces for game-based tablet learning  

E-print Network

This thesis describes the production of Sanctuary, a multiplayer learning game to be played on two tablet computers. Sanctuary's principle innovation is the splitting of the user interface onto two tablets, separating ...

Haas, Jason M. (Jason Matthew)

2013-01-01

375

Instructor Use of Tablet PCs in a College Pre-Calculus Course: Implementation & Assessment  

ERIC Educational Resources Information Center

A group of six math instructors used tablet PCs to teach their individual sections of a high enrollment gateway Pre-Calculus course in a diverse urban four-year college. Student performance in the experimental sections were compared to those in 31 other sections in terms of student retention, pass rates, and score on the department-wide…

Connelly Stockton, Julianna; Gregory, Peter

2012-01-01

376

[Formulation of calcium carbonate tablets with various binding substances].  

PubMed

The test results of calcium carbonate tablets, made of different binding substances (microcrystal cellulose, gelatin, 7pp sodium carboxymethylcellulose and starch) were presented. The content of calcium-carbonate in tablets as well as varying, solidity, prodigality and aptness to decay was determined. The best properties were observed in tablets made with starch. PMID:9214090

Gazikalovi?, E; Obrenovi?, D; Nidzovi?, Z; Toski?-Radojici?, M

1996-01-01

377

21 CFR 520.1720a - Phenylbutazone tablets and boluses.  

Code of Federal Regulations, 2010 CFR

...055246 for use of 100-mg tablets in dogs. (5) No. 000143 for use of 1-g tablets in horses. (6) No. 058829 for use of 100-mg or 1-g tablets in dogs and horses, or 1-g...amended at 74 FR 1146, Jan. 12,...

2010-04-01

378

Design of Sustained Release Tablet Containing Fucoidan.  

PubMed

The study introduced a new therapeutic agent,fucoidan, which can offer potential medical treatments including anti-inflammatory and anti-coagulant activities, as well as anti-proliferative effects on cancer cells. Fucoidan was included in sustained release formulations expected for aneffective plasma drug concentration for approximately 24 h. The matrices based on the two polymers hydroxypropylmethycellulose (HPMC) and polyethylene oxide (PEO) were prepared with various ratios between the polymers and fucoidan. The dissolution profiles of various matrix tablets performed in enzyme-free simulated intestinal fluid (pH 6.8) for 24 h indicated a higher potential of PEO-based matrix tablets in sustaining release of fucoidan. The swelling and erosion of the tablets were also characterized to elucidate the difference among those dissolution profiles. PMID:25382179

Tran, Thao Truong-Dinh; Ngo, Dai Kieu-Phuong; Vo, Toi Van; Tran, Phuong Ha-Lien

2014-11-01

379

Evaluation of the performance characteristics of bilayer tablets: Part II. Impact of environmental conditions on the strength of bilayer tablets.  

PubMed

Ambient air humidity and temperature are known to influence the mechanical strength of tablets. The objective of this work is to understand the influence of processing parameters and environmental conditions (humidity and temperature) on the strength of bilayer tablets. As part of this study, bilayer tablets were compressed with different layer ratios, dwell times, layer sequences, material properties (plastic and brittle), first and second layer forces, and lubricant concentrations. Compressed tablets were stored in stability chambers controlled at predetermined conditions (40C/45%RH, 40C/75%RH) for 1, 3, and 5 days. The axial strength of the stored tablets was measured and a statistical model was developed to determine the effects of the aforementioned factors on the strength of bilayer tablets. As part of this endeavor, a full 3?×?2(4) factorial design was executed. Responses of the experiments were analyzed using PROC GLM of SAS (SAS Institute Inc, Cary, North Carolina, USA). A model was fit using all the responses to determine the significant interactions (p?tablets. For Avicel-lactose and lactose-Avicel tablets, tablet strength decreased with the increasing humidity and storage time. But for lactose-lactose tablets, due to the formation of solid bridges upon storage, an increase in tablet strength was observed. Significant interactions were observed between processing parameters and storage conditions on the strength of bilayer tablets. PMID:22965660

Kottala, Niranjan; Abebe, Admassu; Sprockel, Omar; Bergum, James; Nikfar, Faranak; Cuitiño, Alberto M

2012-12-01

380

Soy polysaccharide as a novel superdisintegrant in sildenafil citrate sublingual tablets: preparation, characterization, and in vivo evaluation  

PubMed Central

Sildenafil citrate (SC), a drug used to treat erectile dysfunction, is available in tablet form but has three major problems. First, the drug displays inadequate aqueous solubility, which delays the onset of its action. Second, the drug undergoes extensive first-pass metabolism, resulting in a low (40%) bioavailability. Third, the gastrointestinal effects of SC include dyspepsia and a burning sensation. The aim of this research was to prepare SC as a sublingual tablet utilizing soy polysaccharide as novel superdisintegrant to mitigate the abovementioned problems. The solubility of SC in various hydrophilic carrier solutions was estimated in order to prepare the drug as a coprecipitate. Sublingual tablets were prepared and evaluated for hardness, friability, drug content, wetting time, water absorption ratio, in vitro dispersion time, dissolution rate, and stability study. The pharmacokinetic study of the tablets was carried out on healthy volunteers. The results indicated that the co-precipitation of SC with polyvinylpyrollidone K30 enhanced the solubility of SC by more than eight folds. The tablet contained 8% soy polysaccharide as a superdisintegrant and provided a wetting time of 25 seconds, and in vitro dispersion times of 55 seconds. The drug release was found to be 95.6%. The prepared SC sublingual tablet also exhibited a rapid onset of action, and its bioavailability was enhanced 1.68-fold compared with that of the marketed tablets. It can be concluded that SC sublingual tablet is a promising formulation that results in higher solubility, faster dispersion and onset of action, higher release rate, and higher systemic bioavailability. PMID:25624751

Hosny, Khaled Mohamed; Mosli, Hisham Ahmed; Hassan, Ali Habiballah

2015-01-01

381

Soy polysaccharide as a novel superdisintegrant in sildenafil citrate sublingual tablets: preparation, characterization, and in vivo evaluation.  

PubMed

Sildenafil citrate (SC), a drug used to treat erectile dysfunction, is available in tablet form but has three major problems. First, the drug displays inadequate aqueous solubility, which delays the onset of its action. Second, the drug undergoes extensive first-pass metabolism, resulting in a low (40%) bioavailability. Third, the gastrointestinal effects of SC include dyspepsia and a burning sensation. The aim of this research was to prepare SC as a sublingual tablet utilizing soy polysaccharide as novel superdisintegrant to mitigate the abovementioned problems. The solubility of SC in various hydrophilic carrier solutions was estimated in order to prepare the drug as a coprecipitate. Sublingual tablets were prepared and evaluated for hardness, friability, drug content, wetting time, water absorption ratio, in vitro dispersion time, dissolution rate, and stability study. The pharmacokinetic study of the tablets was carried out on healthy volunteers. The results indicated that the co-precipitation of SC with polyvinylpyrollidone K30 enhanced the solubility of SC by more than eight folds. The tablet contained 8% soy polysaccharide as a superdisintegrant and provided a wetting time of 25 seconds, and in vitro dispersion times of 55 seconds. The drug release was found to be 95.6%. The prepared SC sublingual tablet also exhibited a rapid onset of action, and its bioavailability was enhanced 1.68-fold compared with that of the marketed tablets. It can be concluded that SC sublingual tablet is a promising formulation that results in higher solubility, faster dispersion and onset of action, higher release rate, and higher systemic bioavailability. PMID:25624751

Hosny, Khaled Mohamed; Mosli, Hisham Ahmed; Hassan, Ali Habiballah

2015-01-01

382

Enhanced bioavailability of buspirone hydrochloride via cup and core buccal tablets: formulation and in vitro/in vivo evaluation.  

PubMed

This work aims to prepare sustained release buccal mucoadhesive tablets of buspirone hydrochloride (BH) to improve its systemic bioavailability. The tablets were prepared according to 5×3 factorial design where polymer type was set at five levels (carbopol, hydroxypropyl methylcellulose, sodium alginate, sodium carboxymethyl cellulose and guar gum), and polymer to drug ratio at three levels (1:1, 2:1 and 3:1). Mucoadhesion force, ex vivo mucoadhesion time, percent BH released after 8 h (Q8h) and time for release of 50% BH (T(??%)) were chosen as dependent variables. Additional BH cup and core buccal tablets were prepared to optimize BH release profile and make it uni-directional along with the tablets mucoadhesion. Tablets were evaluated in terms of content uniformity, weight variation, thickness, diameter, hardness, friability, swelling index, surface pH, mucoadhesion strength and time and in vitro release. Cup and core formula (CA10) was able to adhere to the buccal mucosa for 8h, showed the highest Q8h (97.91%) and exhibited a zero order drug release profile. Pharmacokinetic study of formula CA10 in human volunteers revealed a 5.6 fold increase in BH bioavailability compared to the oral commercial Buspar® tablets. Conducting level A in vitro/in vivo correlation showed good correlation (r²=0.9805) between fractions dissolved in vitro and fractions absorbed in vivo. PMID:24412520

Kassem, Mohamed A A; Elmeshad, Aliaa N; Fares, Ahmed R

2014-03-10

383

Preparation and characterisation of Kolliphor® P 188 and P 237 solid dispersion oral tablets containing the poorly water soluble drug disulfiram.  

PubMed

The oral route of administration is the most common and preferred route of drug delivery due to its ease of administration, cost-effectiveness and flexibility in design. However, limited aqueous solubility of the active pharmaceutical ingredient can result in poor bioavailability, which is a major issue for the pharmaceutical industry. Increasing numbers of new drugs are falling into class II of the Biopharmaceutical Classification System (BCS), where they have a low solubility and high tissue permeability, meaning that bioavailability is solubility dependent. Here we demonstrate the development and characterisation of solid dispersion oral tablets, containing the poorly water-soluble drug disulfiram, prepared using both the hot melt and solvent evaporation methods and manufactured from two different polymers, Kolliphor(®) P 188 and P 237, specifically designed for the manufacture of solid dispersions. This paper demonstrates that the disulfiram solid dispersions tablets have an enhanced release rate of disulfiram compared to the control tablets. The Kolliphor(®) P 188 polymer control tablets released approximately 48.8% of their disulfiram content over 8h, with the solvent evaporated tablets releasing approximately 65.8%, while the 60 and 80 °C hot melt tablets released approximately 73.2 and 100% of their disulfiram content respectively. A similar trend was seen with Kolliphor(®) P 237 as the control tablets released approximately 50.5% of their disulfiram content over 8h, while the solvent evaporated tablets released approximately 79.5% and the 60 and 80 °C hot melt tablets released 100.2 and 100.3% respectively. Depending on what method and polymer is used to manufacture the solid dispersions the disulfiram is either maintained completely or partially in its amorphous state and it is this which enhances its solubility and release rate from the tablets. The disulfiram in the Kolliphor(®) P 188 solvent evaporated and 60 °C hot melt tablets retained 50.5 and 44.1% of its crystallinity, while the disulfiram in the 80 °C hot melt tablets was completely amorphous. Whereas the disulfiram in the Kolliphor(®) P 237 solvent evaporated tablets retained 45.2% crystallinity, while the disulfiram in both of the hot melt tablets was completely in its amorphous form. PMID:25218186

Ramadhani, Nisrina; Shabir, Mehwish; McConville, Christopher

2014-11-20

384

Miconazole mucoadhesive tablet for oropharyngeal candidiasis  

PubMed Central

Oropharyngeal candidiasis is a commonly encountered problem in daily clinical practice. Topical therapies for oropharyngeal candidiasis are considered preferable to systemic therapies in most patient populations. However, traditional topical therapies have limitations including short contact time with the oral mucosa and the need for multiple doses each day. Miconazole mucoadhesive tablet has recently been approved in Europe (Loramyc®) and the USA (Oravig™) for the treatment of oropharyngeal candidiasis. This tablet adheres to the oral mucosa and provides sustained local release of miconazole over a period of several hours with just one daily application. This article reviews the pharmacology, safety and efficacy of this novel agent. PMID:21171872

Lalla, Rajesh V; Bensadoun, René-Jean

2011-01-01

385

The ACTION study: a randomized, open-label, multicenter trial comparing once-a-day extended-release morphine sulfate capsules (AVINZA) to twice-a-day controlled-release oxycodone hydrochloride tablets (OxyContin) for the treatment of chronic, moderate to severe low back pain.  

PubMed

This large, open-label, randomized, parallel-group, multicenter study compared two oral sustained-release opioids (SROs)--AVINZA (A-MQD), morphine sulfate extended-release capsules given once a day, and OxyContin (O-ER), oxycodone modified-release tablets given twice a day--in SRO-naive subjects ages 30 to 70 with chronic, moderate to severe low back pain. Of the 392 subjects enrolled and randomized, 266 (132 in the A-MQD group and 134 in the O-ER group) completed the opioid dose titration phase and entered an eight-week evaluation phase. During the evaluation phase, A-MQD achieved significantly better pain control than O-ER, as demonstrated by a greater decrease from baseline in pain scores obtained four times daily during weeks one, four, and eight (p = 0.002). The number of breakthrough-pain rescue medication doses adjusted for the number of patient days was significantly lower in the A-MQD group (p < 0.0001). Better pain control with A-MQD was achieved with a significantly lower daily opioid dose than with O-ER (mean 69.9 mg and 91 mg morphine equivalents, respectively; p = 0.0125). Quality of sleep was significantly better with A-MQD for the entire evaluation phase (p = 0.0026). The incidence and severity of elicited opioid side effects were similar in the two groups. This trial demonstrated that once-daily A-MQD provides consistent around-the-clock pain relief in patients with low back pain. In patients who completed opioid dose titration, A-MQD was significantly better than O-ER for reducing pain and improving sleep, while requiring a lower daily opioid dose. PMID:17319449

Rauck, Richard L; Bookbinder, Stephen A; Bunker, Timothy R; Alftine, Christopher D; Ghalie, Richard; Negro-Vilar, Andres; de Jong, Egbert; Gershon, Steven

2006-01-01

386

Formulation and in vitro and in vivo evaluation of film-coated montelukast sodium tablets using Opadry® yellow 20A82938 on an industrial scale  

PubMed Central

Purpose: The aim of this study was to formulate stable film-coated montelukast sodium (MS) tablets using Opadry® yellow 20A82938 (Montikast® tablets) and to evaluate their in vitro and in vivo release profile. Methods: MS core tablets were manufactured using a direct compression method. Opadry yellow 20A82938 aqueous coating dispersion was used as the film-coating material. Dissolution of the film-coated tablets was tested in 900 mL of 0.5% sodium lauryl sulfate solution and the bioequivalence of the tablets was tested by comparing them with a reference formulation – Singulair® tablets. In vitro–in vivo correlation was evaluated. The stability of the obtained film-coated tablets was evaluated according to International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use guidelines. Results: The efficiency of the film coating was determined by subjecting the coated tablets to gastric pH and drug release was analyzed using high-performance liquid chromatography. The coated tablets had no obvious defects. MS release met the study criterion of not less than 80% dissolved after 30 minutes in 0.5% sodium lauryl sulfate solution. Statistical comparison of the main pharmacokinetic parameters clearly indicated no significant difference between test and reference in any of the calculated pharmacokinetic parameters. Level A correlation between in vitro drug release and in vivo absorption was found to be satisfactory. Conclusion: These findings suggest that aqueous film coating with Opadry yellow 20A82938 is an easy, reproducible, and economical approach for preparing stable MS film-coated tablets without affecting the drug-release characteristics. PMID:23430138

Zaid, Abdel Naser; Natour, Salam; Qaddomi, Aiman; Abu Ghoush, Abeer

2013-01-01

387

Effect of compression pressure, preservative, and storage with potassium chloride on the microbiological quality of tablets formulated with Terminalia randii Gum (Combretaceae).  

PubMed

Gums are used as binders in tablets and also as emulsion stabilisers, suspending agents and thickeners in syrups. The need for other natural gums apart from the conventional gums to be employed as binding agents in tablets formulation led to this study. A gum obtained from the incised trunk of Terminalia randii (Combretaceae) was evaluated for the effect of compression pressure, methyl paraben preservative and storage with potassium chloride, on the microbial load of tablets formulated with the gum. The microbial load was determined by surface spread method on the processed gum at suitable dilutions, and tablets formulated from the gum at different compression pressures. The formulated tablets were evaluated for microbial load, also when stored in potassium chloride for 8 and 12 weeks with and without preservation with 1% Methyl Paraben. In each case the compressed tablets were incubated in 0.1% peptone water as control. The microbial load recorded reflected generally, reduction in microbial counts in tablets formulated with the gum as a binder both in terms of compression at different pressures and when the different compression pressures were associated with or without 1% methyl paraben in the presence of potassium chloride. Comparatively, the processed gum showed higher microbial load than the pressure compressed tablets. Besides the different compression pressures, duration of storage was also found to cause reduction of microbial load, particularly in the formulated tablets compressed with methyl paraben stored in potassium chloride such that after 8 weeks, the microbial load was zero. The studies showed that compression pressures and duration of storage caused marked reduction in microbial load of the tablets formulated with the processed gum of Terminalia randii as a binder. PMID:23009993

Oluremi, Bolaji Bosede; Bamiro, Oluyemisi Adebowale; Idowu, Abel Olusola; Oduneye, Olayinka Annegret

2012-10-01

388

Sucrose esters with various hydrophilic-lipophilic properties: novel controlled release agents for oral drug delivery matrix tablets prepared by direct compaction.  

PubMed

Sucrose esters (SE) are esters of sucrose and fatty acids with various hydrophilic-lipophilic properties which have attracted interest from being used in pharmaceutical applications. This study aimed to gain insight into the use of SE as controlled release agents for direct compacted matrix tablets. The study focused on the effect of hydrophilic-lipophilic properties on tableting properties and drug release. Sucrose stearate with hydrophilic-lipophilic balance (HLB) values ranging from 0 to 16 was systematically tested. Tablet formulations contained SE, metoprolol tartrate as a highly soluble model drug and dibasic calcium phosphate dihydrate as a tablet formulation filler in the ratio 1:1:2. The compaction behaviour of matrix tablets was compared with the compacts of individual starting materials as reference. SE incorporation improved the plasticity, compressibility and lubricating property of powder mixtures. The hydrophilic-lipophilic properties of SE affected tableting properties, drug release rate and release mechanism. Increasing hydrophilicity corresponding to the increased monoesters in SE composition increased the relative porosity, elastic recovery and tensile strength of the tablets due to the increased hydrogen bonding between the monoesters. This also facilitated the swelling behaviour of SE, which sustained the drug release rate. A sustained release effect prevailed in tablets containing SE with HLB values of 3-16. The ability to improve the tableting properties as well as sustain the drug release rate of the highly soluble model drug via gelation of SE highlights SE as promising controlled release regulators for direct compacted matrix tablets comprising drugs with various solubilities according to the Biopharmaceutics Classification System. PMID:20132913

Chansanroj, K; Betz, G

2010-08-01

389

Design and evaluation of osmotic pump tablets of naproxen sodium.  

PubMed

Osmotic pump tablets (OPTs) deliver a constant, predetermined amount of drug in solution form over a fixed span of time, independent of external environmental conditions. OPTs of naxopren sodium (NPS) were made and evaluated with the principal aim of limiting the drug's frequently experienced gastrointestinal side effects, by preventing the undissolved drug from coming in to contact with the gastric mucosa. OPTs with and without the osmotic driving agent, sodium chloride (SCL), with different membrane thicknesses, and with and without an orifice were designed. In vitro release profiles of the OPTs, when compared to a conventional marketed tablet (Xenobid 275), were highly controlled and exhibited an almost perfect zero-order release pattern. The magnitudes of lag times and average release rates were found to depend on the amount of SCL present in the formulation which decreased the drug's solubility within the system. The release rates were found to be independent of stirring rate and decreased with increasing membrane thickness. Release profiles of the OPTs with and without an orifice were found to be comparable. PMID:11802660

Ramakrishna, N; Mishra, B

2001-12-01

390

Formulation and In Vitro Evaluation of Bilayer Tablets of Nebivolol Hydrochloride and Nateglinide for the Treatment of Diabetes and Hypertension  

PubMed Central

Diabetes mellitus (DM) and hypertension are two common diseases that often coexist. The most common cause of death in the diabetic patient is heart disease. In the present investigation we combine Nebivolol and Nateglinide for better patient compliance. IR layer was formulated using various superdisintegrants like Crospovidone, Croscarmellose sodium, and sodium starch glycolate and SR layer was formulated using polymers and gums like HPMC E15, ethyl cellulose, Gaur gum, and Xanthan gum. The disintegration and dissolution study of both layers showed that inclusion of surfactant (sodium lauryl sulphate) to the tablet formulation (IR) and dissolution medium (SR) enhanced the release of drugs from both layers. Kinetic studies of optimized IR layer (NBL8) and SR layer (N9) showed good linearity with regression coefficient of 0.9714 (Higuchi model) and 0.9931 (zero order kinetics), respectively. The above results reveal that the optimized IR layer of Nebivolol (NBL8) and SR layer of Nateglinide (N9) might be suitable for the treatment of diabetes and hypertension by sequential release of the two drugs in a bilayer tablet. IR-immediate release, SR-sustain release, NBL8-Nebivolol 8, N9-Nateglinide 9. PMID:25648606

Ryakala, Harika; Dineshmohan, S.; Ramesh, Alluri; Gupta, V. R. M.

2015-01-01

391

Dissolution of tablet-in-tablet formulations studied with ATR-FTIR spectroscopic imaging.  

PubMed

This work uses ATR-FTIR spectroscopic imaging to study the dissolution of delayed release and pH resistant compressed coating pharmaceutical tablets. Tablets with an inner core and outer shell were constructed using a custom designed compaction cell. The core of the delayed release tablets consisted of hydroxypropyl methylcellulose (HPMC) and caffeine. The shell consisted of microcrystalline cellulose (MCC) and glucose. The core of the pH resistant formulations was an ibuprofen and PEG melt and the shell was constructed from HPMC and a basic buffer. UV/vis spectroscopy was used to monitor the lag-time of drug release and visible optical video imaging was used as a complementary imaging technique with a larger field of view. Two delayed release mechanisms were established. For tablets with soluble shell sections, lag-time was dependent upon rapid shell dissolution. For tablets with less soluble shells, the lag-time was controlled by the rate of dissolution medium ingress through the shell and the subsequent expansion of the wet HPMC core. The pH resistant formulations prevented crystallization of the ibuprofen in the core during dissolution despite an acidic dissolution medium. FTIR imaging produced important information about the physical and chemical processes occurring at the interface between tablet sections during dissolution. PMID:23291036

Wray, Patrick S; Clarke, Graham S; Kazarian, Sergei G

2013-03-12

392

Treatment of vulvovaginal candidiasis with a 500-mg vaginal tablet of clotrimazole.  

PubMed

A prospective, randomized, double-blind trial compared the efficacy and safety of a new one-dose clotrimazole regimen and placebo. Twenty-six patients with clinically and mycologically proven vulvovaginal candidiasis received either a 500-mg tablet of clotrimazole or a placebo. Follow-up visits were performed approximately one week and one month after treatment. Efficacy was evaluated in 23 patients. There was a highly significant difference in clinical and mycological responses to the two regimens (P = 0.0001, Fisher's exact test). Nine (90%) of the ten patients in the clotrimazole group showed mycological and clinical clearance of infection one month after treatment, while all 13 patients who had received placebo were classified as treatment failures at the first follow-up visit and were dropped from the study at this point. No patients experienced adverse effects attributable to clotrimazole or the placebo. The findings indicate that a single 500-mg tablet of clotrimazole is effective and safe in the treatment of vaginal candidiasis and suggest that the efficacy and safety of the one-dose regimen are comparable to those of more prolonged courses with the 100-mg tablet of clotrimazole. The convenient one-dose regimen promises to eliminate the widespread problem of patient noncompliance, especially when the tablet is inserted by the physician at the time of diagnosis. PMID:6383612

Hughes, D; Kriedman, T

1984-01-01

393

Fluid-loading solutions and plasma volume: Astro-ade and salt tablets with water  

NASA Technical Reports Server (NTRS)

Fluid loading with salt and water is a countermeasure used after space flight to restore body fluids. However, gastrointestinal side effects have been frequently reported in persons taking similar quantities of salt and water in ground-based studies. The effectiveness of the Shuttle fluid-loading countermeasure (8 gms salt, 0.97 liters of water) was compared to Astro-ade (an isotonic electrolyte solution), to maintain plasma volume (PV) during 4.5 hrs of resting fluid restriction. Three groups of healthy men (n=6) were studied: a Control Group (no drinking), an Astro-ade Group, and a Salt Tablet Group. Changes in PV after drinking were calculated from hematocrit and hemoglobin values. Both the Salt Tablet and Astro-ade Groups maintained PV at 2-3 hours after ingestion compared to the Control Group, which had a 6 percent decline. Side effects (thirst, stomach cramping, and diarrhea) were noted in at least one subject in both the Astro-ade and Salt Tablet Groups. Nausea and vomiting were reported in one subject in the Salt Tablet Group. It was concluded that Astro-ade may be offered as an alternate fluid-loading countermeasure but further work is needed to develop a solution that is more palatable and has fewer side effects.

Fortney, Suzanne M.; Seinmann, Laura; Young, Joan A.; Hoskin, Cherylynn N.; Barrows, Linda H.

1994-01-01

394

Graphics Tablet for the BBC Microcomputer.  

ERIC Educational Resources Information Center

Describes an inexpensive solution to the problem of transferring pictures onto a television screen using the analog part of the Model "B" BBC Microcomputer. Instruction for building the graphics tablet (which can easily be constructed by secondary students), program listing for required software, and documentation are included. (JN)

Whale, R.

1984-01-01

395

MEASUREMENT OF BOUNDARIES USING A DIGITIZER TABLET  

EPA Science Inventory

The perimeter is the most error prone of the primary measurements (length, perimeter and area) made when using a device such as a digitizer tablet to trace profiles on micrographs. o allow for minimization of this error an expression is developed relating the error in the perimet...

396

Touch Tablet Surprises: A Preschool Teacher's Story  

ERIC Educational Resources Information Center

A year and a half ago, Rena, Cheri, and Cassandra were introduced to each other by a colleague because they shared an interest in exploring the impact newer technologies have on learning in early childhood classrooms. They meet regularly to share ideas and information on how to incorporate tablets using best practices. Cassandra's preschool…

Shifflet, Rena; Toledo, Cheri; Mattoon, Cassandra

2012-01-01

397

Form recognition from ink strokes on tablet  

Microsoft Academic Search

This paper proposes a method for form recognition from handwritten input captured as digital ink on a tablet. Form recognition is an important step of form processing to read the data on a filled form. This type of recognition is different from traditional image matching (searching and retrieving) because the query image (data ink) has but few common characteristics with

De Cao Tran; Patrick Franco; Jean-Marc Ogier

2010-01-01

398

You May Now Open Your Test Tablets...  

ERIC Educational Resources Information Center

Tony Alpert, chief operating officer for the Smarter Balanced Assessment Consortium (SBAC), ponders whether to allow tablet computers--and particularly iPads--to be used for summative testing online. As Alpert points out, not only would student cheating compromise the validity of the individual student's test event, "worse yet, it could expose…

Schaffhauser, Dian

2012-01-01

399

21 CFR 520.1616 - Orbifloxacin tablets.  

Code of Federal Regulations, 2011 CFR

...CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1616 Orbifloxacin tablets...c) of this chapter. (c) Conditions of use in dogs and cats —(1) Amount . 2.5 to 7.5 mg per kilogram body...

2011-04-01

400

21 CFR 520.1900 - Primidone tablets.  

Code of Federal Regulations, 2011 CFR

...CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1900 Primidone tablets...species, as primidone appears to have a specific neurotoxicity in cats. Federal law restricts this drug to use by or on the order...

2011-04-01