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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.

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

2013-08-25

3

Formulation Design of Fast Disintegrating Tablets Using Disintegrant Blends  

PubMed Central

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, crospovidone (up to 3% w/w) and croscarmellose sodium (up to 5% w/w) in combination were used as superdisintegrants. Since disintegrants complement each other, accelerating the disintegration process when used together. Estimation of prochlorperazine maleate in the prepared tablet formulations was carried out by extracting the drug with methanol and measuring the absorbance at 254.5nm. The prepared formulations were further evaluated for hardness, friability, drug content uniformity, in vitro dispersion time, wetting time and water absorption ratio. Based on in vitro dispersion time (approximately 12 s), one promising formulation was tested for in vitro drug release pattern in phosphate buffer pH 6.8 and short-term stability (at 40°/70% RH for 3 mo), drug-excipient interaction (IR spectroscopy) were studied. Among the formulations tested, formulation DCPC4 containing 5% w/w of croscarmellose sodium and 3% w/w of crospovidone as superdisintegrant emerged as the overall best (t50% 7.0 min) based on drug release characteristics in pH 6.8 phosphate buffer compared to commercial conventional tablet formulation (t50% 17.4 min). Short-term stability studies on the promising formulation indicated that there were no significant changes in drug content and in vitro dispersion time (p<0.05).

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

2010-01-01

4

Guidance for Industry Orally Disintegrating Tablets.  

National Technical Information Service (NTIS)

This guidance provides pharmaceutical manufacturers of new and generic drug products with an Agency perspective on the definition of an orally disintegrating tablet (ODT)which is a different dosage form than, for example, a chewable tablet or a tablet tha...

2008-01-01

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.

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

2011-01-01

6

Dissolution testing of orally disintegrating tablets.  

PubMed

For industrially manufactured pharmaceutical dosage forms, product quality tests and performance tests are required to ascertain the quality of the final product. Current compendial requirements specify a disintegration and/or a dissolution test to check the quality of oral solid dosage forms. These requirements led to a number of compendial monographs for individual products and, at times, the results obtained may not be reflective of the dosage form performance. Although a general product performance test is desirable for orally disintegrating tablets (ODTs), the complexity of the release controlling mechanisms and short time-frame of release make such tests difficult to establish. For conventional oral solid dosage forms (COSDFs), disintegration is often considered to be the prerequisite for subsequent dissolution. Hence, disintegration testing is usually insufficient to judge product performance of COSDFs. Given the very fast disintegration of ODTs, the relationship between disintegration and dissolution is worthy of closer scrutiny. This article reviews the current status of dissolution testing of ODTs to establish the product quality standards. Based on experimental results, it appears that it may be feasible to rely on the dissolution test without a need for disintegration studies for selected ODTs on the market. PMID:22686339

Kraemer, Johannes; Gajendran, Jayachandar; Guillot, Alexis; Schichtel, Julian; Tuereli, Akif

2012-04-08

7

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

2013-03-13

8

Formulation study for lansoprazole fast-disintegrating tablet. III. Design of rapidly disintegrating tablets.  

PubMed

Lansoprazole fast-disintegrating tablets (LFDT) are a patient-friendly formulation that rapidly disintegrates in the mouth. LFDT consist of enteric-coated microgranules (mean particle size, approximately 300 microm) and inactive granules. In the design of the inactive granules, mannitol was used as a basic excipient. Microcrystalline cellulose, low-substituted hydroxypropyl cellulose (L-HPC), and crospovidone were used as binders and disintegrants. A new grade of L-HPC (L-HPC-33), with a hydroxypropoxy group content of 5.0-6.9%, was developed and it has no rough texture due to a decrease in water absorption. It was clarified that L-HPC-33 could be useful as a binder and disintegrant in rapidly disintegrating tablets. LFDT contain enteric-coated microgranules in tablet form. The enteric-coated microgranule content in LFDT affect qualities such as tensile strength, disintegration time in the mouth, and dissolution behavior in the acid stage and in the buffer stage of LFDT. The 47.4% content of the enteric-coated microgranules was selected to give sufficient tensile strength (not less than 30 N/cm(2)), rapid disintegration time in the mouth (not more than 30 s), and dissolution behavior in the acid stage and buffer stage similar to current lansoprazole capsules. Compression force affected the tensile strength and the disintegration time in the mouth, but did not affect the dissolution behavior in the acid and buffer stages. PMID:14519914

Shimizu, Toshihiro; Sugaya, Masae; Nakano, Yoshinori; Izutsu, Daisuke; Mizukami, Yoshio; Okochi, Kazuhiro; Tabata, Tetsuro; Hamaguchi, Naoru; Igari, Yasutaka

2003-10-01

9

Development of sildenafil-loaded orally disintegrating tablet with new lactate salt.  

PubMed

To develop a sildenafil lactate-loaded orally disintegrating tablet with a faster drug effect onset and immediate action of erection, the orally disintegrating tablets were prepared with various amounts of menthol and colloidal silica using the direct compression technique followed by vacuum drying. Their tablet properties such as friability, hardness, wetting time and disintegration time were investigated. The oral bioavailability of sildenafil in the orally disintegrating tablet was then compared with the sildenafil citrate-loaded commercial tablet (Viagra(®)) in rabbits. Sildenafil lactate was a new salt form with more improved solubility and alleviated bitterness compared with commercial salt, sildenafil citrate. As the amount of menthol in the orally disintegrating tablet increased, the friability increased and hardness decreased, resulting in a shorter wetting time and disintegration time. Colloidal silica did the opposite. The sildenafil lactate-loaded orally disintegrating tablet prepared with 45 mg/tab of menthol and 1.5 mg/tab of colloidal silica gave a hardness of 3-4 KP, friability less than 0.5% and disintegration time less than 30 s, suggesting that it was a practical and commercial product with good tablet property and excellent efficacy. Furthermore, it gave higher AUC and C(max), and shorter T(max) values than did the commercial tablet, indicating that it improved the oral bioavailability of sildenafil in rabbits compared with the commercial tablet. Thus, the sildenafil lactate-loaded orally disintegrating tablet might induce a fast onset of action and immediate erection compared with the sildenafil citrate-loaded commercial tablet. PMID:22010981

Jung, Si-Young; Kim, Dong-Wuk; Seo, Youn Gee; Woo, Jong Soo; Yong, Chul Soon; Choi, Han-Gon

2011-10-19

10

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

2013-03-19

11

Olanzapine orally disintegrating tablet: a review of efficacy and compliance.  

PubMed

Medication nonadherence, especially in psychiatric disorders, has been associated with treatment failure and other negative outcomes. Orally disintegrating formulations have been developed as an alternative to improve medication adherence. This report reviews the properties, efficacy, and safety profile of olanzapine as an orally disintegrating tablet, and explores their association with medication compliance compared with standard oral formulation. Medical literature, published on orally disintegrating formulation of olanzapine identified using Pubmed and EMBASE, was used. Additional references were identified from the reference lists of published articles. Bibliographical information, including contributory unpublished data, was also requested from the company developing the drug. Studies evaluating the biostability, biodisposability, pharmacokinetics, efficacy, and safety of orally disintegrating olanzapine as treatment of patients with psychiatric disorders were reviewed. Measurement tools included the Positive and Negative Syndrome Scale (PANSS), Clinical Global Impressions-Severity (CGI-S), Simpson-Angus Scale (SAS), Abnormal Involuntary Movement Scale, and Nursing Assessment of Medication Acceptance (NAMA). Orally disintegrating olanzapine, an effective atypical antipsychotic with an acceptable safety profile, can facilitate the burden of treatment on patients and caregivers due to its ease of administration. This is especially important in diseases such as schizophrenia and bipolar disorder, which can be chronic and require long-term treatment. PMID:18801113

San, Luis; Casillas, Marta; Ciudad, Antonio; Gilaberte, Inmaculada

2008-01-01

12

Fast disintegrating tablets: Opportunity in drug delivery system  

PubMed Central

Fast disintegrating tablets (FDTs) have received ever-increasing demand during the last decade, and the field has become a rapidly growing area in the pharmaceutical industry. Oral drug delivery remains the preferred route for administration of various drugs. Recent developments in the technology have prompted scientists to develop FDTs with improved patient compliance and convenience. 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. The popularity and usefulness of the formulation resulted in development of several FDT technologies. FDTs are solid unit dosage forms, which disintegrate or dissolve rapidly in the mouth without chewing and water. FDTs or orally disintegrating tablets provide an advantage particularly for pediatric and geriatric populations who have difficulty in swallowing conventional tablets and capsules. This review describes various formulations and technologies developed to achieve fast dissolution/dispersion of tablets in the oral cavity. In particular, this review describes in detail FDT technologies based on lyophilization, molding, sublimation, and compaction, as well as approaches to enhancing the FDT properties, such as spray drying and use of disintegrants. In addition, taste-masking technologies, experimental measurements of disintegration times, and dissolution are also discussed.

Parkash, Ved; Maan, Saurabh; Deepika; Yadav, Shiv Kumar; Hemlata; Jogpal, Vikas

2011-01-01

13

Plantago ovata Mucilage in the Design of Fast Disintegrating Tablets  

PubMed Central

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°/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 (t50% 3.3 min) based on the in vitro drug release characteristics compared to conventional commercial tablets formulation (t50% 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).

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

2009-01-01

14

Fast relief from migraine attacks using fast-disintegrating sublingual zolmitriptan tablets.  

PubMed

Zolmitriptan is a potent molecule for treatment of migraine. Its current oral therapies present drawbacks such as slow onset of action, low bioavailability and large inter-subject variability. Fast disintegrating sublingual zolmitriptan tablet (FDST) using freeze-drying technique has been developed to enhance tablet disintegration and dissolution with the intention of speeding drug absorption and onset of effect, hence mitigating the effects on the gastrointestinal dysmotility that typically accompanies the migraine attack. The FDSTs were prepared using different concentrations of gelatin as binder and mannitol or L-alanine as matrix supporting/disintegration enhancing agents. The effect of formulation variables on the physicochemical and solid-state properties, as well as the dissolution behaviour of the tablets, was studied. The formulated FDSTs disintegrated within 30 s and showed significantly faster dissolution rate of zolmitriptan compared to the zolmitriptan oral tablet. Tablet containing 2% gelatin and mannitol showed acceptable weight variation, drug content and friability values. Furthermore, it had a low in-vitro and in-vivo disintegration time (11 s) and it reached 100% of drug release within 30 s. This sublingual formulation gave faster and higher zolmitriptan plasma concentration in rabbits compared to the oral zolmetriptan market product. Zolmitriptan FDST may therefore constitute an advance in the management of acute migraine attacks. PMID:22023340

Mahmoud, Azza A; Salah, Salwa

2011-10-24

15

Design and evaluation of taste masked dextromethorphan hydrobromide oral disintegrating tablets.  

PubMed

The present study is aimed to develop dextromethorphan hydrobromide (DXM) oral disintegrating tablets (ODT) with acceptable palatability to help patients of all age groups. The bitter taste of the drug was masked by binding the drug to ion exchange resin. The effect of the particle size of resin on drug loading was studied. In vitro and in vivo disintegration time and in vitro drug release studies were performed. Drug loading increased significantly with a decrease in the particle size of the resin. DSC and XRPD studies reveal that the molecular state of the drug changed from crystalline to amorphous form. The dissolution efficiency calculated for optimized ODT and conventional directly compressed tablet were almost comparable, indicating free dissociation of the drug from the resinate. The bitter taste of DXM can be masked by binding with ion exchange resin and the resinate can be successfully formulated into oral disintegrating tablets. PMID:21134862

Malladi, Madhusudhan; Jukanti, Raju; Nair, Rashmi; Wagh, Sanjay; Padakanti, Hari Shanker; Mateti, Ashok

2010-09-01

16

Further improvement of orally disintegrating tablets using micronized ethylcellulose.  

PubMed

The aim of this study is to design a new orally disintegrating tablet (ODT) containing micronized ethylcellulose (MEC). The new ODT was prepared by physical mixing of rapidly disintegrating granules (RDGs) with MEC. To obtain RDGs, mannitol was spray-coated with a suspension of corn starch and crospovidone (9:1, w/w ratio) using a fluidized-bed granulator (suspension spray-coating method). The new ODTs were evaluated for their hardness, friability, thickness, internal structure (X-ray-CT scanning), in vivo disintegration time, and water absorption rate. Since MEC increases tablet hardness by increasing the contact frequency between the granules, the new ODTs could obtain high hardness (>50 N) and low friability (<0.5 %) with relatively low compression force. In addition, fine capillary channels formed in ODTs facilitated the wicking action and enabled rapid disintegration in vivo (<30 s). On the other hand, since MEC has low hygroscopicity, the tablet hardness of ODTs containing MEC remained high for 1 month in high-humidity conditions. In conclusion, the new ODTs containing MEC developed in this study possessed superior properties for clinical use and are expected to be applied for a wide range of functionally released drugs for bitter taste masking, sustained release, and controlled release (pH-dependent film coating, matrix, and microcapsule). PMID:22138608

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

2011-11-26

17

Disintegration of highly soluble immediate release tablets: a surrogate for dissolution.  

PubMed

The purpose of the work was to investigate correlation between disintegration and dissolution for immediate release tablets containing a high solubility drug and to identify formulations where disintegration test, instead of the dissolution test, may be used as the acceptance criteria based on International Conference on Harmonization Q6A guidelines. A statistical design of experiments was used to study the effect of filler, binder, disintegrating agent, and tablet hardness on the disintegration and dissolution of verapamil hydrochloride tablets. All formulation variables, i.e., filler, binder, and disintegrating agent, were found to influence tablet dissolution and disintegration, with the filler and disintegrating agent exerting the most significant influence. Slower dissolution was observed with increasing disintegration time when either the filler or the disintegrating agent was kept constant. However, no direct corelationship was observed between the disintegration and dissolution across all formulations due to the interactions between different formulation components. Although all tablets containing sodium carboxymethyl cellulose as the disintegrating agent, disintegrated in less than 3 min, half of them failed to meet the US Pharmacopeia 30 dissolution criteria for the verapamil hydrochloride tablets highlighting the dependence of dissolution process on the formulation components other than the disintegrating agent. The results identified only one formulation as suitable for using the disintegration test, instead of the dissolution test, as drug product acceptance criteria and highlight the need for systematic studies before using the disintegration test, instead of the dissolution test as the drug acceptance criteria. PMID:19387843

Gupta, Abhay; Hunt, Robert L; Shah, Rakhi B; Sayeed, Vilayat A; Khan, Mansoor A

2009-04-23

18

Correlation Between the Disintegration Time and the Bioavailability of Vitamin C Tablets  

Microsoft Academic Search

The goal of this study was to examine if the current USP disintegration standard for vitamin C tablets (max. 30 min in water at 37°C with disks) is adequate or if a tighter disintegration standard (e.g., European compendia max. 15 min) should be recommended based on bioavailability considerations. Four formulations of 500-mg vitamin C tablets ranging in mean disintegration time

Hemmige N. Bhagavan; Brigitte I. Wolkoff

1993-01-01

19

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

20

Formulation and evaluation of taste-masked levocetirizine dihydrochloride orally disintegrating tablets.  

PubMed

Orally disintegrating tablets of levocetirizine dihydrochloride were formulated with different superdisintegrants (sodium starch glycollate, croscarmellose sodium, and crospovidone) using mannitol as a diluent. Tulsion-335, Indion-204, and poly kyron T-134 cation exchange resins were used as taste-masking agents. The drug and resin complex was prepared by the kneading method. Ten formulations were prepared with varying combinations of superdisintegrants and ion-exchange resins by the wet granulation technique, using polyvinylpyrrolidone K-30 as the binder. The prepared tablets were evaluated for degree of taste masking, weight variation, hardness, friability, in vitro and in vivo disintegration time, content uniformity, and water absorption ratio. Dissolution studies were performed in two dissolution media: 0.1N HCl and distilled water. The corresponding dissolution rates were compared with the marketed formulation. Differential scanning calorimetry studies were carried out on the drug-resin complexes. Prepared tablets were good in appearance and showed acceptable results for hardness and friability. In vitro and in vivo disintegration times for the optimum formulation (F-1) were found to be 22 and 55 s, respectively. Relatively acceptable taste was achieved with both Indion-204 and Tulsion-335. Rapid disintegration time was achieved in tablets containing crosspovidone as the superdisintegrant. Dissolution studies indicated the formation of the complex of drug and resin. Differential scanning calorimetry studies indicated the formation of drug-resin complex. PMID:20169858

Devireddy, Srinivas Reddy; Gonugunta, Chandra Sekhara Rao; Veerareddy, Prabhakar Reddy

21

Fast-disintegrating sublingual tablets: Effect of epinephrine load on tablet characteristics  

Microsoft Academic Search

The aim of this study was to evaluate the effect of increasing epinephrine load on the characteristics of fast-disintegrating\\u000a sublingual tablets for the potential emergency treatment of anaphylaxis. Four tablet formulations, A, B, C, and D, containing\\u000a 0%, 6%, 12%, and 24% of epinephrine bitartrate, respectively, and microcrystalline cellulose:low-substituted hydroxypropyl\\u000a cellulose (9?1), were prepared by direct compression, at a range

Mutasem M. Rawas-Qalaji; F. Estelle; R. Simons; Keith J. Simons

2006-01-01

22

Improved stability of Opalmon tablets under humid conditions IV: effect of polysaccharides and disintegrants on the stability and dissolution property of Opalmon tablets.  

PubMed

We studied the effects of dextran, dextrin, and disintegrants on the chemical stability of Opalmon tablets containing Limaprost-alfadex (Limaprost/alpha-cyclodextrin complex) and found that the addition of dextran or dextrin significantly improved the chemical stability of Opalmon tablets under high humidity, compared to lactose. We also examined how dextran stabilizes Limaprost in Opalmon tablets and studied the formulation of Opalmon tablets in order to achieve higher chemical stability, rapid dissolution and reduced stickiness. The results suggested that dextran increases stabilization after moisture adsorption by decreasing the dissociation of Limaprost-alfadex to the free drug and alpha-cyclodextrin in the dextran matrix, when compared with the lactose matrix. The stickiness of Opalmon tablets containing dextran and dextrin was negligible when dextran and dextrin amounted to less than 20% of the formulation. By selecting a proper disintegrant, we obtained Opalmon tablets with higher chemical stability and rapid dissolution properties. PMID:18175966

Sekiya, Noboru; Nishiwaki, Atsushi; Nishiura, Akio; Yamamoto, Masanobu; Takeda, Kazuhisa; Iohara, Daisuke; Hirayama, Fumitoshi; Arima, Hidetoshi; Uekama, Kaneto

2008-01-01

23

Miconazole nitrate oral disintegrating tablets: in vivo performance and stability study.  

PubMed

The interest in and need for formulating miconazole nitrate (MN), a broad-spectrum antifungal, as an oral disintegrating tablet for treatment of some forms of candidiasis have increased. Formulation of MN in this dosage form will be more advantageous, producing dual effect: local in the buccal cavity and systemic with rapid absorption. Four formulations were prepared utilizing the foam granulation technique. The prepared tablets were characterized by measuring the weight uniformity, thickness, tensile strength, friability, and drug content. In addition, tablet disintegration time, in vitro dissolution, and in vivo disintegration time were also evaluated. Stability testing for the prepared tablets under stress and accelerated conditions in two different packs were investigated. Each pack was incubated at two different elevated temperature and relative humidity (RH), namely 40 ± 2°C/75 ± 5% RH and 50 ± 2°C/75 ± 5% RH. The purpose of the study is to monitor any degradation reactions which will help to predict the shelf life of the product under the defined storage conditions. Finally, in vivo study was performed on the most stable formula to determine its pharmacokinetic parameters. The results revealed that all the prepared tablets showed acceptable tablet characteristics and were stable under the tested conditions. The most stable formula was that containing magnesium stearate as lubricant, hydrophobic Aerosil R972 as glidant, low urea content, mannitol/microcrystalline cellulose ratio 2:1, and 9% Plasdone XL100 as superdisintegrant. The in vivo results revealed that the tested formula showed rapid absorption compared to the physical blend (t (max) were 1 and 4 h, respectively), while the extent of absorption was almost the same. PMID:22585373

Ahmed, Tarek A; El-Say, Khalid M; Mahmoud, Maged F; Samy, Ahmed M; Badawi, Alia A

2012-05-15

24

Evaluation of Chlorpheniramine Maleate microparticles in orally disintegrating film and orally disintegrating tablet for pediatrics.  

PubMed

Abstract Objective: To mask the bitterness of Chlorpheniramine Maleate via encapsulating drug into Eudragit EPO microparticles, and then incorporate these microparticles into orally disintegrating films (ODF) and orally disintegrating tablets (ODT) for pediatric uses. Methods: Spray drying of water-in-oil emulsion was utilized to encapsulate Chlorpheniramine Maleate into Eudragit EPO microparticles. Based on an orthogonal experimental design L9 (3(3)), polynomial regression models were developed to evaluate correlation between microparticle properties (encapsulation efficiency and drug release) and variables (X1: weight ratio of polymer to drug, X2: volume ratio of oil to water and X3: Q-flow of spray dryer). ODF and ODT formulations were evaluated including weight variation, content uniformity, tensile strength, disintegration time, friability and dissolution profiles. The bitterness taste test was evaluated in 10 adult volunteers. Results and discussion: From polynomial regression analysis, the best values of variables leading to the optimized microparticles were X1?=?10, X2?=?3 and X3?=?45. The optimized microparticles were incorporated into ODF and ODT with satisfactory weight and drug content uniformity, and acceptable physical strength. Both dosage forms disintegrated immediately (less than 40?s) in simulated saliva solutions. The outcome of taste-masking test indicated that microparticles alleviated drug bitterness significantly; bitterness was not discernible with microparticles incorporated in ODT, whereas only slight bitterness was detected from microparticles incorporated into ODF. Conclusion: Both ODF and ODT are shown to be suitable vehicles for taste masked Chlorpheniramine Maleate microparticles with potential for pediatric uses. PMID:23621768

Lou, Hao; Liu, Min; Qu, Wen; Hu, Zheyi; Brunson, Ed; Johnson, James; Almoazen, Hassan

2013-04-26

25

[Preparation of orally disintegrating tablets for masking of unpleasant taste: comparison with corrective-adding methods].  

PubMed

Many orally disintegrating tablets have recently been developed to improve oral ingestion and usability and are widely administered clinically, resulting in improved quality of life for patients. Since orally disintegrating tablets rapidly disintegrate in the mouth, the masking of unpleasant taste is important. We investigated the masking of the taste of furosemide (FU) as a model drug with correctives and prepared orally disintegrating tablets. Using maltitol (MA) as a corrective, granules were prepared employing mixing, coating, and mixing/coating methods using a desktop granulator. Each preparation was subjected to tasting. The taste was masked well when granules were prepared by the mixing and mixing/coating methods. Tablets were prepared from these granules with mannitol and crystalline cellulose added as fillers. Tablets made from granules prepared by the mixing and mixing/coating methods showed appropriate strength and disintegrated rapidly. When the amount of MA was increased in the mixing method, the disintegration time was prolonged, and thus the amount should be determined considering both taste masking and disintegration property. The results showed that orally disintegrating tablets of insoluble drugs with an unpleasant taste such as FU should be prepared with the taste masked employing the methods used in this study. PMID:20046069

Kawano, Yayoi; Ito, Akihiko; Sasatsu, Masanaho; Machida, Yoshiharu

2010-01-01

26

Comparison of an orally disintegrating ondansetron tablet with the conventional ondansetron tablet for cyclophosphamide-induced emesis in cancer patients: A multicenter, double-masked study  

Microsoft Academic Search

A total of 427 cancer patients receiving cyclophosphamide chemotherapy participated in this multicenter, double-masked, double-dummy, parallel-group, randomized study comparing the antiemetic efficacy and safety of an 8-mg conventional ondansetron tablet (OT, n = 212) taken twice daily with an 8-mg orally disintegrating ondansetron tablet (ODT, n = 215) taken twice daily for 3 days. In the primary efficacy analysis, complete

Neville Davidson; Bernardo Rapoport; Bjorn Erikstein; Bernard L'Esperance; Paul Ruff; Walter Paska; Irene Miller; Paula Curtis

1999-01-01

27

A new formulation for orally disintegrating tablets using a suspension spray-coating method.  

PubMed

The aim of this study was to design a new orally disintegrating tablet (ODT) that has high tablet hardness and a fast oral disintegration rate using a new preparation method. To obtain rapid disintegration granules (RDGs), a saccharide, such as trehalose, mannitol, or lactose, was spray-coated with a suspension of corn starch using a fluidized-bed granulator (suspension method). As an additional disintegrant, crospovidone, light anhydrous silicic acid, or hydroxypropyl starch was also included in the suspension. The RDGs obtained possessed extremely large surface areas, narrow particle size distribution, and numerous micro-pores. When tabletting these RDGs, it was found that the RDGs increased tablet hardness by decreasing plastic deformation and increasing the contact frequency between granules. In all tablets, a linear relationship was observed between tablet hardness and oral disintegration time. From each linear correlation line, a slope (D/H value) and an intercept (D/H(0) value) were calculated. Tablets with small D/H and D/H(0) values could disintegrate immediately in the oral cavity regardless of the tablet hardness and were considered to be appropriate for ODTs. Therefore, these values were used as key parameters to select better ODTs. Of all the RDGs prepared in this study, mannitol spray-coated with a suspension of corn starch and crospovidone (2.5:1 w/w ratio) showed most appropriate properties for ODTs; fast in vivo oral disintegration time, and high tablet hardness. In conclusion, this simple method to prepare superior formulations for new ODTs was established by spray-coating mannitol with a suspension of appropriate disintegrants. PMID:19686825

Okuda, Y; Irisawa, Y; Okimoto, K; Osawa, T; Yamashita, S

2009-08-15

28

A novel approach to optimize and formulate fast disintegrating tablets for nausea and vomiting.  

PubMed

The aim of this study was to optimize and formulate fast disintegrating tablets (FDTs) for nausea and vomiting using aminoacetic acid, carmellose and sodium alginate with enough mechanical strength. Ondansetron HCl (water soluble) or domperidone (water insoluble) drug were added to FDTs and their disintegration behaviour was evaluated. Plackett Burman Screening Design was used to screen the independent active process variables [concentration of aminoacetic acid (X (1)), concentration of carmellose (X (2)) and tablet crushing strength (X (3))] which were found to actively influence the dependent variables [disintegration time in the mouth (DT), wetting time (WT), and water absorption ratio (WAR)] for both the drugs. Also, the coefficients of active variables (DT, WT and WAR) of FDTs containing domperidone was found to be significantly different (P < 0.05) from the coefficients of active factors (X (1), X (2) and X (3)) containing ondansetron HCl FDTs. Further, FDTs containing domperidone was prepared according to central composite design for estimating the effect of active factors (X (1), X (2), X (3)) in extended spherical domain. The regression analysis of quadratic fit revealed that DT, WT and WAR were 98% correlated with active factors (X (1), X (2) or X (3)). The optimized domperidone FDTs were further compared with superdisintegrants (croscarmellose sodium or crospovidone). The data revealed that optimized domperidone FDTs were better than domperidone FDTs containing croscarmellose or crospovidone. Hence, this novel excipients combination can be used for delivery of water insoluble drugs in place of superdisintegrants. PMID:18584333

Goel, Honey; Vora, Nishant; Rana, Vikas

2008-06-27

29

A Novel Approach to Optimize and Formulate Fast Disintegrating Tablets for Nausea and Vomiting  

PubMed Central

The aim of this study was to optimize and formulate fast disintegrating tablets (FDTs) for nausea and vomiting using aminoacetic acid, carmellose and sodium alginate with enough mechanical strength. Ondansetron HCl (water soluble) or domperidone (water insoluble) drug were added to FDTs and their disintegration behaviour was evaluated. Plackett Burman Screening Design was used to screen the independent active process variables [concentration of aminoacetic acid (X1), concentration of carmellose (X2) and tablet crushing strength (X3)] which were found to actively influence the dependent variables [disintegration time in the mouth (DT), wetting time (WT), and water absorption ratio (WAR)] for both the drugs. Also, the coefficients of active variables (DT, WT and WAR) of FDTs containing domperidone was found to be significantly different (P?compared with superdisintegrants (croscarmellose sodium or crospovidone). The data revealed that optimized domperidone FDTs were better than domperidone FDTs containing croscarmellose or crospovidone. Hence, this novel excipients combination can be used for delivery of water insoluble drugs in place of superdisintegrants.

Goel, Honey; Vora, Nishant

2008-01-01

30

Design of Fast Disintegrating Tablets of Prochlorperazine Maleate by Effervescence Method  

PubMed Central

In the present work, fast disintegrating tablets of prochlorperazine maleate were designed with a view to enhance patient compliance by effervescent method. In this method, mixtures of sodium bicarbonate and anhydrous citric acid in different ratios along with crospovidone (2-10% w/w), croscarmellose sodium (2-10% w/w) were used as superdisintegrants. Estimation of prochlorperazine maleate in the prepared tablet formulations was carried out by extracting the drug with methanol and measuring the absorbance at 254.5 nm. The prepared formulations were further evaluated for hardness, friability, drug content uniformity and in vitro dispersion time. Based on in vitro dispersion time (approximately 13-21 s), two promising formulations (one from each super-disintegrant) were tested for in vitro drug release pattern in pH 6.8 phosphate buffer, short-term stability (at 40°/75% relative humidity for 3 mo) and drug-excipient interaction (IR spectroscopy). Among the two promising formulations, the formulation containing 10% w/w of crospovidone and mixture of 20% w/w sodium bicarbonate and 15% w/w of citric acid emerged as the overall best formulation (t50% 6 min) based on drug release characteristics in pH 6.8 phosphate buffer compared to commercial conventional tablet formulation (t50% 17.4 min). Short-term stability studies on the promising formulations indicated that there are no significant changes in drug content and in vitro dispersion time (p<0.05).

Shirsand, S. B.; Suresh, Sarasija; Para, M. S.; Swamy, P. V.

2009-01-01

31

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

32

Formulation study for lansoprazole fast-disintegrating tablet. I. Effect of compression on dissolution behavior.  

PubMed

Lansoprazole fast-disintegrating tablet (LFDT) is a new patient-friendly formulation of lansoprazole. Since lansoprazole is an antiulcer agent and is unstable under acidic conditions, we have developed LFDT as an orally disintegrating tablet containing enteric-coated microgranules. The effect of compression on dissolution behavior was investigated, as compression affected cleavage and crushing of the enteric layer. To decrease cleavage and crushing of the enteric layer, the effects of the combined ratio of methacrylic acid copolymer dispersion to ethyl acrylate-methyl methacrylate copolymer dispersion and the concentration of triethyl citrate on the dissolution in the acid stage and the dissolution in the buffer stage were evaluated. By adjusting the ratio of methacrylic acid copolymer dispersion to ethyl acrylate-methyl methacrylate copolymer dispersion to 9 : 1 and adding a 20% triethyl citrate concentration, sufficient flexibility of the enteric layer and sufficient stability against compression forces were achieved. Agglomeration of enteric-coated microgranules during the coating process was decreased at the optimized concentration of triethyl citrate and glyceryl monostearate. We compared the absorption properties of LFDT and lansoprazole capsules in dogs. The absorption profiles of LFDT were similar to those of lansoprazole capsules. PMID:12913232

Shimizu, Toshihiro; Nakano, Yoshinori; Morimoto, Shuji; Tabata, Tetsuro; Hamaguchi, Naoru; Igari, Yasutaka

2003-08-01

33

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

2012-02-03

34

A Novel Approach to Optimize and Formulate Fast Disintegrating Tablets for Nausea and Vomiting  

Microsoft Academic Search

The aim of this study was to optimize and formulate fast disintegrating tablets (FDTs) for nausea and vomiting using aminoacetic\\u000a acid, carmellose and sodium alginate with enough mechanical strength. Ondansetron HCl (water soluble) or domperidone (water\\u000a insoluble) drug were added to FDTs and their disintegration behaviour was evaluated. Plackett Burman Screening Design was\\u000a used to screen the independent active process

Honey Goel; Nishant Vora; Vikas Rana

2008-01-01

35

Disintegration of Highly Soluble Immediate Release Tablets: A Surrogate for Dissolution  

Microsoft Academic Search

The purpose of the work was to investigate correlation between disintegration and dissolution for immediate release tablets\\u000a containing a high solubility drug and to identify formulations where disintegration test, instead of the dissolution test,\\u000a may be used as the acceptance criteria based on International Conference on Harmonization Q6A guidelines. A statistical design\\u000a of experiments was used to study the effect

Abhay Gupta; Robert L. Hunt; Rakhi B. Shah; Vilayat A. Sayeed; Mansoor A. Khan

2009-01-01

36

Predicting orally disintegrating tablets formulations of ibuprophen tablets: an application of the new SeDeM-ODT expert system.  

PubMed

This article provides a new innovative tool for pharmaceutical preformulation to predict whether a disintegrant excipient or mixture of powder containing API+excipients is suitable to obtain a bucodispersible tablet by direct compression or not. This innovative tool is the new model SeDeM-ODT that provides the Index of Good Compressibility and Bucodispersibility (IGCB index), which is based on the previous SeDeM expert system that indicates the aptitude of a powder to be compressed. The IGCB index is composed of six main factors (from 15 pharmaceutical raw parameters), which indicate whether a mixture of powder has the aptitude to be compressed by direct compression and at the same time indicates whether these tablets are suitable to be used as a bucodispersible tablet (disintegration time lower than 3 min). PMID:22245156

Aguilar-Díaz, Johnny Edward; García-Montoya, Encarna; Suñe-Negre, José María; Pérez-Lozano, Pilar; Miñarro, Montserrat; Ticó, José Ramón

2012-01-05

37

Orally disintegrating mini-tablets (ODMTs) – A novel solid oral dosage form for paediatric use  

Microsoft Academic Search

The new European regulations on paediatric medicines and recent WHO recommendations have induced an increased need for research into novel child-appropriate dosage forms. The aim of this study was the development of orally disintegrating mini-tablets (ODMTs) as a suitable dosage form for paediatric patients. The suitability of five commercially available ready-to-use tableting excipients, Ludiflash®, Parteck® ODT, Pearlitol® Flash, Pharmaburst® 500

I. Stoltenberg; J. Breitkreutz

2011-01-01

38

The efficacy of postoperative ondansetron (Zofran) orally disintegrating tablets for preventing nausea and vomiting after acoustic neuroma surgery.  

PubMed

Postoperative nausea and vomiting is a frequent complication of craniotomy. We evaluated the ability of intraoperative IV ondansetron followed by postoperative ondansetron in an orally disintegrating tablet formulation to reduce the frequency and severity of postoperative nausea and vomiting in a prospective, randomized, placebo-controlled double-blind trial of 60 patients undergoing acoustic neuroma resection. Each patient received intraoperative ondansetron (4 mg IV) or placebo 30 min before case end. Postoperatively, patients received ondansetron in an orally disintegrating tablet formulation (8 mg BID) or placebo twice a day for up to 72 h. Metoclopramide was available as rescue therapy for both groups. Severity of nausea (as measured on a 10-cm visual scale), number of emetic episodes, and requirement for rescue therapy were recorded. In the immediate postoperative period, nausea severity was less in patients treated with ondansetron than placebo (3.3 +/- 4.1 versus 7.3 +/- 4.2; P < 0.001) and fewer patients experienced vomiting (3 of 28 versus 11 of 32; chi2 P < 0.01). More patients required some form of rescue treatment in the placebo group on the first postoperative day (26 of 32 versus 16 of 28; chi2 P < 0.01). We conclude that after acoustic neuroma surgery IV ondansetron treatment prevents immediate postoperative nausea and vomiting. Postoperative treatment with ondansetron in an orally disintegrating tablet formulation was associated with less frequent rescue therapy as compared with placebo on the first postoperative day. PMID:16244017

Hartsell, Theresa; Long, Donlin; Kirsch, Jeffrey R

2005-11-01

39

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

2013-07-09

40

Disintegration  

Microsoft Academic Search

The silver lining behind the Supreme Court's decision to disintegrate the Seattle and Louisville public schools is that the decision also runs the risk of disintegrating judicial review. Parents Involved in Community Schools v. Seattle School District No. 1 holds that the Constitution bars voluntary, race-conscious efforts by two local school boards to retain the racial integration that they worked

Girardeau A. Spann

2008-01-01

41

Development and Evaluation of Artemether Taste Masked Rapid Disintegrating Tablets with Improved Dissolution Using Solid Dispersion Technique  

Microsoft Academic Search

The purpose of this research was to mask the intensely bitter taste of artemether (ARM) and to formulate a rapid-disintegrating\\u000a tablet (RDT) of the taste-masked drug. Taste masking was done by solid dispersion with mono amino glycyrrhyzinate pentahydrate\\u000a (GLY) by solvent evaporation method. To characterize and formulate taste masked rapid disintegrating tablets (RDTs) of ARM,\\u000a the 1:1M solid dispersion was

Punit P. Shah; Rajashree C. Mashru

2008-01-01

42

Ondansetron oral disintegrating tablets for the prevention of postoperative vomiting in children undergoing strabismus surgery  

PubMed Central

Strabismus surgery in pediatric patients is associated with a high incidence of postoperative nausea and vomiting (PONV). Ondansetron disintegrating tablets (ODT), an oral freeze-dried formulation of the 5-HT3 antagonist, are well-tolerated and have been shown to reduce chemotherapy-induced vomiting. The purpose of this study was to assess the efficacy of the ODT in preventing postoperative vomiting (POV) in children undergoing strabismus repair. Healthy children aged 4–12 years of age were administered a 4 mg ODT 30 minutes prior to the induction of general anesthesia. Induction and maintenance of anesthesia were standardized; each child received acetaminophen and ketorolac pre-emptively for analgesia. This study group was compared with a historical control group who received a placebo in previously conducted identical trials of POV. The 35 children included in this study were compared with 31 controls. The incidence and severity of POV and use of rescue antiemetics were significantly lower in children who received ODT compared with placebo (p ? 0.001). The acute complete response (ie, no emesis and no rescue antiemetics in 24 hours) was 76% in the ODT group compared with 16% in the controls (p ? 0.001). Results suggest that ODT given preoperatively reduces the incidence and severity of POV in children undergoing strabismus surgery.

Wagner, Deborah S; Gauger, Virginia; Chiravuri, Devi; Faust, Kristin

2007-01-01

43

Ondansetron oral disintegrating tablets for the prevention of postoperative vomiting in children undergoing strabismus surgery.  

PubMed

Strabismus surgery in pediatric patients is associated with a high incidence of postoperative nausea and vomiting (PONV). Ondansetron disintegrating tablets (ODT), an oral freeze-dried formulation of the 5-HT(3) antagonist, are well-tolerated and have been shown to reduce chemotherapy-induced vomiting. The purpose of this study was to assess the efficacy of the ODT in preventing postoperative vomiting (POV) in children undergoing strabismus repair. Healthy children aged 4-12 years of age were administered a 4 mg ODT 30 minutes prior to the induction of general anesthesia. Induction and maintenance of anesthesia were standardized; each child received acetaminophen and ketorolac pre-emptively for analgesia. This study group was compared with a historical control group who received a placebo in previously conducted identical trials of POV. The 35 children included in this study were compared with 31 controls. The incidence and severity of POV and use of rescue antiemetics were significantly lower in children who received ODT compared with placebo (p compared with 16% in the controls (p

Wagner, Deborah S; Gauger, Virginia; Chiravuri, Devi; Faust, Kristin

2007-08-01

44

Comparison of an orally disintegrating ondansetron tablet with the conventional ondansetron tablet for cyclophosphamide-induced emesis in cancer patients: a multicenter, double-masked study. Ondansetron Orally Disintegrating Tablet Emesis Study Group.  

PubMed

A total of 427 cancer patients receiving cyclophosphamide chemotherapy participated in this multicenter, double-masked, double-dummy, parallel-group, randomized study comparing the antiemetic efficacy and safety of an 8-mg conventional ondansetron tablet (OT, n = 212) taken twice daily with an 8-mg orally disintegrating ondansetron tablet (ODT, n = 215) taken twice daily for 3 days. In the primary efficacy analysis, complete or major control of emesis (0 to 2 emetic episodes) between days 1 and 3 was seen in 80% of OT and 78% of ODT patients. The 90% confidence interval for the differences between treatments was -8.6% to 4.4% (defined interval of equivalence, +/-15%), showing that the formulations were equivalent. In the secondary efficacy analysis, no significant differences were observed in the rates of complete control of emesis (no episodes of emesis) over 3 days (63% and 64% of the respective groups) and on day 1 (84% and 81%, respectively) and in the complete control of nausea over 3 days (37% and 43%, respectively) and on day 1 (59% and 61% of patients, respectively). The taste of ODT was acceptable to the majority of patients (89%) who received it. OT and ODT were both well tolerated. Thus 8 mg ODT twice daily represents a palatable, well-tolerated, and effective antiemetic treatment for the control of cyclophosphamide-induced emesis and nausea and provides equivalent treatment to OT 8 mg twice daily. PMID:10321418

Davidson, N; Rapoport, B; Erikstein, B; L'Esperance, B; Ruff, P; Paska, W; Miller, I; Curtis, P

1999-03-01

45

Controlled Drug Release of Highly Water-Soluble Pentoxifylline from Time-Limit Disintegration-Type Wax Matrix Tablets  

Microsoft Academic Search

A pulsatile drug release system with a dry-coated tablet containing pentoxifylline was investigated for controlling drug release\\u000a in the gastrointestinal tract. The system consisted of a core tablet with disintegrator and outer layer, which obtained compression\\u000a from the ground mixtures of pentoxifylline and behenic acid. Drug release from a dry-coated tablet was investigated at 37°C\\u000a in JPXII 2nd fluid at

Makoto Otsuka; Yoshihisa Matsuda

1994-01-01

46

Controlled drug release of highly water-soluble pentoxifylline from time-limit disintegration-type wax matrix tablets.  

PubMed

A pulsatile drug release system with a dry-coated tablet containing pentoxifylline was investigated for controlling drug release in the gastrointestinal tract. The system consisted of a core tablet with disintegrator and outer layer, which obtained compression from the ground mixtures of pentoxifylline and behenic acid. Drug release from a dry-coated tablet was investigated at 37 degrees C in JPXII 2nd fluid at pH 6.8. The drug release from the outer layer was fitted to the Cobby model. The drug release from the wax matrix increased significantly after tablet distintegration; therefore, the drug release profiles showed typical sigmoidal curves. The disintegration time depended on the weight fraction of the core tablet, and the drug release rate after disintegration increased with increasing drug concentration in the core tablet. The relationship between the time required for 50% drug release and the disintegration time was linear, indicating that the drug release rate was controlled by regulating the disintegration time. PMID:8008697

Otsuka, M; Matsuda, Y

1994-03-01

47

[Preparation and evaluation of taste masked orally disintegrating tablets with granules made by the wet granulation method].  

PubMed

Using furosemide (FU) as a model drug, we examined the wet granulation method as a way to improve the taste masking and physical characteristics of orally disintegrating tablets (ODTs). In the wet granulation method, yogurt powder (YO) was used as a corrective and maltitol (MA) was used as a binding agent. The taste masked FU tablets were prepared using the direct compression method. Microcrystalline cellulose (Avicel® PH-302) and mannitol were added as excipients at a mixing ratio of 1/1 by weight. Based on the results of sensory test on taste, the prepared granules markedly improved the taste of FU, and a sufficient masking effect was obtained at the YO/FU ratio of 1 or more. Furthermore, it was found that the masking effect achieved by YO granules made with the wet granulation method was similar to or better than that produced by the granules made with dry granulation method. All types of tablets displayed sufficient hardness (over 3.5×10(-2) kN), and rapidly disintegrating tablets were obtained with YO granules produced at a mixing ratio of FU/YO=1/1, which disintegrated within 20 s. Disintegration time lengthened as the mixing ratio of YO to FU increased. In the mixing ratio of FU/YO=1/1, the hardness of tablets with granules made by the wet granulation method exceeded that of tablets with granules made by the dry granulation method, with minimal differences in disintegration time. The hardness and disintegration time of the tablets with granules made by the wet granulation method could be controlled by varying the compression force. In conclusion, YO was found to be a useful additive for masking unpleasant tastes. FU ODTs with improved taste, rapid disintegration and greater hardness could be prepared with YO-containing granules made by the wet granulation method using MA as a binding agent. PMID:21139401

Kawano, Yayoi; Ito, Akihiko; Sasatsu, Masanaho; Machida, Yoshiharu; Onishi, Hiraku

2010-12-01

48

Development of sustained release fast-disintegrating tablets using various polymer-coated ion-exchange resin complexes.  

PubMed

Complex formation between drugs and ion-exchange resins was investigated and the effects of coating by various aqueous polymeric dispersions on the complexes were evaluated for developing new sustained-release fast-disintegrating tablets (FDTs). Complexes of ion-exchange resin and dextromethorphan, a model drug, were prepared using different particle sizes of the resins. Aqueous colloidal dispersions of ethylcellulose (EC) and poly(vinyl acetate) (Kollicoat SR30D) were used for fluid-bed coating. Based on drug loading, release profiles, and scanning electron microscopy (SEM) images, the coated particles were granulated with suitable tablet excipients and then compressed into the tablets. Drug release profiles and SEM pictures were compared before and after the manufacturing processes. As the particle size of resins increased, the drug loading and release rate decreased due to the reduced effective diffusion coefficient and surface area. Higher coating level decreased the release rate further. In contrast to EC, Kollicoat SR30D coated particles could be compressed into tablets without any rupture or cracks on the coating since the mechanical properties of the polymer was more resistant to the manufacturing processes. This resulted in no significant changes in release rates. SEM showed the mechanical strength of the polymers affected the morphological change after compression. When the drug release profiles were applied into Boyd model and Higuchi equation, the linear relationship was observed, indicating that the diffusion within the resin matrix is the rate-controlling step. PMID:18164882

Jeong, Seong Hoon; Park, Kinam

2007-11-24

49

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

50

Fabrication and evaluation of taste masked resinate of risperidone and its orally disintegrating tablets.  

PubMed

The present investigation was undertaken to design a simple, rapid, cost effective and highly efficient process to fabricate a tasteless complex of risperidone using ion exchange resin (IER), evaluate the molecular properties of the resinate and finally incorporate it into orally disintegrating tablets (ODT). The resinate formation using Amberlite IRP64, was confirmed using the characterization methods: Fourier transform-infrared (FT-IR), X-ray diffraction (XRD) and differential scanning calorimetry (DSC). The maximum loading efficiency achieved was 99.72+/-0.16% in 1 : 4 (drug : resin weight) ratio at pH 6.0, temperature at 22 degrees C in a period of 1.5 h using ethanol : water (1 : 1, v/v) as the complexation medium. The complex was compressed into orally disintegrating tablet. The drug release from the complex was about 2.5% in 120 s in 5 ml of pH 6.8 phosphate buffer which has been used to mimic the salivary fluid volume and pH. Dissolution studies using 500 ml of 0.1 N HCl at 50 rpm in USP Apparatus II released 92% in 5 min, indicating complete drug release from the complex in the stomach. Resinate was tasteless while the fabricated ODTs were pleasantly tasting without any bitterness of drug as confirmed by the taste panel. PMID:19336927

Shukla, Dali; Chakraborty, Subhashis; Singh, Sanjay; Mishra, Brahmeshwar

2009-04-01

51

Characterization, optimisation and process robustness of a co-processed mannitol for the development of orally disintegrating tablets.  

PubMed

This is a study to fully assess a commercially available co-processed mannitol for its usefulness as an off-the-shelf excipient for developing orally disintegrating tablets (ODTs) by direct compression on a pilot scale (up to 4 kg). This work encompassed material characterization, formulation optimisation and process robustness. Overall, this co-processed mannitol possessed favourable physical attributes including low hygroscopicity and compactibility. Two design-of-experiments (DoEs) were used to screen and optimise the placebo formulation. Xylitol and crospovidone concentrations were found to have the most significant impact on disintegration time (p < 0.05). Higher xylitol concentrations retarded disintegration. Avicel PH102 promoted faster disintegration than PH101, at higher levels of xylitol. Without xylitol, higher crospovidone concentrations yielded faster disintegration and reduced tablet friability. Lubrication sensitivity studies were later conducted at two fill loads, three levels for lubricant concentration and number of blend rotations. Even at 75% fill load, the design space plot showed that 1.5% lubricant and 300 blend revolutions were sufficient to manufacture ODTs with ? 0.1% friability and disintegrated within 15 s. This study also describes results using a modified disintegration method based on the texture analyzer as an alternative to the USP method. PMID:22582882

Soh, Josephine Lay Peng; Grachet, Maud; Whitlock, Mark; Lukas, Timothy

2012-05-14

52

Simple preparation of coated resin complexes and their incorporation into fast-disintegrating tablets.  

PubMed

Even though ion-exchange resins are good drug carriers to get sustained release properties, it may not be good enough only with themselves. For further sustained release effect, a diffusion barrier or coating on the resins' surface can be utilized. Initially, microencapsulation using a w/o/w double emulsion method was used to apply ethylcellulose (EC) onto the drug/resin complexes. Typical pharmaceutical waxes can be alternative materials to delay the drug release from the complex. After the coating, the coated resin particles were incorporated into fast-disintegrating tablets to get an idea regarding the effects of wet granulation and compression on the release. Among the different grades of ECs tested (Ethocel 20, 45, and 100), more viscous EC resulted in better morphologies and sustained release effects. Because the drug release rate was significantly dependent on the coating level, the release rate can be modified easily by changing different levels of the coating. The drug release rate was also strongly dependent on the granulation and compaction process as the coated particles were incorporated into the tablet dosage form. Among the tested waxes, stearic acid had an effect on the sustained release together with lubrication and wetting properties. Even though microencapsulation or wax coating may not be practical for real manufacturing, the results may give valuable information how to formulate sustained release dosage forms and their properties on the tablet preparation. PMID:20191352

Jeong, Seong Hoon; Park, Kinam

2010-02-27

53

Development of novel sustained-release system, disintegration-controlled matrix tablet (DCMT) with solid dispersion granules of nilvadipine (II): in vivo evaluation.  

PubMed

A novel sustained-release (SR) system, disintegration-controlled matrix tablet (DCMT), was developed for poorly water-soluble drugs. DCMT, consisting of wax and solid dispersion (SD) granules containing a disintegrant, could control the release of nilvadipine (NiD), a model compound, by its disintegration. In the present study, two DCMTs (DCMT-1 and DCMT-2) with different release rates of NiD were orally administered to beagle dogs, and in vivo absorption of NiD from DCMTs was compared with that from immediate-release (IR) tablets. DCMTs successfully sustained the absorption of NiD longer than IR tablets, while they did not decrease the bioavailability of NiD. DCMT-2, providing the slower release of NiD than DCMT-1, prolonged the absorption longer than DCMT-1. In vivo absorption profiles of NiD from DCMTs were significantly correlated with in vitro release profiles, suggesting that the release property from DCMTs would maintain regardless of the change in physiological condition through the gastrointestinal tract. Furthermore, the food intake did not affect the absorption of NiD after oral administration of DCMT-2. The present results strongly indicate that the DCMT system would be a promising SR system, which could improve the solubility and sustain the absorption of poorly water-soluble drugs. PMID:16545477

Tanaka, Nobuyuki; Imai, Keiji; Okimoto, Kazuto; Ueda, Satoshi; Tokunaga, Yuji; Ibuki, Rinta; Higaki, Kazutaka; Kimura, Toshikiro

2006-03-20

54

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

2012-03-20

55

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

PubMed Central

The purpose of this research was to obtain directly compressible agglomerates of naproxen containing disintegrant by spherical crystallization technique. Acetone–water containing hydroxypropyl celloluse (HPC) and disintegrant was used as the crystallization system. In this study croscarmellose sodium (Ac–Di–Sol) was employed as disintegrant. The agglomerates were characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (XRPD), and scanning electron microscopy and were evaluated for flow, packing and tableting properties and drug release. The growth of particle size and the spherical form of the agglomerates resulted in formation of products with good flow and packing properties. The improved compaction properties of the agglomerated crystals were due to their fragmentation occurred during compression. DSC and XRPD studies showed that naproxen particles, crystallized in the presence of HPC and Ac–Di–Sol did not undergo structural modifications. The dissolution rate of naproxen from tablets made of naproxen–(Ac–Di–Sol) agglomerates was enhanced significantly because of including the disintegrant in to the particles. This was attributed to an increase in the surface area of the practically water insoluble drug is exposed to the dissolution medium. In conclusion the spherical crystallization technique developed in this study is suitable for obtaining agglomerates of drug with disintegrant.

Nokhodchi, A.

2008-01-01

56

Preparation of orally disintegrating tablets with taste-masking function: masking effect in granules prepared with correctives using the dry granulation method and evaluation of tablets prepared using the taste-masked granules.  

PubMed

We investigated several methods of taste masking in the preparation of orally disintegrating tablets (ODTs), using furosemide (FU) as a model drug. Four types of FU preparations were prepared: granules with maltitol (MA), granules with yogurt powder (YO), a physical mixture of FU and MA, and a physical mixture of FU and YO. All taste-masking granules were prepared using the dry granulation method. The taste of each type of preparation was evaluated. All four preparations markedly improved the taste of the FU tablets, but the mixing ratios of the correctives did not affect the masking effect. No difference in masking effect was found between MA and YO in the physical mixtures, but the masking effect in the granules with YO was superior to that of the granules with MA. Taste-masked FU tablets were prepared using the direct compression method; crystalline cellulose (Avicel PH-302) and mannitol were added as excipients at the mixing ratio of 1/1. All four types of tablets displayed sufficient hardness, but MA-containing tablets were harder than YO-containing tablets. The hardness of the tablets prepared from YO granules increased as the YO content increased. The most rapidly disintegrating tablets were those of YO granules prepared at a mixing ratio of FU/YO=1/1, which disintegrated within 20 s, followed by the tablets of MA granules prepared at a mixing ratio of FU/MA=1/1. The disintegration times of the tablets made from physical mixtures, in contrast, were longer than 200 s. Disintegration time lengthened as the mixing ratio of YO or MA increased. The hardness and disintegration time of these tablets could be controlled by varying the compression pressure. We found that YO is more useful than MA in masking unpleasant tastes and confirmed that orally disintegrating tablets with taste-masking function can be prepared using granules of YO prepared using the dry granulation method as a new corrective. PMID:20046070

Kawano, Yayoi; Ito, Akihiko; Sasatsu, Masanaho; Machida, Yoshiharu

2010-01-01

57

Development of novel sustained-release system, disintegration-controlled matrix tablet (DCMT) with solid dispersion granules of nilvadipine (II): In vivo evaluation  

Microsoft Academic Search

A novel sustained-release (SR) system, disintegration-controlled matrix tablet (DCMT), was developed for poorly water-soluble drugs. DCMT, consisting of wax and solid dispersion (SD) granules containing a disintegrant, could control the release of nilvadipine (NiD), a model compound, by its disintegration. In the present study, two DCMTs (DCMT-1 and DCMT-2) with different release rates of NiD were orally administered to beagle

Nobuyuki Tanaka; Keiji Imai; Kazuto Okimoto; Satoshi Ueda; Yuji Tokunaga; Rinta Ibuki; Kazutaka Higaki; Toshikiro Kimura

2006-01-01

58

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.

Green, Roger; Hicks, Rodney W

2011-01-01

59

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

60

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

2013-04-09

61

Desmopressin melt improves response and compliance compared with tablet in treatment of primary monosymptomatic nocturnal enuresis.  

PubMed

Primary nocturnal enuresis is a prevalent childhood condition that can persist into adulthood. Desmopressin is an antidiuretic available as orally disintegrating lyophilisate (melt) or solid tablet. Recent findings suggesting different food interactions and clinical characteristics, including compliance, between desmopressin melt and tablet motivated a post hoc analysis of a previously reported randomised, crossover study. The efficacy of desmopressin melt compared with tablet was evaluated using the International Children's Continence Society (ICCS) responder definitions. Compliance was further analysed using detailed criteria, and the association between efficacy and compliance was examined. In total, 221 patients aged 5-15 years, already receiving desmopressin tablets were randomised to the treatment sequence melt (120/240 ?g)/tablet (0.2/0.4 mg) or tablet/melt in two consecutive 3-week periods. The probability of being a responder (partial or full) during either period was significantly more likely with desmopressin melt compared with tablet (odds ratio, 2.0; confidence intervals, 1.07-3.73; p?=?0.03). There was no period effect on compliance in the tablet/melt sequence and no difference in the number of completely compliant patients in each formulation group; however, more patients were >75 % compliant in period 1 compared with period 2 in the melt/tablet sequence. Increased compliance was associated with greater reductions in the number of wet nights for both formulations. Conclusions: Desmopressin melt, compared with tablet, improves the probability of being a responder. Switching from tablet to melt formulation increased patient compliance. Increased compliance was associated with increased efficacy. Switching to desmopressin melt may benefit patients with suboptimal responses to desmopressin tablet. PMID:23677249

Juul, Kristian Vinter; Van Herzeele, Charlotte; De Bruyne, Pauline; Goble, Sandra; Walle, Johan Vande; Nørgaard, Jens Peter

2013-05-16

62

The Effects of Oral Ondansetron Disintegrating Tablets for Prevention of At-Home Emesis in Pediatric Patients After Ear-Nose-Throat Surgery  

Microsoft Academic Search

BACKGROUND: Tonsillectomy and adenoidectomy are associated with a frequent incidence of vomiting, both in the hospital and at home. We evaluated the effects of oral ondansetron disintegrating tablets (ODT) on the incidence of at-home emesis in children undergoing tonsillectomy with and without adenoidectomy and with and without bilateral myringotomy and tube insertion. METHODS: All patients underwent inhaled mask induction with

Peter J. Davis; Kathleen M. Fertal; Karen R. Boretsky; Gina M. Fedel; Michael D. Ingram; Susan K. Woelfel; Paul C. Hoffmann; Harshad Gurnaney; Michael C. Young

2008-01-01

63

Formulation study for lansoprazole fast-disintegrating tablet. II. Effect of triethyl citrate on the quality of the products.  

PubMed

The purpose of this study was to develop enteric-coated microgranules for the lansoprazole fast-disintegrating tablet (LFDT), which is a rapidly disintegrating tablet containing enteric-coated microgranules. In our previous study, it was clarified that sufficient flexibility of the enteric layer was achieved by the optimized combined ratio of methacrylic acid copolymer dispersion to ethyl acrylate-methyl methacrylate copolymer dispersion and adding the optimized concentration of triethyl citrate to reduce the damage during the compression process. However, since triethyl citrate has an unpleasant bitter taste and is especially incompatible with lansoprazole, it adversely affects the taste and stability of lansoprazole in the enteric-coated microgranules. The enteric layer containing macrogol 6000 was proven useful to improve the unpleasant bitter taste and stability of lansoprazole, because macrogol 6000 does not have an unpleasant bitter taste and is more compatible than triethyl citerate. By covering the inner (first enteric layer) and outer side (third enteric layer) of the enteric layer containing triethyl citrate (second enteric layer) with the enteric layer containing macrogol 6000, we resolved the stability problem of lansoprazole and the unpleasant bitter taste. Finally, we developed enteric-coated microgranules comprising seven layers: 1) core, 2) active compound layer, 3) intermediate layer, 4) first enteric layer, 5) second enteric layer, 6) third enteric layer, and 7) over coating layer. The enteric-coated microgranules have the multiple functions of reducing the damage to the enteric layer during the compression process, improving the stability of lansoprazole, and masking the unpleasant bitter taste. PMID:12951443

Shimizu, Toshihiro; Kameoka, Norio; Iki, Hiroshi; Tabata, Tetsuro; Hamaguchi, Naoru; Igari, Yasutaka

2003-09-01

64

Pharmacokinetics of olanzapine after single-dose oral administration of standard tablet versus normal and sublingual administration of an orally disintegrating tablet in normal volunteers.  

PubMed

Olanzapine (OLZ) is a second-generation antipsychotic agent available in 2 solid oral dosage forms, a standard oral tablet (SOT) and an orally disintegrating tablet (ODT). This study assessed the absorption of each by different routes of administration. Secondarily, the influence of P-glycoprotein (P-gp) genotype was assessed. It was hypothesized that more rapid absorption of the OLZ ODT would occur when administered sublingually versus standard oral administration. A randomized, 3-way crossover study assessed the 5-mg OLZ formulations in healthy volunteers (n = 10). Blood was collected (0-8 hours) to assess OLZ pharmacokinetics using liquid chromatography/mass spectrometry. Both routes of ODT administration resulted in more measurable early concentrations relative to SOT. However, there were no statistically significant differences observed between any of the OLZ exposures for observed pharmacokinetic parameters (C(max), T(max), AUC(0-8h)). The homozygous TT genotype for P-gp resulted in an increased AUC of OLZ for SOT administration but not for either condition where sublingual absorption could occur. PMID:16432268

Markowitz, John S; DeVane, C Lindsay; Malcolm, Robert J; Gefroh, Holly A; Wang, Jun-Sheng; Zhu, Hao-Jie; Donovan, Jennifer L

2006-02-01

65

Formulation, Characterization and Evaluation of Rapid Disintegrating Tablet of atifloxacin Sesquihydrate by ion exchange resin technique  

Microsoft Academic Search

Gatifloxacin Sesquihydrate is a Broad Spectrum Antimicrobial agent active against Gram Positive and Gram Negative Organism. It is slightly bitter in taste. In the present study an attempt has been made to prepare bitterless fast dissolving tablet of Gatifloxacin Sesquihydrate using Indion 204, Indion 214, Indion 234, Tulsion 335 (ion exchange resin) as a taste masking agent. X-ray powder diffractometry,

P. S. Gangane; K. G. Mahajan; H. S. Sawarkar; V. S. Adhao

66

Amorphous to crystalline transformation in maltose: Implications for orally disintegrating tablets  

Microsoft Academic Search

The purpose of the present study was to determine how environmental factors affected the crystallization of amorphous maltose, determine how those factors affected the post compaction hardening of oral fast dissolve tablets containing amorphous maltose, and to determine the crystallization kinetics and activation energy of amorphous maltose crystallization and separate out the activation energy of nucleation of amorphous maltose. The

Scott Eric Hostetler

2002-01-01

67

Taste masking of ondansetron hydrochloride by polymer carrier system and formulation of rapid-disintegrating tablets  

Microsoft Academic Search

The purpose of this research was to mask the intensely bitter taste of ondansetron HCl and to formulate a rapiddisintegrating\\u000a tablet (RDT) of the taste-maske drug. Taste masking was done by complexing ondansetron HCl with aminoalkyl methacrylate copolymer\\u000a (Eudragit EPO) in different ratios by the precipitation method. Drug-polymer complexes (DPCs) were tested for drug content,\\u000a in vitro taste in simulated

Shagufta Khan; Prashant Kataria; Premchand Nakhat; Pramod Yeole

2007-01-01

68

A prospective randomized trial of the antiemetic efficacy and cost-effectiveness of intravenous and orally disintegrating tablet of ondansetron in children with cancer.  

PubMed

Orally disintegrating tablet (ODT) of ondansetron is a new formulation, which instantaneously disintegrates and disperses in the saliva without need for ingestion of a liquid. This makes the formulation suitable for administration in children. The objective of this study was to compare the relative efficacy and cost of ODT and intravenous (IV) formulation of ondansetron in controlling nausea and vomiting in children receiving chemotherapy regimens without cisplatin. This prospective randomized trial was performed in a single institution to compare ODT and IV formulation of ondansetron for the prevention of acute emesis in a group of 22 children. Study agents were administered 30 min before chemotherapy and 12 hourly after chemotherapy (5 mg/m2 IV or 4-8 mg oral according to body surface area in 56 and 39 courses, respectively). After randomization, IV formulation was administered to some children instead of ODT due to unavailability of this formulation. Complete and major control of emesis was obtained in 92% of patients in the IV group and 93% of patients in the ODT group. In 56 courses with grade III-IV emetogenicity, complete response rates were not different between the two treatment arms. In the courses without corticosteroids complete response rates were not also different between the two arms. The mean costs per successfully controlled courses were 121.3 USD for the IV formulation whereas 63.2 USD for the ODT formulation. The results of this study confirmed that ODT formulation of ondansetron is a safe, well-tolerated, and cost-effective antiemetic for children during non-cisplatin-containing moderately and highly emetogenic chemotherapy. PMID:15804995

Corapçioglu, Funda; Sarper, Nazan

2005-03-01

69

[Method for the evaluation of the stability and usability after opening packages of orally disintegrating tablets: case of amlodipine besilate products].  

PubMed

Orally disintegrating (OD) tablets are widely used in clinical practice. However, drug information on the choice and dispensing based on their stability after opening packages and usability in patients and dispensaries is not sufficient. The aim of this study was to investigate possible evaluation methods of the stability and usability of amlodipine OD tablets. Additives of the brand were changed in April 2009, and therefore the previous and current forms and two generics, current and newly marketed (in November 2009) products of different firms, were used. OD tablets were stored at 25 degrees C and 75% relative humidity for 3 months after opening the packages, and their physicochemical properties were evaluated. Their weight, diameter, thickness, and color difference increased slightly from the initial state. The extent of the change in their hardness, disintegration time, and friability was different among products. These physicochemical changes were acceptable in dispensary practice. Storage after opening the packages did not affect their dissolution rate. The dissolution rate at the initial state of the current brand was slower than that of the previous one. All products used were able to be dispensed by an automatic tablet-packing machine and applied to the so-called simple suspension method for intubational administration. Sensory evaluation tests revealed no major difference in the oral disintegration time, taste, impression, and preference among products. In conclusion, the stability and usability of amlodipine OD tablets used in this study were examined using several methods, and they can be used equivalently from the stability and usability viewpoints. PMID:20686207

Hori, Katsuhito; Yoshida, Naoko; Okumura, Tomonori; Okamura, Yasufumi; Kawakami, Junichi

2010-08-01

70

Efficacy of an ondansetron orally disintegrating tablet: a novel oral formulation of this 5-HT(3) receptor antagonist in the treatment of fractionated radiotherapy-induced nausea and emesis. Emesis Study Group for the Ondansetron Orally Disintegrating Tablet in Radiotherapy Treatment.  

PubMed

A significant number of patients who are receiving radiotherapy experience the distressing side effects of emesis and nausea. Although prophylactic antiemetics are often given to patients who are receiving single-fraction, high-dose radiotherapy to the abdomen, a survey has revealed that antiemetic prophylaxis is not routinely offered to those receiving fractionated radiotherapy. Hence there is a need for an effective treatment of emesis for use in this group of patients. Ondansetron is an effective and well-tolerated antiemetic, which is used for the prevention of both chemotherapy and radiotherapy-induced emesis and nausea. This agent has been developed as a novel freeze-dried oral formulation. Ondansetron orally disintegrating tablets (ondODT) disperse rapidly when placed on the tongue. As the tablet does not need to be swallowed with water, it is a particularly useful formulation for patients who have difficulty with swallowing or who do not feel able to drink. This study was undertaken to investigate the efficacy of ondODT in the treatment of established emesis and nausea induced by radiotherapy. Two doses of ondODT, 8 mg and 16 mg, were compared with placebo in patients who developed emesis and/or moderate/severe nausea after receiving fractionated radiotherapy to sites located between the thorax and the pelvis. The study showed that ondODT was clinically superior to placebo in treating emesis and nausea successfully over a 12-hour period after taking the medication. There were no statistically significant differences between the two doses of ondODT. In the 2 hours after taking the study medication, patients who received ondODT (8 mg and 16 mg) had significantly fewer emetic episodes compared with those who received placebo. They also experienced significantly less nausea. In conclusion, ondODT 8 mg is effective in the treatment of radiotherapy-induced emesis and nausea and provides an effective alternative to the conventional ondansetron tablet. PMID:10591823

LeBourgeois, J P; McKenna, C J; Coster, B; Feyer, P; Franzén, L; Goedhals, L; Marzecki, Z; Souhami, L; Stewart, A; Tønnessen, F; Haigh, C; Mitchell, T; Wilkinson, J R; Graham, E

1999-01-01

71

A comparative study of dissolution characteristics of polymeric and wax granulations of theophylline and their tablets.  

PubMed

Matrix (non disintegrating) granules of theophylline have been formed and their dissolution characteristics investigated for sustained release application. The polymeric granulations were formed by massing the drug powder with a concentrated (40% w/w) ethanolic solution of an acrylatemethacrylate copolymer (ERS100R). Wax granulations were also formed by massing the drug powder with previously melted carnuba wax followed by screening and drying. The content of polymer or wax in the resulting granules was 16.7% w/w. Conventional granules of theophylline were formed by massing the drug powder with starch mucilage (20% w/v). Resulting granules were subjected to particle size analysis and in vitro dissolution tests. The granules were further compressed to tablets (weight 500+/-4.2 mg each) at a constant load (30 arbitrary units on the load scale). The tablets were subjected to hardness, disintegration and dissolution tests. The dissolution kinetics were also considered. The mean granule size was 646.5+/-4.3 microm (conventional), 821.4+/-4.8 microm (polymeric granulations) and 892.7+/-5.4 microm (wax granulations), the matrix granules were therefore larger than the conventional granules. Dissolution of the granules generally followed a first order rate kinetic. The rate constant (k(1)) for the conventional, polymeric and wax granulations were (h(-1)): 0.53, 0.31 and 0.27 respectively. Thus, the wax granulations appeared to be more effective than the polymeric granulations in retarding drug release from the granules but the difference was not statistically significant (p>0.05). The tensile strength of tablets derived from the conventional, polymeric and wax granulations were (MNm(-2)) 0.85, 1.68 and 1.96 respectively, indicating that the matrix granules (compared with the conventional granules) produced harder tablets at the same compression load. The corresponding first order dissolution rate constants were (h(-1)): 0.46, 0.28 and 0.21. Thus, tableting of the matrix granules produced a slight but significant decrease in dissolution rates, attributable to the disintegration of the tablets to more compact particles. PMID:18614417

Uhumwangho, Michael U; Okor, Roland S

2008-07-01

72

A comparative study of genetic and neurobiological findings in disintegrative psychosis and infantile autism.  

PubMed

Although disintegrative psychosis (DP) was first described in 1908, the validity of the syndrome has not yet been fully documented. To investigate the validity of DP as defined in ICD-9, 13 cases of DP were compared with 39 cases of infantile autism with reference to lifetime parental psychopathology, neuroradiological findings and genetic abnormalities. The groups were matched for gender, age, intellectual level and social class. Apart from a significantly higher rate of electroencephalogram abnormalities in the disintegrative group there was very little in the neurobiological background to support a clear distinction between DP and infantile autism. PMID:10997861

Mouridsen, S E; Rich, B; Isager, T

2000-08-01

73

A comparative study of the dissolution characteristics of capsule and tablet dosage forms of melt granulations of paracetamol--diluent effects.  

PubMed

The dissolution characteristics of melt granulations of paracetamol in capsule and tablet dosage form were compared to determine whether the dissolution characteristics of the granules can be actualized by formulating them as rapidly disintegrating tablets. The term melt granulation refers here to the wax-matrix granules that were formed by triturating the drug powder (paracetamol) with a melted carnauba wax. The matrix granules were admixed with diluents (lactose, alpha-cellulose or microcrystalline cellulose) also in granular form to prevent size separation during encapsulation or tableting. The granules were filled into hard gelatin capsules (mean content weight, 500 +/- 6.2 mg) or tableted (mean weight 500 +/- 5.1 mg, and tensile strength 1.36 +/- 0.2 to 1.7 +/- 0.3 MN/m2). The capsules and tablets were subjected to disintegration and in vitro dissolution tests. The dissolution data were analyzed on the basis of zero, first order rate kinetics and Higuchi square root of time relationship. The results showed that the dissolution profiles were generally consistent with a first order rate kinetics (r = 0.95). The first order dissolution rate constants of capsules and tablets of the matrix granules only (without diluents) were 0.31 +/- 0.02 min(-1) and 0.20 +/- 0.03 min(-1), respectively, indicating faster dissolution from the capsules. Therefore, the dissolution characteristics of the matrix particles were not intact after tableting. Addition of diluents to the capsule formulations had no effect on dissolution rates, whereas in the tablets, dissolution rates increased. For instance, inclusion of a diluent up to 50% w/w in the tablets increased the dissolution rate constants to 0.34 +/- 0.04 min(-1) (lactose), 0.42 +/- 0.02 min(-1) (alpha-cellulose), and 0.46 +/- 0.03 min(-1) (microcrystalline cellulose). Thus, alpha-cellulose and microcrystalline cellulose produced greater enhancer effect on the tablet dissolution rates compared to lactose. Both the capsules and the tablets disintegrated rapidly within 2 to 3 minutes. The dissolution enhancer effect of the diluents in the tablets only, relates to the aqueous swelling of the disintegrated particles. PMID:17665854

Uhumwangho, Michael U; Okor, Roland S

74

Efficacy and safety of desmopressin orally disintegrating tablet in patients with central diabetes insipidus: results of a multicenter open-label dose-titration study.  

PubMed

Central diabetes insipidus (CDI) is associated with arginine vasopressin (AVP) deficiency with resultant polyuria and polydipsia. Intranasal desmopressin provides physiological replacement but oral formulations are preferred for their ease of administration. This study aimed to demonstrate the efficacy and safety of desmopressin orally disintegrating tablet (ODT) in the treatment of Japanese patients with CDI, and confirm that antidiuresis is maintained on switching from intranasal desmopressin to desmopressin ODT. A total of 20 patients aged 6-75 years with CDI were included in this 4-week multicenter, open-label study. Following observation, patients switched from intranasal desmopressin to desmopressin ODT with titration to optimal dose over ?5 days at the study site. Following three consecutive doses with stable patient fluid balance, patients were discharged with visits at Weeks 2 and 4. Following titration from intranasal desmopressin to ODT, the mean 24-hour urine volume was unchanged, indicating similar antidiuresis with both formulations. The proportion of patients with endpoint measurements (urine osmolality, 24-hour urine volume, hourly diuresis rate and urine-specific gravity) within normal range at Days 1-2 (intranasal desmopressin) and Week 4 (desmopressin ODT) was similar. The mean daily dose ratio of intranasal desmopressin to desmopressin ODT (Week 4) was 1:24 but a wide range was observed across individuals to maintain adequate antidiuretic effect. Hyponatraemia was generally mild and managed by dose titration. Desmopressin ODT achieved sufficient antidiuretic control compared to intranasal therapy and was well tolerated over long-term treatment. The wide range of intranasal:ODT dose ratios underline the importance of individual titration. PMID:23811987

Arima, Hiroshi; Oiso, Yutaka; Juul, Kristian Vinter; Nørgaard, Jens Peter

2013-06-28

75

Ondansetron, orally disintegrating tablets versus intravenous injection for prevention of intrathecal morphine-induced nausea, vomiting, and pruritus in young males.  

PubMed

In this study we compared the efficacy of orally disintegrating tablets (ODT) and IV ondansetron for preventing spinal morphine-induced pruritus and postoperative nausea and vomiting (PONV) in healthy young male patients. Patients who received bupivacaine with 0.20 mg morphine for spinal anesthesia were randomly assigned to the ODT group (ODT ondansetron 8 mg, n = 50), the IV group (4 mg ondansetron IV, n = 50), or the placebo group (n = 50). Each individual was assessed for pruritus, postoperative nausea and vomiting, and pain at 0, 2, 6, 12, 18, and 24 h after surgery using three distinct visual analog scales. The frequencies of postoperative nausea and vomiting and frequencies of requirement for rescue antiemetic and antipruritic were recorded. There were no significant differences among the three groups with respect to incidence or severity of PONV or postoperative pain visual analog scale scores. The incidences of pruritus in the ODT (56%) and IV (66%) groups were significantly different from that in the placebo group (86%) (P < 0.02 for both). Only the ODT group had significantly lower mean pruritus visual analog scale scores at 0, 2, 6, and 12 h postsurgery than the placebo group (P < 0.023 for all). The frequency of requirement for rescue antipruritic was significantly less in the ODT group than the placebo group (P = 0.013). Both ODT ondansetron 8 mg and IV ondansetron 4 mg are more effective than placebo for preventing spinal morphine-induced pruritus, but neither form of this agent reduces spinal morphine-induced postoperative nausea and vomiting in this patient group. PMID:16243989

Pirat, Arash; Tuncay, Senay F; Torgay, Adnan; Candan, Selim; Arslan, Gulnaz

2005-11-01

76

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.

Odeku, Oluwatoyin A.; Akinwande, Babatunde L.

2011-01-01

77

Comparative bioavailability: Eight commercial prednisone tablets  

Microsoft Academic Search

Two four-treatment crossover bioavailability studies were performed in panels of 12 adult male volunteers with eight different commercial prednisone tablets. Plasma samples from the first study were assayed by radioimmunoassay for both prednisone and prednisolone. Plasma samples from the second study were assayed for prednisolone only. Statistical analyses of the data showed significant differences in the rate of appearance of

Timothy J. Sullivan; Margarette R. Hallmark; Ermelinda Sakmar; Donald J. Weidler; Robert H. Earhart; John G. Wagner

1976-01-01

78

Formulation of fast disintegrating tablets of ternary solid dispersions consisting of TPGS 1000 and HPMC 2910 or PVPVA 64 to improve the dissolution of the anti-HIV drug UC 781.  

PubMed

Solid dispersion formulations made up of d-alpha-tocopheryl polyethylene glycol succinate 1000 (TPGS 1000) and polyvinyl pyrrolidone co-vinyl acetate 64 (PVPVA 64) or hydroxy propyl methyl cellulose 2910 (HPMC 2910) were developed in order to improve the dissolution of UC 781. UC 781 dissolution rate was markedly improved as compared to the physical mixtures and the pure drug, attaining maximum drug releases of up to 100% after only 5 min in the case of TPGS 1000-UC 781-PVPVA 64 solid dispersions and 30 min in TPGS 1000-UC 781-HPMC 2910. The increased UC 781 dissolution rate could be maintained when formulating UC 781 in PVPVA 64 tablets. The latter disintegrated in only 4 min, reaching drug releases of up to 90% (w/w). In addition, as opposed to the corresponding solid dispersions, no decrease in drug release occurred upon dissolution of PVPVA 64 tablets when the pH was increased to 6.8. Contrary to the PVPVA 64 tablet formulations, HPMC 2910 tablets showed a slow dissolution process due to the gelling nature of the polymer. The drug was slowly released as HPMC 2910 dissolved in the medium, however also in this case 90% (w/w) of the drug was dissolved after 4 h. Both polymers formed compatible blends in combination with the drug. Thermal analysis of the ternary mixtures revealed eutectic behavior exhibiting an extremely fine dispersion of the drug in the carrier. This was confirmed by the fact that no drug crystals could be detected using X-ray diffraction (XRD). As opposed to the physical mixtures, PVPVA 64 and HPMC 2910 solid dispersions did not contain any isolated polymer-rich phases, hence showed improved homogeneity. Amorphous TPGS 1000 clusters occurred in PVPVA 64 and HPMC 2910 formulations upon addition of at least 10% (w/w) UC 781, showing extremely low glass transition temperatures depending of the thermal history of the samples. PMID:18602800

Goddeeris, Caroline; Willems, Tom; Van den Mooter, Guy

2008-07-07

79

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.

Lakshmi, PK; Sridhar, M; Shruthi, B

2013-01-01

80

An in vitro and in vivo comparative study of directly compressed solid dispersions and freeze dried sildenafil citrate sublingual tablets for management of pulmonary arterial hypertension.  

PubMed

Sildenafilcitrate (SILD) orodispersable sublingual tablets (ODSTs) have been developed using two comparative techniques for improving their oral disintegration, dissolution and bioavailability in order to manage acute attacks of pulmonary arterial hypertension (PAH). The techniques employed were direct compression of SILD-poloxamer 188 solid dispersions (SDs) and freeze drying using various excipients. The physicochemical and solid-state properties, as well as the dissolution behavior of the tablets were evaluated. Moreover, SILD bioavailability in human volunteers from the prepared ODSTs was compared to that of the conventional oral tablet. Incorporation of SD of poloxamer188 in sublingual tablets together with Pharmaburst using the direct compression technique enhanced the extent and dissolution rate of SILD with 100% of drug being dissolved after 7 minutes. However, the lyophilization process was superior in enhancing dissolution and 100% of SILD was dissolved after only one minute. Moreover, the in vivo study showed that the AUC???? of lyophilized tablets was significantly higher than that of directly compressed tablets, with bioavailability values of 159.81 and 140.85%, respectively, compared to the commercial oral product. PMID:23470352

Zayed, Reham; Kamel, Amany O; Shukr, Marwa; El-Shamy, Abd El-Hamid

2012-11-01

81

A comparative study of development and symptoms among disintegrative psychosis and infantile autism with an without speech loss  

Microsoft Academic Search

To investigate clinical pictures and the validity of disintegrative psychosis (DP) as defined in ICD-9, 18 cases of DP were compared with 51 and 145 cases of infantile autism (IA) with and without speech loss, respectively, on clinical variables. The DP cases showed clearer regression after more satisfactory development than the IA cases with speech loss. Around age 7, about

Hiroshi Kurita; Michiko Kita; Yuko Miyake

1992-01-01

82

Hydrodynamic, mass transfer, and dissolution effects induced by tablet location during dissolution testing.  

PubMed

Tablets undergoing dissolution in the USP Dissolution Testing Apparatus II are often found at locations on the vessel bottom that are off-center with respect to the dissolution vessel and impeller. A previously validated CFD approach and a novel experimental method were used here to examine the effect of tablet location on strain rates and dissolution rates. Dissolution tests were conducted with non-disintegrating tablets (salicylic acid) and disintegrating tablets (Prednisone) immobilized at different locations along the vessel bottom. CFD was used to predict the velocity profiles and strain rates when the tablets were placed at such locations. A CFD-based model was derived to predict the mass transfer coefficient and dissolution curves, which were then compared to the experimental results. Both non-disintegrating and disintegrating off-center tablets experimentally produced higher dissolution rates than centered tablets. The CFD-predicted strain rate distribution along the bottom was highly not uniform and the predicted strain rates correlated well with the experimental mass transfer coefficients. The proposed CFD-based model predicts mass transfer rates that correlate well with the experimental ones. The exact tablet location has a significant impact on the dissolution profile. The proposed model can satisfactorily predict the mass transfer coefficients and dissolution profiles for non-disintegrating tablets. PMID:18781589

Bai, Ge; Armenante, Piero M

2009-04-01

83

Leaching of indium from obsolete liquid crystal displays: Comparing grinding with electrical disintegration in context of LCA  

SciTech Connect

Highlights: Black-Right-Pointing-Pointer Two pre-treatment methods, prior to leaching of indium from obsolete LCD modules, were described. Black-Right-Pointing-Pointer Conventional grinding and electrical disintegration have been evaluated and compared in the context of LCA. Black-Right-Pointing-Pointer Experimental data on the leaching capacity for indium and the electricity consumption of equipment were inputted into the LCA model in order to compare the environmental performance of each method. Black-Right-Pointing-Pointer An estimate for the environmental performance was calculated as the sum of six impact categories. Black-Right-Pointing-Pointer Electrical disintegration method outperforms conventional grinding in all impact categories. - Abstract: In order to develop an effective recycling system for obsolete Liquid Crystal Displays (LCDs), which would enable both the leaching of indium (In) and the recovery of a pure glass fraction for recycling, an effective liberation or size-reduction method would be an important pre-treatment step. Therefore, in this study, two different types of liberation methods: (1) conventional grinding, and (2) electrical disintegration have been tested and evaluated in the context of Life Cycle Assessment (LCA). In other words, the above-mentioned methods were compared in order to find out the one that ensures the highest leaching capacity for indium, as well as the lowest environmental burden. One of the main findings of this study was that the electrical disintegration was the most effective liberation method, since it fully liberated the indium containing-layer, ensuring a leaching capacity of 968.5 mg-In/kg-LCD. In turn, the estimate for the environmental burden was approximately five times smaller when compared with the conventional grinding.

Dodbiba, Gjergj, E-mail: dodbiba@sys.t.u-tokyo.ac.jp [Department of System Innovation, Graduate School of Engineering, University of Tokyo (Japan); Nagai, Hiroki; Wang Lipang; Okaya, Katsunori; Fujita, Toyohisa [Department of System Innovation, Graduate School of Engineering, University of Tokyo (Japan)

2012-10-15

84

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.

Alanazi, Fars Kaed

2010-01-01

85

Pharmaceutical development of ondansetron tablets.  

PubMed

Ondansetron tablets contain ondansetron base as the hydrochloride dihydrate, lactose, microcrystalline cellulose, starch and magnesium stearate. Tablets sampled at the beginning and end of the compression process have good content uniformity and drug content, showing that there is no segregation or loss of the drug substance during tabletting. The release of drug substance is related to the tablet disintegration time. Tablets with disintegration times of 3 and 10 min release 85% of the drug substance in approximately 6 and 20 min respectively. Satisfactory bioavailability has been demonstrated. The tablets have good stability, and have a shelf life of 2 years when stored below 30 degrees C. PMID:2533901

Leak, R E; Woodford, J D

1989-01-01

86

Leaching of indium from obsolete liquid crystal displays: comparing grinding with electrical disintegration in context of LCA.  

PubMed

In order to develop an effective recycling system for obsolete Liquid Crystal Displays (LCDs), which would enable both the leaching of indium (In) and the recovery of a pure glass fraction for recycling, an effective liberation or size-reduction method would be an important pre-treatment step. Therefore, in this study, two different types of liberation methods: (1) conventional grinding, and (2) electrical disintegration have been tested and evaluated in the context of Life Cycle Assessment (LCA). In other words, the above-mentioned methods were compared in order to find out the one that ensures the highest leaching capacity for indium, as well as the lowest environmental burden. One of the main findings of this study was that the electrical disintegration was the most effective liberation method, since it fully liberated the indium containing-layer, ensuring a leaching capacity of 968.5mg-In/kg-LCD. In turn, the estimate for the environmental burden was approximately five times smaller when compared with the conventional grinding. PMID:22677013

Dodbiba, Gjergj; Nagai, Hiroki; Wang, Li Pang; Okaya, Katsunori; Fujita, Toyohisa

2012-06-06

87

Binding effectiveness of Colocassia esculenta gum in poorly compressible drugs-paracetamol and metronidazole tablet formulations.  

PubMed

The effectiveness of a polysaccharide gum obtained from the cormels of Colocassia esculenta was evaluated comparatively with acacia and methylcellulose as binders in the formulation of poorly compressible drugs. The granules of these drugs produced by wet massing method using colocassia and acacia gums as binders have high compressibility index indicating poor flow. Based on this parameter, the granules produced with methylcellulose as binder seem to flow better. The properties of tablets evaluated include breaking strength, friability, disintegration time and dissolution rate. The new polysaccharide gum showed better concentration-strength profile than acacia while methylcellulose yielded mechanically more stable tablets than the two binders. The resistance of tablets to abrasion was poor in metronidazole tablets formulated with colocassia gum. The in vitro availability characteristics showed that tablets produced with the new gum show acceptable disintegration time and release profile within a certain range of its concentration in tablets. At 4% w/w nominal concentration of colocassia gum in metronidazole tablets and 6% w/w in paracetamol, tablets show very long disintegration time and prolonged release profile. The binders used for comparison yielded tablets that show better in vitro release characteristics. PMID:10920535

Chukwu, K I; Udeala, O K

88

Adverse effects of iron supplementation: a comparative trial of a wax-matrix iron preparation and conventional ferrous sulfate tablets.  

PubMed

The acceptability of supplemental iron delivered from a wax-matrix tablet of ferrous sulfate was compared with that of a conventional ferrous sulfate tablet in a single-blind, parallel-group study. Both tablets were formulated to deliver 50 mg of elemental iron. The incidence of adverse effects was found to be significantly greater among 272 subjects taking the conventional tablets than among 271 subjects taking the wax-matrix preparation. Eighty-one percent of the subjects taking the wax-matrix preparation experienced no severe or moderate side effects as compared with only 50% of those taking the conventional tablets. PMID:4053146

Brock, C; Curry, H; Hanna, C; Knipfer, M; Taylor, L

1985-01-01

89

A comparative study of glycerin fatty acid ester and magnesium stearate on the dissolution of acetaminophen tablets using the analysis of available surface area  

Microsoft Academic Search

To study the effect of glycerin fatty acid ester (Poem TR-FB) concentrations on the dissolution rate of acetaminophen (APAP), the dissolution and disintegration behaviors of APAP tablets formulated using various lubricants were examined. The change over time in the available surface area of APAP (S(t)), which is in direct contact with solvent, was also analyzed using these dissolution data. In

Takeaki Uchimoto; Yasunori Iwao; Kana Takahashi; Shoko Tanaka; Yasuyoshi Agata; Takeru Iwamura; Atsuo Miyagishima; Shigeru Itai

2011-01-01

90

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

2013-08-27

91

Comparing the effects of three pre-treatment disintegration techniques on aerobic sludge digestion: biodegradability enhancement and microbial community monitoring by PCR-DGGE.  

PubMed

The objectives of this work were to compare and investigate the effect of three activated sludge disintegration processes before aerobic sludge digestion on 1) aerobic biodegradability enhancement and 2) microbial community evolution using the polymerase chain reaction-denaturant gel gradient electrophoresis (PCR-DGGE) technique. The comparison of three disintegration processes: thermal treatment (95 degrees C, 2h), sonication (100,000 kJ/kgTS) and ozonation (0.108 g O3/gTS) showed that the disintegration processes acted differently according to the composition of the soluble phase and to the DNA damage. Thermal treatment led to significant protein solubilization and to DNA modification. Sonication and ozonation resulted in similar soluble phase compositions and did not lead to any DNA modifications. During activated sludge aerobic digestion, intrinsic biodegradability enhancement was observed for thermal and ozone activated sludge pre-treatments. The analysis of the DGGE patterns at the end of aerobic digestion showed that population diversity was affected by both the aerobic digestion and the pre-treatment. The dissimilarity percentages measured at the end of aerobic digestion in the control sample and in the treated sludge were equal to 22, 25 and 20% for thermal treatment, sonication and ozonation respectively. This study indicated that PCR-DGGE could be a useful tool for the comparison of disintegration processes before and after aerobic digestion. PMID:22856319

Jaziri, Kais; Casellas, Magali; Dagot, Christophe

2012-06-01

92

Comparative anti-caries effects of tablet and liquid fluorides in cleft children.  

PubMed

Children with cleft lip and/or palate are at a higher risk for developing caries of the primary incisors compared with non-cleft children. To determine whether fluoride in tablet or liquid form would be more efficacious with children with cleft lip and/or palate, a two-year clinical investigation was conducted to test the anti-caries effects. One-hundred and fifteen cleft children (59 boys and 56 girls) between 22 and 26 months old were randomly selected into control, tablet and liquid fluoride groups. The amount of administered fluoride was 0.25 mg F daily in non-fluoridated Taiwan. Dental examinations were conducted using mirrors and #23 explorers. Caries were assessed using the DMF index in the baseline, first year and second year. The results showed that children in the tablet and liquid groups had a significantly lower DMFT increment than in the control group (p < 0.05). In the DMFS index, children in the liquid group showed a significantly lower caries increment than in the control group (p < 0.01), and children in the tablet group presented a borderline, but non-significant statistical difference when compared with the control group (p = 0.065). No significant statistical difference was found in either DMFT or DMFS between tablet and liquid fluoride administrations (p = 0.521 and p = 0.383, respectively). It is concluded that dietary fluoride supplements in liquid form show efficacy in reducing early childhood caries in the cleft children. Liquid fluoride showed slightly better numerical anti-caries effect than tablet fluoride, which is possibly due to its ease of administration with small children. PMID:11460274

Lin, Y T; Tsai, C L

2000-01-01

93

Tablets containing drug-loaded polymeric nanocapsules: an innovative platform.  

PubMed

The aim of the present work was to evaluate the feasibility to convert drug-loaded nanocapsule suspensions in a solid dosage form (tablets). Dexamethasone was used as a model drug due to its low aqueous solubility and fast drug release from conventional tablets. Granules containing dexamethasone-loaded nanocapsules were obtained by a wet granulation process using a dispersion of polyvinylpirrolidone/nanocapsules as a binder system. Granules were compressed in an eccentric compression machine (D-NC-T). A control formulation (tablets without nanocapsules) was also prepared (D-T). Tablets were characterized by means of mean weight, hardness, friability, diameter, thickness, disintegration time, drug content, morphological analysis by scanning electron microscopy (SEM), and in vitro drug release studies. D-NC-T showed adequate physicochemical characteristics according to the pharmacopeial requirements in terms of mean weight, hardness, friability, disintegration time and drug content. Intact nanocapsules in tablets were observed by SEM. In vitro drug release studies showed a slower release of dexamethasone from these tablets (D-NC-T) compared to the control formulation (D-T). Results showed that these tablets represent an interesting platform to the development of oral drug delivery systems containing polymeric nanocapsules. PMID:21133121

Friedrich, R B; Bastos, M O; Fontana, M C; Ourique, A F; Beck, R C R

2010-09-01

94

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.

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

2013-01-01

95

Efficacy of oral powder compared with chewable tablets for lanthanum carbonate administration in hemodialysis patients.  

PubMed

Lanthanum carbonate (LC) has been administered in a chewable tablet form for patients with hyperphosphatemia undergoing dialysis. However, some patients have difficulty chewing the tablets. LC oral powder has recently been released in Japan. The purpose of this study was to clarify the efficacy of LC oral powder form compared with that of chewable tablet form. The efficacy and safety of LC oral powder was retrospectively assessed in hemodialysis patients who switched from chewable tablet form to oral powder form without dose modification. Thirty-six patients (mean age, 66.8?±?10.5 years; male, 64%; 39% with diabetes; mean duration of dialysis treatment, 99.2?±?95.6 months) were enrolled in this study between June and July of 2012. Changes in clinical data and adverse events after the switch to oral powder form were investigated. The average dose of LC was 1180?±?520?mg/day. Serum phosphorus levels were significantly decreased after the switch from chewable tablet form to oral powder form (5.3?±?1.7?mg/dL at baseline vs. 4.9?±?1.2?mg/dL at after 1 month after, P?=?0.038). In contrast, no significant differences were observed in serum calcium and parathyroid hormone levels. Furthermore, no significant differences were evident in weight gain after the switch to oral powder form (2.5?±?1.2?kg at baseline vs. 2.4?±?1.1?kg at 1 month after the switch, P?=?0.29). No serious adverse events were recorded. Our results suggest that LC is more effective in oral powder form than chewable tablet form for hemodialysis patients. PMID:24134326

Sakurada, Tsutomu; Oishi, Daisuke; Shibagaki, Yugo; Yasuda, Takashi; Kimura, Kenjiro

2013-10-01

96

Material and tablet properties of pregelatinized (thermally modified) Dioscorea starches.  

PubMed

The material and tablet formation properties of pregelatinized (thermally modified) forms of four Dioscorea starches have been investigated. Dioscorea starches were pregelatinized followed by either oven drying (PS) or freeze drying (FD) and used as excipient in direct compression. The physicochemical, morphological and material properties of the pregelatinized starches have been investigated. The tablet formation properties were assessed using the 3-D modeling parameters, the Heckel equation and the force-displacement profiles. The tablet properties were evaluated using the elastic recovery, compactibility plots and the disintegration test. The results indicate that pregelatinization improved the compressibility and flowability of the Dioscorea starches. The high bulk and tap densities of PS coupled with their good flowability offer a unique possibility of the starches being used as filler in capsule formulations. The modified starches generally showed differences in their time and pressure dependent deformation behaviour. PS exhibited higher elasticity during tableting. FD Chinese and FD Bitter showed higher plasticity and low fast elastic deformation than the PS forms of the starches indicating that the FD starches undergo the highest plastic deformation. However, FD starches generally showed higher compactibility compared to the PS forms of the Dioscorea starches. While FD White and FD Water showed fast disintegration time and high compactibility, FD Chinese and FD Bitter were non-disintegrating and showed high compactibility. The high compactibility observed with the FD starches appears to be as a result of material change occurring during tableting probably due to the effect of temperature or pressure or a combination of both factors. Thus, FD White and FD Water starches could be useful when high crushing force and fast disintegration are of concern while FD Chinese and FD Bitter, which were non-disintegrating, could find application as excipients for controlled drug delivery. PMID:18562187

Odeku, Oluwatoyin A; Schmid, Wolfgang; Picker-Freyer, Katharina M

2008-04-24

97

Formulation and evaluation of aceclofenac mouth-dissolving tablet  

PubMed Central

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.

Solanki, Shailendra Singh; Dahima, Rashmi

2011-01-01

98

Improved calcium absorption from a newly formulated beverage compared with a calcium carbonate tablet  

Microsoft Academic Search

This trial assessed calcium excretion, as an indicator of calcium absorption, in 50 healthy men and postmenopausal women (ages 45-75), from a beverage containing calcium, magnesium, vitamins C, D, K, zinc, phosphorous, soy isoflavones, and inulin, compared with a calcium carbonate (CaCO3) tablet. At the end of each 4-week treatment period, subjects consumed a standardized low calcium meal plus the

Kevin C Maki; Mary R Dicklin; MarySue Cyrowski; Denise M Umporowicz; Yasuo Nagata; Grace Moon; Sam Forusz; Michael H Davidson

2002-01-01

99

????????????????????????????????????????????????????????????????????????????????? STUDY ON ANTIOXIDANT OF EXTRACTS FROM RICE BRAN TABLETS COMPARED WITH OTHERS  

Microsoft Academic Search

A comparative study of antioxidant activities of soft rice bran tablets (sRBT), which was formulated and processed for future use as a health product, , defatted rice bran (dRB), crude rice bran oil (cRBO) and refined rice bran oil (rRBO) by analyzing of scavenging effect on 1,1- diphenyl-2-picrylhydrazyl (DPPH) free radicals. The formulation of sRBT selected for investigations contained 200

Aroonsri Priprem; Padungkwan Chitropas; Pramote Mahakunakorn; Chidchanok Khamlert; Bungorn Sripanidkulchai

100

Development and validation of NIR-chemometric methods for chemical and pharmaceutical characterization of meloxicam tablets.  

PubMed

Abstract Context: Near-Infrared (NIR) spectroscopy is an important component of a Process Analytical Technology (PAT) toolbox and is a key technology for enabling the rapid analysis of pharmaceutical tablets. Objective: The aim of this research work was to develop and validate NIR-chemometric methods not only for the determination of active pharmaceutical ingredients content but also pharmaceutical properties (crushing strength, disintegration time) of meloxicam tablets. Materials and methods: The development of the method for active content assay was performed on samples corresponding to 80%, 90%, 100%, 110% and 120% of meloxicam content and the development of the methods for pharmaceutical characterization was performed on samples prepared at seven different compression forces (ranging from 7 to 45?kN) using NIR transmission spectra of intact tablets and PLS as a regression method. Results: The results show that the developed methods have good trueness, precision and accuracy and are appropriate for direct active content assay in tablets (ranging from 12 to 18 mg/tablet) and also for predicting crushing strength and disintegration time of intact meloxicam tablets. Discussion: The comparative data show that the proposed methods are in good agreement with the reference methods currently used for the characterization of meloxicam tablets (HPLC-UV methods for the assay and European Pharmacopeia methods for determining the crushing strength and disintegration time). Conclusion: The results show the possibility to predict both chemical properties (active content) and physical/pharmaceutical properties (crushing strength and disintegration time) directly, without any sample preparation, from the same NIR transmission spectrum of meloxicam tablets. PMID:23594301

Tomuta, Ioan; Iovanov, Rares; Bodoki, Ede; Vonica, Loredana

2013-04-17

101

Childhood Disintegrative Disorder  

MedlinePLUS

... may be reprinted for personal, noncommercial use only. Childhood disintegrative disorder By Mayo Clinic staff Original Article: http://www.mayoclinic.com/health/childhood-disintegrative-disorder/DS00801 Definition Symptoms Causes Preparing for ...

102

Attractiveness of reformulated OxyContin(R) tablets: assessing comparative preferences and tampering potential.  

PubMed

Reformulated OxyContin® (oxycodone HCl controlled-release or ORF) was developed as a tamper and abuse-deterrent product, to reduce the risk of product abuse, misuse and their consequences. This noninterventional single-session study asked participants who were medically-healthy recreational opioid users, aged 18 years and older, to consider how they would use commonly available supplies to tamper with placebo ORF and placebo original OxyContin (OC) tablets, and how they would assess the attractiveness of tampering and abusing ORF tablets, as compared with other opioid formulations. Participants provided information on past opioid use, and they assessed the properties of five nonhypothetical oxycodone products and two hypothetical oxycodone products. Participants provided feedback on tampering preferences, preferred tamper methods for each product, overall tampering potential and product preferences. We had 30 participants (27 males and 3 females; mean age 35 years, range 18-51) complete both the interview and tampering sessions. Participants judged OC as the most attractive, valuable, desirable and most likely to be tampered with, from among all opioid products studied. By contrast, they rated ORF as the least attractive, least valuable, least desirable, and least likely to be tampered with among all the nonhypothetical opioid products studied. These results suggested that recreational drug abusers view ORF tablets as tamper-deterrent products. PMID:23784739

Sellers, Edward M; Perrino, Peter J; Colucci, Salvatore V; Harris, Stephen C

2013-06-19

103

Comparative effects of xylitol- and sucrose-sweetened chew tablets and chewing gums on plaque quantity.  

PubMed

The effects of chewing gums and chew tablets sweetened with sucrose or xylitol on the quantity and adhesivity of dental plaque were studied with 14 volunteer dental students (mean age 23.2). The subjects participated in a four-phase study in which one of four different test products was used during each period. The 3-d periods were interspaced with 4-d normalization phases. The following four experimental products were tested: chewing gums (CG) and chew tablets (CT), sweetened with sucrose (s) or xylitol (x). The amount of plaque was determined through an automatic planimetric procedure on teeth treated with Dentotest. The total plaque areas before brushing were significantly larger in the CTs group compared with the CTx group. After brushing, the plaque areas remained larger in the CTs group. In the determination of the thick plaque areas, the use of CTx was associated with significantly smaller plaque scores than the use of CTs. In the adhesivity studies CGx consistently yielded the lowest plaque scores, but the differences between x and s were not significant. The comparison between CT and CG suggested that CTx produced significantly smaller plaque scores than CGx before brushing, but not after. This finding was considered to result from the differences involved in the texture and chemical composition between tablets and chewing gums. The present study showed that the use of CGx and CTx was associated with clinically more advantageous plaque effects than the use of corresponding products sweetened with sucrose. PMID:6952539

Rekola, M

1981-10-01

104

Absorption of folic acid from a softgel capsule compared to a standard tablet.  

PubMed

Consumption of 400 ?g folic acid per day from fortified foods and/or supplements, plus food folate from a varied diet is recommended for women of childbearing potential to reduce the risk for neural tube defects during fetal development. This randomized crossover study was designed to evaluate the bioavailability of folic acid from a multivitamin softgel capsule vs a folic acid tablet in 16 premenopausal women (18 to 45 years of age). Participants were randomly assigned to receive a single dose of ?1,000 ?g folic acid in two tablets or ?1,000 ?g folic acid in a multivitamin softgel capsule, and then crossed over to receive the other study product ?1 week later. Products were administered with a low-folate breakfast. Blood samples were collected predose (0 hour) and 1, 2, 3, 4, 6, and 8 hours post-dose for serum folate analysis. Repeated measures analysis of variance was used to compare responses between treatments. Data from the two sequence groups (n=8 per sequence) were pooled. Mean serum folate total and net incremental areas under the curve (AUC(0-8 hours)) were not significantly different between tablets and softgel capsule (AUC(0-8 hours) 214.9±11.2 hours×ng/mL [487±25.4 hours×nmol/L] and 191.6±13.3 hours×ng/mL [434.2±30.1 hours×nmol/L]; net incremental AUC(0-8 hours) 117.3±8.5 hours×ng/mL [265.8±19.3 hours×nmol/L] and 105.8±12.5 hours×ng/mL [239.7±28.3 hours×nmol/L], respectively), nor was maximum folate concentration (45.1±2.5 ng/mL [102.2±5.7 nmol/L] and 42.5±3.8 ng/mL [96.3±8.6 nmol/L], respectively). Time to peak folate concentration was significantly (P<0.001) delayed for the softgel capsule vs tablet (3.9±0.3 vs 1.7±0.2 hours, respectively). In conclusion, apparent bioavailability of folic acid was similar for the folic acid tablets and a multivitamin softgel capsule. PMID:22579722

Maki, Kevin C; Ndife, Louis I; Kelley, Kathleen M; Lawless, Andrea L; Brooks, James R; Wright, Shannon B; Shields, Jocelyn M; Dicklin, Mary R

2012-05-11

105

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.

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

2011-01-01

106

Tablet Splitting of a Narrow Therapeutic Index Drug: A Case with Levothyroxine Sodium  

PubMed Central

Levothyroxine is a narrow therapeutic index, and to avoid adverse effect associated with under or excessive dosage, the dose response is carefully titrated. The tablets are marketed with a score providing an option to split. However, there are no systematic studies evaluating the effect of splitting on dose accuracy, and current study was undertaken to evaluate effects of splitting and potential causes for uniformity failures by measuring assay and content uniformity in whole and split tablets. Stability was evaluated by assaying drug for a period of 8 weeks. Effect of formulation factors on splittability was evaluated by a systematic investigation of formulation factors by preparing levothyroxine tablets in house by varying the type of excipients (binder, diluent, disintegrant, glidant) or by varying the processing factors (granulating liquid, mixing type, compression pressure). The tablets were analyzed using novel analytical tool such as near infrared chemical imaging to visualize the distribution of levothyroxine. Assay was not significantly different for whole versus split tablets irrespective of method of splitting (hand or splitter), and splitting also had no measurable impact on the stability. Split tablets either by hand or splitter showed higher rate of content uniformity failures as compared to whole tablets. Tablet splitter produced more fragmentation and, hence, more content uniformity and friability failures. Chemical imaging data revealed that the distribution of levothyroxine was heterogeneous and was dependent on type of binder and the process used in the manufacture of tablets. Splitting such tablets could prove detrimental if sub- or super-potency becomes an issue.

Shah, Rakhi B.; Collier, Jarrod S.; Sayeed, Vilayat A.; Bryant, Arthur; Habib, Muhammad J.

2010-01-01

107

Orodispersible tablets: A new trend in drug delivery  

PubMed Central

The most common and preferred route of drug administration is through the oral route. Orodispersible tablets are gaining importance among novel oral drug-delivery system as they have improved patient compliance and have some additional advantages compared to other oral formulation. They are also solid unit dosage forms, which disintegrate in the mouth within a minute in the presence of saliva due to super disintegrants in the formulation. Thus this type of drug delivery helps a proper peroral administration in pediatric and geriatric population where swallowing is a matter of trouble. Various scientists have prepared orodispersible tablets by following various methods. However, the most common method of preparation is the compression method. Other special methods are molding, melt granulation, phase-transition process, sublimation, freeze-drying, spray-drying, and effervescent method. Since these tablets dissolve directly in the mouth, so, their taste is also an important factor. Various approaches have been taken in order to mask the bitter taste of the drug. A number of scientists have explored several drugs in this field. Like all other solid dosage forms, they are also evaluated in the field of hardness, friability, wetting time, moisture uptake, disintegration test, and dissolution test.

Dey, Paramita; Maiti, Sabyasachi

2010-01-01

108

Pharmaceutical evaluation of multipurpose excipients for direct compressed tablet manufacture: comparisons of the capabilities of multipurpose excipients with those in general use.  

PubMed

Recently, a novel type of multipurpose excipient (MPE) with high binding characteristics and high fluidity has been developed. In this study, the capabilities of MPEs (Ludipress and Microcelac) were compared with those of excipients in general use. Also, the effects on powder and tableting characteristics of the physical properties and contents of active ingredients were examined in tablets prepared with these MPEs by the direct compression method. Multipurpose excipients mixed with adjuvants such as fillers, binders, lubricants, disintegrants, and the like show superior fluidity and compressibility. Tablets containing very small amounts of highly active ingredients with little dispersion were prepared. However, with increases in active ingredient content, each of the physical properties was affected strongly by the properties of the active ingredient. Tablets with appropriate hardness and disintegration characteristics could be prepared by mixing of different types of MPEs. PMID:10434130

Goto, K; Sunada, H; Danjo, K; Yonezawa, Y

1999-08-01

109

Childhood Disintegrative Disorder  

Microsoft Academic Search

Childhood disintegrative disorder (CDD) is a clinical syndrome characterized by disintegration of mental functions and regression of acquired language and intellectual functions after a period of normal development typically of 3 to 4 years. Although recognized for many years, research on this condition is less advanced than that in autism. Epidemiological data are limited but the condition is much less

Savita Malhotra; Nitin Gupta

1999-01-01

110

Fluoride Tablets and Salivary Fluoride Levels  

Microsoft Academic Search

Mixed salivary fluoride levels have been measured after 9 subjects sucked or slowly dissolved three different brands of 1 mg F–– fluoride tablets. Results indicate that for all preparations the maximum salivary F–– concentration was obtained when a tablet was sucked rather than dissolved. However, salivary F–– retention was greatly enhanced under conditions which allowed undisturbed disintegration of each formulation.

D. McCall; K. W. Stephen; S. G. McNee

1981-01-01

111

Orally disintegrating olanzapine review: effectiveness, patient preference, adherence, and other properties  

PubMed Central

Orally disintegrating olanzapine (ODO) is a rapid-dissolving formulation of olanzapine which disintegrates in saliva almost immediately, developed as a convenient and adherence-enhancing alternative to the standard olanzapine-coated tablet (SOT). Clinical studies, which form the basis of this review, have shown ODO and SOT to have similar efficacy and tolerability profiles. However, ODO appears to have a number of advantages over SOT in terms of adherence, patient preference, and reduction in nursing burden. Overall, the existing clinical data suggests that compared to SOT, ODO is not only well-suited for difficult-to-treat, agitated, and/or nonadherent patients but, due to its potential ability to improve adherence and greater patient preference, may also be an appropriate formulation for the majority of patients for which olanzapine is the antipsychotic of choice.

Montgomery, William; Treuer, Tamas; Karagianis, Jamie; Ascher-Svanum, Haya; Harrison, Gavan

2012-01-01

112

A single blind normal volunteer bioavailability study of a new microencapsulated potassium chloride tablet compared with two reference potassium formulations  

Microsoft Academic Search

Summary  A single blind placebo controlled, cross-over study comparing a new microencapsulated potassium chloride tablet (MET) with\\u000a two reference formulations of oral potassium, potassium chloride solution (PS) and potassium chloride wax-matrix tablets (WMT),\\u000a was performed in 12 normal healthy volunteers. Urinary potassium excretion was the main criterion of comparison.\\u000a \\u000a \\u000a Results showed that all three formulations have excellent bioavailability. This indicates that

H. Caplain; R. Dahan; R. Pamphile; J. J. Thebault

1991-01-01

113

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

2013-03-27

114

Preparation and evaluation of medicinal carbon tablets with different saccharides as binders.  

PubMed

Medicinal carbon (MC) tablets were prepared with several saccharides to improve the formability and absorption ability of MC tablets made with maltitol (MT). The MC tablets were made by the wet granule compression method, in which maltitol, xylitol (XYL), mannitol (MAN), and sorbitol (SOR) were used as binders. Granule and tablet formability, tablet strength, disintegration, and MC adsorption potential were evaluated for each formulation. Acetaminophen (AA) was used in checking effect of binders on adsorption. Due to low water solubility, MAN was added only up to 30% (w/w) of MC; in greater concentrations, the tablet could not be formed. However, tablets formed easily when using XYL or SOR at 120% (w/w) of the MC amount. This result was similar for MT. The XYL, SOR, and MT tablets displayed sufficient hardness and rapid disintegration. The tensile strength of the SOR tablets exceeded that of the MT tablets, which in turn had greater tensile strength than the XYL tablets. In addition, the XYL tablets disintegrated more quickly than the MT tablets, which disintegrated more quickly than the SOR tablets. The MC adsorption capacity was slightly decreased by XYL and SOR, but to a lesser extent than the decrease caused by MT. Overall, XYL and SOR were superior to MT as binding agents for preparation of MC tablets. Therefore, we recommend preparing the tablets with XYL or SOR as a binder using the wet granule compression method to produce a compact dosage form of MC. PMID:19801858

Yamamoto, Kenta; Ito, Akihiko; Machida, Yoshiharu

2009-10-01

115

Development and evaluation of controlled-release diclofenac microspheres and tabletted microspheres.  

PubMed

Diclofenac wax microspheres were prepared using the congealable dispersephase encapsulation method. Emulsifiers, glyceryl monostearate (GMS) and stearic acid, were added to improve the efficiency of emulsification. Microspheres containing either of the emulsifiers or both showed a high drug content (80-90%) and the particle size distribution was log-normal compared with microspheres without the emulsifiers. Increase in GMS concentration decreased the drug release and, in contrast, stearic acid appeared to channel the drug from the wax matrix. The addition of both emulsifiers at different concentrations modified drug release. Increase in dispersant (PVP) concentration, and decrease in microsphere size accelerated the rate of drug release. Higuchi/Baker Londsdale spherical matrix dissolution kinetics was followed. Disintegrating tableted microspheres were prepared with Avicel and Explotab. With the increase in compression pressure the crushing force and disintegrating time increased, but the thickness decreased, and the dissolution profile did not appear to be affected. Slightly faster release was noticed with tableted microspheres compared with that of uncompressed microspheres. Tablets containing 40 and 60% microsphere loadings had disintegration times of 5.12 +/- 0.63 and 57.73 +/- 3.53 min, respectively. In contrast, tablet formulation containing 80% microsphere load had a significant increase in disintegration time (130.83 +/- 4.26 min). The dissolution from this formulation also showed a lag time of 30 min in contrast with the other two formulations, which showed no lag time. Increased microsphere size from 215 to 630 microns had no effect on tableting properties (such as hardness and thickness); and only very little effect on dissolution. The microspheres appeared deformed but intact irrespective of compression pressures on scanning electron micrographs. PMID:7931945

Vilivalam, V D; Adeyeye, C M

116

Comparative bioavailability study of cefuroxime axetil (equivalent to 500 mg cefuroxime/tablet) tablets (Zednad® versus Zinnat®) in healthy male volunteers.  

PubMed

This study was performed to investigate the bioequivalence of cefuroxime axetil tablets between a generic test product (A) Zednad® Tablet (500 mg cefuroxime/ tablet, Diamond Pharma, Syria), and the Reference Product (B) Zinnat® Tablet (500 mg cefuroxime/tablet, GlaxoSmithKline, Saudi Arabia). The bioavailability study was carried out for 24 healthy male volunteers. The subjects received 1 Zednad® Tablet (500 mg/ tablet) and 1 Zinnat® Tablet (500 mg/tablet) in a randomized, two-way crossover design fashion on 2 treatment days, after an overnight fast of at least 10 h, with a washout period of 7 days. 24 volunteers plus 2 alternatives completed the crossover. The bioanalysis of clinical plasma samples was accomplished by HPLC method, which was developed and validated in accordance with international guidelines. Pharmacokinetic parameters, determined by standard non-compartmental methods, and ANOVA statistics were calculated using SAS Statistical Software. The significance of a sequence effect was tested using the subjects nested in sequence as the error term. The 90% confidence intervals for the ratio between the test and reference product pharmacokinetic parameters of AUC0?t, AUC0??, and Cmax were calculated and found to be within the confidence limits of 80.00 - 125.00% for AUC0?t, AUC0?? and Cmax. The study demonstrated that the test product (A) was found bioequivalent to the reference product (B) following an oral dose of 500 mg tablet. Therefore, the two formulations were considered to be bioequivalent. PMID:21888870

Asiri, Y A; Al-Hadiya, B M; Kadi, A A; Al-Khamis, K I; Mowafy, H A; El-Sayed, Y M

2011-09-01

117

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

118

Comparative study of chewable pyrantel pamoate: should standards for chewable tablets be revised?  

PubMed

Chewable pyrantel pamoate tablets were administered to children randomly assigned to three treatment groups. Individuals in each group were instructed either to swallow whole, to chew and swallow, or to swallow previously pulverized tablets. With respect to Ascaris, results of posttreatment stool examinations indicated no differences in cure rates and egg reduction rates between the different modes of treatment. However, for both hookworm and Trichuris, mean egg counts increased for both swallow and chew groups, but decreased in the pulverized group. In addition to the highest egg reduction rates, the most parasitological cures were also seen in the pulverized group for these two worms. The status of standards for chewable tablets is discussed. Until the standards are changed it is recommended that all chewable tablets be crushed before swallowing. PMID:7863722

Wesche, D; Lutz, S; Barnish, G

1994-03-01

119

Methadone toxicity: comparing tablet and syrup formulations during a decade in an academic poison center of Iran.  

PubMed

Abstract Context. Due to an increase in the number of methadone maintenance clinics in the past decade in Iran, acute methadone overdose has become one of the common poisonings in our society. Objective. To compare the characteristics of methadone poisoning between syrup and tablet formulation as well as to discuss the relative advantages and disadvantages of poisoning from the perspective of toxicity. Material and methods. In a retrospective cross-sectional study from 2000 to 2010, sampled data of all hospitalized methadone-overdosed patients were collected through chart review of hospital records. Concurrently, the total number of methadone sales was gathered. Results. A total of 1426 patients with methadone poisoning had been hospitalized, including 1072 cases who consumed syrup or tablet solely. Mean ± SD milligram ingested dose of syrup and tablet were 153 ± 339 and 88 ± 274, respectively (p < 0.001). The mean time elapsed since ingestion was 9 ± 9 and 7 ± 7 h, respectively. Most of the accidental poisoning cases occurred as a result of syrup formulation, particularly by children under 12 years old after being mistaken for cough mixture or water. Conversely, exposure to methadone tablets was more common in patients with suicidal intent. There was no statistically significant difference between the rates of intubation and death between the two groups. Discussion. Higher doses of methadone in the syrup form appear to exert a similar severity of poisoning and outcomes compared to lesser doses of that in the tablet form. Similarities in outcomes, despite differences in exposure history, may reflect relatively prompt transfer to hospital and adequate provision of clinical care, including supportive care and naloxone. Conclusion. In order to reduce the rate of poisoning, we recommend the use of child-resistant containers for dispensing syrup, reduction in methadone concentration, adding a coloring agent, special flavor, and education of patients on the safe storage of methadone in their home in order to reduce the occurrence of accidental poisonings. PMID:23972442

Shadnia, S; Rahimi, M; Hassanian-Moghaddam, H; Soltaninejad, K; Noroozi, A

2013-08-23

120

A COMPARATIVE STUDY OF DISSOLUTION CHARACTERISTICS OF POLYMERIC AND WAX GRANULATIONS OF THEOPHYLLINE AND THEIR TABLETS  

Microsoft Academic Search

Matrix (non disintegrating) granules of theophylline have been formed and their dissolution characteristics investigated for sustained release application. The polymeric granulations were formed by massing the drug powder with a concentrated (40%w\\/w) ethanolic solution of an acrylatemethacrylate copolymer (ERS100 R ). Wax granulations were also formed by massing the drug powder with previously melted carnuba wax followed by screening and

MICHAEL U UHUMWANGHO; ROLAND S OKOR

121

Development and in vitro evaluation of ibuprofen mouth dissolving tablets using solid dispersion technique.  

PubMed

The aim of present study was to prepare and evaluate mouth dissolving tablets of ibuprofen (IBU). Ternary solid dispersion (SD) of IBU was prepared using PEG 4000 as carrier and Tween 80 as surfactant. The SD formulations were prepared by solvent evaporation and melt solvent method by varying ratio of PEG 4000. Different weight ratio of carrier, drug and surfactant 5 : 5 : 1, 10 : 5 : 1, 25 : 5 : 1, 35 : 5 : 1 and 45 : 5 : 1 was taken. The prepared SD formulations were characterized by Fourier Transform Infra-Red (FT-IR) spectroscopy, differential scanning calorimetry (DSC), X-ray diffraction (XRD) and in vitro drug release. Mouth dissolving tablets of IBU were formulated using optimized SD formulation of carrier : drug : surfactant ratio, 10 : 5 : 1 along with super-disintegrants. The best developed formulation was compared with marketed tablet product of IBU. From IR and XRD studies, it may be concluded that there is change in crystalline form of drug into amorphous during formation of SD. From DSC studies, it was predicted that drug was completely dissolved in the carrier. Mouth dissolving tablets containing Ac-Di-Sol (12%) as super-disintegrant showed the fastest disintegration (202s) and in vitro drug release (84.57%). The release pattern of all developed formulations followed Peppas-Korsmeyer model as the plot between log cumulative % drug released versus log time showed good linearity (r>0.99) with a comparatively high slope (n) value within the range of 0.44-0.67. The tablets containing SD exhibited better dissolution profile than commercial tablets. PMID:20686256

Jain, Sunil Kumar; Shukla, Meenakshi; Shrivastava, Vivek

2010-08-01

122

Studies on cyclodextrin polymer. Part 1: The effect of CDP on indomethacin tablet formulation.  

PubMed

Cyclodextrin polymer (CDP), which is a cross-linked derivative of beta-cyclodextrin, has been used as binder and disintegrating agent in tablet formulation. In this study different tablet formulations of indomethacin, which is a nonsteroid anti-inflammatory drug were prepared by direct compression method. Corn starch, lactose and Esma-Spreng were used besides CDP as disintegrating agent. The hardness, friability, disintegration time and dissolution rate of the tablet were determined. The data were also evaluated kinetically. It was found that CDP is a good disintegrating agent and significantly increased the dissolution rate of the poorly soluble indomethacin. PMID:3174808

Tarimci, N; Celebi, N

1988-05-01

123

Tramadol\\/acetaminophen combination tablets and codeine\\/acetaminophen combination capsules for the management of chronic pain: a comparative trial  

Microsoft Academic Search

Background: Opioid\\/acetaminophen (APAP) combination analgesics are widely prescribed for the relief of moderate pain. Tramadol is a synthetic analgesic that has been shown to be effective both alone and in combination with APAP.Objective: The purpose of this study was to compare the efficacy and tolerability of tramadol\\/APAP tablets with codeine\\/APAP capsules.Methods: This 4-week, randomized, double-blind, parallel-group, active-control, double-dummy, multicenter trial

William S Mullican; Joseph R Lacy

2001-01-01

124

Double-blind randomized multicenter study comparing Maalox TC tablets and ranitidine in healing of duodenal ulcers  

Microsoft Academic Search

The efficacy of ranitidine 150 mg twice daily and Maalox TC three tablets four times daily were compared in patients with endoscopically confirmed duodenal ulcer. Seventy-nine patients were randomly allocated to double-blind, double-dummy treatment, stratified for smokers. Endoscopy was repeated after four weeks. Those unhealed continued treatment for a further two weeks before final endoscopy. Per protocol analysis in 53

J. O. Hunter; R. J. Walker; J. Crowe; R. R. Gillies; K. R. Gillies; K. R. Gough; S. Lorber

1991-01-01

125

A multinational, multicentre, non-blinded, randomized study of moxifloxacin oral tablets compared with co-amoxiclav oral tablets in the treatment of acute exacerbation of chronic bronchitis.  

PubMed

The aim of this study was to compare the efficacy and safety of once daily dosing with moxifloxacin (BAY 12-8039) with that of coamoxiclav given three times daily for the treatment of acute exacerbation of chronic bronchitis (AECB). Moxifloxacin (one 400 mg tablet daily) was administered orally for 5 days and co-amoxiclav (three 625 mg tablets daily) was given orally for 7 days. The study was randomized, non-blinded, multinational (12 countries) and multicentre (68 centres). A total of 575 patients, all with clear signs of AECB, were treated, 292 with moxifloxacin and 283 with co-amoxiclav. Of these, 512 patients were evaluable for efficacy (261 in the moxifloxacin group and 251 in the co-amoxiclav group). The primary efficacy parameter was clinical response at 14 days in the evaluable population. A clinical success was classified as resolution or improvement of symptoms. Variables used to assess clinical response included wheeze, cough, dyspnoea, sputum volume, rales and rhonchi. The success rate for moxifloxacin in the evaluable patients was 96.2% and that for co-amoxiclav was 91.6%. The 95% confidence intervals for this difference (0.4%; 8.7%) indicate equivalence in the treatments. Sputum samples were taken from patients and 140 of these contained a pathogen, Haemophilus influenzae being the most frequently isolated. Moraxella catarrhalis and Streptococcus pneumoniae were also commonly isolated pathogens. The eradication rate at 14 days in the evaluable patients was 87.7% in the moxifloxacin group and 89.6% in the coamoxiclav group. Both drugs were well tolerated with no significant differences in the numbers of drug-related adverse events or the numbers of patients withdrawing because of an adverse event. These results and the broad spectrum of antibacterial activity make moxifloxacin a promising and safe alternative to conventional therapy for the empirical treatment of AECB. PMID:11675905

Schaberg, T; Ballin, I; Huchon, G; Bassaris, H; Hampel, B; Reimnitz, P

126

A single blind normal volunteer bioavailability study of a new microencapsulated potassium chloride tablet compared with two reference potassium formulations.  

PubMed

A single blind placebo controlled, cross-over study comparing a new microencapsulated potassium chloride tablet (MET) with two reference formulations of oral potassium, potassium chloride solution (PS) and potassium chloride wax-matrix tablets (WMT), was performed in 12 normal healthy volunteers. Urinary potassium excretion was the main criterion of comparison. Results showed that all three formulations have excellent bioavailability. This indicates that potassium absorption in the stomach is similar to that in more distant portions of the gut. The slow-release characteristics of both MET and WMT were confirmed. Clinical and pharmacological tolerance was excellent and no side-effects were reported with any of the potassium formulations studied. PMID:1814742

Caplain, H; Dahan, R; Pamphile, R; Thebault, J J

127

Orally disintegrating systems: innovations in formulation and technology.  

PubMed

Orally disintegrating systems have carved a niche amongst the oral drug delivery systems due to the highest component of compliance they enjoy in patients especially the geriatrics and pediatrics. In addition, patients suffering from dysphagia, motion sickness, repeated emesis and mental disorders prefer these medications because they cannot swallow large quantity of water. Further, drugs exhibiting satisfactory absorption from the oral mucosa or intended for immediate pharmacological action can be advantageously formulated in these dosage forms. However, the requirements of formulating these dosage forms with mechanical strength sufficient to with stand the rigors of handling and capable of disintegrating within a few seconds on contact with saliva are inextricable. Therefore, research in developing orally disintegrating systems has been aimed at investigating different excipients as well as techniques to meet these challenges. A variety of dosage forms like tablets, films, wafers, chewing gums, microparticles, nanoparticles etc. have been developed for enhancing the performance attributes in the orally disintegrating systems. Advancements in the technology arena for manufacturing these systems include the use of freeze drying, cotton candy, melt extrusion, sublimation, direct compression besides the classical wet granulation processes. Taste masking of active ingredients becomes essential in these systems because the drug is entirely released in the mouth. Fluid bed coating, agglomeration, pelletization and infusion methods have proven useful for this purpose. It is important to note that although, freeze dried and effervescent disintegrating systems rapidly disintegrate in contact with fluids, they do not generally exhibit the required mechanical strength. Similarly, the candy process cannot be used for thermolabile drugs. In the light of the paradoxical nature of the attributes desired in orally disintegrating systems (high mechanical strength and rapid disintegration), it becomes essential to study the innovations in this field and understand the intricacies of the different processes used for manufacturing these systems. This article attempts at discussing the patents relating to orally disintegrating systems with respect to the use of different formulation ingredients and technologies. PMID:19075912

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

2008-01-01

128

Comparative study of netbooks and tablet PCs for fostering face-to-face collaborative learning  

Microsoft Academic Search

With the recent appearance of netbooks and low-cost tablet PCs, a study was undertaken to explore their potential in the classroom and determine which of the two device types is more suitable in this setting. A collaborative learning activity based on these devices was implemented in 5 sessions of a graduate engineering course of 20 students, most of whom were

Claudio Alvarez; Christian Brown; Miguel Nussbaum

2011-01-01

129

Childhood Disintegrative Disorder.  

ERIC Educational Resources Information Center

|This article reviews what is known about childhood distintegrative disorder (CDD), a clinical syndrome characterized by disintegration of mental functions and regression of acquired language and intellectual functions after a period (usually 3-4 years) of normal development. It reviews the condition's epidemiology, onset and progression,…

Malhotra, Savita; Gupta, Nitin

1999-01-01

130

Spray-dried cellulose nanofibers as novel tablet excipient.  

PubMed

The purpose of this study was to evaluate the potential of cellulose nanofibers (also referred as microfibrillated cellulose, nanocellulose, nanofibrillated, or nanofibrillar cellulose) as novel tabletting material. For this purpose, physical and mechanical properties of spray-dried cellulose nanofibers (CNF) were examined, and results were compared to those of two commercial grades of microcrystalline cellulose (MCC), Avicel PH101 and Avicel PH102, which are the most commonly and widely used direct compression excipients. Chemically, MCC and CNF are almost identical, but their physical characteristics, like mechanical properties and surface-to-volume ratio, differ remarkably. The novel material was characterized with respect to bulk and tapped as well as true density, moisture content, and flow properties. Tablets made of CNF powder and its mixtures with MCC with or without paracetamol as model compound were produced by direct compression and after wet granulation. The tensile strength of the tablets made in a series of applied pressures was determined, and yield pressure values were calculated from the measurements. With CNF, both wet granulation and direct compression were successful. During tablet compression, CNF particles were less prone to permanent deformation and had less pronounced ductile characteristics. Disintegration and dissolution studies showed slightly faster drug release from direct compression tablets with CNF, while wet granulated systems did not have any significant difference. PMID:22005956

Kolakovic, Ruzica; Peltonen, Leena; Laaksonen, Timo; Putkisto, Kaisa; Laukkanen, Antti; Hirvonen, Jouni

2011-10-18

131

A study of the properties of tablets from coprocessed dry binders composed of alpha-lactose monohydrate and different types of cellulose.  

PubMed

The paper evaluates the differences between the properties of tablets from two coprocessed dry binders based on alpha-lactose monohydrate and cellulose, MicroceLac 100 and Cellactose 80. The substances differ in the type of contained cellulose; MicroceLac 100 contains 25% of microcrystalline cellulose, Cellactose 80, 25% of powdered cellulose. The properties under study included the tensile strength and disintegration time in dependence on compression force, addition of two concentrations of the lubricant sodium stearylfumarate (Pruv) and a 50% addition of the active ingredients ascorbic acid and acetylsalicylic acid. Using one of the compression forces, the effect of Pruv and magnesium stearate on the above-mentioned properties were compared. In the compression forces of 6 and 8 kN the strength of the compacts from pure Cellactose 80 was lower than that of those from MicroceLac 100 both without and with the lubricant. The lubricant sensitivity of dry binders depended on compression force. Pruv decreased the strength of compacts less than magnesium stearate. The tablets from Cellactose 80 possessed a longer disintegration time than those from MicroceLac 100, excepting the tableting materials containing 0.4 Pruv with a compression force of 6 kN. Disintegration time was prolonged with the use of sodium stearylfumarate and it was increased with compression force much more markedly in the case of Cellactose 80. In the presence of ascorbic acid, the strength of tablets was decreased in the case of both dry binders, but it was higher with MicroceLac100, disintegration time was very short and independent of the type of the dry binder. In the case of acetylsalicylic acid, the strength of tablets was higher with a lesser influence of the type of the dry binder, and disintegration time was longer and especially in the case of Cellactose 80 increased with increasing concentration of Pruv. PMID:18257417

Muzíková, J; Zvolánková, J

2007-12-01

132

Evaluation of a novel sugar coating method for moisture protective tablets.  

PubMed

A novel method of manufacturing one-step dry-coated (OSDRC) tablets, which we recently invented, was used to produce sugar-coated tablets protected from moisture without the need for a conventional complicated sugar coating process. Amorphous sucrose was selected for the outer layer of the OSDRC tablets as sugar-coated layer. The isothermal crystallization behavior and characteristics such as water vapor permeability, tensile strength, and disintegration time of compressed amorphous sucrose were investigated. Water vapor adsorption measurements showed the crystallization behavior of amorphous tablets to be similar to that of amorphous powder, although it was affected by compression pressure. We found that the crystallized amorphous sucrose after compression at 200 MPa was moisture protective, and the water vapor permeability coefficient was decreased to 1/2000 or less compared with a tablet prepared with a lactose-microcrystalline cellulose (MCC) mixture, hydroxypropylmethylcellulose (HPMC), and sucrose crystal. The water vapor permeability and physicochemical characteristics were influenced by the amorphous content or additive content. It was confirmed that a new sugar-coated tablet using amorphous sucrose and OSDRC technology was moisture protective, therefore, it was concluded that the novel sugar coating method was very useful to obtain a moisture protective tablet. PMID:17258875

Ando, Masaki; Ito, Rina; Ozeki, Yuichi; Nakayama, Yukiharu; Nabeshima, Toshitaka

2006-12-16

133

Formulation and evaluation of bi-layer tablet of metoclopramide hydrochloride and ibuprofen.  

PubMed

The aim of this study was to prepare bi-layer tablet of Metoclopramide Hydrochloride (MTH) and Ibuprofen (IB) for the effective treatment of migraine. MTH and IB were formulated as immediate and sustained release layer respectively. MTH was formulated as immediate release layer by using various disintegrants like Ac-Di-Sol, Polyplasdone XL, Explotab, Agar and Gellan Gum. Treated form of gellan gum and agar was prepared and compared for their disintegrant efficiency with other disintegrants. IB was formulated as sustained release layer using hydrophilic matrix (hydroxypropylmethylcellulose [HPMC K(4)M]). The effect of concentration of hydrophilic matrix (HPMC K(4)M), binder (polyvinylpyrollidone [PVP K(30)]) and buffer (sodium bicarbonate) on IB release was studied. The dissolution study of sustained release layer showed that an increasing amount of HPMC or PVP K(30) results in reduced IB release. The inclusion of buffer (sodium bicarbonate) enhanced the release of IB from sustained release layer. The rational for formulation of bi-layer tablet of these two drugs in combination was (1) MTH increases the absorption of acidic non-steroidal anti-inflammatory drug (NSAID) by increasing gastric motility. So sequential release of MTH (as immediate release) and IB (as sustained release) was suitable for treatment of migraine. (2) MTH was degraded when prolonged contact with acidic NSAID. Bi-layer tablet was suitable for preventing direct contact of these two drugs and thus to maximize the efficacy of combination of two drugs for migraine. PMID:18612830

Shiyani, Bhavesh; Gattani, Surendra; Surana, Sanjay

2008-07-09

134

Effect of polymer, plasticizer and filler on orally disintegrating film.  

PubMed

Abstract Context: Difficulty in swallowing tablets or capsules has been identified as one of the contributing factors to non-compliance of geriatric patients. Although orally disintegrating tablet was designed for fast disintegration in mouth, the fear of taking solid tablets and the risk of choking for certain patient populations still exist. Objective: The objective of this study was to develop and characterize orally disintegrating film (ODF), which was prepared using different combinations of polymers, plasticizers and fillers. Materials and methods: Effects of hydroxypropyl methylcellulose (HPMC), polyethylene glycol 400 (PEG 400), glycerin, polyvinyl pyrrolidone (PVP), mannitol and microcrystalline cellulose (MCC) on physical property of ODF formed were studied. The ODF was prepared using the solvent casting method. Results: Increase in HPMC concentration formed ODF with greater tensile strength. Incorporation of plasticizer (PEG 400 and glycerin) reduced tensile strength but increased elasticity of the ODF formed. PVP increased both tensile strength and elasticity of the ODF. Increase in MCC:mannitol ratio reduced the tensile strength and elasticity of the ODF. Disintegration time of film decreased corresponding to decrease in tensile strength of the film. Formulation R with the optimum tensile strength (13.10?N/mm(2)), bending flexibility (40 times) and disintegration time (41.50?s) was chosen as final formulation. A total of 80% of the drug was released within five minutes and the ODF was stable at least for one year actual condition. Conclusion: An ODF containing donepezil HCl was developed and characterized. The donepezil HCl ODF has the potential to improve the compliance of Alzheimer disease patients. PMID:23311593

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

2013-01-11

135

Use of aerosil for tableting some hydrophobic medicinal preparations  

Microsoft Academic Search

In view of the properties mentioned above, in this work we used aerosil for the preparation of tablets of Ethoxide, Nigeksin, and Methisazone with disintegration properties satisfying the requirements of GFX. (Aerosil has been approved for use as a filler for the tableting of medicinal preparations by the Pharmacological Committee of the Ministry of Health, April 5, 1968, Report No.

L. P. Volkovinskaya; N. A. Koroleva; E. A. Ivanovskaya; A. M. Pozharskaya

1970-01-01

136

Pharmacokinetics and relative bioavailability after single dose administration of 25 mg ketoprofen solution as compared to tablets.  

PubMed

The relative bioavailability of ketoprofen from a liquid formulation as compared to a tablet formulation as reference after single oral dose administration was investigated in 16 healthy male subjects. The subjects received in a randomized, crossover design during one study period of 5 days 2.5 mg of ketoprofen as tablet or liquid formulation administered as single dose with a washout interval of 48 h. The plasma concentrations of S(+)- and R(-)-ketoprofen were determined before and up to 24 h post-administration. S(+)- and R(-)-ketoprofen in the collected plasma samples was determined using an internally standardized validated HPLC method. Regarding the geometric mean concentration-time courses there were no relevant differences between the two ketoprofen enantiomers for both formulations. Remarkable differences in the shape of concentration-time courses between the two formulations were found with higher Cmax (by about 70%) and earlier tmax (by 15 min) values for the ketoprofen solution. The treatments were widely equivalent with regard to AUC. The quotients of geometric means as well as 90% confidence intervals for AUC of R(-)-ketoprofen were 95.72% (92.55-99.00%) and for S(+)-ketoprofen 94.23% (89.91-98.76%). The administration of the ketoprofen solution resulted earlier in higher concentrations (by about 70%) for both enantiomers, whereas the extent of absorption expressed by AUC was nearly the same (about 95%) as compared to the equimolar tablet formulation. The differences between the two formulations for Cmax,norm and tmax were statistically significant. PMID:7674700

Stiegler, S; Birkel, M; Jost, V; Lange, R; Lücker, P W; Wetzelsberger, N

1995-03-01

137

Evaluation of the effects of khaya gum on the mechanical and release properties of paracetamol tablets.  

PubMed

A study of the comparative effects of khaya gum and two standard binding agents-polyvinylpyrrolidone (PVP) and gelatin--on crushing strength and friability, and the disintegration and dissolution characteristics of paracetamol tablets was made. The crushing strength-friability ratio (CSFR), the disintegration times, D, and the dissolution times t50, t90, and t1 (derived from the equation of Noyes and Whitney), all increased with an increase in binder concentration; however, the dissolution rate constants, k1 and k2, decreased. The ranking for the values of CSFR for tablets containing the different binders was PVP > gelatin > khaya gum. The ranking for D and the dissolution times was gelatin > khaya gum > PVP, whereas the ranking for the dissolution rate constants was PVP > khaya gum > gelatin. There were significant linear correlations between CSFR, D, t50, t90, and t1 for the tablets. There were also significant correlations between k1 and D, t50, t90, and t1, and between k2 and t90. The results suggest that khaya gum could be useful as an alternative binding agent to produce tablets with particular mechanical strength and drug release profiles. PMID:12741612

Odeku, O A; Itiola, O A

2003-03-01

138

Fast dispersible\\/slow releasing ibuprofen tablets  

Microsoft Academic Search

Eight formulations were developed containing ibuprofen in the form of orally disintegrating tablets. To prevent bitter taste and side effects of the drug, the drug was associated with Phospholipon 80H, a saturated lecithin, by wet granulation. The granules were then coated using different film forming agents (Kollicoat SR 30, Amprac 01, Kollidon 90F, Eudragit RD 100) obtaining four lots 1–4.

Adamo Fini; Valentina Bergamante; Gian Carlo Ceschel; Celestino Ronchi; Carlos Alberto Fonseca de Moraes

2008-01-01

139

Medicinal carbon tablets for treatment of acetaminophen intoxication: adsorption characteristics of medicinal carbon powder and its tablets.  

PubMed

Adsorption characteristics of medicinal carbon powder (JP 14) for acetaminophen were examined at 37 degrees C using conventional incubation in an attempt to obtain an effective oral dosage form. Hydroxypropyl cellulose (HPC) and maltitol (MT), being able to act as a binding agent, were tested as additives. Tablets of medicinal carbon were produced by the wet granulation method. The rate and extent of adsorption of the medicinal carbon powder were roughly similar in water, JP 14 1st fluid (pH 1.2) and JP 14 2nd fluid (pH 6.8). The relationship between concentrations of free and adsorbed acetaminophen indicated that the adsorption followed the Langmuir mode. The maximal adsorption of acetaminophen in water was 0.219 g per gram medicinal carbon powder, little influenced by the addition of MT, but slightly reduced by the addition of HPC. The tablet prepared using MT as a binding agent displayed a favorable hardness and adequate disintegration time. The tablet showed good adsorption potential for acetaminophen, though the adsorption rate and extent of the tablet were reduced to some extent as compared with powder. PMID:16508192

Yamamoto, Kenta; Onishi, Hiraku; Ito, Akihiko; Machida, Yoshiharu

2006-03-01

140

Failure analysis of disintegrator beaters  

Microsoft Academic Search

Fatigue failure analysis of two of 36 disintegrator’s beaters is presented. The beaters assembly was fixed on a shaft rotating at 750rpm. The beater material was low carbon low alloy steel with bainitic structure. The failure analysis was performed on the ground of metallographic examination using light microscopy, scanning electron microscopy (SEM) and estimation of stress concentration using finite element

B. Ku?nicka; P. Stró?yk

2006-01-01

141

Disintegration of liquid sheets  

NASA Astrophysics Data System (ADS)

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

1990-05-01

142

Mechanical disintegration of sewage sludge.  

PubMed

Mechanical disintegration can be used for an accelerated and improved anaerobic digestion of excess sludge. The hydrolysis is the limiting step of this process. Mechanical disintegration can be used to disrupt the cell walls and to cause the release of the organic material from the cells. Particle size analysis describes the size reduction but is not suitable for characterising the release of the organic material and the cell disruption. Two biochemical methods were developed for these phenomena. One of the parameters provides information about the disruption of micro-organisms, the other one gives information about the release of organic material. Different ultrasonic homogenizers, a high pressure homogenizer and stirred ball mills were used for disintegration experiments using various parameters. The influences of a mechanical disintegration on the particle size and of the energy intensity on the disintegration were investigated. Further investigations had to detect the influence of the solid content on the disintegration results. For sludge with a higher solid content better results in terms of energy consumption could be achieved. An optimum of the bead diameter and the stress intensity in stirred ball mills could be detected. A comparison of the results of different methods of sludge disintegration shows that the investigated ultrasonic homogenizers are inferior to a high pressure homogenizer and a stirred ball mill in terms of energy consumption. PMID:11379090

Lehne, G; Müller, A; Schwedes, J

2001-01-01

143

Significant improvements in self-reported gastrointestinal tolerability, quality of life, patient satisfaction, and adherence with lopinavir\\/ritonavir tablet formulation compared with soft gel capsules  

Microsoft Academic Search

BACKGROUND: The tablet formulation of ritonavir-boosted lopinavir (LPV\\/r; Kaletra®) has many advantages over the soft gel capsule (SGC) formulation, including lower pill count, no refrigeration requirement, and no dietary restrictions. These advantages may help improve patient compliance and therefore increase adherence to treatment. However, there are limited data regarding patient preferences and only recently was the comparative efficacy and tolerability

Shannon Schrader; Susan K Chuck; Laurie W Rahn; Paras Parekh; Katherine G Emrich

2008-01-01

144

Formulation of fast disintegrating tablets of ternary solid dispersions consisting of TPGS 1000 and HPMC 2910 or PVPVA 64 to improve the dissolution of the anti-HIV drug UC 781  

Microsoft Academic Search

Solid dispersion formulations made up of d-?-tocopheryl polyethylene glycol succinate 1000 (TPGS 1000) and polyvinyl pyrrolidone co-vinyl acetate 64 (PVPVA 64) or hydroxy propyl methyl cellulose 2910 (HPMC 2910) were developed in order to improve the dissolution of UC 781. UC 781 dissolution rate was markedly improved as compared to the physical mixtures and the pure drug, attaining maximum drug

Caroline Goddeeris; Tom Willems; Guy Van den Mooter

2008-01-01

145

Studies on the response of nitroglycerin oral spray compared with sublingual tablets for angina pectoris patients with dry mouth. A multicenter trial.  

PubMed

Nitroglycerin (glyceryl trinitrate, CAS 55-63-0, NTG) administered with an oral spray may be more effective in relieving anginal pain than sublingual tablets especially when the patient's mouth is dry. In this study, the effect of a NTG oral spray (Myocor Spray) on exercise-induced angina was compared with that of a sublingual tablet in relation to the oral dryness. In 17 patients with effort angina, graded bicycle exercise was performed twice at an interval of one week. Exercise was discontinued upon the onset of moderate anginal pain. Immediately after exercise, the oral dryness was evaluated by touching the tip of the tongue with a blotting paper for a moment. Then, 0.3 mg of NTG was administered by either a squirt of spray or a sublingual tablet in a randomized crossover fashion. Exercise results were reproducible between two exercise tests. According to the extent of the wet area of the blotting paper, the subjects were divided into two groups. In 7 patients of the wet group, the remission times of chest pain and ST segment depression were not significantly different by the formulation of NTG. In 10 patients of the dry group, however, both chest pain and ST depression more rapidly recovered with use of the oral spray (p < 0.05 and p < 0.05, respectively). These results strongly suggest that the NTG oral spray is superior to the sublingual tablet in relieving anginal attacks, when the oral wetness is decreased. PMID:9079231

Sato, H; Koretsune, Y; Taniguchi, T; Fukui, S; Shimazu, T; Sugii, M; Matsuyama, T; Karita, M; Hori, M

1997-02-01

146

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.

Sabale, Vidya; Patel, Vandana; Paranjape, Archana

2012-01-01

147

Porous magnesium aluminometasilicate tablets as carrier of a cyclosporine self-emulsifying formulation.  

PubMed

The aim of this study was to investigate the ability of liquid loadable tablets (LLT) to be loaded with a self-microemulsifying drug delivery system (SMEDDS) containing cyclosporine (CyA). LLT were prepared by direct compression of the porous carrier magnesium aluminometasilicate and subsequently loaded with SMEDDS by a simple absorption method. SMEDDS was evaluated regarding visual appearance and droplet size distribution after dispersion in aqueous media. The developed SMEDDS was found to be similar to Neoral. LLT were characterized before and after loading regarding weight variation, tablet hardness, disintegration time, and in vitro drug release. It was found that LLT with high porosities suitable for liquid loading and further processing could be prepared. Adding a tablet disintegrant was found to improve in vitro drug release. Additionally, the volume-based loading capacity of LLT was evaluated and found to be comparable to soft gelatin and hard two-piece capsules. Furthermore, the pharmacokinetic performance of CyA from loaded LLT was tested in two PK-studies in dogs. Absorption of CyA from SMEDDS loaded into LLT was found in the first study to be significantly lower than the absorption of CyA from SMEDDS filled into a capsule. However, addition of a superdisintegrant improved the absorption markedly. The bioavailability of CyA from SMEDDS loaded into disintegrating LLT was found in the second study to be at the same level as from capsule formulation. In conclusion, the LLT technology is therefore seen as a promising alternative way of achieving a solid dosage form from liquid drug delivery systems. PMID:19936938

Sander, Camilla; Holm, Per

2009-11-20

148

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).

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

2013-01-01

149

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

150

[Acute sedative effect of a herbal relaxation tablet as compared to that of bromazepam].  

PubMed

The relaxing effect and the systemic tolerance of a single oral dose of Valverde relaxation dragées have been examined double-blinded against 3 mg of bromazepam and placebo in groups of 20 healthy male volunteers each treatment. The systemic tolerance was assessed at the end of the examination, relying on spontaneous remarks or comments made on side effects upon questioning. As the four plants from which Valverde has been extracted (valerian, balm, passion-flower, and pestilence wort) have a reputation of being tranquilizing agents with spasmolytic effect, not only this effect needs to be demonstrated, but also sedative side effects and impairment of vigilance must be assessed to explore the risk for accident proneness. We expected that the relaxing-tranquilizing effect of bromazepam as well as of Valverde relaxation dragées compared with placebo is perceived subjectively. A potentially existing impairment of performance due to Valverde was assumed to be milder than impairment due to bromazepam. The study, however, inspite of a sophisticated test battery with extended testing, could not detect any effect for either of the two drugs; nor could it detect a side effect. The sedation and reduction of vigilance observed in a pre-study without placebo controls (Gerhard and Hobi, unpublished) was explained by natural fatigue which appeared in the course of the morning also under placebo. Therefore, sedative side effects, leading to an impairment in performance, can be excluded for both drugs at the studied dose level. PMID:1815310

Gerhard, U; Hobi, V; Kocher, R; König, C

1991-12-27

151

Comparative bioavailability study of two salbutamol tablets in healthy adult volunteers.  

PubMed

This study was carried out to compare the rate and extent of absorption of a generic salbutamol in oral dosage form (Brethmol, 4 mg) with the proprietary equivalent product (Ventolin, 4 mg), in healthy adult subjects, under fasting conditions. The study was a single dose, randomized, two way crossover study with a four-week washout period. It involved 22 healthy volunteers who received a single dose (4 mg) of the test and the reference products after an overnight fast of at least 10 hours. Blood samples were collected at pre-dose and a serial of 14 samples were collected from each of the subject from 1 h until 48 h post-dose. Plasma concentrations of salbutamol were analyzed using GCMS method. The mean AUC(0-yen) values were 91.26 and 96.45 h.ng/ml for reference and test product, respectively. The mean C(max) values were 12.26 and 12.38 ng/ml and the mean t(max) values were 2.80 and 2.33 hours for reference and test product, respectively. Analysis of variance showed that the 90% confidence intervals on the relative difference of the ratio for the AUC(0-yen) and the C(max) for the test and reference products were contained within the bioequivalence limit (80 - 125%) (C(max): 89.8 - 110.5% and AUC(0-yen): 91.6 - 121.5%). There was no statistically significant difference for the t(max) between the test and reference formulations (p = 0.30). The test formulation was found to be bioequivalent to the reference formulation with regard to AUC(0-yen) and C(max). There was no statistically significant difference in Brethmol and Ventolin t(max). In conclusion, Brethmol and Ventolin are bioequivalent in healthy subjects. PMID:19473604

Chik, Z; Basu, R C; Pendek, R; Lee, T C; Mohamed, Z

2009-06-01

152

The Disintegration of Teacher Preparation  

ERIC Educational Resources Information Center

The disintegration of teacher certification programs in the united States holds an eerie similarity to the recent meltdown of American financial institutions. Similarly, the No Child Left Behind Act of 2001, whose purported purpose was to ensure that all students get highly qualified teachers (HQT), has had an unintentionally devastating effect on…

Baines, Lawrence A.

2010-01-01

153

Creation of a tablet database containing several active ingredients and prediction of their pharmaceutical characteristics based on ensemble artificial neural networks.  

PubMed

A tablet database containing several active ingredients for a standard tablet formulation was created. Tablet tensile strength (TS) and disintegration time (DT) were measured before and after storage for 30 days at 40 degrees C and 75% relative humidity. An ensemble artificial neural network (EANN) was used to predict responses to differences in quantities of excipients and physical-chemical properties of active ingredients in tablets. Most classical neural networks involve a tedious trial and error approach, but EANNs automatically determine basal key parameters, which ensure that an optimal structure is rapidly obtained. We compared the predictive abilities of EANNs in which the following kinds of training algorithms were used: linear, radial basis function, general regression (GR), and multilayer perceptron. The GR EANN predicted pharmaceutical responses such as TS and DT most accurately, as evidenced by high correlation coefficients in a leave-some-out cross-validation procedure. When used in conjunction with a tablet database, the GR EANN is capable of identifying acceptable candidate tablet formulations. PMID:20310024

Takagaki, Keisuke; Arai, Hiroaki; Takayama, Kozo

2010-10-01

154

Exploration of Novel Co-processed Multifunctional Diluent for the Development of Tablet Dosage Form.  

PubMed

The aim of this investigation was to develop a novel multifunctional co-processed diluent consisting of microcrystalline cellulose (Avicel PH 102), crospovidone (Polyplasdone XL) and polyethylene glycol 4000. Colloidal silicon dioxide and talc were also incorporated as minor components in the diluent to improve tableting properties. Melt granulation was adopted for preparation of co-processed diluent. Percentage of Avicel PH 102, Polyplasdone XL and polyethylene glycol 4000 were selected as independent variables and disintegration time was chosen as a dependent variable in simplex lattice design. The co-processed diluent was characterised for angle of repose, bulk density, tapped density, Carr's index, percentage of fines and dilution potential study. Acetaminophen and metformin were used as poorly compressible model drugs for preparation of tablets. The blend of granules of drug and extra-granular co-processed diluent exhibited better flow as compared to the blend of drug granules and physical mixture of diluents blend. The diluent exhibited satisfactory tableting properties. The tablets exhibited fairly rapid drug release. In conclusion, melt granulation is proposed as a method of preparing co-processed diluent. The concept can be used to bypass patents on excipient manufacturing. PMID:23716865

Gohel, M C; Patel, T M; Parikh, R K; Parejiya, P B; Barot, B S; Ramkishan, A

2012-09-01

155

Exploration of Novel Co-processed Multifunctional Diluent for the Development of Tablet Dosage Form  

PubMed Central

The aim of this investigation was to develop a novel multifunctional co-processed diluent consisting of microcrystalline cellulose (Avicel PH 102), crospovidone (Polyplasdone XL) and polyethylene glycol 4000. Colloidal silicon dioxide and talc were also incorporated as minor components in the diluent to improve tableting properties. Melt granulation was adopted for preparation of co-processed diluent. Percentage of Avicel PH 102, Polyplasdone XL and polyethylene glycol 4000 were selected as independent variables and disintegration time was chosen as a dependent variable in simplex lattice design. The co-processed diluent was characterised for angle of repose, bulk density, tapped density, Carr's index, percentage of fines and dilution potential study. Acetaminophen and metformin were used as poorly compressible model drugs for preparation of tablets. The blend of granules of drug and extra-granular co-processed diluent exhibited better flow as compared to the blend of drug granules and physical mixture of diluents blend. The diluent exhibited satisfactory tableting properties. The tablets exhibited fairly rapid drug release. In conclusion, melt granulation is proposed as a method of preparing co-processed diluent. The concept can be used to bypass patents on excipient manufacturing.

Gohel, M. C.; Patel, T. M.; Parikh, R. K.; Parejiya, P. B.; Barot, B. S.; Ramkishan, A.

2012-01-01

156

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.

Malik, Karan; Arora, Gurpreet; Singh, Inderbir

2011-01-01

157

Non-wood Fibre Production of Microcrystalline Cellulose from Sorghum caudatum: Characterisation and Tableting Properties  

PubMed Central

The microcrystalline cellulose is an important ingredient in pharmaceutical, food, cosmetic and other industries. In this study, the microcrystalline cellulose, obtained from the stalk of Sorghum caudatum was evaluated for its physical and tableting characteristics with a view to assessing its usefulness in pharmaceutical tableting. The microcrystalline cellulose, obtained from the stalk of Sorghum caudatum, obtained by sodium hydroxide delignification followed by sodium hypochlorite bleaching and acid hydrolysis was examined for its physicochemical and tableting properties in comparison with those of the well-known commercial microcrystalline cellulose grade, Avicel PH 101. The extraction yield of this microcrystalline cellulose, obtained from the stalk of Sorghum caudatum was approximately 19%. The cellulose material was composed of irregularly shaped fibrous cellulose particles and had a moisture content of 6.2% and total ash of 0.28%. The true density was 1.46. The flow indices showed that the microcrystalline cellulose, obtained from the stalk of Sorghum caudatum flowed poorly. The hydration, swelling and moisture sorption capacities were 3.9, 85 and 24%, respectively. Tablets resulting from these cellulose materials were found to be without surface defects, sufficiently hard and having disintegration time within 15 min. The study revealed that the microcrystalline cellulose, obtained from the stalk of Sorghum caudatum compares favourably with Avicel PH 101 and conformed to official requirement specified in the British Pharmacopoeia 1993 for microcrystalline cellulose.

Ohwoavworhua, F. O.; Adelakun, T. A.

2010-01-01

158

The Disintegration of Cu61  

Microsoft Academic Search

By the use of very thin and uniform sources that were prepared by thermal evaporation, the positron spectrum of Cu61 continues to show an excess of particles in the low energy region. The presence of nuclear gramma-rays and internal conversion electrons indicates that the disintegration of Cu61 is complex. Magnetic spectrometer studies of the radiations from Cu61 have led to

George E. Owen; C. Sharp Cook; Paul H. Owen

1950-01-01

159

Formulation development and in vitro evaluation of solidified self-microemulsion in the form of tablet containing atorvastatin calcium.  

PubMed

Aim: The objective of our present study was to prepare solid self-microemulsion in the form of tablet of a poorly water soluble drug, Atorvastatin calcium (ATNC) to increase the solubility, dissolution rate, and minimize the hazards experienced from liquid emulsions. Materials and methods: Self-microemulsifying ATNC tablet was formulated mainly by using self-emulsifying base, solidifying agent silicon dioxide and sodium starch glycolate as tablet disintegrant. Self-emulsifying base containing Transcutol P, Gelucire 44/14, and Lutrol F68 with their ratios in the formulation, were best selected by solubility study and ternary phase diagram in different vehicles. Particle size of microemulsion from tablet, physical parameters of the tablet and drug content has been checked. In vitro drug release rate has been carried out in phosphate buffer medium (pH 6.8). Physicochemical characterization of the drug in the optimized formulation has been performed to check drug-excipient incompatibility, if any. Results: Average particle diameter of the emulsions formed from the tablet was found to be below 100?nm in case of formulation F4 and F5, which indicated microemulsions has been formed. In vitro drug release from the formulations F3, F4, and F5 was found to be >90%, indicated the enhancement of solubility of ATNC compared to parent drug. Differential thermal analysis (DTA), Powder X-ray Diffraction (X-RD) and Fourier transform infra red (FTIR) study proved the identity of the drug in the optimized formulation. Conclusion: The tablet form of self-microemulsifying (SME) drug delivery is good for solubility enhancement. PMID:23216220

Ali, Kazi Asraf; Mukherjee, Biswajit; Bandyopadhyay, Amal Kumar

2012-12-06

160

Cost-effectiveness of the once-daily efavirenz/emtricitabine/tenofovir tablet compared with the once-daily elvitegravir/cobicistat/emtricitabine/tenofovir tablet as first-line antiretroviral therapy in HIV-infected adults in the US  

PubMed Central

Background February 2013 US treatment guidelines recommend the once-daily tablet of efavirenz/emtricitabine/tenofovir (Atripla®) as a preferred regimen and the once-daily tablet of elvitegravir/cobicistat/emtricitabine/tenofovir (Stribild™) as an alternative regimen for first-line treatment of human immunodeficiency virus (HIV). This study assessed the clinical and economic trade-offs involved in using Atripla compared with Stribild as first-line antiretroviral therapy in HIV-infected US adults. Methods A Markov cohort model was developed to project lifetime health-related outcomes, costs, quality-adjusted life years (QALYs), and cost-effectiveness of Stribild compared with Atripla as first-line antiretroviral therapy in HIV-1-infected US patients. Patients progressed in 12-week cycles through second-line, third-line, and nonsuppressive therapies, acquired immune deficiency syndrome, and death. Baseline characteristics and first-line virologic suppression, change in CD4 count, and adverse effects (lipid, central nervous system, rash, renal) were based on 48-week clinical trial results. These results demonstrated equivalent virologic suppression between the two regimens. Point estimates for virologic suppression (favoring Stribild) were used in the base case, and equivalency was used in the scenario analysis. Published sources and expert opinion were used to estimate costs, utilities, risk of acquired immune deficiency syndrome, mortality, subsequent-line CD4 count, clinical efficacy, and adverse events. Costs were reported in 2012 US dollars. Sensitivity analyses were conducted to assess robustness of results. Results Compared with patients initiating Atripla, patients initiating Stribild were estimated to have higher lifetime costs. Stribild added 0.041 QALYs over a lifetime at an additional cost of $6,886, producing an incremental cost-effectiveness ratio of $166,287/QALY gained. Results were most sensitive to first-line response rates, product costs, and likelihood of renal adverse events. When equivalent efficacy was assumed, Atripla dominated Stribild with lower costs and greater QALYs. Conclusion At a societal willingness to pay of $100,000/QALY, Stribild was not cost-effective in the base case compared with Atripla for first-line HIV treatment.

Juday, Timothy; Correll, Todd; Anene, Ayanna; Broder, Michael S; Ortendahl, Jesse; Bentley, Tanya

2013-01-01

161

Preparation and optimization of mouth/orally dissolving tablets using a combination of glycine, carboxymethyl cellulose and sodium alginate: a comparison with superdisintegrants.  

PubMed

The purpose of the research was to prepare metoclopramide HCl mouth/orally dissolving tablets (MDTs) using glycine, carboxy methyl cellulose and sodium alginate with sufficient mechanical integrity and disintegration time comparable to superdisintegrants. Application of Plackett-Burman design revealed that concentration of glycine (X(1)), concentration of carboxy methyl cellulose (X(2)) and tablet crushing strength (X(4)) were found to actively influence the dependent variables (disintegration time in oral cavity (DT), wetting time (WT), porosity (P(0)) and water absorption ratio (WA). Additional MDTs were prepared utilizing central composite design for estimating extended effect in a spherical domain. The regression statistics (performed using Statistica(R)-7.0) of quadratic model revealed that DT, WT, P(0) were 97% correlated with active factors (X(1), X(2) or X(4)). The results revealed that optimized MDTs were capable of simulating DT comparable to MDTs containing croscarmellose sodium or crospovidone. Further, it can be envisaged that optimized MDTs were found to be superior to MDTs containing croscarmellose sodium or crospovidone in terms of friability and tablet crushing strength. PMID:18484492

Vora, Nishant; Rana, Vikas

2008-01-01

162

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

163

Investigation of vitamin and mineral tablets and capsules on the Canadian market  

Microsoft Academic Search

PURPOSE: The goal of this study was to investigate the disintegrating properties of tablets and capsules containing minerals and vitamins commercially available on the Canadian market and to review their label information. METHODS: The labels were examined for product-related information. The first disintegration test stage was performed using Simulated Intestinal Fluid (SIF) pH 6.8 for 20 minutes. Products which did

Raimar Löbenberg; Wayne Steinke

2006-01-01

164

156 Economic Evaluation of Grass Tablets for Immunotherapy (oralair) Compared to Placebo in Adults and Children in Italy  

PubMed Central

Background Specific immunotherapy is based on the regular administration over time of a maintenance dose of allergen extracts to allergic patients in order to modify the immune response, thus achieving a decrease in symptoms/drug intake and an improvement in quality of life, possibly on the long-term. Grass pollen tablet, Oralair (Stallergenes, Antony Cedex, France), were developed and registered for rhinoconjunctivitis allergy induced by grass pollen. There is sufficient evidence for the clinical efficacy of the product, but pharmaco-economy data are lacking. Methods An economic analysis, using a rescue medication adjusted score (AASS) was performed, based on the available registration trials—to assess the magnitude of Oralair effect if patients had not taken any rescue medication. In the present study the results of an adult and a pediatric study are pooled together with economic data in order to perform a cost–effectiveness analysis from the third party payer perspective. Medical visits, diagnostic exams, skin prick test, and drugs were valorized in euros according to the National tariffs and the standard drug prices in the Italian setting. The estimated ROC also enabled us to quantify the effectiveness in terms of Quality Adjusted Life Years (QALY). A decision tree was structured in order to model the possible outcomes and costs, according to a low, moderate and high AASS in adults and pediatric patients. A probabilistic sensitivity analysis was finally conducted to test the robustness of the results as well as the consistency with an assumed cost effectiveness threshold of euros 30.000/QALY. Results The results showed a relative difference of 1.84 in favor of the active treatment versus placebo in absolute value in adult study and of 1.64 in pediatric study. The results also show how the Oralair administration costs 1024 euro/QALY with high and moderate AASS. Including also the loss of productivity the incremental cost-effectiveness ratio (ICER) in adults is 700 euro/QALY. The 95% of the simulation performed by sensitivity analysis shows an ICER below the threshold of 30.000 euro/QALY. Conclusions In conclusion our results show that Oralair grass tablet is a cost effective strategy in adults and pediatric patients with moderate and severe AASS.

Cicchetti, Amerigo; Ruggeri, Matteo; Fiocchi, Alessandro; Bonini, Sergio; Puccinelli, Paola; Passalacqua, Giovanni; Frati, Franco

2012-01-01

165

Preparation and Evaluation of Orodispersible Tablets of Pheniramine Maleate by Effervescent Method  

PubMed Central

In the present work, orodispersible tablets of pheniramine maleate were designed with a view to enhance patient compliance by effervescent method. In the effervescent method, mixture of sodium bicarbonate and tartaric acid (each of 12% w/w concentration) were used along with super disintegrants, i.e., pregelatinized starch, sodium starch glycolate, croscarmellose sodium and crospovidone. The prepared batches of tablets were evaluated for hardness, friability, drug content uniformity and in vitro dispersion time. Based on in vitro dispersion time (approximately 60 s), three formulations were tested for in vitro drug release pattern (in pH 6.8 phosphate buffer), short-term stability (at 40±2°/75±5% RH for 3 mo) and drug-excipient interaction (IR spectroscopy). Among three promising formulations, formulation ECP4 containing 4% w/w crospovidone and mixture of sodium bicarbonate and tartaric acid (each of 12% w/w) emerged as the overall best formulation (t70% = 1.65 min) based on the in vitro drug release characteristics compared to commercial conventional tablet formulation. Short-term stability studies on the formulations indicated no significant changes in the drug content and in vitro dispersion time (P < 0.05).

Swamy, P. V.; Divate, S. P.; Shirsand, S. B.; Rajendra, P.

2009-01-01

166

Rapid development and optimization of tablet manufacturing using statistical tools.  

PubMed

The purpose of this paper was to develop a statistical methodology to optimize tablet manufacturing considering drug chemical and physical properties applying a crossed experimental design. The assessed model drug was dried ferrous sulphate and the variables were the hardness and the relative proportions of three excipients, binder, filler and disintegrant. Granule properties were modeled as a function of excipient proportions and tablet parameters were defined by the excipient proportion and hardness. The desirability function was applied to achieve optimal values for excipient proportions and hardness. In conclusion, crossed experimental design using hardness as the only process variable is an efficient strategy to quickly determine the optimal design process for tablet manufacturing. This method can be applied for any tablet manufacturing method. PMID:18459048

Fernández, Eutimio Gustavo; Cordero, Silvia; Benítez, Malvina; Perdomo, Iraelio; Morón, Yohandro; Morales, Ada Esther; Arce, Milagros Gaudencia; Cuesta, Ernesto; Lugones, Juan; Fernández, Maritza; Gil, Arturo; Valdés, Rodolfo; Fernández, Mirna

2008-05-06

167

Effect of diluents on tablet integrity and controlled drug release.  

PubMed

The objective of this study was to evaluate the effect of diluents and wax level on tablet integrity during heat treatment and dissolution for sustained-release formulations and the resultant effect on drug release. Dibasic calcium phosphate dihydrate (DCPD), microcrystalline cellulose (MCC), and lactose were evaluated for their effect on tablet integrity during drug dissolution and heat treatment in wax matrix formulations. A newly developed direct compression diluent, dibasic calcium phosphate anhydrous (DCPA), was also evaluated. Compritol 888 ATO was used as the wax matrix material, with phenylpropanolamine hydrochloride (PPA) as a model drug. Tablets were made by direct compression and then subjected to heat treatment at 80 degrees C for 30 min. The results showed that MCC, lactose, and DCPA could maintain tablets intact during heat treatment above the melting point of wax (70 degrees C-75 degrees C). However, DCPD tablets showed wax egress during the treatment. MCC tablets swelled and cracked during drug dissolution and resulted in quick release. DCPD and lactose tablets remained intact during dissolution and gave slower release than MCC tablets. DCPA tablets without heat treatment disintegrated very quickly and showed immediate release. In contrast, heat-treated DCPA tablets remained intact through the 24-hr dissolution test and only released about 80% PPA at 6 hr. In the investigation of wax level, DCPD was used as the diluent. The drug release rate decreased as the wax content increased from 15% to 81.25%. The dissolution data were best described by the Higuchi square-root-of-time model. Diluents showed various effects during heat treatment and drug dissolution. The integrity of the tablets was related to the drug release rate. Heat treatment retarded drug release if there was no wax egress. PMID:10872095

Zhang, Y E; Schwartz, J B

2000-07-01

168

Comparative bioavailability of two moxifloxacin tablet products after single dose administration under fasting conditions in a balanced, randomized and cross-over study in healthy volunteers.  

PubMed

Moxifloxacin, a 4th generation of fluoroquinolones, is a broad spectrum antibacterial agent against respiratory tract pathogens, including Gram-positive and Gram-negative bacteria, anaerobic bacteria and atypical respiratory tract pathogens. In order to evaluate the efficacy and safety of generic moxifloxacin products, the bioequivalence of these generic products with an approved reference formulation should be demonstrated. Thus, the aim of this study was to compare the rate and extent of absorption of a new generic film coated moxifloxacin tablet product (Rapiflox®, Atlantic Laboratories Corporation Ltd., Bangkok, Thailand) with that of a reference product (Avelox®, Bayer Health Care AG, Leverkusen, Germany) when given as a single dose. A crossover study was performed in 20 healthy Thai volunteers. The subjects received either a 400 mg tablet of the reference or test product after overnight fasting. Blood samples were collected at pre-dose (0 hour) and at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 and 34 hours post-dose. Moxifloxacin plasma level was measured by a validated HPLC method with fluorescence detector. Pharmacokinetic parameters were calculated using a non-compartmental model. The geometric mean of maximum concentration (Cmax) of the test product was 4,069.64 ng/ml, with median time to achieve maximum concentration (tmax) at 2 hours (range 0.25 - 6.00 hours), while the geometric mean Cmax and median tmax of the reference product was 4,211.98 ng/ml and 2.00 hours (range 0.25 - 8.00 hours). Furthermore, the geometric means of AUC0-tlast and AUC0-? for the test product were 49,731.66 and 51,865.89 ng×h/ml while those of the reference product were 51,927.97 and 54,455.93 ng×h/ml. The geometric mean of the ratios of Test/Reference for the logtransformed Cmax, AUC0-tlast and AUC0-? of moxifloxacin and their 90% CIs were 96.62% (83.21 - 112.19%), 95.77% (87.07 - 105.34%) and 95.24 (86.52 - 104.85%), respectively. Therefore, it can be concluded that these two moxifloxacin tablet products were bioequivalent in healthy Thai volunteers under fasting condition. PMID:23357835

Kanjanawart, Sirimas; Gaysonsiri, Dhanu; Phunikom, Katcharin; Simasathiansopon, Sontaya; Tangsucharit, Panot; Vannaprasaht, Suda; Kaewkamson, Thanawat; Tassaneeyakul, Wichittra

2013-03-01

169

Oral liquid L-thyroxine (L-t4) may be better absorbed compared to L-T4 tablets following bariatric surgery.  

PubMed

Drug malabsorption is a potential concern after bariatric surgery. We present four case reports of hypothyroid patients who were well replaced with thyroxine tablets to euthyroid thyrotropin (TSH) levels prior to Roux-en-Y gastric bypass surgery. These patients developed elevated TSH levels after the surgery, the TSH responded reversibly to switching from treatment with oral tablets to a liquid formulation. PMID:23824980

Pirola, Ilenia; Formenti, Anna M; Gandossi, Elena; Mittempergher, Francesco; Casella, Claudio; Agosti, Barbara; Cappelli, Carlo

2013-09-01

170

Multiple-scored tablets. Weight and content uniformity of subdivisions and distribution of active constituent within and between tablets.  

PubMed

Using three brands of multiple-scored levodopa tablets, B.P. (500 mg) and one brand of sulphamethoxypyridazine tablets B.P. (500 mg) the weight and content uniformity of the subdivisions has been examined. It is shown that quartering of such tablets can result in subunits which do not conform to recognized standards of weight uniformity, and in some instances content uniformity may be questionable. The homogeneity of distribution of active constituent between tablets has been determined and compared with that within tablets (between quarters of individual tablets). Statistical evaluation of the results is presented. PMID:27603

Walker, J; Abdulsalam, A; Theobald, A E; Subrahmanyam, R; Verma, S K

1978-07-01

171

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. © 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 102:3678-3686, 2013. PMID:23897300

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

2013-07-29

172

Evaluation of binders in the preparation of medicinal carbon tablets by wet granule compression.  

PubMed

Medicinal carbon (MC) tablets were prepared to obtain an oral dosage form that can be easily taken. The MC tablets were made by the wet granule compression method, in which hydroxypropyl cellulose (HPC), carboxymethyl cellulose sodium (CMC-Na) and maltitol (MT) were applied as binders. Brilliant Blue FCF (BB) was used as a model drug. The binders were evaluated in terms of formability of the granules and tablets, their strength, disintegration of the tablets, and their effect on the adsorption potential of MC. HPC and CMC-Na gave the strong granules at a fairly low concentration, but more MT was needed to obtain the strong granules. The tablets could be formed only when using MT at 120% (w/w) of the MC amount. The tablet displayed good hardness and rapid disintegration. The adsorption potential was not affected by CMC-Na, and slightly prevented by MT. However, the adsorption ability of MC was lowered more with the increase in HPC. The granules and tablets exhibited similar adsorption potentials, which were a little lower than that of MC suspended in MT aqueous solution. Similar adsorption characteristics were also observed in a real drug, acetaminophen. It is suggested that the MC tablets prepared by the wet granule compression using MT as a binder should be useful as a compact dosage form of MC. PMID:16596024

Ito, Akihiko; Onishi, Hiraku; Yamamoto, Kenta; Machida, Yoshiharu

2006-04-01

173

A mini review of scientific and pharmacopeial requirements for the disintegration test.  

PubMed

Disintegration is a performance test for oral dosage forms that is described in the United States Pharmacopeia (USP), the European Pharmacopeia (EP) and the Japanese Pharmacopeia (JP, chapter 14, 2001). This review lists changes that have been made since the USP 23 and compares them to those in the USP 30, EP 5.3 and JP XIV. The differences between the disintegration test methods in the three pharmacopeias are discussed. Examples are provided where disintegration can be used as a performance test for ensuring the drug release. PMID:17935916

Donauer, Nina; Löbenberg, Raimar

2007-09-01

174

A study of the properties of tablets from the mixtures of directly compressible starch and directly compressible lactitol.  

PubMed

The paper deals with the evaluation of tablets from the mixtures of directly compressible starch Starch 1500 and directly compressible lactitol Lacty-Tab in a ratio of 3:1 and 1:1. The examination included the tensile strength and disintegration time of tablets in dependence on compression force, addition of two concentrations of sodium stearyl fumarate (Pruv) as the lubricant, and a 50% content of the model active ingredient acetylsalicylic acid. Tensile strength of tablets increased with compression force and the effect of Pruv decreased it in both mixtures. Tablets from the mixture of dry binders in a ratio 1:1 without the lubricant possessed highest values of tensile strength. After an addition of the lubricant, no statistically significant difference was found in this mixture between interventions of 0.5 and 1% Pruv concentrations into strength. Disintegration time increased with compression force; it was the shortest in tablets with 1% Pruv in the case of the mixture of Starch 1500 and lactitol 3:1; in the case of the mixture 1:1 it was the longest. Tablets containing acetylsalicylic acid possessed higher values of tensile strength in the case of the mixture of dry powders in a ratio of 1:1, the strength decreasing with increasing Pruv concentration. Tablets from this mixture also possessed a longer period of disintegration time which increased with increasing Pruv concentration. PMID:17969317

Muzíková, J; Vajglová, J

2007-07-01

175

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

2012-03-30

176

The use of the SeDeM Diagram expert system to determine the suitability of diluents-disintegrants for direct compression and their use in formulation of ODT.  

PubMed

The new SeDeM Diagram expert system was used to analyze the suitability of 43 excipients for direct compression with disintegrant properties from eight chemical families. The SeDeM Diagram expert system is a new method for use in tablet preformulation and formulation studies. It provides the profile of a substance in powder form in terms of its suitability for direct compression. This study, which was based on the current concept of "Quality by Design ICH Q8", evaluated the pharmacotechnical properties of disintegrants in powder form and selected the candidates that were most suitable for direct compression and their use in formulation of orally disintegrating tablets (ODT). To achieve this, each disintegrant and its chemical families were individually analyzed. It was concluded that nine disintegrants had an SeDeM value with the index of good compression (IGC) over 5. Most of these disintegrants were from the microcellulose family. Other disintegrants had indexes that were close to 5. It is assumed that these excipients can be used in direct compression, when they are added to other excipients. PMID:19602435

Aguilar-Díaz, Johnny Edward; García-Montoya, Encarnación; Pérez-Lozano, Pilar; Suñe-Negre, José María; Miñarro, Montserrat; Ticó, José Ramón

2009-07-12

177

Model Test of Anchoring Effect on Zonal Disintegration in Deep Surrounding Rock Masses  

PubMed Central

The deep rock masses show a different mechanical behavior compared with the shallow rock masses. They are classified into alternating fractured and intact zones during the excavation, which is known as zonal disintegration. Such phenomenon is a great disaster and will induce the different excavation and anchoring methodology. In this study, a 3D geomechanics model test was conducted to research the anchoring effect of zonal disintegration. The model was constructed with anchoring in a half and nonanchoring in the other half, to compare with each other. The optical extensometer and optical sensor were adopted to measure the displacement and strain changing law in the model test. The displacement laws of the deep surrounding rocks were obtained and found to be nonmonotonic versus the distance to the periphery. Zonal disintegration occurs in the area without anchoring and did not occur in the model under anchoring condition. By contrasting the phenomenon, the anchor effect of restraining zonal disintegration was revealed. And the formation condition of zonal disintegration was decided. In the procedure of tunnel excavation, the anchor strain was found to be alternation in tension and compression. It indicates that anchor will show the nonmonotonic law during suppressing the zonal disintegration.

Chen, Xu-Guang; Zhang, Qiang-Yong; Wang, Yuan; Liu, De-Jun; Zhang, Ning

2013-01-01

178

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.

Okunlola, Adenike; Odeku, Oluwatoyin A.

2011-01-01

179

A compressibility and compactibility study of real tableting mixtures: the effect of granule particle size.  

PubMed

This study investigates the effect of particle size on the compression characteristics of wet- (fluid-bed granulation - FBG) and dry-granulated (slugging - DGS) tableting mixtures. Particle-size distribution, flowability, compressibility, using the Heckel and Walker model, compactibility and elastic recovery as well as friability and disintegration were determined and compared between the two particle size fractions (180-400 ?m, 400-710 ?m) and initial unsieved mixtures. The results showed that the particle size of granules had no effect on the compressibility of the FBG and DGS mixtures, due to the high fragmenting nature of the formulation used in this study. On the other hand, compactibility was particle size dependent, as larger-sized fractions showed higher crushing strength, lower friability, and lower elastic recovery. This was attributed to increased fragmentation of larger particles, allowing stronger bonding between uncontaminated surface areas. As a result of better rearrangement of particles, both initial tableting mixtures showed lower compressibility and lower compactibility compared to their sieved fractions. PMID:23470346

Šantl, Maja; Ili?, Ilija; Vre?er, Franc; Baumgartner, Saša

2012-11-01

180

Improvement in the disintegration of shellac-coated soft gelatin capsules in simulated intestinal fluid.  

PubMed

Shellac is a natural enteric polymer, which results in good gastric resistance; however, it often dissolves too slowly in intestinal fluids. The objective of this study was to improve the disintegration of shellac-coated soft gelatin capsules in simulated intestinal fluids (phosphate buffer pH 6.8) through the addition of pore-formers, such as organic acids and hydrophilic polymers, while retaining gastric resistance. The mechanical properties (% elongation at rupture, puncture strength at break and modulus at puncture), media uptake and weight loss of shellac films were determined upon exposure in 0.1 N HCl and/or phosphate buffer pH 6.8. Organic acids (e.g., sorbic acid) acted as plasticizers, they reduced the glass transition temperature of ethanol-cast shellac films. The addition of additives effectively decreased the disintegration times in phosphate buffer pH 6.8, while the behavior in 0.1 N HCl remained unchanged. In addition, the hardness and disintegration of shellac-coated soft gelatin capsules were monitored through the whole disintegration experiments. The best disintegration was achieved with sorbic acid as pore-former. Sorbic acid remained in the shellac coating at low pH, but leached in pH 6.8 buffer, thus resulting in good gastric resistance and rapid disintegration in simulated intestinal fluids. The disintegration time of ethanolic shellac-coated soft gelatin capsules decreased with increasing amount of pore-former. The slow disintegration of aqueous shellac-coated soft gelatin capsules could be also improved by the addition of hydrophilic polymers, such as hydroxypropyl methylcellulose (HPMC). However, higher HPMC concentrations were required when compared to sorbic acid. PMID:14744483

Pearnchob, Nantharat; Dashevsky, Andrei; Bodmeier, Roland

2004-02-10

181

Internal solitary waves: propagation, deformation and disintegration  

Microsoft Academic Search

Internal solitary waves are a common feature of the coastal ocean. In this talk I will describe, using model equations of the Korteweg-de Vries type, how these waves are affected by variable bottom topography. The scenarios range from adiabatic deformation, to disintegration and transformation into wave trains with very different features. Although the context is that of internal waves in

Roger Grimshaw

2010-01-01

182

Ultrasonic disintegration of biosolids for improved biodegradation  

Microsoft Academic Search

Biological cell lysis is known to be the rate-limiting step of anaerobic biosolids degradation. Shear forces generated by low frequency ultrasound can be used to disintegrate bacterial cells in sewage sludge. Thus, the quantity of dissolved organic substrate is increased. Consequently, the degradation rate and the biodegradability of organic biosolids mass are improved. Fundamental pilot-studies showed a significantly accelerated biosolids

Klaus Nickel; Uwe Neis

2007-01-01

183

Further Measurements on the Disintegration Curve of Mesotrons  

Microsoft Academic Search

Further measurements have been made on the disintegration curve of mesotrons. An extensive set of data gives a mean lifetime of 2.15+\\/-0.07 microseconds as calculated from the differential disintegration curve.

Norris Nereson; Bruno Rossi

1943-01-01

184

Experimental Determination of the Disintegration Curve of Mesotrons  

Microsoft Academic Search

The disintegration curve of mesotrons has been experimentally determined by investigating the delayed emission of disintegration electrons which takes place after the absorption of mesotrons by matter. Within the experimental errors, the disintegration curve is exponential and corresponds to a mean lifetime of 2.3+\\/-0.2 microseconds.

Bruno Rossi; Norris Nereson

1942-01-01

185

Formulation of a extended release tablet containing dexibuprofen.  

PubMed

Dexibuprofen, or S(+)-ibuprofen, is the pharmacologically effective enantiomer of racemic ibuprofen. Since dexibuprofen has a low melting point, the amorphous form having a high melting point was prepared with the fused solid dispersion method. With the fused solid dispersion of dexibuprofen, immediate release tablets, extended release tablets, and dual release tablets were compressed and their dissolution profiles compared. The dissolution profiles of the extended release and the dual release tablet depended on the amount of used release modulators (PEO 5,000,000). The release profiles of extended release tablets and extended release part of dual release tablets were well fitted to zero-order release model. The correlation coefficient ranged from 0.982 to 0.995. A pharmacokinetic evaluation where healthy volunteers took tablets of DRT-1 (300 mg) once and the reference drug, two tablets of conventional immediate release tablet (Daxfen, 300 mg), with a 6-h interval between them was studied. The 90% confidence interval for the ratio of the logarithmically transformed AUC (0-24 h), Cmax (0-6 h), and Cmax (6-24 h) values of the dual release tablet compared to those of the conventional immediate release tablet were calculated to be between 0.9176 and 1.0007, 0.9240 and 1.1968, and 0.8713 and 1.1414, respectively. When the immediate release tablet was taken two times with a six hour interval between doses it showed a bioequivalent effect to taking the dual release tablet once within 12 h. The Cmax was reached due to the rapid absorption of the immediate release portion of the dual release tablet and the AUC was maintained due to continuous absorption of the extended release portion. PMID:19099235

Yi, Hong Gi; Chi, Moon Hyuk; Kim, Yong-Il; Woo, Jong Soo; Park, Eun-Seok

2008-12-20

186

Formulation design of carbamazepine fast-release tablets prepared by melt granulation technique.  

PubMed

This work describes a new approach to prepare a fast-release dosage form for carbamazepine (CBZ), involving the use of melt granulation process in high shear mixer for the production of tablets. In particular, the granules containing CBZ were prepared using polyethylene glycol (PEG) 4000 as a melting binder and lactose monohydrate as a hydrophilic filler. The potential of the intragranular addition of crospovidone as a dissolution enhancer and a disintegrant agent was also evaluated. After the analysis of their solid state performed by means of X-ray powder diffraction (XRD) and differential scanning calorimetry (DSC), the granules were characterised from the technological and dissolution point of view. The subsequent step encompassed the preparation and the evaluation of the tablets, including the effect of the extragranular introduction of crospovidone. Besides the remarkable enhancement of drug dissolution rate of the granulates in comparison to physical mixtures and pure drug, no significant differences were found between the dissolution profiles of the granulates containing lactose or crospovidone. However, the difficult disintegration and bad dissolution performance of the tablets not containing intragranular crospovidone highlight the necessity of this disintegrant in the granulating mixture. Moreover, the extragranular addition of a small amount of crospovidone gave rise to a further amelioration of the disintegration and dissolution performances. PMID:12695011

Perissutti, Beatrice; Rubessa, Fulvio; Moneghini, Mariarosa; Voinovich, Dario

2003-04-30

187

External scintigraphy in monitoring the behavior of pharmaceutical formulations in vivo I: technique for acquiring high-resolution images of tablets  

SciTech Connect

A new method for monitoring tablet disintegration in vivo was developed. In this method, the tablets were labeled with a short-lived radionuclide, technetium 99m, and monitored by a gamma camera. Several innovations were introduced with this method. First, computer reconstruction algorithms were used to enhance the scintigraphic images of the disintegrating tablet in vivo. Second, the use of a four-pinhole collimator to acquire multiple views of the tablet resulted in high count rates and reduced acquisition times of the scintigraphic images. Third, the magnification of the scintigraphic images achieved by pinhole collimation led to significant improvement in resolution. Fourth, the radioinuclide was incorporated into the granulation so that the whole mass of the tablet was uniformly labeled with high levels of activity. This technique allowed the continuous monitoring of the disintegration process of tablets in vivo in experimental animals. Multiple pinhole collimation and the labeling process permitted the acquisition of quality scintigraphic images of the labeled tablet every 30 sec. The resolution of the method was tested in vitro and in vivo.

Theodorakis, M.C.; Simpson, D.R.; Leung, D.M.; Devous, M. Sr.

1983-02-01

188

Post-market in vitro bioequivalence study of six brands of ciprofloxacin tablets\\/caplets in Jos, Nigeria  

Microsoft Academic Search

Six brands of ciprofloxacin 500 mg tablets have been evaluated using some quality control tests of uniformity of weight, hardness, friability, assay, disintegration and dissolution with the aim to assess its bioequivalence. The results obtained have been discussed in some details using monographs in the two Pharmacopeia (United States Pharmacopeia, USP and British Pharmacopeia, BP). The results were also subjected

N. C. Ngwuluka; K. Lawal; P. O. Olorunfemi; N. A. Ochekpe

189

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

190

Combination of alkaline and microwave pretreatment for disintegration of meat processing wastewater sludge.  

PubMed

Meat processing wastewater sludge has high organic content but it is very slow to degrade in biological processes. Anaerobic digestion may be a good alternative for this type of sludge when the hydrolysis, known to be the rate-limiting step of biological sludge anaerobic degradation, could be eliminated by disintegration. This investigation deals with disintegration of meat processing wastewater sludge. Microwave (MW) irradiation and combined alkaline pretreatment and MW irradiation were applied to sludge for disintegration purposes. Disintegration performance of the methods was evaluated with disintegration degree based on total and dissolved organic carbon calculations (DD(TOC)), and the solubilization of volatile solids (S(VS)) in the pretreated sludge. Optimum conditions were found to be 140 degrees C and 30 min for MW irradiation using response surface methodology (RSM) and pH = 13 for combined pretreatment. While DD(TOC) was observed as 24.6% and 54.9, S(VS) was determined as 8.54% and 42.5% for MW pretreated and combined pretreated sludge, respectively. The results clearly show that pre-conditioning of sludge with alkaline pretreatment played an important role in enhancing the disintegration efficiency of subsequent MW irradiation. Disintegration methods also affected the anaerobic biodegradability and dewaterability of sludge. An increase of 23.6% in biogas production in MW irradiated sludge was obtained, comparing to the raw sludge at the end of the 35 days of incubation. This increase was observed as 44.5% combined pretreatment application. While MW pretreatment led to a little improvement of the dewatering performance of sludge, in combined pretreatment NaOH deteriorates the sludge dewaterability. PMID:23837322

Erden, G

191

Charge distribution in disintegration of uranium isotopes  

NASA Astrophysics Data System (ADS)

Charge distributions of the fragments emitted from the disintegration of uranium isotopes 235U and 238U at various excitation energies up to 10 MeV per nucleon were investigated on the basis of a statistical approach. The calculations reproduce the fundamental properties of the fission at low excitation energies for E* <= 0.5 MeV/A. The variation of the average value of the maximal charge, < Zmax>, of the emitted fragments with excitation energy is determined.

Eren, N.; Buyukcizmeci, N.; Ogul, R.

2013-04-01

192

Disintegration of materials by cavitating microjets  

NASA Astrophysics Data System (ADS)

In the paper is presented an investigation of material disintegration by cavitating microjets. Cavitating microjet develops behind the micro-orifice at high flow speeds, when local pressure drop initiates a cavitation phenomenon. Described is a method and presented are selected results of experiments. Experiments were carried out with 2 micro-orifices at different flow conditions (cavitation number, distance between sample and micro-orifice). Experiments are based on flow visualisation as well as on a character of material displacement.

Knížat, B.; Mlkvik, M.; Olšiak, R.

2013-04-01

193

The disintegration of nitrogen by fast neutrons  

Microsoft Academic Search

The disintegration of nitrogen by fast neutrons was studied using a grid-; type ionization chamber filled with nitrogen or a nitrogen-argon mixture. ; Monoenergetic neutrons for studying the reactions from a neutron energy of 1.3 to ; 8.2 Mev were produced by the T³(p,n)He³ and D(d.n)He³ reactions. ; One group of protons. three alpha particle groups, and a group of

F. Gabbard; H. Bichsel; T. W. Bonner

1959-01-01

194

Application of some polymers in the physiocochemical design of tablet formulation.  

PubMed

Polyethylene glycol 4000 did not apprecialbly affect the rate of drug release from tablets. The use of sodium alginate the a tablet binder showed variable effects on the rate of drug release from the tablet i.e. The incorporation of only 2.5% of sodium alginate caused enhancement in the release rate of the drug based on its action as disintegration inducer. On the other hand, the incorporation of 20, 35 and 50% of sodium alginate showed a pronounced retardation in the rate of drug release from the tablets. This retardation was more pronounced in acid than in alkaline media. Accordingly, sodium alginate could be favourably suggested as tablet binder when retarded gastric absorption is the therapeutic aim required. Carbopol 940 when used as a tablet binder in a concentration of 2.5%, showed a marked enhancement of the release rate of the drug. On the contrary, it exerted a remarkable retardation in the rate of drug release from the tablets when incorporated in the relatively large proportions of 20, 35 and 50%. This retardation was more pronounced in alkaline than in acid media. Accordingly, Carbopol 940 would be favourably suggested in the physiocohemical design of prolonged-release tablet formulations. PMID:1019194

Salib, N N; El-Gamal, S A

1976-01-01

195

Innovations in education : tablets  

Microsoft Academic Search

In this group of three separate articles the authors discuss the use of tablet PCs in educational applications at their schools. In 'Tablets: the smart medicine for teaching and learning', Lee Bond explains how Immanuel Lutheran College on the Sunshine Coast in Queensland is using ICT to make real systemic change in the delivery of education in physics, chemistry, biology

Lee Bond

2009-01-01

196

Teaching with Tablet PC's  

Microsoft Academic Search

Tablet PC's are traditional notebook computers with the ability to process digital ink by writing with a stylus. They have recently attracted attention as a potential tool for educational use. This paper describes the author's experience using the Tablet PC to conduct a CS1 course and a software engineering (SWE) course. The SWE course consisted primarily of PowerPoint lectures while

Kenrick Mock

2004-01-01

197

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

2012-12-14

198

Tablet Fluoridation Influences the Calcification of Primary Tooth Pulp  

Microsoft Academic Search

This study was conducted to determine the influence of long-term tablet fluoridation on primary pulp calcification by light microscopy. Twenty-four caries-free primary molars (after continuous postpartally initiated 1- to 10-year tablet fluoridation) were compared to 17 primary molars of children without fluoride prophylaxis. Pulp calcification in children with tablet fluoridation was significantly more frequent and more pronounced than in untreated

Eva-Andrea Holtgrave; Werner Hopfenmüller; Sandra Ammar

2001-01-01

199

Reduction of excess sludge production using mechanical disintegration devices.  

PubMed

The usability of mechanical disintegration techniques for the reduction of excess sludge production in the activated sludge process was investigated. Using three different disintegration devices (ultrasonic homogeniser, stirred media mill, high pressure homogeniser) and different operational parameters of the disintegration, the effect of mechanical disintegration on the excess sludge production and on the effluent quality was studied within a continuously operated, laboratory scale wastewater treatment system with pre-denitrification. Depending on the operational conditions and the disintegration device used, a reduction of excess sludge production of up to 70% was achieved. A combination of mechanical disintegration with a membrane bioreactor process with high sludge age is more energy effective concerning reduction of sludge production than with a conventional activated sludge process at lower sludge ages. Depending on the disintegration parameters, the disintegration has no, or only minor, negative effect on the soluble effluent COD and on the COD-removal capacity of the activated sludge process. Nitrogen-removal was slightly deteriorated by the disintegration, whereas the system used was not optimised for nitrogen removal before disintegration was implemented. PMID:17087371

Strünkmann, G W; Müller, J A; Albert, F; Schwedes, J

2006-01-01

200

Modes of Disintegration of Solid Foods in Simulated Gastric Environment  

PubMed Central

A model stomach system was used to investigate disintegration of various foods in simulated gastric environment. Food disintegration modes and typical disintegration profiles are summarized in this paper. Mechanisms contributing to the disintegration kinetics of different foods were investigated as related to acidity, temperature, and enzymatic effect on the texture and changes in microstructure. Food disintegration was dominated by either fragmentation or erosion, depending on the physical forces acting on food and the cohesive force within the food matrix. The internal cohesive forces changed during digestion as a result of water penetration and acidic and enzymatic hydrolysis. When erosion was dominant, the disintegration data (weight retention vs. disintegration time) may be expressed with exponential, sigmoidal, and delayed-sigmoidal profiles. The different profiles are the result of competition among the rates of water absorption, texture softening, and erosion. A linear-exponential equation was used to describe the different disintegration curves with good fit. Acidity and temperature of gastric juice showed a synergistic effect on carrot softening, while pepsin was the key factor in disintegrating high-protein foods. A study of the change of carrot microstructure during digestion indicated that degradation of the pectin and cell wall was responsible for texture softening that contributed to the sigmoidal profile of carrot disintegration.

Kong, Fanbin

2009-01-01

201

Plasma concentration profiles and antihypertensive effect of conventional and extended-release felodipine tablets.  

PubMed Central

1. The rate and extent of felodipine absorption from an oral solution, conventional and extended-release tablets were investigated in two groups of healthy volunteers (n = 18 + 15). 2. The antihypertensive effect of felodipine conventional tablets twice daily (n = 71) and extended-release tablets once daily (n = 76) were compared in a parallel-group study in hypertensive patients. 3. As from a solution, felodipine was completely absorbed from the two solid dosage forms. The rate of absorption increased in the order extended-release tablets, conventional tablets, solution. 4. The extended-release tablet gave more sustained plasma concentrations than the conventional tablet. 5. The extended-release tablet given once daily gave similar blood pressure control to the conventional tablet given twice daily.

Blychert, E; Wingstrand, K; Edgar, B; Lidman, K

1990-01-01

202

In vitro and in vivo evaluation of single-unit commercial conventional tablet and sustained-release capsules compared with multiple-unit polystyrene microparticle dosage forms of ibuprofen  

Microsoft Academic Search

The major aims of the present study were (1) to select a multiple-unit formulation that matched the in vitro dissolution profile\\u000a of single-unit sustained-release commercial capsules, (2) to compare the sustaining\\/controlling efficacy of the selected multiple-unit\\u000a formulation with that of the single-unit commercial conventional tablet and sustained-release capsules, and (3) to determine\\u000a whether an in vitro-in vivo correlation exists for

Shunmugaperumal Tamilvanan; Biswanath Sa

2006-01-01

203

Comparison between ozone and ultrasound disintegration on sludge anaerobic digestion.  

PubMed

This paper deals with the comparison of ultrasound (mechanical) and ozone (chemical) pre-treatment on the performances of excess sludge semi-continuous digestion. Sludge solubilisation has been investigated by varying specific energy input. For each pre-treatment, long anaerobic digestion tests were carried out by two parallel digesters: one reactor, as control unit, was fed with untreated waste activated sludge, and the other one was fed with disintegrated sludge. To evaluate and compare the efficacy of both pre-treatments, the specific energy was maintained approximately the same. The digestion tests were carried out to investigate the feasibility of anaerobic digestion performance (total biogas production, volatile solids removal, sludge dewaterability) and to assess the heat balance. Results obtained from the digestion of sonicated sludge at 4% disintegration degree (? 2500 kJ/kg TS) showed that the ultrasound pre-treatment may be effective both in increasing VS destruction (+19%) and cumulative biogas production (+26%). On the contrary, the digestion test with ozonized sludge (ozone dose of 0.05 g O(3)/g TS corresponding to ? 2000 kJ/kg TS) did not indicate a significant improvement on the digestion performances. By doubling the ozone dose an improvement in the organics removal and cumulative biogas production was observed. Relevant differences in terms of colloidal charge and filterability were discussed. PMID:20719427

Braguglia, C M; Gianico, A; Mininni, G

2010-08-16

204

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

205

Novel mesalamine-loaded beads in tablets for delayed release of drug to the colon.  

PubMed

Novel 'beads-in-a-tablet' formulations (total weight ?740-780?mg) have been prepared that meet USP 31 requirements for Delayed Release of mesalamine. Several methods are presented that overcome breakage of beads during tablet compaction were explored. Bead formulations comprise a combination of extrusion and spheronization to produce a relatively high drug load (80%), followed by coating (25%) with a colonic-targeted drug release polymer (polymethacrylates, Eudragit(®) S100), overcoated (3%) with hydroxypropyl methylcellulose (Opadry(®)) to improve bead binding and compactability, and using 20% coat of lactose/sodium starch glycolate (Explotab(®)) as binder/disintegrant/cushioning agent, thus allowing a sufficiently thick coating to be uniform and without being broken during tablet compaction. Then, the aforementioned beads were compressed into tablets at 1500 pounds of pressure containing 400?mg of mesalamine, and finally coating the compressed tablets with Surelease(®) (ethylcellulose):Opadry(®)?=?1:0.5 ranging from 1.5-2.5% weight gain; the resulting tablets met USP 31 dissolution requirements for delayed release tablets. PMID:20923254

Nguyen, Chien; Christensen, J Mark; Ayres, James W

2010-10-05

206

Formulation and Evaluation of Bilayer Tablet of Metoclopramide Hydrochloride and Ibuprofen  

Microsoft Academic Search

The aim of this study was to prepare bi-layer tablet of Metoclopramide Hydrochloride (MTH) and Ibuprofen (IB) for the effective\\u000a treatment of migraine. MTH and IB were formulated as immediate and sustained release layer respectively. MTH was formulated\\u000a as immediate release layer by using various disintegrants like Ac-Di-Sol, Polyplasdone XL, Explotab, Agar and Gellan Gum.\\u000a Treated form of gellan gum

Bhavesh Shiyani; Surendra Gattani; Sanjay Surana

2008-01-01

207

Risedronate-loaded Eudragit S100 microparticles formulated into tablets.  

PubMed

Abstract Risedronate, an anti-osteoporotic drug, is associated with low patient compliance due to the upper gastrointestinal side-effects and stringent dosing regimes. This study aimed to prepare and characterize risedronate-loaded Eudragit® S100 microparticles and develop a final dosage form by the compression of microparticles using direct tableting excipients. Microparticles were prepared by spray-drying and presented yield of 54%, encapsulation efficiency higher than 90%, mean diameter of 3.3?µm, moisture content around 8% and exhibited spherical shape and poor flowability. At pH 1.2, 23% of risedronate was released from microparticles in 120?min, while at pH 6.8 the drug took 90?min to reach 99.5%. Microparticles were compressed into tablets using microcrystalline cellulose, magnesium stearate, colloidal silicon dioxide and 2 polyvinylpyrrolidone concentrations (5% and 15%). Tablets presented low variations in weight, thickness and drug content. Besides, the formulations showed sufficient hardness, low friability and disintegrated in less than 15 min. In acid medium, no more than 16% of the drug was released in 120?min, while in intestinal medium the formulations prolonged the risedronate release for 240?min. Finally, the developed tableted microparticles can be considered a promising dosage form for oral risedronate administration. PMID:23506303

Velasquez, Aline A; Mattiazzi, Juliane; Ferreira, Luana M; Pohlmann, Lauren; Silva, Cristiane B; Rolim, Clarice M B; Cruz, Letícia

2013-03-19

208

Cefuroxime Axetil tablet  

Center for Drug Evaluation (CDER)

Text Version... Contains Nonbinding Recommendations Draft Guidance on Cefuroxime Axetil ... Active ingredient: Cefuroxime Axetil Form/Route: Tablet/Oral ... More results from www.fda.gov/downloads/drugs/guidancecomplianceregulatoryinformation

209

Calcification Prevention Tablets.  

National Technical Information Service (NTIS)

Citric acid tablets, which slowly release citric acid when flushed with water, are under development by the Navy for calcification prevention. The citric acid dissolves calcium carbonate deposits and chelates the calcium. For use in urinals, a dispenser i...

G. A. Lindsay M. A. Hasting M. A. Gustavson

1991-01-01

210

Bioavailability of Buprenorphine from Crushed and Whole Buprenorphine (Subutex) Tablets  

Microsoft Academic Search

Background: Buprenorphine (Subutex) is the most abused opioid in Finland. In order to curb the abuse potential of this drug, many treatment centers and prisons crush Subutex tablets before administering them to patients. To date, there are no published studies comparing the efficacy and bioavailability of crushed and whole Subutex tablets. Methods: A total of 16 opioid-dependent patients stabilized on

Kaarlo Simojoki; Pirjo Lillsunde; Nicholas Lintzeris; Hannu Alho

2010-01-01

211

A systematic and mechanistic evaluation of aspartic acid as filler for directly compressed tablets containing trimethoprim and trimethoprim aspartate.  

PubMed

The generally accepted paradigm of 'inert' and 'mono functional' excipient in dosage form has been recently challenged with the development of individual excipients capable of exhibiting multiple functions (e.g. binder-disintegrants, surfactant which affect P-gp function). The proposed study has been designed within the realm of multifunctionality and is the first and novel investigation towards evaluation of aspartic acid as a filler and disintegration enhancing agent for the delivery of biopharmaceutical class IV model drug trimethoprim. The study investigated powder characteristics using angle of repose, laser diffractometry and scanning electron microscopy (SEM). The prepared tablets were characterised using Heckel analysis, disintegration time and tensile strength measurements. Although Heckel analysis revealed that both TMP and TMP aspartate salt have high elasticity, the salt form produced a stronger compact which was attributed to the formation of agglomerates. Aspartic acid was found to have high plasticity, but its incorporation into the formulations was found to have a negative impact on the compaction properties of TMP and its salt. Surface morphology investigations showed that mechanical interlocking plays a vital role in binding TMP crystals together during compaction, while the small particle size of TMP aspartate agglomerates was found to have significant impact on the tensile strength of the tablets. The study concluded that aspartic acid can be employed as filler and disintegrant and that compactability within tablets was independent of the surface charge of the excipients. PMID:23207325

ElShaer, Amr; Hanson, Peter; Mohammed, Afzal R

2012-12-01

212

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

213

[Studies of the properties of tablets made from directly compressible starch and its mixtures with directly compressible lactose].  

PubMed

The paper studies the strength and disintegration time of compacts made from directly compressible Starch 1500 and its mixtures with directly compressible lactose Pharmatosa DCL 15 in different relative proportions in dependence on the added lubricant magnesium stearate and the model active ingredient ascorbic acid. The dry binders under study differ in their mechanisms of compression and thus in their sensitivity to the addition of the lubricant, which is manifested in decreased strengths of the compacts as well as the mechanism of disintegration of the compacts. The mixtures of substances under study were in the relative representations of 1:3, 1:1 and 3:1. The employed concentration of the lubricant magnesium stearate was 0.4%, that of ascorbic acid, 50%. The study has confirmed and quantitatively evaluated the sensitivity of directly compressible starch to the addition of magnesium stearate. A higher share of directly compressible lactose in the mixture decreased the sensitivity of tableting material to the addition of the lubricant and shortened disintegration time. The presence of stearate did not negatively influence disintegration time, with an exception of the mixture of Starch 1500 and Pharmatosa DCL 15 1:3. An addition of the model active ingredient ascorbic acid decreased the strength of the compacts and shortened the disintegration time in all tableting materials tested. PMID:17128594

Muzíková, J; Moucková, E

2006-09-01

214

The tableting properties of melibiose monohydrate.  

PubMed

In this research, the tableting properties of ?-melibiose monohydrate were studied. Melibiose is a disaccharide which bears structural resemblance to lactose, because they both consist of galactose and glucose monosaccharide subunits. Compactibility and deformation behavior of two melibiose batches from different suppliers were studied and compared with ?-lactose monohydrate and some other typical tableting excipients. Differences in the deformation behavior were determined comparing the shape of the Heckel plots, the yield pressure values and the strain rate sensitivity (SRS) indexes. In addition, the effect of moisture on the tabletability was studied. According to the yield pressures and SRS indexes melibiose was concluded to be fragmenting, even at higher degree than lactose monohydrate. However, the overall deformation behavior of melibiose was found to be similar to that of lactose monohydrate. Increase in moisture content resulted in higher tensile strengths of tablets for both melibiose batches, but it seemed to have more effect on compactibility of the other batch. In conclusion, melibiose has potential to be used as an excipient in tablet formulations. PMID:23994759

Lakio, Satu; Sainio, Janne; Heljo, Petteri; Ervasti, Tuomas; Kivikero, Niina; Juppo, Anne

2013-08-28

215

Bulk Raman analysis of pharmaceutical tablets.  

PubMed

We compare and contrast two Raman collection geometries, backscattering and transmission, to identify their potential for monitoring the bulk chemical composition of turbid media. The experiments performed on pharmaceutical tablets confirm the expected strong bias of the backscattering Raman collection towards surface layers of the probed sample. However, this bias is largely absent with the transmission geometry, exhibiting gross insensitivity to the depth of impurities within the sample. The results are supported by Monte-Carlo simulations. The applicability of transmission geometry to tablets without any thinning is possible because of long migration times of Raman photons in non-absorbing powder media. The absolute measured intensity of the Raman signal was only 12 times lower in transmission geometry compared with backscattering geometry for a standard paracetamol tablet with a thickness of 3.9 mm. This makes detection relatively straightforward, and detectable Raman signals were observed even after propagation through three paracetamol tablets. Given its properties and instrumental simplicity, the transmission method is particularly well suited to the on-line analysis of bulk content of tablets in pharmaceutical applications. PMID:17217583

Matousek, P; Parker, A W

2006-12-01

216

ELECTRONIC ANALOG COMPUTER FOR DETERMINING RADIOACTIVE DISINTEGRATION  

DOEpatents

A computer is presented for determining growth and decay curves for elements in a radioactive disintegration series wherein one unstable element decays to form a second unstable element or isotope, which in turn forms a third element, etc. The growth and decay curves of radioactive elements are simulated by the charge and discharge curves of a resistance-capacitance network. Several such networks having readily adjustable values are connected in series with an amplifier between each successive pair. The time constant of each of the various networks is set proportional to the half-life of a corresponding element in the series represented and the charge and discharge curves of each of the networks simulates the element growth and decay curve.

Robinson, H.P.

1959-07-14

217

Influence of layer position on in vitro and in vivo release of levodopa methyl ester and carbidopa from three-layer matrix tablets  

Microsoft Academic Search

A versatile oral controlled release system for the simultaneous delivery of levodopa methyl ester and carbidopa, consisting of a three-layer matrix tablet, has been studied and developed. Each individual layer of the matrix exhibited a different release mechanism, i.e. the first layer was swellable (S), the second one was erodible (E) and the third one was disintegrating (D). The three

R Bettini; D Acerbi; G Caponetti; R Musa; N Magi; P Colombo; D Cocconi; P Santi; P. L Catellani; P Ventura

2002-01-01

218

Evaluation of Water Sterilizing Tablets.  

National Technical Information Service (NTIS)

Water sterilizing tablets were evaluated for efficiency of kill of micro-organisms, effect of inhibitors and palatability. The effect of long term use is discussed. The water sterilizing tablet recommended for disinfection of personal drinking water, on t...

G. F. Thomson K. W. James G. E. Driver A. T. Hancock

1985-01-01

219

Preparation and In Vitro/In Vivo Characterization of Porous Sublingual Tablets Containing Ternary Kneaded Solid System of Vinpocetine with ?-Cyclodextrin and Hydroxy Acid  

PubMed Central

The demand for sublingual tablets has been growing during the previous decades especially for drugs with extensive hepatic first-pass metabolism. Vinpocetine, a widely used neurotropic agent, has low oral bioavailability due to its poor aqueous solubility and marked first-pass metabolism. Accordingly, the aim of this work was to develop tablets for the sublingual delivery of vinpocetine. Initially, the feasibility of improving vinpocetine’s poor aqueous solubility by preparing kneaded solid systems of the drug with ?-Cyclodextrin and hydroxy acids (citric acid and tartaric acid) was assessed. The solid system with improved solubility and dissolution properties was incorporated into porous tablets that rapidly disintegrate permitting fast release of vinpocetine into the sublingual cavity. The pores were induced into these tablets by directly compressing the tablets’ excipients with a sublimable material, either camphor or menthol, which was eventually sublimated leaving pores. The obtained results demonstrated that the tablets prepared using camphor attained sufficient mechanical strength for practical use together with rapid disintegration and dissolution. In vivo absorption study performed in rabbits indicated that the sublingual administration of the proposed porous tablets containing vinpocetine solid system with ?-Cyclodextrin and tartaric acid could be useful for therapeutic application.

Aburahma, Mona H.; El-Laithy, Hanan M.; Hamza, Yassin El-Said

2010-01-01

220

Development and characterization of buccoadhesive nifedipine tablets.  

PubMed

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 drug release kinetic. The adhesion force was significantly affected by the mixing ratio of CP:CMC in the tablets. The weakest and highest adhesion force was observed at the mixing ratios of 1:0 and 8:2 of CP:CMC, respectively. The tablets containing 15% CMC and 35% CP adhered for over 8h to the upper gums of six healthy human volunteers. These tablets released about 56% of the loaded drug after 8h in vivo with a rate of 2.17h(-1) and were perfectly tolerated, while they released about 100% of their content after the same time with a rate of 3.49h(-1) in vitro. A good correlation (r(2)=0.989) was observed between drug-released in vitro and in vivo. PMID:12191683

Varshosaz, J; Dehghan, Z

2002-09-01

221

Mechanistic investigation of food effect on disintegration and dissolution of BCS class III compound solid formulations: the importance of viscosity.  

PubMed

A negative food effect, i.e. a decrease in bioavailability upon the co-administration of compounds together with food, has been attributed particularly with high solubility/low permeability compounds (BCS class III). Different mechanisms have been proposed including intestinal dilution leading to a lower concentration gradient across the intestinal wall as well as binding of the active pharmaceutical ingredient to food components in the intestine and thereby decreasing the fraction of the dose available for absorption. These mechanisms refer primarily to the compound and not to the dosage form. An increase in viscosity of the dissolution fluid will in particular affect the absorption of BCS type III compounds with preferential absorption in the upper small intestine if the API release is delayed from the dosage form. The present study demonstrated that the increase in viscosity of the dissolution medium, following ingestion of a solid meal, may drastically reduce disintegration and dissolution. For that purpose the viscosity of the standard FDA meal was determined and simulated by solutions of HPMC in buffer. As model formulations, three commercially available tablets containing trospium chloride, a BCS class III m-cholinoreceptor antagonist was used. Trospium chloride drug products have been described to undergo a negative food effect of more than 80% following ingestion with food. The tablets showed prolonged disintegration times and reduced dissolution rates in viscous media, which could be attributed to changes in the liquid penetration rates. The effect was particularly significant for film-coated tablets relative to uncoated dosage forms. The results show the necessity of considering media viscosity when designing in vitro models of drug release for BCS type III drug formulations. PMID:22782559

Radwan, Asma; Amidon, Gordon L; Langguth, Peter

2012-08-11

222

Pharmaceutical quality of seven generic Levodopa/Benserazide products compared with original Madopar(R) / Prolopa(R)  

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.

2013-01-01

223

Tabletability assessment of conventional formulations containing Vitamin E tocopheryl polyethylene glycol succinate.  

PubMed

Vitamin E tocopheryl polyethylene glycol succinate (TPGS) is known to enhance the bioavailability of poorly water-soluble drugs via solubility and permeability enhancement. Few studies have evaluated feasibility of formulating TPGS in conventional solid dosage forms such as tablets due to processing challenges resulting from its waxy nature and low melting point (approximately 37 degrees C). The objective of this study is to systematically investigate the tabletability of conventional high shear wet granulation (WG) formulations incorporated with Vitamin E TPGS. Impact of critical formulation variables such as levels of TPGS, hydroxypropyl cellulose (binder) and Prosolv (extragranular filler) on product quality attributes was studied using a full factorial experimental design. The potential influence of temperature elevation during processing was assessed through a heated die fitted onto a compaction simulator. Bilayer tabletability of the TPGS formulation was also assessed in combination with a secondary non-TPGS formulation. TPGS levels significantly impacted tensile strength (TS), disintegration time and dissolution. Heat sensitivity studies indicated that TS reduction upon exposure to heat was minimized by higher levels of extragranular fillers. Acceptable interfacial strength of bilayer tablets was achieved and tablets could be coated without the need for hydroalcoholic solutions. The study demonstrates preliminary feasibility to develop monolithic and bilayer coated tablet formulations containing up to 10% (w/w) TPGS for the given compound and drug load. Further studies are required to validate these findings at larger scales. PMID:20083178

Jin, Feiyan; Tatavarti, Aditya

2010-01-18

224

Are tablets a practical source of protein substitute in phenylketonuria?  

PubMed Central

Background: A phenylalanine-free amino acid based protein substitute is necessary to provide the major source of protein in phenylketonuria (PKU). Protein substitutes in PKU are usually given as drinks. These are unpalatable and compliance is often poor. Tablets containing a suitable mixture of phenylalanine-free amino acids (Aminogran Food Supplement, UCB) are now available. Aims: To compare the effectiveness and acceptability of these tablets with conventional protein substitute drinks. Methods: Twenty one subjects with PKU, aged 8–25 years, participated in a randomised crossover study. During one phase, subjects received at least 40% of their protein substitute requirements from the amino acid tablets and the rest from their usual protein substitute tablets. During the other phase, they received their usual protein substitute. Each period lasted 12 weeks. Blood phenylalanine concentrations were measured at least once every two weeks and other plasma amino acids were measured at the beginning, at crossover, and at the end of the study. The subjects kept a diary of all protein substitute taken. Results: Compliance appeared to be better with the new tablets than with patients' usual protein substitutes. Ninety per cent (18/20) recorded that they took the tablets as prescribed, compared with 65% (13/20) fully compliant with their usual protein substitute. Moreover, plasma phenyalanine was lower on the amino acid tablets, and the median difference in blood concentrations between the two groups was 46 µmol/l (95% CI 14.8 to 89.0, p = 0.02). Tyrosine increased by a median of 16 µmol/l daily on the amino acid tablets (95% CI 7.1 to 40.5, p = 0.01). Most subjects (70%) preferred incorporating the new tablets into their usual protein substitute regimen. Conclusions: Amino acid tablets are an effective and relatively popular protein substitute in older children, teenagers, and adults with PKU.

MacDonald, A; Ferguson, C; Rylance, G; Morris, A; Asplin, D; Hall, S; Booth, I

2003-01-01

225

The use of the SeDeM Diagram expert system to determine the suitability of diluents–disintegrants for direct compression and their use in formulation of ODT  

Microsoft Academic Search

The new SeDeM Diagram expert system was used to analyze the suitability of 43 excipients for direct compression with disintegrant properties from eight chemical families. The SeDeM Diagram expert system is a new method for use in tablet preformulation and formulation studies. It provides the profile of a substance in powder form in terms of its suitability for direct compression.This

Johnny Edward Aguilar-Díaz; Encarnación García-Montoya; Pilar Pérez-Lozano; José María Suñe-Negre; Montserrat Miñarro; José Ramón Ticó

2009-01-01

226

Sustained-release dosage form of phenylpropanolamine hydrochloride. Part II: Formulation and in vitro release kinetics from tableted microcapsules.  

PubMed

This work was planned to prepare sustained-action preparations of phenylpropanolamine hydrochloride by microencapsulation and by tableted microcapsules. Dissolution from both suspended microcapsules and the tablets was studied using the USP XXII basket method in simulated gastric and intestinal fluid without enzyme. The results were applied to zero-order, first-order, Hixson Crowell, RRSBW, Q/square root of t, (Bt)a and Higuchi kinetic models. Dissolution of PPA.HCl was found to be governed by the core:wall ratio, drug particle size, media pH and type of disintegrating agent. Dissolution kinetics were studied and evaluated. PMID:8064557

Sevgi, F; Ozyazici, M; Güneri, T

227

Comparative efficacy of a spot-on formulation containing emodepside and praziquantel (Profender ®, Bayer) and praziquantel and pyrantel oral tablets (Drontal ® for Cats) against experimental Ancylostoma ceylanicum infections in cats.  

PubMed

Ancylostoma ceylanicum is a common zoonotic hookworm of dogs and cats throughout Asia and has also been reported to occur within the Australasian region. The aim of this study to was to determine the efficacy of a spot-on formulation containing emodepside and praziquantel (Profender(®), Bayer) and praziquantel and pyrantel oral tablets (Drontal(®) for Cats, Bayer) against experimental A. ceylanicum infections in cats. Twenty-four kittens were each subcutaneously injected with 100 infective third-stage larvae of A. ceylanicum. Kittens were stratified by egg count and randomly allocated equally into control and two treatment groups. The first group were treated with emodepside 2.1%/praziquantel 8.6% (Profender®, Bayer) at the recommended label dose. The second group was treated with 80 mg pyrantel and 20mg praziquantel (Drontal(®) for Cats, Bayer) at the recommended label dose. The kittens in the control group were not treated. Egg counts were performed daily until the end of the study period and compared for the treated and control groups. No eggs were detected in the treated group of kittens within 4 days of treatment and faecal samples from this group remained negative throughout the rest of the study, resulting in a treatment efficacy (egg reduction) of 100% (P<0.0001). The egg counts remained high (993 ± 666 epg) in the untreated control group for the rest of the study period. This study demonstrated that both combination products containing topical emodepside/praziquantel (Profender(®), Bayer) and praziquantel/pyrantel oral tablets (Drontal(®) for Cats, Bayer) given at the recommended dose is highly effective against infection with A. ceylanicum in cats. PMID:23026558

Taweethavonsawat, Piyanan; Chungpivat, Sudchit; Watanapongchati, Supoj; Traub, Rebecca J; Schaper, Roland

2012-09-04

228

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…

Rapp, David

2011-01-01

229

The Nebusarsekim Tablet  

Microsoft Academic Search

During the summer of 2007 an internet hype was unleashed by the breaking news that an Old Testament name of some importance, figuring in the Book of Jeremiah Ch. 39, had been positively identified on a cuneiform clay tablet, viz. a bill of receipt from the time of this prophet's floruit. Many a scholar of sorts was quick to claim

H. A. I. Stadhouders

2008-01-01

230

[When latex disintegrates, or a mechanical pyloric ulcer].  

PubMed

Complications of Celestin oesophageal tube disintegration are discussed with reference to the case of a patient with a tube inserted because of extrinsic stenosis presenting with upper abdominal complaints. PMID:2234165

Dees, A; Hoff, A M; Mali, S P; Hordijk, M L

1990-10-13

231

Waste activated sludge hydrolysis during ultrasonication: two-step disintegration.  

PubMed

In order to clearly describe the hydrolysis of waste activated sludge (WAS) during ultrasonication by a 2-step disintegration process, concentrations of ribonucleic acid (RNA) and bound extracellular polymeric substance (EPS) were measured. Apparently, different decreasing patterns of RNA and EPS concentrations during WAS hydrolysis made it possible to distinguish the floc disintegration (FD) and cell lysis (CL). Initially, FD and CL appear to take simultaneously, but the dominant hydrolytic process is shifted from FD to CL after 10 min of ultrasonication. Additional kinetic analysis of WAS hydrolysis was also conducted. A five-fold greater hydrolysis rate constant of FD relative to that of CL was observed, reflecting the different strengths of floc and cells. Therefore, different rates of increased solubilization during WAS hydrolysis appear to account for the initial disintegration of the rather loose part (sludge floc) and the subsequent disintegration of the rigid part (microbial cells). PMID:22850171

Cho, Si-Kyung; Shin, Hang-Sik; Kim, Dong-Hoon

2012-07-16

232

Technological evaluation and equivalence assessment of lorazepam tablets in rabbits.  

PubMed

Four different oral lorazepam tablets (Tavor tablets as reference preparation and three generic tablet formulations, A, B and C) were investigated after administration to 12 rabbits to evaluate their bioequivalence. A single 2 mg/kg dose was administered orally as powder and lorazepam plasma concentrations were determined by a validated HPLC method. Maximum plasma concentrations (Cmax), of 207 ng/ml (reference), 198 ng/ml (A), 166 ng/ml (B) and 169 ng/ml (C) were achieved. Lorazepam appeared in the plasma at 0.66 h (Tmax) for all formulations, probably because the disintegration step was bypassed due to the pulverization of the administered doses. Areas under the plasma concentration-time curves (AUC(0-t) and AUC(0-infinity)) were determined. The obtained AUC(0-t) values were 556.57 ng h/ml (reference), 554.70 ng h/ml (A), 493.08 ng h/ml (B), and 487.88 ng h/ml (C). ANOVA results (P > or = 0.05) and 90% confidence intervals for the mean ratio (T/R) of AUC(0-t), AUC(0-infinity), and Cmax were within the EMEA acceptance range. Pharmacokinetic and statistical results of this study show that the four tested drug products (Tavor, A, B, C) are to be considered bioequivalent and interchangeable in medical practice. PMID:17718192

Ventura, C A; Giannone, I; Musumeci, T; Pignatello, R; Puglisi, G

2007-07-01

233

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.

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

2013-01-01

234

The General Theory of Fluctuations in Radioactive Disintegration  

Microsoft Academic Search

The chance, Wn(0,t), that n atoms of a radioactive source will disintegrate in the interval (0,t) may be found if we know fr(t)dt, the chance that a disintegration will occur in dt at t after r have occurred in (0,t). Bateman's differential equation is generalized to cover the case in which fr depends on t and r. The solution is

Arthur Ruark; Lee Devol

1936-01-01

235

Detection of Nuclear Disintegration in a Photographic Emulsion  

Microsoft Academic Search

IT has been shown recently by Chadwick and Goldhaber1, and by Fermi and his collaborators2, that some light nuclei, particularly lithium and boron, are disintegrated by slow neutrons. In the case of boron, the mass-energy relations seemed best satisfied by assuming a disintegration into three particles1. The simplest reaction, namely: should, according to the accepted masses of the particles, release

H. J. Taylor; M. Goldhaber

1935-01-01

236

Ultrasonic waste activated sludge disintegration for improving anaerobic stabilization  

Microsoft Academic Search

The pretreatment of waste activated sludge by ultrasonic disintegration was studied in order to improve the anaerobic sludge stabilization. The ultrasound frequency was varied within a range from 41 to 3217kHz. The impact of different ultrasound intensities and treatment times was examined. Sludge disintegration was most significant at low frequencies. Low-frequency ultrasound creates large cavitation bubbles which upon collapse initiate

A Tiehm; K Nickel; M Zellhorn; U Neis

2001-01-01

237

Application of guar gum biopolymer in the prescription of tablets with sodium ibuprofen--quality tests and pharmaceutical availability in vitro.  

PubMed

The increasing interest of the technology of drug form in natural biopolymers has become the reason for undertaking investigations on the possibility of guar gum application in the prescription of oral solid form of a drug. Alternative compositions and technology of the production of tablets of regulated in time sodium ibuprofen release were worked out for children. Two series of tablets were prepared with guar gum (5 and 10% content) and a series without the biopolymer. The tablet mass in each case contained keryostatic sorbitol and bioadhesive polyvinylpyrrolidone. All tablets were tested as regards the quality of production, compliance with the requirements of Polish Pharmacopoeia VI and potential therapeutic usefulness, manifestation of which is pharmaceutical availability of the therapeutic agent (sodium ibuprofen). The tests demonstrated that the produced tablets with sodium ibuprofen have proper physicochemical properties, in compliance with Polish Pharmacopoeia VI requirements. Application of biopolymer of guar gum type as adjuvant substance contributes to the improvement of the tablet hardness parameters and prevents technological problems (lining mixture of powders to tableting machine punch). The designed tablets demonstrate proper pharmaceutical availability of over 80%. Introduction of guar gum into their prescription prolonged their disintegration time and the rate of sodium ibuprofen release, which predisposes the produced form of a drug to have the function of a tablet with slowed-down release. PMID:17402228

Berner-Strzelczyk, Aneta; Ko?odziejska, Justyna; Zgoda, Marian Miko?aj

2006-01-01

238

Characterization of low crystallinity cellulose as a direct compression excipient: Effects of physicochemical properties of cellulose excipients on their tabletting characteristics  

NASA Astrophysics Data System (ADS)

A scale-up method for the preparation of a new excipient, low crystallinity powder cellulose (LCPC), was established. Physicochemical characterization of a series of LCPC materials was performed, and compared to the physicochemical properties of commercially existing cellulose excipients, microcrystalline cellulose (AvicelsRTM) and powdered celluloses (Solka Flocs RTM). Low crystallinity cellulose powders had high amorphous contents (>50%) and a low degree of polymerization (<40 anhydroglucose units). They were dense aggregates with porosity values less than 62%. Low crystallinity cellulose was found to contain cellulose II as the predominant polymorphic form in the crystalline regions. LCPC particles, obtained from larger scale preparations (>2 kg), typically showed low yield pressures (<75 MPa), high compressibility (>200 MPa), and intermediate compactability (250--600 MPa2) values. Mechanical characterization of the three types of cellulose materials, and the statistical models obtained for the results, indicated that a high porosity (>810%), a high average of amorphous content (>40%) and moisture content (>4%), and a low degree of polymerization (<150) significantly lowered the yield pressures, and significantly enhanced the compressibility and compactability. The bonding indices of microcrystalline celluloses (0.013 to 0.031) and LCPC materials (0.011 to 0.020) investigated indicated a ductile behavior. The LCPC compacts showed a higher brittle fracture propensity (0.42 to 0.55) as compared to the brittle fracture indices (0.02 to 0.19) seen for the Avicel RTM compacts. Heckel analysis of different particle size fractions of LCPC and the surface area results of the LCPC compacts indicated that the particles do not fragment on uniaxial compression. The rapid disintegration times (5 to 90 seconds) for LCPC tablets at low as well as high solid fractions suggest the high affinity of these materials to water, due to their high amorphous contents that expose a larger number of hydroxyl groups to water, compared to the more crystalline materials, such as microcrystalline celluloses, the tablets of which showed extremely long disintegration times (24 to 6000 seconds). The physicochemical and mechanical characterization of low crystallinity cellulose suggests it to be a promising direct compression excipient for immediate release tablet formulations.

Kothari, Sanjeev Hukmichand

239

The natural history of somatic morbidity in disintegrative psychosis and infantile autism: a validation study  

Microsoft Academic Search

In order to study the validity of disintegrative psychosis (DP) as defined in ICD-9, we compared the natural history of somatic morbidity of 13 patients given this diagnosis in childhood with a control group of 39 patients with infantile autism (IA) matched for gender, age, IQ and social class. Average follow-up time was 22 and 23 (11–33) years, respectively. Significantly

Svend Erik Mouridsen; Bente Rich; Torben Isager

1999-01-01

240

Modulation of drug release kinetics of shellac-based matrix tablets by in-situ polymerization through annealing process.  

PubMed

A new oral-controlled release matrix tablet based on shellac polymer was designed and developed, using metronidazole (MZ) as a model drug. The shellac-based matrix tablets were prepared by wet granulation using different amounts of shellac and lactose. The effect of annealing temperature and pH of medium on drug release from matrix tablets was investigated. The increased amount of shellac and increased annealing temperature significantly affected the physical properties (i.e., tablet hardness and tablet disintegration) and MZ release from the matrix tablets. The in-situ polymerization played a major role on the changes in shellac properties during annealing process. Though the shellac did not dissolve in acid medium, the MZ release in 0.1N HCl was faster than in pH 7.3 buffer, resulting from a higher solubility of MZ in acid medium. The modulation of MZ release kinetics from shellac-based matrix tablets could be accomplished by varying the amount of shellac or annealing temperature. The release kinetics was shifted from relaxation-controlled release to diffusion-controlled release when the amount of shellac or the annealing temperature was increased. PMID:18362064

Limmatvapirat, Sontaya; Limmatvapirat, Chutima; Puttipipatkhachorn, Satit; Nunthanid, Jurairat; Luangtana-anan, Manee; Sriamornsak, Pornsak

2008-02-05

241

Glycerin fatty acid esters as a new lubricant of tablets.  

PubMed

Lubrication properties were compared among glycerin fatty acid esters (Poem TR-FB and Poem TR-HB), magnesium stearate (Mg-St), and a sucrose fatty acid ester (RYOTO SUGAR ESTER S-370F: SSE). Granules containing 50% acetaminophen were prepared, and improvements in their fluidity by the lubricants were compared. The lubricant effects of TR-FB and HB during tablet punching (pressure transmission ratio, ejection force) were similar to those of Mg-St and were better than those of SSE. When the lubricant content, mixing time, and tabletting pressure were changed, TR-FB and TR-HB provided better tablet hardness than Mg-St. TR-FB and TR-HB made tablets more disintegratable than Mg-St. When the effects of these lubricants on the stability of acetylsalicylic acid (ASA) were compared, Mg-St promoted its hydrolysis, but TR-FB or TR-HB did not affect its stability. PMID:15778041

Aoshima, Hiroyuki; Miyagisnima, Atsuo; Nozawa, Yasuo; Sadzuka, Yasuyuki; Sonobe, Takashi

2005-04-11

242

Preparation and in vitro/in vivo characterization of porous sublingual tablets containing ternary kneaded solid system of vinpocetine with î-cyclodextrin and hydroxy Acid.  

PubMed

The demand for sublingual tablets has been growing during the previous decades especially for drugs with extensive hepatic first-pass metabolism. Vinpocetine, a widely used neurotropic agent, has low oral bioavailability due to its poor aqueous solubility and marked first-pass metabolism. Accordingly, the aim of this work was to develop tablets for the sublingual delivery of vinpocetine. Initially, the feasibility of improving vinpocetineâs poor aqueous solubility by preparing kneaded solid systems of the drug with Î-Cyclodextrin and hydroxy acids (citric acid and tartaric acid) was assessed. The solid system with improved solubility and dissolution properties was incorporated into porous tablets that rapidly disintegrate permitting fast release of vinpocetine into the sublingual cavity. The pores were induced into these tablets by directly compressing the tabletsâ excipients with a sublimable material, either camphor or menthol, which was eventually sublimated leaving pores. The obtained results demonstrated that the tablets prepared using camphor attained sufficient mechanical strength for practical use together with rapid disintegration and dissolution. In vivo absorption study performed in rabbits indicated that the sublingual administration of the proposed porous tablets containing vinpocetine solid system with Î-Cyclodextrin and tartaric acid could be useful for therapeutic application. PMID:21179352

Aburahma, Mona H; El-Laithy, Hanan M; Hamza, Yassin El-Said

2010-05-17

243

A study of the properties of tablets made of directly compressible maltose.  

PubMed

The paper deals with the study of the strength and disintegration time of tablets made of directly compressible maltose Advantose 100. It studies the differences of the effects of two types of lubricants, magnesium stearate and sodium stearylfumarate, on the above-mentioned properties, and it also tests the mixtures of the substance with microcrystalline cellulose Vivapur 102 in a ratio of 1:1 and with ascorbic and acetylsalicylic acids. The compacts are obtained by using three compression forces, excepting mixtures with active ingredients, where one compression force is used. In the compression forces of 6 and 8 kN, no statistically significant difference was found in the intervention of the lubricants into the strength of the compacts made of Advantose 100, only in the compression force of 10 kN Pruv decreased the strength more than stearate. The mixture of Advantose 100 and Vivapur 102 yielded the strongest tablets, an addition of Pruv to it decreased the strength of compacts more than stearate. The periods of disintegration time of Advantose compacts as well as those of the mixture of dry binders were longer with an addition of Pruv. The compacts with acetylsalicylic acid possessed higher strength and a longer period of disintegration than those with ascorbic acid. There was no statistically significant difference within the type of the lubricant employed, both in the case of Advantose 100 and its mixture with Vivapur 102, between the values of strength of the compacts with acetylsalicylic acid. PMID:18383920

Muzíková, J; Balhárková, J

2008-01-01

244

In-line monitoring of the drug content of powder mixtures and tablets by near-infrared spectroscopy during the continuous direct compression tableting process.  

PubMed

Continuous manufacturing methods offer economic and quality advantages when compared with batch manufacturing methods. In continuous manufacturing, one requires real time assurance of quality of product via the implementation of PAT tools. This study focuses on an in-line near-infrared (NIR) spectroscopic method for determining the drug content of powder mixtures and tablets during a continuous tableting process. Tablets consisting of acetaminophen (20-30%), lactose (69.07-78.93%) and magnesium stearate (0.93-1.07%) were prepared in a continuous direct compression line that consisted of two loss-in-weight feeders, one for acetaminophen and one for premixed lactose and magnesium stearate, and a continuous mixer followed by a rotary tablet press. NIR spectroscopy was applied to the continuous mixer and tablet press to perform a 100% product check at full tableting speed. The UV-spectrophotometric method was used as an off-line reference method to determine the acetaminophen content in the samples. The powder mixture and tablet samples were taken during the process for the calibration of continuous mixer and tablet press, respectively. For the continuous mixer, model creation with the PLS method yielded R-Square and RMSEC (root mean square error of calibration) values of 0.975% and 0.56%, respectively. For the tablet press, the corresponding R-Square and RMSEC values were 0.943% and 0.75%, respectively. A test run demonstrated good predictability in the estimation of the API content in the powder mixtures and tablets during the continuous tableting process. For the continuous mixer and tablet press, the RMSEP (root mean square error of prediction) values were 0.96% and 1.37%, respectively. This study demonstrates that an NIR instrument capable of fast spectra acquisition can be a valuable tool for the in-line monitoring of the continuous mixing and tableting processes. PMID:23313622

Järvinen, Kristiina; Hoehe, Wolfgang; Järvinen, Maiju; Poutiainen, Sami; Juuti, Mikko; Borchert, Sven

2013-01-10

245

A randomized, open-label, comparative efficacy trial of artemether-lumefantrine suspension versus artemether-lumefantrine tablets for treatment of uncomplicated Plasmodium falciparum malaria in children in western Kenya  

Microsoft Academic Search

BACKGROUND: Artemether\\/lumefantrine (AL) has been adopted as the treatment of choice for uncomplicated malaria in Kenya and other countries in the region. Six-dose artemether\\/lumefantrine tablets are highly effective and safe for the treatment of infants and children weighing between five and 25 kg with uncomplicated Plasmodium falciparum malaria. However, oral paediatric formulations are urgently needed, as the tablets are difficult

Elizabeth A Juma; Charles O Obonyo; Willis S Akhwale; Bernhards R Ogutu

2008-01-01

246

[A study of the properties of tablets from mixtures of two size degrees of alpha-lactose monohydrate and microcrystalline cellulose].  

PubMed

The paper examines the strength and disintegration time of compacts from the mixtures of two types of Tablettosas. Tablettosa 70 and Tablettosa 100 with microcrystalline cellulose represented by Vivapur 102. The mixtures of dry binders were prepared in the ratios of 3:1, 1:1, and 1:3. The effect of two concentrations of the lubricant magnesium stearate on the strength and disintegration time of compacts was also examined. Tablet strength increased with higher representation of microcrystalline cellulose in the mixture, and decreased with higher stearate concentration. The compacts from the mixtures with Tablettosa 100 showed higher strength. Disintegration time was highest in the compacts with the largest perccintage of microcrystalline cellulose, and longer in the case of the mixtures with Tablettosa 100. Stearate did not exert a negative effect on disintegration time. In the mixtures of Tablettosas with Vivapur 102 in a ratio of 1:1, the effect of the model active ingredient acetylsalicylic acid on the above-mentioned properties of tablets was tested. acetylsalicylic acid produced a further decrease in the strength of compacts and shortened the disintegration time in more instances in the cased of the mixtures with Tahlettosa 100. PMID:16570584

Muzíková, J

2006-03-01

247

Study plasma disintegration based on the fluorescence spectroscopy  

NASA Astrophysics Data System (ADS)

It is known that plasma is very important in the diagnosis and therapy of disease so that more and more scientific workers attach importance to the plasma storage life or storage environment. We research plasma disintegration with the increases of storage time based on the fluorescence spectroscopy. Based on the experimental researches and theoretical analysis, we find that their plasma fluorescence intensity is increasing within about 10 hours, and but is decreasing gradually and is nearly a straight line after this. It is indicated that plasma proteins have begun to disintegrate so as to make the fluorescence quenching after storage time beyond 10 hours. And the disintegration speed of plasma in the case of different concentration is different, the concentration is higher and the speed is lower in them, and but they are almost same after about 35 hours. Therefore, we think that plasma under higher concentration is deposited easier. These research consequences may order a theoretical and experimental reference to know the changes of plasma in structure in different disintegration time. It may make sense for understand the plasma disintegrative mechanism and distinguishing the fine plasma with faulty.

Gao, Shumei; Li, Rongqing; Chen, Guoqing; Lu, Jun

2007-10-01

248

The Dynamic Mu Transpososome: MuB activation prevents disintegration  

PubMed Central

Summary DNA transposases use a single active center to sequentially cleave the transposable element DNA and join this DNA to a target site. Recombination requires controlled conformational changes within the transposase to ensure that these chemically distinct steps occur at the right time and place, and that the reaction proceeds in the net forward direction. Mu transposition is catalyzed by a stable complex of MuA transposase bound to paired Mu DNA ends (a transpososome). We find that Mu transpososomes efficiently catalyze disintegration when recombination on one end of the Mu DNA is blocked. The MuB activator protein controls the integration vs. disintegration equilibrium. When MuB is present, disintegration occurs slowly and transpososomes that have disintegrated catalyze subsequent rounds of recombination. In the absence of MuB, disintegration goes to completion. These results together with experiments mapping the MuA-MuB contacts during DNA joining suggest that MuB controls progression of recombination by specifically stabilizing a concerted transition to the ‘joining’ configuration of MuA. Thus, we propose that MuB's interaction with the transpososome actively promotes coupled joining of both ends of the element DNA into the same target site and thus may provide a mechanism to antagonize formation of single-end transposition products.

Lemberg, Kathryn M.; Schweidenback, Caterina T. H.; Baker, Tania A.

2007-01-01

249

A randomised trial of glucose tablets to aid smoking cessation  

Microsoft Academic Search

Rationale Oral glucose has been found to decrease tobacco craving among abstaining smokers. One study has demon- strated an effect of glucose on short-term abstinence. There is a need to examine any long-term benefit of glucose on abstinence. Objectives To assess whether glucose tablets improve 6-month continuous abstinence rates compared with low- calorie placebo tablets. Methods Smokers attempting to stop

Robert West; Sylvia May; Andy McEwen; Hayden McRobbie; Peter Hajek; Eleni Vangeli

2009-01-01

250

Photoimages and the release characteristics of lipophilic matrix tablets containing highly water-soluble potassium citrate with high drug loadings.  

PubMed

Two types of the carnauba wax-based lipophilic matrix tablet using spray-dried granules (SDT) or directly compressible powdered mixtures (DCT) were prepared for sustained release. The model drug was a highly water-soluble potassium citrate and loaded about 74% of the total tablet weight. The SDT slowly eroded and disintegrated during the release study without showing sustained release when the hydrophilic excipients were added. In contrast, the DCT was more efficient for sustained release. The release rate decreased with increasing carnauba wax concentration. In particular, the sustained release rate was markedly pronounced when the lipophilic stearyl alcohol and stearic acid were combined with the carnauba wax. The surface of the intact DCT appeared to be smooth and rusty. The DCT rose to the surface from the bottom of the vessel during the release test, and numerous pores and cracks with no signs of disintegration were also observed after the release test. The release profile was dependent on the formulation composition and preparation method of the matrix tablet. Diffusion-controlled leaching through the channels of the pores and cracks of the lipophilic matrix tablet (DCT) is a key to the sustained release. PMID:17532156

Cao, Qing-Ri; Kim, Tae-Wan; Lee, Beom-Jin

2007-04-24

251

Unwrapping and Visualizing Cuneiform Tablets  

Microsoft Academic Search

Thousands of historically revealing cuneiform clay tablets, which were inscribed in Mesopotamia millenia ago, still exist today. Visualizing cuneiform writing is important when deciphering what is written on the tab- lets. It is also important when reproducing the tablets in papers and books. Unfortunately, scholars have found photographs to be an inadequate visualization tool, for two reasons. First, the text

Sean Eron Anderson; Marc Levoy

2002-01-01

252

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

253

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

254

Functional assessment of four types of disintegrants and their effect on the spironolactone release properties.  

PubMed

Spironolactone is a drug derived from sterols that exhibits an incomplete oral absorption due to its low water solubility and slow dissolution rate. In this study, formulations of spironolactone with four disintegrants named as croscarmellose sodium, crospovidone, sodium starch glycolate and microcrystalline cellulose II (MCCII) were conducted. The effect of those disintegrants on the tensile strength, disintegration time and dissolution rate of spironolactone-based compacts was evaluated using a factorial design with three categorical factors (filler, lubricant, and disintegrant). The swelling values, water uptake and water sorption studies of these disintegrants all suggested that MCCII compacts disintegrate by a wicking mechanism similar to that of crospovidone, whereas a swelling mechanism was dominant for sodium starch glycolate and croscarmellose sodium. The disintegration time of MCCII and sodium starch glycolate remained unchanged with magnesium stearate. However, this lubricant delayed the disintegration time of crospovidone and croscarmellose sodium. MCCII presented the fastest disintegration time independent of the medium and lubricant employed. The water sorption ratio and swelling values determined sodium starch glycolate followed by croscarmellose sodium as the largest swelling materials, whereas crospovidone and MCCII where the least swelling disintegrants. The swelling property of sodium starch glycolate and croscarmellose sodium was strongly affected by the medium pH. The disintegration time of spironolactone compacts was faster when starch was used as a filler due to the formation of soft compacts. In this case, the type of filler employed rather than the disintegrant had a major effect on the disintegration and dissolution times of spironolactone. PMID:22899380

Rojas, John; Guisao, Santiago; Ruge, Vanesa

2012-08-17

255

Dabrowski's Theory of Positive Disintegration and Giftedness: Overexcitability Research Findings  

Microsoft Academic Search

During the past 20 years, a significant body of literature has emerged focusing on the application ofDabrowski's theory ofpositive disintegration (TPD) to the study ofgifted individuals. Although much of this literature is prescriptive, some research reports spanning this time period are available. A perusal of research on TPD's appli- cability to gifted individuals indicates that the focus has been Dabrowski's

Sal Mendaglio

256

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

257

Dabrowski's Theory of Positive Disintegration and Giftedness: Overexcitability Research Findings  

ERIC Educational Resources Information Center

|During the past 20 years, a significant body of literature has emerged focusing on the application of Dabrowski's theory of positive disintegration (TPD) to the study of gifted individuals. Although much of this literature is prescriptive, some research reports spanning this time period are available. A perusal of research on TPD's applicability…

Mendaglio, Sal; Tillier, William

2006-01-01

258

Preparation, characterization and tableting of cilnidipine solid dispersions.  

PubMed

Solid dispersion technique has been developed many years for improving solubility of water-insoluble drugs, aiming to achieve a better oral bioavailability. However, this technique exhibits many inconveniences when used for large-scale tableting procedures. The objective of current research work was to develop cilnidipine solid dispersions (SDs) to improve the dissolution behaviors of this water-insoluble drug. Moreover, an innovative granulation method was designed to simplify the traditional tableting technology used in solid dispersion technique. Three different kinds of polymers, polyethylene glycol (PEG), polyvinylpyrrolidone (PVP) and poloxamer, were used as carriers to prepare solid dispersions. The interactions in the solid state were characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and FT-IR spectroscopy. The designed granulation method was employed to prepare solid dispersion tablets and the formulation was optimized through investigating the dissolution behaviors. The results indicated PEG solid dispersion showed the best effect both on physical characterizations and dissolution studies. Furthermore, all type of solid dispersions significantly improved the dissolution rates when compared to pure drug and its corresponding physical mixture (PM). The solid dispersion tablets prepared in simplified tableting method exhibited better operability, stability and dissolution behavior than the tablets prepared in traditional ways, which brought more opportunities to solid dispersion technique for industrial production. PMID:23625441

Hu, Liandong; Song, Weihua; Niu, Feng; Jiao, Kuiliang; Jia, Zheng

2013-05-01

259

Soyabean Powder as a Novel Diluent in Tablet Formulation of Simvastatin  

PubMed Central

The present research paper introduces soyabean nuggets powder, as a novel excipient with nutraceutical value for tablets containing cholesterol lowering drug, simvastatin. Experiments were carried out to evaluate the suitability of soyabean nuggets powder as a diluent by incorporating in tablet formulation of simvastatin. The formulation was compared with the marketed product to determine its relative efficacy. Soyabean nuggets powder was found to be a promising diluent for tablets for both pharmaceutical and nutraceutical purposes. Simavastatin soya tablet showed acceptable pharmacotechnical properties and assay requirement.

Swami, G.; Gupta, Khushboo; Kymonil, K. M.; Saraf, Shubhini

2010-01-01

260

Comparison between disintegrated and fermented sewage sludge for production of a carbon source suitable for biological nutrient removal.  

PubMed

There is a need to investigate processes that enable sludge re-use while enhancing sewage treatment efficiency. Mechanically disintegrated thickened surplus activated sludge (SAS) and fermented primary sludge were compared for their capacity to produce a carbon source suitable for BNR by completing nutrient removal predictive tests. Mechanically disintegration of SAS using a deflaker enhanced volatile fatty acids (VFAs) content from 92 to 374 mg l(-1) (4.1-fold increase). In comparison, primary sludge fermentation increased the VFAs content from 3.5 g l(-1) to a final concentration of 8.7 g l(-1) (2.5-fold increase). The carbon source obtained from disintegration and fermentation treatments improved phosphate (PO(4)-P) release and denitrification by up to 0.04 mg NO(3)-Ng(-1)VSS min(-1) and 0.031 mg PO(4)-Pg(-1)VSS min(-1), respectively, in comparison to acetate (0.023 mg NO(3)-Ng(-1)VSS min(-1)and 0.010 mg PO(4)-Pg(-1)VSS min(-1)). Overall, both types of sludge were suitable for BNR but disintegrated SAS displayed lower carbon to nutrient ratios of 8 for SCOD:PO(4)-P and 9 for SCOD:NO(3)-N. On the other hand, SAS increased the concentration of PO(4)-P in the settled sewage by a further 0.97 g PO(4)-P kg(-1)SCOD indicating its potential negative impact towards nutrient recycling in the BNR process. PMID:19932559

Soares, Ana; Kampas, Pantelis; Maillard, Sarah; Wood, Elizabeth; Brigg, Jon; Tillotson, Martin; Parsons, Simon A; Cartmell, Elise

2009-10-27

261

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'

262

The influence of swelling capacity of superdisintegrants in different pH media on the dissolution of hydrochlorothiazide from directly compressed tablets  

Microsoft Academic Search

The purpose of this study was to investigate the efficiency of superdisintegrants in promoting tablet disintegration and drug\\u000a dissolution under varied media pH. Significant reductions in the rate and extent of water uptake and swelling were observed\\u000a for both sodium starch glycolate (Primojel) and croscarmellose sodium (Ac-Di-Sol) in an acidic medium (0.1 N HCl) but not\\u000a for crospovidone NF (Polyplasdone

Na Zhao; Larry L. Augsburger

2005-01-01

263

Fentanyl buccal tablet.  

PubMed

Studies of populations with chronic cancer pain have shown a high prevalence of breakthrough pain (BTP), defined as transitory, severe flares of pain that occur on a background of otherwise controlled, persistent pain. High BTP prevalence rates have also been reported in patients with chronic noncancer pain, although data in these patient populations are more limited. The incidence of BTP appears to be associated with progression of chronic disease, with more than 80% of patients reporting BTP with far-advanced, end-stage cancer and noncancer terminal conditions (1). The most widely accepted therapeutic approach for the management of BTP involves use of short-acting opioids taken as needed in addition to the around-the-clock opioid regimen being used for the continuous component of the persistent pain syndrome. For some patients, an optimal treatment outcome for BTP may be unattainable because of a mismatch between the time course of the BTP episode and the onset of analgesia of short-acting opioids. Breakthrough pain typically reaches peak intensity within a few minutes, whereas the onset of analgesia with traditional, orally administered short-acting opioids is between 30 and 60 minutes (2-7). Consequently, treatment outcomes for BTP are likely to be improved with agents that have a more rapid onset of analgesia. Fentanyl buccal tablet (FBT) is a new formulation of fentanyl indicated for the management of BTP in patients with cancer who are already receiving, and who are tolerant to, opioid therapy for their underlying persistent cancer pain. The FBT formulation uses OraVescent (Cephalon, Inc., Frazer, PA, USA) drug delivery technology to provide rapid absorption of fentanyl through the buccal mucosa. In pharmacokinetic studies in healthy volunteers, FBT demonstrated high, early systemic absorption. In addition, FBT delivered a larger proportion of the fentanyl dose transmucosally and produced a greater early systemic exposure than oral transmucosal fentanyl citrate (OTFC), which is also indicated for the management of BTP in opioid-tolerant cancer patients. A number of short-term studies have evaluated the efficacy, safety and tolerability of FBT in the management of BTP in opioid-tolerant patients with chronic pain. All these studies included an open-label dose-titration phase prior to randomized, placebo-controlled, double-blind treatment. Pain Intensity of a BTP episode was measured using an 11-point scale (0 = no pain, 10 = worst pain), and the primary outcome measure was the Summed Pain Intensity Difference (SPID) at a specified time point. Secondary efficacy measures included Pain Relief, Pain Intensity Differences, and the proportion of BTP episodes demonstrating >or=33% and >or=50% improvement in Pain Intensity scores at each time point postdose, and the proportion of BTP episodes requiring supplemental medication. In a pivotal study of opioid-tolerant patients with cancer-related chronic pain and BTP, the primary outcome measure, SPID at 30 minutes (SPID(30)), significantly favored FBT compared with placebo (mean +/- SE: 3.0 +/- 0.12 vs. 1.8 +/- 0.18, p<0.0001). Better efficacy was also observed with FBT compared with placebo for pain relief, Pain Intensity Differences, and the proportion of episodes showing >or=33% and >or=50% improvement in Pain Intensity Scores. Treatment with FBT was generally well tolerated. Most adverse events were mild to moderate in severity and typical of those associated with opioid use (e.g., nausea, dizziness) (8). Similar results have been observed in studies of opioid-tolerant patients with BTP in association with noncancer-related chronic pain. In a study of patients with chronic low back pain, the primary outcome measure, SPID(60), significantly favored FBT over placebo (mean +/- SE: 8.3 +/- 0.66 vs. 3.6 +/- 0.57, p <0.0001). All secondary efficacy measures were similarly improved, with Pain Intensity Differences and Pain Relief scores showing significant differences versus placebo as early as 10 and 15 minutes, respectively. As in the study of cancer patient

Messina, John; Darwish, Mona; Fine, Perry G

2008-01-01

264

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

2007-12-14

265

Floating tablet of trimetazidine dihydrochloride: an approach for extended release with zero-order kinetics.  

PubMed

Trimetazidine dihydrochloride is an effective anti-anginal agent; however, it is freely soluble in water and suffers from a relatively short half-life. To solve this encumbrance, it is a prospective candidate for fabricating trimetazidine extended-release formulations. Trimetazidine extended-release floating tablets were prepared using different hydrophilic matrix forming polymers including HPMC 4000 cps, carbopol 971P, polycarbophil, and guar gum. The tablets were fabricated by dry coating technique. In vitro evaluation of the prepared tablets was performed by the determination of the hardness, friability, content uniformity, and weight variation. The floating lag time and floating duration were also evaluated. Release profile of the prepared tablets was performed and analyzed. Furthermore, a stability study of the floating tablets was carried out at three different temperatures over 12 weeks. Finally, in vivo bioavailability study was done on human volunteers. All tablet formulas achieved < 0.5 min of floating lag time, more than 12 h of floating duration, and extended t (1/2). The drug release in all formulas followed zero-order kinetics. T4 and T8 tablets contained the least polymer concentration and complied with the dissolution requirements for controlled-release dosage forms. These two formulas were selected for further stability studies. T8 exhibited longer expiration date and was chosen for in vivo studies. T8 floating tablets showed an improvement in the drug bioavailability compared to immediate-release tablets (Vastrel® 20 mg). PMID:20582493

Abdelbary, Ahmed; El-Gazayerly, Omaima N; El-Gendy, Nashwa A; Ali, Adel A

2010-06-26

266

Pre-Service Teacher Training in Mathematics Using Tablet PC Technology  

Microsoft Academic Search

This study focuses on the use of innovative Tablet PC technology in learning and teaching mathematics. Specifically the effects of incorporating Tablet PC technology in pre-service teachers' mathematics education were analyzed. The significant impact of technology use in mathematics ed- ucation was assessed by evaluating and comparing students' final project and course grades. Grade performance of two groups of students

Olga Kosheleva; Ana Medina-Rusch; Vera Ioudina

2007-01-01

267

Evaluation of a novel cellulose powder as a filler-binder for direct compression of tablets  

Microsoft Academic Search

A novel form of cellulose powder was evaluated as a filler-binder in tablets. The particle, powder, flow and binding properties of this experimental cellulose material were compared with those of two commercial microcrystalline celluloses, Avicel® PH 101 and Emcocel®. The effect of various storage conditions on the physical stability of tablets compressed from celluloses was also evaluated. The particle size

Timo Pesonen; Petteri Paronen; Terttu Puurunen

1989-01-01

268

Self-disintegrating ferrochrome aluminothermal slag – semifunctional technogenic raw material  

Microsoft Academic Search

On the basis of studying the chemical and mineral compositions, microstructure and properties of self-disintegrating ferrochrome\\u000a aluminothermal slag a fundamentally new highly effective waste-free technology has been developed for preparing fuzed alloyed\\u000a spinel Mg(Al, Cr)2O4. The test slag exhibits binding properties. After spinel extraction its limestone-silicate-aluminate\\u000a component may be used for producing more than ten forms of product: cement, pigments,

V. A. Perepelitsyn; V. M. Rytvin; S. I. Gil’varg; V. G. Ignatenko; V. G. Kutalov; N. N. Arzamastsev

2009-01-01

269

Evidence for the disintegration of KIC 12557548 b  

NASA Astrophysics Data System (ADS)

Context. The Kepler object KIC 12557548 b is peculiar. It exhibits transit-like features every 15.7 h that vary in depth between 0.2% and 1.2%. Rappaport et al. (2012, ApJ, 752, 1) explain the observations in terms of a disintegrating, rocky planet that has a trailing cloud of dust created and constantly replenished by thermal surface erosion. The variability of the transit depth is then a consequence of changes in the cloud optical depth. Aims: We aim to validate the disintegrating-planet scenario by modeling the detailed shape of the observed light curve, and thereby constrain the cloud particle properties to better understand the nature of this intriguing object. Methods: We analyzed the six publicly-available quarters of raw Kepler data, phase-folded the light curve and fitted it to a model for the trailing dust cloud. Constraints on the particle properties were investigated with a light-scattering code. Results: The light curve exhibits clear signatures of light scattering and absorption by dust, including a brightening in flux just before ingress correlated with the transit depth and explained by forward scattering, and an asymmetry in the transit light curve shape, which is easily reproduced by an exponentially decaying distribution of optically thin dust, with a typical grain size of 0.1 ?m. Conclusions: Our quantitative analysis supports the hypothesis that the transit signal of KIC 12557548 b is due to a variable cloud of dust, most likely originating from a disintegrating object.

Brogi, M.; Keller, C. U.; de Juan Ovelar, M.; Kenworthy, M. A.; de Kok, R. J.; Min, M.; Snellen, I. A. G.

2012-09-01

270

In vitro and in vivo evaluation of medicinal carbon granules and tablet on the adsorption of acetaminophen.  

PubMed

Medicinal carbon (MC) granules were prepared by wet granulation using maltitol (MT), and the MC tablet was produced by compression of the granules. The physical properties and the in vitro adsorption capacity for AA of the formulations were examined. Further, the effects of MC alone and the granules on gastrointestinal absorption of AA were examined in rats when they were administered intragastrically at 15 or 45 min after the intragastrical administration of AA. AA was rapidly adsorbed by MC, and the maximum adsorption capacity of MC was 0.329g AA per gram MC. The granules and tablet exhibited adequate strength, and the tablet disintegrated rapidly. The granules and tablet showed similar adsorption profiles, but somewhat lower adsorption capacity than MC alone. MC alone and granules administered at 15 min reduced the AUC(0-infinity) significantly against the control (no treatment); however, the suppression effect on the plasma concentration was lower with the granules than with MC alone. Thus, granules and tablet are useful as a compact dosage form of MC; though the reduced adsorption capacity must be taken into account in order to expect efficacy equivalent to that of MC alone. PMID:16942843

Yamamoto, Kenta; Onishi, Hiraku; Ito, Akihiko; Machida, Yoshiharu

2006-08-01

271

Spray-dried O-carboxymethyl chitosan as potential hydrophilic matrix tablet for sustained release of drug.  

PubMed

Abstract Objective: The aim of the present investigation was to evaluate the use of spray-dried O-carboxymethyl chitosan (OCMCS) as potential hydrophilic matrix excipient for sustained release of drug. Methods: The polymer was synthesized from chitosan, then spray-dried and characterized. Tablets with different OCMCS concentrations (80, 50, 30, 5 and 2% w/w), containing diltiazem (DTZ) as model drug, were prepared for direct compression (DC) and after the wet granulation method (WG). Results: The spray-dried OCMCS powder was spherical, with a smooth surface and an average size of 2.2?µm. The tablets prepared for WG disintegrated in time less than 30?min. The tablets obtained for DC presented high retention of the drug, with zero order or Higuchi release kinetic. There was a direct relationship between the OCMCS concentration and the release ratio, swelling degree and water uptake behavior. DC tablets containing 80% OCMCS presented behavior as an effective swelling-control system. The DC tablets with 5% OCMCS showed a similar release profile at formulations with 30% HPMC. Conclusion: Spray-dried OCMCS showed great potential as hydrophilic matrices for drug-sustained release. PMID:23594298

Bresolin, José R; Largura, Maria-Claudia T; Dalri, Camila C; Hoffer, Geórgia; Rodrigues, Clóvis A; Lucinda-Silva, Ruth M

2013-04-17

272

Formulation development and optimization of Ibuprofen tablets by direct compression method.  

PubMed

Ibuprofen is widely used as a prescription and non-prescription medicine. The aim of study is to prepare Ibuprofen tablets (200mg) using direct compression technique which is now days considered a cost effective and simple method of manufacturing. It is considered as an appropriate method for hygroscopic and thermolabile substances. In order to obtain the best, optimized product, nine different formulations were developed. Diluent (X1), disintegrant (X2) and lubricant (X3) were taken as independent variables. Weight variation (Y1), thickness (Y2), length and width (Y3), hardness (Y4), friability (Y5), disintegration (Y6), dissolution (Y7) and pharmaceutical assay (Y8) were studied as response variables. The results of all nine formulations were found within the acceptable limits conforming to those given in official compendia. However, F-6 was selected as an optimized product on the basis of high dissolution (99.05%) and Assay (100.04%). The variation of weight among the tablets of F-6 was least which showed best ratio of excipients in the formulation. Optimization has proven as an effective tool in product development. This is because no clear relationship exists between the variables. PMID:18390440

Bushra, Rabia; Shoaib, Muhammad Harris; Aslam, Nousheen; Hashmat, Durriya; Ur-Rehman, Masud

2008-04-01

273

Continuous direct tablet compression: effects of impeller rotation rate, total feed rate and drug content on the tablet properties and drug release.  

PubMed

Context: Continuous processing is becoming popular in the pharmaceutical industry for its cost and quality advantages. Objective: This study evaluated the mechanical properties, uniformity of dosage units and drug release from the tablets prepared by continuous direct compression process. Materials and methods: The tablet formulations consisted of acetaminophen (3-30% (w/w)) pre-blended with 0.25% (w/w) colloidal silicon dioxide, microcrystalline cellulose (69-96% (w/w)) and magnesium stearate (1% (w/w)). The continuous tableting line consisted of three loss-in-weight feeders and a convective continuous mixer and a rotary tablet press. The process continued for 8?min and steady state was reached within 5?min. The effects of acetaminophen content, impeller rotation rate (39-254?rpm) and total feed rate (15 and 20?kg/h) on tablet properties were examined. Results and discussion: All the tablets complied with the friability requirements of European Pharmacopoeia and rapidly released acetaminophen. However, the relative standard deviation of acetaminophen content (10% (w/w)) increased with an increase in impeller rotation rate at a constant total feed rate (20?kg/h). A compression force of 12?kN tended to result in greater tablet hardness and subsequently a slower initial acetaminophen release from tablets when compared with those made with the compression force of about 8?kN. Conclusions: In conclusion, tablets could be successfully prepared by a continuous direct compression process and process conditions affected to some extent tablet properties. PMID:23163644

Järvinen, Maiju A; Paaso, Janne; Paavola, Marko; Leiviskä, Kauko; Juuti, Mikko; Muzzio, Fernando; Järvinen, Kristiina

2012-11-19

274

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.

Jacob, S.; Shirwaikar, A.

2009-01-01

275

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

276

21 CFR 520.312 - Carnidazole tablets.  

Code of Federal Regulations, 2010 CFR

...Conditions of use â(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

277

Controlled release matrix tablets of olanzapine: influence of polymers on the in vitro release and bioavailability.  

PubMed

Controlled-release (CR) tablet formulation of olanzapine was developed using a binary mixture of Methocel® K100 LV-CR and Ethocel® standard 7FP premium by the dry granulation slugging method. Drug release kinetics of CR tablet formulations F1, F2, and F3, each one suitably compressed for 9-, 12-, and 15-kg hardness, were determined in a dissolution media of 0.1 N HCl (pH 1.5) and phosphate buffer (pH 6.8) using type II dissolution apparatus with paddles run at 50 rpm. Ethocel® was found to be distinctly controlling drug release, whereas the hardness of tablets and pH of the dissolution media did not significantly affect release kinetics. The CR test tablets containing 30% Methocel® and 60% Ethocel® (F3) with 12-kg hardness exhibited pH-independent zero-order release kinetics for 24 h. In vivo performance of the CR test tablet and conventional reference tablet were determined in rabbit serum using high-performance liquid chromatography coupled with electrochemical detector. Bioavailability parameters including C(max), T(max), and AUC(0-48 h) of both tablets were compared. The CR test tablets produced optimized C(max) and extended T(max) (P < 0.05). A good correlation of drug absorption in vivo and drug release in vitro (R(2) = 0.9082) was observed. Relative bioavailability of the test tablet was calculated as 94%. The manufacturing process employed was reproducible and the CR test tablets were stable for 6 months at 40 ± 2°C/75 ± 5% relative humidity. It was concluded that the CR test tablet formulation successfully developed may improve tolerability and patient adherence by reducing adverse effects. PMID:20824513

Badshah, Amir; Subhan, Fazal; Rauf, Khalid

2010-09-08

278

Galileo's Telescopy and Jupiter's Tablet  

NASA Astrophysics Data System (ADS)

A previous paper (BAAS 33:4, 1363, 2001) reported on the dramatic scene in Shakespeare's Cymbeline that features the descent of the deity Jupiter. The paper suggested that the four ghosts circling the sleeping Posthumus denote the four Galilean moons of Jupiter. The god Jupiter commands the ghosts to lay a tablet upon the prone Posthumus, but says that its value should not be overestimated. When Posthumus wakens he notices the tablet, which he calls a "book." Not only has the deity's "tablet" become the earthling's "book," but it appears that the book has covers which Posthumus evidently recognizes because without even opening the book he ascribes two further properties to it: rarity, and the very property that Jupiter had earlier attributed, viz. that one must not read too much into it. The mystery deepens when the Jovian gift undergoes a second metamorphosis, to "label." With the help of the OED, the potentially disparate terms "tablet," "book," and "label," may be explained by terms appropriate either to supernatural or worldly beings. "Tablet" may recognize the Mosaic artifact, whereas "book" and "label" are probably mundane references to Galileo's Sidereus Nuncius which appeared shortly before Cymbeline. The message of the Olympian god indicates therefore that the book is unique even as its contents have limited value. The first property celebrates the fact that Galileo's book is the first of its kind, and the second advises that all results except the discovery of Jupiter's moons have been reported earlier, in Hamlet.

Usher, P. D.

2003-12-01

279

Updating a near-infrared multivariate calibration model formed with lab-prepared pharmaceutical tablet types to new tablet types in full production.  

PubMed

Determining active pharmaceutical ingredient (API) tablet concentrations rapidly and efficiently is of great importance to the pharmaceutical industry in order to assure quality control. Using near-infrared (NIR) spectra measured on tablets in conjunction with multivariate calibration has been shown to meet these objectives. However, the calibration is typically developed under one set of conditions (primary conditions) and new tablets are produced under different measurement conditions (secondary conditions). Hence, the accuracy of multivariate calibration is limited due to differences between primary and secondary conditions such as tablet variances (composition, dosage, and production processes and precision), different instruments, and/or new environmental conditions. This study evaluates application of Tikhonov regularization (TR) to update NIR calibration models developed in a controlled primary laboratory setting to predict API tablet concentrations manufactured in full production where conditions and tablets are significantly different than in the laboratory. With just a few new tablets from full production, it is found that TR provides reduced prediction errors by as much as 64% in one situation compared to no model-updating. TR prediction errors are reduced by as much as 51% compared to local centering, another calibration maintenance method. The TR updated primary models are also found to predict as well as a full calibration model formed in the secondary conditions. PMID:22154647

Farrell, Jeremy A; Higgins, Kevin; Kalivas, John H

2011-11-17

280

Multispectral imaging of tablets in blister packaging  

Microsoft Academic Search

This experiment tested the hypothesis that using near-infrared (IR) imaging spectrometry on tablets through blister packs\\u000a permits the identification and composition of multiple individual tablets to be determined simultaneously. Aspirin was selected\\u000a for this study because its breakdown mechanism is well understood. Near-IR cameras were used to collect thousands of spectra\\u000a simultaneously from a field of packaged aspirin tablets. Tablets

Imran Malik; Mela Poonacha; Jennifer Moses; Robert A. Lodder

2001-01-01

281

[Preparation of sucking tablet of shengmei] off.  

PubMed

The Sucking Tablet of Shengmei is made from eight Chinese traditional drugs including Radix Adenophorae, Fructus Mume, etc. The effective rate of the tablet in treating chronic pharyngitis reaches up to 96 percent. The working mechanism related to the fact that the tablet is bacteria-resistant and helps to strengthen the body function. This paper presents the preparation process of the Sucking Tablet along with solutions for some problems encountered in the process and appropriate standards for quality control. PMID:1418578

Jiang, J; Shao, J; Zhu, Z; Dai, Y; Xu, C

1992-06-01

282

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

PubMed Central

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.

Patel, DM; Patel, BK; Patel, HA; Patel, CN

2011-01-01

283

Tablet - next generation sequence assembly visualization  

Microsoft Academic Search

Summary: Tablet is a lightweight, high-performance graphical viewer for next generation sequence assemblies and alignments. Supporting a range of input assembly formats, Tablet provides high- quality visualizations showing data in packed or stacked views, al- lowing instant access and navigation to any region of interest, and whole contig overviews and data summaries. Tablet is both multi- core aware and memory-efficient,

Iain Milne; Micha Bayer; Linda Cardle; Paul Shaw; Gordon Stephen; Frank Wright; David Marshall

2010-01-01

284

Mathematics instruction and the tablet PC  

Microsoft Academic Search

The use of tablet PCs in teaching is a relatively new phenomenon. A cross between a notebook computer and a personal digital assistant (PDA), the tablet PC has all of the features of a notebook with the additional capability that the screen can also be used for input. Tablet PCs are usually equipped with a stylus that allows the user

K. Renee Fister; Maeve L. McCarthy

2008-01-01

285

Using Tablet PCs in Engineering Education  

Microsoft Academic Search

This paper describes the experiences of using Tablet PCs along with associated software, such as Classroom Presenter and OneNote, in a course entitled Introduction to Computer Engineering. Twenty tablet PCs were distributed in a classroom of 40 students. Students used the tablets on a daily basis throughout the semester to take notes, to respond to in-class exercises, and to perform

Joseph G. Tront

286

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

287

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

2007-08-15

288

Treatment of respiratory allergy with allergy immunotherapy tablets.  

PubMed

Allergy immunotherapy tablets (AIT) have expanded the treatment options for patients suffering from respiratory allergies. Efficacy is established in adults and children for two different commercially available grass AITs. The ALK grass AIT has an efficacy comparable to subcutaneous immunotherapy (SCIT), with a proven disease-modifying effect after treatment completion. Safety profiles favour AIT over SCIT. Studies suggest that tablets in all aspects are superior to sublingual drops. AITs for other allergies including house dust mite and birch and ragweed pollen are in development. PMID:21668858

Bachert, C

2011-07-01

289

A randomised trial of glucose tablets to aid smoking cessation  

Microsoft Academic Search

Rationale  Oral glucose has been found to decrease tobacco craving among abstaining smokers. One study has demonstrated an effect of\\u000a glucose on short-term abstinence. There is a need to examine any long-term benefit of glucose on abstinence.\\u000a \\u000a \\u000a \\u000a Objectives  To assess whether glucose tablets improve 6-month continuous abstinence rates compared with low-calorie placebo tablets.\\u000a \\u000a \\u000a \\u000a Methods  Smokers attempting to stop (n?=?928) were randomised to receive

Robert West; Sylvia May; Andy McEwen; Hayden McRobbie; Peter Hajek; Eleni Vangeli

2010-01-01

290

Tablet potency of Tianeptine in coated tablets by near infrared spectroscopy: model optimisation, calibration transfer and confidence intervals.  

PubMed

A near infrared (NIR) method was developed for determination of tablet potency of active pharmaceutical ingredient (API) in a complex coated tablet matrix. The calibration set contained samples from laboratory and production scale batches. The reference values were obtained by high performance liquid chromatography (HPLC) and partial least squares (PLS) regression was used to establish a model. The model was challenged by calculating tablet potency of two external test sets. Root mean square errors of prediction were respectively equal to 2.0% and 2.7%. To use this model with a second spectrometer from the production field, a calibration transfer method called piecewise direct standardisation (PDS) was used. After the transfer, the root mean square error of prediction of the first test set was 2.4% compared to 4.0% without transferring the spectra. A statistical technique using bootstrap of PLS residuals was used to estimate confidence intervals of tablet potency calculations. This method requires an optimised PLS model, selection of the bootstrap number and determination of the risk. In the case of a chemical analysis, the tablet potency value will be included within the confidence interval calculated by the bootstrap method. An easy to use graphical interface was developed to easily determine if the predictions, surrounded by minimum and maximum values, are within the specifications defined by the regulatory organisation. PMID:20965682

Boiret, Mathieu; Meunier, Loïc; Ginot, Yves-Michel

2010-10-01

291

Chitosan and Enteric Polymer Based Once Daily Sustained Release Tablets of Aceclofenac: In Vitro and In Vivo Studies  

PubMed Central

The purpose of this study was to develop a once daily sustained release tablet of aceclofenac using chitosan and an enteric coating polymer (hydroxypropyl methylcellulose phthalate or cellulose acetate phthalate). Overall sustained release for 24 h was achieved by preparing a double-layer tablet in which the immediate release layer was formulated for a prompt release of the drug and the sustained release layer was designed to achieve a prolonged release of drug. The preformulation studies like IR spectroscopic and differential scanning calorimetry showed the absence of drug–excipient interactions. The tablets were found within the permissible limits for various physicochemical parameters. Scanning electron microscopy was used to visualize the surface morphology of the tablets and to confirm drug release mechanisms. Good equivalence in the drug release profile was observed when drug release pattern of the tablet containing chitosan and hydroxypropyl methylcellulose phthalate (M-7) was compared with that of marketed tablet. The optimized tablets were stable at accelerated storage conditions for 6 months with respect to drug content and physical appearance. The results of pharmacokinetic studies in human volunteers showed that the optimized tablet (M-7) exhibited no difference in the in vivo drug release in comparison with marketed tablet. No significant difference between the values of pharmacokinetic parameters of M-7 and marketed tablets was observed (p?>?0.05; 95% confidence intervals). However the clinical studies in large scale and, long term and extensive stability studies at different conditions are required to confirm these results.

Manoj, Krishnan; Reddy, Meka Sreenivasa; Kushtagi, Pralhad; Usha, Achutha Nayak; Anju, Parambil; Ranjith, Averineni Kumar; Udupa, Nayanabhirama

2008-01-01

292

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

293

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

2011-12-21

294

Gastro-floating tablets of cephalexin: preparation and in vitro/in vivo evaluation.  

PubMed

Gastro-floating tablets of cephalexin were developed to prolong the residence time in major absorption sites. Gastro-floating tablets were prepared and optimized using hydroxypropyl methylcellulose (HPMC K100M) as matrix and sodium bicarbonate as a gas-forming agent. The properties of the tablets in terms of floating lag time, floating time and in vitro release were evaluated. Furthermore, in vivo pharmacokinetic study in fed and fasted beagle dogs was performed. The gastro-floating tablets had short floating lag time and exhibited a satisfactory sustained-release profile in vitro. Compared with conventional capsules, the gastro-floating tablets presented a sustained-release behavior with a relative bioavailability of 99.4%, while the reference sustained-release tablets gave a relative bioavailability of only 39.3%. Meanwhile, the food had significant effect on the pharmacokinetics of sustained-release tablets. It was concluded that the gastro-floating tablets had a sustained-release effect in vitro and in vivo, as well as desired pharmacokinetic properties in both fed and fasted conditions. PMID:23680730

Yin, Lifang; Qin, Chao; Chen, Kaisheng; Zhu, Chunli; Cao, Hui; Zhou, Jianping; He, Wei; Zhang, Qiang

2013-05-13

295

Calcium phosphates in pharmaceutical tableting. 2. Comparison of tableting properties.  

PubMed

Ten calcium phosphates suitable for direct compression (dibasic calcium phosphate dihydrate, dibasic calcium phosphate anhydrous and hydroxylapatite) were investigated with respect to their compressional behaviour. Except for Di-Cafos A all products gave tablets with sufficient to good mechanical strength. Nevertheless, there were differences between the products. All tablets prepared from the different products showed a high friability. This seems to be a problem of the calcium phosphates in general. On the other hand, the influence of magnesium stearate on the mechanical strength of the tablets was negligible for all products investigated. Moreover, a considerable effect of the particle size on the tensile strength of the tablets was found. The ejection forces and residual pressures were high in general, but critical only in the case of hydroxylapatites. Heckel plots were used to differentiate between plastic deformation and brittle fracture of the particles. In the case of calcium phosphates the slope of the Heckel plots indicated the hardness of the particles rather than their deformation behaviour. PMID:8348107

Schmidt, P C; Herzog, R

1993-06-18

296

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

297

Mass distribution in the disintegration of heavy nuclei  

NASA Astrophysics Data System (ADS)

The disintegration of heavy nuclei at various excitation energies has been investigated on the basis of statistical models. For the fission channels at low energies, we obtain approximate interpolating formulas for masses of fission fragments from the analysis of experimental data. In particular, they describe the transition from symmetric to asymmetric fission. The sequential evaporation from the excited compound nucleus and fission fragments is also taken into account. We show the evolution of mass distributions from low to high excitation energies, and demonstrate a transition to multifragmentation channels at high energies.

Eren, N.; Buyukcizmeci, N.; Ogul, R.; Botvina, A. S.

2013-04-01

298

Brief report: childhood disintegrative disorder as a likely manifestation of vitamin B12 deficiency.  

PubMed

Childhood disintegrative disorder is a rare disorder, characterized by regression of acquired skills after a period of normal development. The case of childhood disintegrative disorder presented here was found to have vitamin B12 deficiency and hyperhomocysteinemia on extensive evaluation to find a probable cause for regression. This case illustrates the need for a thorough evaluation of all cases of childhood disintegrative disorder so that treatable causes of regression, like vitamin B12 deficiency, are not missed. PMID:23334842

Malhotra, Savita; Subodh, B N; Parakh, Preeti; Lahariya, Sanjay

2013-09-01

299

Pharmaceutical quality of seven generic Levodopa/Benserazide products compared with original Madopar(R) / Prolopa(R).  

PubMed

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(R) / Prolopa(R) 125, Roche, Switzerland) in order to evaluate the potential impact of Madopar(R) generics versus branded products for PD patients and clinicians. METHODS: Madopar(R) / Prolopa(R) 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(R)/Prolopa(R), and also invite to further investigations in view of a more comprehensive approach, both pharmaceutical and clinical. PMID:23617953

Gasser, Urs E; Fischer, Anton; Timmermans, Jan P; Arnet, Isabelle

2013-04-23

300

Tablet PCs in undergraduate mathematics  

Microsoft Academic Search

Undergraduate students often struggle to learn mathematics because introductory classes are taught in large lectures that do not engage students in active problem-solving. These students do not connect mathematics to their lives and feel that learning mathematics is a solitary undertaking. We now use Tablet PCs in a networked classroom to address these challenges. Students in classes that use the

Carla A. Romney

2010-01-01

301

The Venus Tablet and Refraction  

Microsoft Academic Search

It is shown that the refraction near the horizon is introducing an additional bias into the Venus Tablet of Ammisaduqa, which is able to influence the interpretation of the data. We then discuss the attempts to link certain solar eclipses to the birth of Shamshi-Adad and conclude that a record of a single solar eclipse without description of details and\\/or

V. G. Gurzadyan

2003-01-01

302

In vivo disintegration of four different luting agents.  

PubMed

The purpose of this study was to evaluate the disintegration of luting agents. An intraoral sample holder was made having four holes of 1.4?mm diameter and 2?mm depth. The holder was soldered onto the buccal surface of an orthodontic band, which was cemented to the first upper molar in 12 patients, average age 26 years. The holes were filled with a zinc phosphate (Phosphate Kulzer), a glass ionomer (Ketac Cem), a resin-modified-glass ionomer (Fuji Plus), and a resin cement (Calibra). Impressions were made at baseline, and 6, 12, and 18 months from which epoxy replicas were made, which were scanned with an optical scanner. Total volume loss was calculated. The rank order of mean volume loss was as follows: Phosphate cement > Ketac Cem = Fuji Plus = Calibra. Cement type and time had statistically significant effects on volume loss of cements (P < 0.001). Under in vivo conditions, zinc phosphate cement disintegrated the most, whereas no significant difference was observed for glass ionomer and resin-based cements. As intraoral conditions are considerably less aggressive than experimental laboratory conditions, the erosion behavior of glass ionomer cement was found to be similar to the resin-based cements in contradiction to previous laboratory results. PMID:22007219

Gemalmaz, Deniz; Pameijer, Cornelis H; Latta, Mark; Kuybulu, Ferah; Alcan, Toros

2011-10-05

303

In Vivo Disintegration of Four Different Luting Agents  

PubMed Central

The purpose of this study was to evaluate the disintegration of luting agents. An intraoral sample holder was made having four holes of 1.4?mm diameter and 2?mm depth. The holder was soldered onto the buccal surface of an orthodontic band, which was cemented to the first upper molar in 12 patients, average age 26 years. The holes were filled with a zinc phosphate (Phosphate Kulzer), a glass ionomer (Ketac Cem), a resin-modified-glass ionomer (Fuji Plus), and a resin cement (Calibra). Impressions were made at baseline, and 6, 12, and 18 months from which epoxy replicas were made, which were scanned with an optical scanner. Total volume loss was calculated. The rank order of mean volume loss was as follows: Phosphate cement > Ketac Cem = Fuji Plus = Calibra. Cement type and time had statistically significant effects on volume loss of cements (P < 0.001). Under in vivo conditions, zinc phosphate cement disintegrated the most, whereas no significant difference was observed for glass ionomer and resin-based cements. As intraoral conditions are considerably less aggressive than experimental laboratory conditions, the erosion behavior of glass ionomer cement was found to be similar to the resin-based cements in contradiction to previous laboratory results.

Gemalmaz, Deniz; Pameijer, Cornelis H.; Latta, Mark; Kuybulu, Ferah; Alcan, Toros

2012-01-01

304

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

305

In vitro and in vivo evaluation of guar gum matrix tablets for oral controlled release of water-soluble diltiazem hydrochloride.  

PubMed

The objective of the study was to develop guar gum matrix tablets for oral controlled release of water-soluble diltiazem hydrochloride. Matrix tablets of diltiazem hydrochloride, using various viscosity grades of guar gum in 2 proportions, were prepared by wet granulation method and subjected to in vitro drug release studies. Diltiazem hydrochloride matrix tablets containing either 30% wt/wt low-viscosity (LM1), 40% wt/wt medium-viscosity (MM2), or 50% wt/wt high-viscosity (HM2) guar gum showed controlled release. The drug release from all guar gum matrix tablets followed first-order kinetics via Fickian-diffusion. Further, the results of in vitro drug release studies in simulated gastrointestinal and colonic fluids showed that HM2 tablets provided controlled release comparable with marketed sustained release diltiazem hydrochloride tablets (D-SR tablets). Guar gum matrix tablets HM2 showed no change in physical appearance, drug content, or in dissolution pattern after storage at 40 degrees C/relative humidity 75% for 6 months. When subjected to in vivo pharmacokinetic evaluation in healthy volunteers, the HM2 tablets provided a slow and prolonged drug release when compared with D-SR tablets. Based on the results of in vitro and in vivo studies it was concluded that that guar gum matrix tablets provided oral controlled release of water-soluble diltiazem hydrochloride. PMID:16353958

Al-Saidan, Saleh M; Krishnaiah, Yellela S R; Patro, Srinivas S; Satyanaryana, Vemulapalli

2005-07-14

306

Formulation, bioavailability, and pharmacokinetics of sustained-release potassium chloride tablets.  

PubMed

The release of potassium chloride incorporated into hydrogenated vegetable oil and hydroxypropyl methylcellulose matrix tablets was studied in vitro. The formulations containing 20% hydrogenated vegetable oil and hydroxypropyl methylcellulose showed a sustained-release profile comparable to that of a standard commercially available sustained-release preparation, containing 8 mEq potassium chloride embedded in a wax material. The formulated and standard sustained-release potassium chloride tablets were compared to a conventional enteric-coated potassium chloride tablet in 10 healthy subjects. Mean recoveries in 24-hr urine potassium levels from four dosage forms (after subtracting normal urine potassium excretion levels) were 76 +/- 32% from hydroxypropyl methylcellulose, 95 +/- 22% from hydrogenated vegetable oil-incorporated matrix tablets, 91 +/- 29% from commercially available sustained-release tablets, and 97 +/- 13% from enteric-coated tablets. There was no significant difference (P greater than 0.05) in the time to reach maximum excretion rates among the three sustained-release tablets. No significant adverse effect was experienced with any of the preparations. PMID:1796051

Senel, S; Capan, Y; Dalkara, T; Inanç, N; Hincal, A A

1991-10-01

307

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

2013-01-25

308

Modified cellulose II powder: preparation, characterization, and tableting properties.  

PubMed

The reaction of UICEL-A/102, a cellulose II powder recently prepared from Avicel(R) PH-102 by treatment with an aqueous sodium hydroxide solution, with glutaraldehyde in 0.01 N HCl has been investigated to improve its binder properties, without adversely affecting the rapid disintegration characteristic. The results showed that UICEL-A/102 and glutaraldehyde when reacted in a 1:0.6 weight ratio at 100 degrees C for 8.5 h produces a product, (hereinafter referred to as UICEL-XL), that, compared to UICEL-A/102, had a lower degree of polymerization, higher crystallinity, lower bulk density, lower tapped density, and higher porosity. Further, it showed lower yield pressure and higher crushing strength, and tensile strength values, indicating that UICEL-XL is more compressible and compactable than the starting material, UICEL-A/102. A comparison of "in-die" and "out-of-die" Heckel data indicated UICEL-XL to be less elastic than UICEL-A/102. Both UICEL-XL and UICEL-A/102 showed similar moisture sorption isotherms, and their compacts disintegrated rapidly in water. In conclusion, the glutaraldehyde-treated cellulose II powder not only serves as good a disintegrant as the untreated cellulose powder but also possesses superior binder properties. PMID:17075860

de la Luz Reus Medina, Maria; Kumar, Vijay

2007-02-01

309

Graft copolymers of ethyl methacrylate on waxy maize starch derivatives as novel excipients for matrix tablets: physicochemical and technological characterisation.  

PubMed

Nowadays, graft copolymers are being used as an interesting option when developing a direct compression excipient for controlled release matrix tablets. New graft copolymers of ethyl methacrylate (EMA) on waxy maize starch (MS) and hydroxypropylstarch (MHS) were synthesised by free radical polymerization and alternatively dried in a vacuum oven (OD) or freeze-dried (FD). This paper evaluates the performance of these new macromolecules and discusses the effect of the carbohydrate nature and drying process on their physicochemical and technological properties. Grafting of EMA on the carbohydrate backbone was confirmed by IR and NMR spectroscopy, and the grafting yields revealed that graft copolymers present mainly a hydrophobic character. The graft copolymerization also leads to more amorphous materials with larger particle size and lower apparent density and water content than carbohydrates (MS, MHS). All the products show a lack of flow, except MHSEMA derivatives. MSEMA copolymers underwent much plastic flow and less elastic recovery than MHSEMA copolymers. Concerning the effect of drying method, FD derivatives were characterised by higher plastic deformation and less elasticity than OD derivatives. Tablets obtained from graft copolymers showed higher crushing strength and disintegration time than tablets obtained from raw starches. This behaviour suggests that these copolymers could be used as excipients in matrix tablets obtained by direct compression and with a potential use in controlled release. PMID:19146956

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

2008-12-25

310

High-throughput NIR-chemometric methods for determination of drug content and pharmaceutical properties of indapamide tablets.  

PubMed

This paper describes the development, validation and application of NIR-chemometric methods for API content and pharmaceutical characterization (disintegration time and crushing strength) of indapamide intact tablets. Development of the method for chemical characterization was performed on samples corresponding to 80, 90, 100, 110 and 120% of indapamide content and for pharmaceutical characterization on samples prepared at nine different compression forces (covering the interval 7-45 kN). NIR spectra of prepared tablets were recorded in transmission mode, and partial least-squares followed by leave-one-out cross-validation were used to develop models for the prediction of the drug content and the pharmaceutical properties of tablets. All developed models were validated in terms of trueness, precision and accuracy. No statistical differences were found between results predicted by NIR-chemometric methods and the ones determined by reference methods. Therefore, the developed NIR-chemometric methods meet the requirements of a high-throughput method for the determination of drug content, pharmaceutical properties of indapamide tablets. PMID:23347649

Tomuta, Ioan; Rus, Lucia; Iovanov, Rares; Rus, Luca Liviu

2012-12-22

311

Aerobic and anaerobic bioprocessing of activated sludge: floc disintegration by enzymes.  

PubMed

Hydrolytic enzymes such as glucosidases, lipases, and proteases have an imperative function at the hydrolysis stage of complex organic structures in the degradation of biodegradable particulate organic matter. As a key factor, extracellular polymeric substances (EPS) control the extracellular hydrolytic enzymes in this degradation mechanism. A flocculated matrix of EPS bridging with bacteria holds back the dewaterability properties of the bioprocessed sludges. Disruption of the flocculated matrix leads to improved solubilization of sludge solids by attacking the hydrolytic enzymes to polymeric substances forming enzyme-substrate complexes. To determine the floc disintegration mechanisms by enzymes during aerobic and anaerobic bioprocessing of sludges, experimental data obtained from three aerobic digesters and three anaerobic digesters were evaluated. As part of a broader project examining the overall fate and effects of hydrolytic enzymes in biological sludge stabilization, this paper compares the performances of aerobic and anaerobic reactors used in this study and reports significant improvements in enzymatic treatment of activated sludge. PMID:18821239

Ayol, Azize; Filibeli, Ayse; Sir, Diclehan; Kuzyaka, Ersan

2008-11-01

312

Comparison of neurofuzzy logic and neural networks in modelling experimental data of an immediate release tablet formulation  

Microsoft Academic Search

This study compares the performance of neurofuzzy logic and neural networks using two software packages (INForm and FormRules) in generating predictive models for a published database for an immediate release tablet formulation. Both approaches were successful in developing good predictive models for tablet tensile strength and drug dissolution profiles. While neural networks demonstrated a slightly superior capability in predicting unseen

Qun Shao; Raymond C. Rowe; Peter York

2006-01-01

313

Early pregnancy termination with intravaginally administered sodium chloride solution–moistened misoprostol tablets: Historical comparison with mifepristone and oral misoprostol  

Microsoft Academic Search

Objective: The purpose of this study was to compare the abortifacient effect of intravaginally administered moistened misoprostol tablets with that of the combination regimen of mifepristone and oral misoprostol. Study Design: One hundred women at ?56 days’ gestation received 800 ?g misoprostol intravaginally in the form of sodium chloride solution–moistened tablets. The dose was repeated 24 hours later if a

John K. Jain; Karen R. Meckstroth; Daniel R. Mishell

1999-01-01

314

Centred compression-wave in polytropic gas, and its disintegration  

NASA Astrophysics Data System (ADS)

The isentropic plane motion of a loaded half-space filled with a polytropic gas is examined. The problem of the one-dimensional motion is formulated assuming that the laws of conservation of mass and momentum are obeyed. A solution is given for the case of a centered cumulation of a straight wave of finite deformation. The isentropic and shock adiabatic properties are discussed and the wave-front configuration after cumulation of the compression wave is analyzed. It is shown that for the polytropic exponent less than or equal to 5/3, disintegration of arbitrary discontinuity generated by the centered compression wave in the polytropic gas can result in the formation of a single shock wave, followed by a contact discontinuity behind which a rarefaction wave moves.

Wlodarczyk, E.

315

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, .

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

2013-01-01

316

Childhood Disintegrative Disorder: Distinction From Autistic Disorder and Predictors of Outcome.  

PubMed

Childhood disintegrative disorder, a rare, relentlessly progressive neurologic disorder, first described by Heller in 1908, remains a condition of great interest. It has long been debated whether it is a discrete disorder or simply a late-onset variant of childhood autism. We have studied 6 cases of childhood disintegrative disorder, collected over 8 years, and followed for 2.5 to 22 years (mean 8.6 years). Childhood disintegrative disorder begins later in life than autism, and following a period of entirely normal development; the regression is more global and more severe than in autism; seizures are more frequent than in autism, yet demonstrable organicity in childhood disintegrative disorder is decidedly rare. Lastly, the prognosis is usually much worse than in autism, but in those cases with neither seizures nor epileptiform activity on electroencephalography (EEG), the outcome may be more favorable. Childhood disintegrative disorder should be viewed as a condition distinct from childhood autism. PMID:23340080

Rosman, N Paul; Bergia, Berta M

2013-03-01

317

A novel approach to crystallisation of nanodispersible microparticles by spray drying for improved tabletability.  

PubMed

High-dose API powders which are to be tableted by direct compression should have high compactibility and compressibility. This note reports on a novel approach to the manufacture of crystalline powders intended for direct compaction with improved compactibility and compressibility properties. The poorly compactable API, chlorothiazide, was spray dried from a water/acetone solvent mix producing additive-free nanocrystalline microparticles (NCMPs) of median particle size 3.5 ?m. Tablets compacted from NCMPs had tensile strengths ranging from 0.5 to 4.6 MPa (compared to 0.6-0.9 MPa for tablets of micronised CTZ) at compression forces ranging from 6 kN to 13 kN. NCMP tablets also had high porosities (34-20%) and large specific surface areas (4.4-4.8m(2)/g). The time taken for tablets made of NCMPs to erode was not statistically longer (p>0.05) than for tablets made of micronised CTZ. Fragmentation of NCMPs on compression was observed. The volume fraction of particles below 1 ?m present in the suspension recovered after erosion of NCMP tablets was 34.8±3.43%, while no nanosized particles were detected in the slurry after erosion of compacted micronised CTZ. PMID:22710254

Paluch, Krzysztof J; Tajber, Lidia; Adamczyk, Bo?ena; Corrigan, Owen I; Healy, Anne Marie

2012-06-15

318

Influence of Compression Force on The Behavior of Mucoadhesive Buccal Tablets  

PubMed Central

The purpose of this research was to study the compression force influence on polymers, tablet behavior and drug release rate. Several tablet batches were produced by varying the compression force and by using hydroxyethyl cellulose (HEC) and Carbopol 940 in the 1:1 ratio as matrix forming polymers. All batches were characterized by DSC and X-ray analyses and in terms of swelling, ex vivo and in vivo mucoadhesive time, ex vivo mucoadhesion force, and in vitro and in vivo release. No significant excipient–excipient or excipient–drug interactions were observed in any of the batches. All the tablets hydrated quickly and their high hydration percentage showed that the compression forces used did not remarkably affect the water penetration and the polymeric chain stretching. Mucoadhesion performances and drug release were mainly influenced by compression force; its increase produced higher ex vivo and in vivo mucoadhesion and the in vitro and in vivo drug releases were seen to decrease with the increase of the compression force. However tablets fabricated by using the lowest compression force showed the best in vivo mucoadhesive time and hydrated faster when compared to the others. Tablets 4 and 5, prepared with the highest forces, caused pain during in vivo application and gave rise to irritation needing to be detached by the volunteers while tablet 1, prepared with the lowest force, gave the best results because it was able to produce the highest drug salivary concentration and no pain. All tablets exhibited an anomalous release mechanism.

Ambrogi, Valeria; Giovagnoli, Stefano; Blasi, Paolo; Mancini, Alessandra; Ricci, Maurizio; Rossi, Carlo

2008-01-01

319

Formulation Design and Optimization of Fast Dissolving Clonazepam Tablets  

PubMed Central

Fast dissolving tablets of clonazepam were prepared by direct compression method with a view to enhance patient compliance. A 32 full factorial design was applied to investigate the combined effect of two formulation variables: amount of crospovidone and microcrystalline cellulose. Crospovidone (2-8% w/w) was used as superdisintegrant and microcrystalline cellulose (20-40% w/w) was used as diluent, along with directly compressible mannitol to enhance mouth feel. The tablets were evaluated for hardness, friability, thickness, drug content uniformity, in vitro dispersion time, wetting time and water absorption ratio. Based on in vitro dispersion time (approximately 16 s); the formulation containing 2% w/w crospovidone and 40% w/w microcrystalline cellulose was found to be promising and tested for in vitro drug release pattern (in pH 6.8 phosphate buffer). Short-term stability (at 40°/75% relative humidity for 3 mo) and drug-excipient interaction. Surface response plots are presented to graphically represent the effect of independent variables on the invitro dispersion time. The validity of the generated mathematical model was tested by preparing two extra-design checkpoints. The optimized tablet formulation was compared with conventional commercial tablet formulation for drug release profiles. This formulation showed nearly five-fold faster drug release (t50% 3.5 min) compared to the conventional commercial tablet formulation (t50% 16.4 min). Short-term stability studies on the formulation indicated that there are no significant changes in drug content and in vitro dispersion time (P<0.05).

Shirsand, S. B.; Suresh, Sarasija; Swamy, P. V.

2009-01-01

320

The Venus Tablet and Refraction  

Microsoft Academic Search

It is shown that the refraction near the horizon is introducing an additional\\u000abias into the Venus Tablet of Ammisaduqa, which is able to influence the\\u000ainterpretation of the data. We then discuss the attempts to link certain solar\\u000aeclipses to the birth of Shamshi-Adad and conclude that a record of a single\\u000asolar eclipse without description of details and\\/or

V. G. Gurzadyan

2003-01-01

321

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

322

BEYOND THE TABLET PC USING THE TABLET PC IN A COLLABORATIVE LEARNING ENVIRONMENT  

Microsoft Academic Search

This research focuses on the use of the Tablet PC in education. The research explores the development of the Tablet PC and introduces the Classroom Presenter software. Implementation efforts of both the Tablet PC and the Classroom Presenter software at Coastal Carolina University are explored.

JEAN H. FRENCH

323

Properties of lipophilic matrix tablets containing phenylpropanolamine hydrochloride prepared by hot-melt extrusion  

Microsoft Academic Search

The objective of the present study was to investigate the influence of formulation factors on the physical properties of hot-melt extruded granules and compressed tablets containing wax as a thermal binder\\/retarding agent, and to compare the properties of granules and tablets with those prepared by a high-shear melt granulation (MG) method. Powder blends containing phenylpropanolamine hydrochloride, Precirol® and various excipients

Jiping Liu; Feng Zhang; James W McGinity

2001-01-01

324

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

325

Formulation and in-vitro evaluation of dextrin matrix tablet of Ibuprofen for colon specific drug delivery.  

PubMed

The objective of the present study is to develop colon targeted drug delivery system by using dextrin (polysaccharide) as a carrier for ibuprofen. Matrix tablets containing various excipients and dextrin were prepared by wet granulation technique using different binder systems. The matrix tablets were evaluated by different IPQC tests, content uniformity and in vitro drug release study. Drug release profile was evaluated in simulated gastric, intestinal fluid and simulated colonic fluid. Best formulation was decided on the basis drug release profile in simulated gastric and intestinal fluid. The matrix tablet containing dextrin as a carrier and ethyl cellulose as binder was found to be suitable for targeting ibuprofen for local action in the colon as compare to other matrix tablets containing different binders because of fewer amounts (8-11%) of drug release in the simulated gastric and intestinal fluid. Matrix tablets containing dextrin released 95-98% of ibuprofen in simulated colonic fluid with 4% human fecal matter solution. Tablets containing dextrin showed no change in physical appearance and dissolution profile upon storage at 40 degrees C/75% relative humidity for three months. The results of in-vitro study indicate that matrix tablets containing dextrin as carrier and ethyl cellulose as binder are most suitable to deliver the drug specifically in colonic region as compare to matrix tablets of dextrin with other binder systems. PMID:18166513

Salunkhe, Kishor Sahebrao; Kulkarni, Mohan Vinayak

2008-01-01

326

Formulation and evaluation of microsphere based oro dispersible tablets of itopride hcl  

PubMed Central

Background The purpose of the present work is to mask the intensely bitter taste of Itopride HCl and to formulate an Oro dispersible tablet (ODT) of the taste-masked drug by incorporation of microspheres in the tablets for use in specific populations viz. pediatrics, geriatrics and patients experiencing difficulty in swallowing. Methods With this objective in mind, microspheres loaded with Itopride HCl were prepared by solvent evaporation method using acetone as solvent for pH-sensitive polymer, Eudragit EPO and light liquid paraffin as the encapsulating medium. The prepared microspheres were characterized with regard to yield, drug content, flow properties, particle size and size distribution, surface features, in vitro drug release and taste. The ODTs so prepared from these microspheres were evaluated for hardness, thickness, weight variation, friability, disintegration time, drug content, wetting time, water absorption ratio, moisture uptake, in vitro dispersion, in vitro disintegration, in vitro drug release and stability. Results The average size of microspheres was found to be satisfactory in terms of the size and size distribution. Microspheres prepared were of a regular spherical shape. Comparison of the dissolution profiles of microspheres in different pH media showed that microspheres having drug: polymer ratio of 1:2 produced a retarding effect in simulated salivary fluid (pH 6.8) and were further used for formulation into ODTs after addition of suitable amounts of excipients such as superdisintegrant, diluent, sweetener and flavor of directly compressible grade. Conclusions Effective taste-masking was achieved for Itopride HCl by way of preparation of microspheres and ODTs of acceptable characteristics.

2012-01-01

327

A laboratory scale model of abrupt ice-shelf disintegration  

NASA Astrophysics Data System (ADS)

An important mode of Earth’s disappearing cryosphere is the abrupt disintegration of ice shelves along the Peninsula of Antarctica. This disintegration process may be triggered by climate change, however the work needed to produce the spectacular, explosive results witnessed with the Larsen B and Wilkins ice-shelf events of the last decade comes from the large potential energy release associated with iceberg capsize and fragmentation. To gain further insight into the underlying exchanges of energy involved in massed iceberg movements, we have constructed a laboratory-scale model designed to explore the physical and hydrodynamic interactions between icebergs in a confined channel of water. The experimental apparatus consists of a 2-meter water tank that is 30 cm wide. Within the tank, we introduce fresh water and approximately 20-100 rectangular plastic ‘icebergs’ having the appropriate density contrast with water to mimic ice. The blocks are initially deployed in a tight pack, with all blocks arranged in a manner to represent the initial state of an integrated ice shelf or ice tongue. The system is allowed to evolve through time under the driving forces associated with iceberg hydrodynamics. Digitized videography is used to quantify how the system of plastic icebergs evolves between states of quiescence to states of mobilization. Initial experiments show that, after a single ‘agitator’ iceberg begins to capsize, an ‘avalanche’ of capsizing icebergs ensues which drives horizontal expansion of the massed icebergs across the water surface, and which stimulates other icebergs to capsize. A surprise initially evident in the experiments is the fact that the kinetic energy of the expanding mass of icebergs is only a small fraction of the net potential energy released by the rearrangement of mass via capsize. Approximately 85 - 90 % of the energy released by the system goes into water motion modes, including a pervasive, easily observed seich mode of the tank. This experimental result confirms observational experience with the full-scale system in Greenlandic fjords, where fjord-bound seiches are commonly generated in the wake of calving and ice-mélange movement. We explore parameter ranges and aspects of initial iceberg stability as a means of understanding what thresholds that may exist in the stability of real ice shelves.

Macayeal, D. R.; Boghosian, A.; Styron, D. D.; Burton, J. C.; Amundson, J. M.; Cathles, L. M.; Abbot, D. S.

2010-12-01

328

Improved Packaging of Water Purification Tablet.  

National Technical Information Service (NTIS)

The new method of packaging the iodine tablets consists of sealing the individual tablets in a blister sheet and packaging two blister sheets in an overwrapper packet. The blister sheet measures 1 3/4 in x 2 1/8 in and contains 12 transparent blister unit...

J. L. Carney

1974-01-01

329

21 CFR 520.1870 - Praziquantel tablets.  

Code of Federal Regulations, 2013 CFR

...2013-04-01 2013-04-01 false Praziquantel tablets. 520.1870 Section 520...FORM NEW ANIMAL DRUGS § 520.1870 Praziquantel tablets. (a) Specifications ...contains: (1) 34 milligrams (mg) praziquantel. (2) 11.5 or 23 mg...

2013-04-01

330

Enhancing Student Performance Using Tablet Computers  

ERIC Educational Resources Information Center

|Tablet PCs have the potential to change the dynamics of classroom interaction through wireless communication coupled with pen-based computing technology that is suited for analyzing and solving engineering problems. This study focuses on how tablet PCs and wireless technology can be used during classroom instruction to create an Interactive…

Enriquez, Amelito G.

2010-01-01

331

Tablet computers in the veterinary curriculum.  

PubMed

Tablet computers offer a new method of information management in veterinary medical education. With the tablet computer, students can annotate class notes using electronic ink, search for keywords, and convert handwriting to text as needed. Additional electronic learning resources, such as medical dictionaries and electronic textbooks, can be readily available. Eleven first-year veterinary students purchased tablet computers and participated in an investigation of their working methods and perceptions of the tablet computer as an educational tool. Most students found the technology useful. The small size and portability of the tablet allowed easy transport and use in a variety of environments. Most students adapted to electronic notetaking by the second week of classes; negative experiences with the tablet centered on a failure to become comfortable with taking notes and navigating on the computer as opposed to writing and searching on paper. A few performance-related problems, including short battery life, were reported. Tablet software allowed conversion of faculty course notes from a variety of original formats, meaning that instructors could maintain their original methods of note preparation. Adopting a consistent naming convention for files helped students to locate the files on their computers, and smaller file sizes helped with computer performance. Collaboration between students was fostered by tablet use, which offers possibilities for future development of collaborative learning environments. PMID:15834829

Eurell, Jo Ann C; Diamond, Nancy A; Buie, Brandon; Grant, David; Pijanowski, Gerald J

2005-01-01

332

Putting Tablet PCs to the Test  

ERIC Educational Resources Information Center

Like many educators, the author and her colleagues (five faculty members and two IT techs) in the department of Media Communications and Technology at East Stroudsburg University in Pennsylvania were interested to find out the status of tablet PCs in education. Microsoft listed 10 manufacturers of tablet PCs following two forms: the slate and the…

Amirian, Susan

2004-01-01

333

Time to stop counting the tablets?  

Microsoft Academic Search

We attempted to assess compliance using both a pharmacologic indicator (low-dose phenobarbital) and a return tablet count in 225 patients who were taking part in three separate studies. There were 216 patients (96%) who kept a follow-up appointment after 28 days; 161 patients appeared to have good compliance (90% to 109%) by return tablet count. Of these 161 patients, 51

Thomas Pullar; Shubha Kumar; Hilary Tindall; Morgan Feely

1989-01-01

334

Using a Tablet PC for Classroom Instruction  

Microsoft Academic Search

An increasing trend for lecture-based courses is for instructors to convert their lecture notes to slides that can be projected electronically. While there are many advantages to electronic projection, a large drawback is the loss of interactivity and spontaneity that can result. The use of a tablet PC by the instructor promises to overcome this difficulty. The tablet PC, combined

Carol C. W. Hulls

2005-01-01

335

Analysis of fatty acids in ecstasy tablets  

Microsoft Academic Search

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

Ines Baer; Pierre Margot

2009-01-01

336

Gastric emptying of enteric-coated tablets  

SciTech Connect

To evaluate the gastric emptying time of pharmaceutical dosage forms in a clinical setting, a relatively simple dual-radionuclide technique was developed. Placebo tablets of six different combinations of shape and size were labeled with indium-111 DTPA and enteric coated. Six volunteers participated in a single-blind and crossover study. Tablets were given in the morning of a fasting stomach with 6 oz of water containing /sup 99m/Tc pertechnetate and continuously observed with a gamma camera. A scintigraph was obtained each minute. The results suggested that the size, shape, or volume of the tablet used in this study had no significant effect in the rate of gastric emptying. The tablets emptied erratically and unpredictably, depending upon their time of arrival in the stomach in relation to the occurrence of interdigestive myoelectric contractions. The method described is a relatively simple and accurate technique to allow one to follow the gastric emptying of tablets.

Park, H.M.; Chernish, S.M.; Rosenek, B.D.; Brunelle, R.L.; Hargrove, B.; Wellman, H.N.

1984-03-01

337

Producing Magnesium Metallic Glass By Disintegrated Melt Deposition  

SciTech Connect

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. [Sch. of Mech. and Aerospace Eng., Nanyang Technological University, Singapore 639798 (Singapore); Dept. of Mechanical Engineering, National University of Singapore, Singapore 117576 (Singapore); Gupta, M. [Dept. of Mechanical Engineering, National University of Singapore, Singapore 117576 (Singapore); Jarfors, A. E. W. [Sch. of Mech. and Aerospace Eng., Nanyang Technological University, Singapore 639798 (Singapore); Singapore Institute of Manufacturing Technology, Singapore 638075 (Singapore); Tan, M. J. [Sch. of Mech. and Aerospace Eng., Nanyang Technological University, Singapore 639798 (Singapore)

2011-01-17

338

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

339

A comparison of posture and muscle activity during tablet computer, desktop computer and paper use by young children.  

PubMed

Computers are now widely used by children. Tablet computers are becoming widely available and promoted for use by school children. The primary objective of this study was to compare the posture and muscle activity of children using a tablet computer to the posture and muscle activity of children using a desktop computer and paper technology. Eighteen children (mean age 5.6 years) performed a colouring-in task in tablet, desktop and paper conditions. 3-D posture and muscle activity around the neck and shoulder was assessed. Tablet computer use was similar to paper use, with less neutral spinal posture, more elevated scapular posture and greater upper trapezius and cervical erector spinae activity. This was offset by greater variability of posture and muscle activity. Tablet computer use clearly results in different musculoskeletal stresses than desktop computer use. Computer use guidelines need to be appropriate to traditional and emerging technologies. Tablet computers are being promoted for use by adults and children. However, the physical impact of using this type of technology is not known. The findings of this study provide the first tablet-specific evidence to inform guidelines on wise use of tablet computers by children. PMID:18357540

Straker, L M; Coleman, J; Skoss, R; Maslen, B A; Burgess-Limerick, R; Pollock, C M

2008-04-01

340

Teaching dynamics using interactive tablet PC instruction software  

Microsoft Academic Search

Is there an advantage of using interactive tablet PC software as opposed to more traditional teaching methods? This work is an innovative use of tablet PC technology to teach an introductory dynamics course. Each student in the classroom used a tablet PC as did the instructor. In addition to using the tablet PCs, each lecture was recorded using screen capture

David Fisher; Phillip Cornwell; Julia Williams

2007-01-01

341

[Tramadol/acetaminophen combination tablets].  

PubMed

Tramadol/acetaminophen fixed-dose combination tablets (Tramse) combine tramadol, a centrally acting week opioid analgesic, with low-dose acetaminophen. The action of tramadol may be described as a weak agonist at the mu-opioid receptor, inhibition of serotonin reuptake, and inhibition of noradrenaline reuptake. The second component in these tablets, acetaminophen mainly appears to act through central mechanism. Chronic pain may be broadly classified into nociceptive, neuropathic and mixed. Tramset may exert additive or synergic benefits in treating the multiple mechanism of pain. Clinical studies have revealed its efficacy and safety for a variety of pain condition such as chronic low back pain, rheumatoid arthritis, fibromyalgia and painful diabetic peripheral neuropathy. It is expected that Tramset is going to induce pain relief and to improve disturbance of daily life in patients with intractable chronic pain. However overuse of Tramset may induce severe adverse effects such as addiction, abuse and hepatotoxicity. Therefore clinician should continuously assess pain intensity, activity of daily life, mode of its consumption, and adverse effects after prescription. PMID:23905401

Yokotsuka, Shoko; Kato, Jitsu

2013-07-01

342

Influence of pH on in vitro disintegration of phosphate binders  

Microsoft Academic Search

Hyperphosphatemia, a common complication in patients with end-stage renal disease, is treated with oral phosphate-binding medications that restrict phosphorus absorption from the gastrointestinal (GI) tract. Impaired product performance, such as failure to disintegrate and\\/or dissolve in the GI tract, could limit the efficacy of the phosphate binder. Disintegration may be as important as dissolution for predicting in vitro product performance

MK Stamatakis; JM Alderman; PJ Meyer-Stout

1998-01-01

343

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

344

Investigations of a novel self-emulsifying osmotic pump tablet containing carvedilol.  

PubMed

Carvedilol has been made into a novel osmotic pump tablet which includes Gelucire 44/14, Lutrol F68, Transcutol P, silicon dioxide, mannitol, citric acid, and sodium hydrogen carbonate. The Self-emulsifying osmotic pump tablet (SEOPT) has two outstanding features. It could improve the bioavailability of carvedilol by self-emulsifying drug delivery system (SEDDS), control the release rate and make the plasma concentrations more stable by elementary osmotic pump tablet. The results of transmission electron microscope (TEM) and particle size assessment showed that the shape of the resultant emulsion was round and regular, the average diameter of the particles was 246 nm. Since the solubility of carvedilol was improved by the emulsion, the elementary SEOPT could guarantee a complete release of carvedilol under the osmotic pressure of mannitol. The cumulative release at 12 hr was 85.18%. Therefore the disadvantage that lipophilic drugs can not be released completely when prepared into elementary osmotic pump tablet was resolved. The results of Differential scanning calorimetry (DSC), Infrared spectroscopy (IR) and X-ray diffraction diffraction (XRD) proved that carvedilol was amorphous in the preparation. The relative bioavailability of carvedilol in beagle dogs was 156.78%. The plasma concentrations were more stable compared with that of commercially available tablet (Luode). And the in vitro and in vivo correlation was good (r = 0.9725). Therefore, the elementary SEOPT developed in this paper might provide a new idea for preparing lipophilic drugs into osmotic pump tablet conveniently. PMID:17891586

Wei, Lanlan; Li, Jie; Guo, Liangran; Nie, Shufang; Pan, Weisan; Sun, Peinan; Liu, Hui

2007-09-01

345

Pharmacokinetics study of bio-adhesive tablet of Panax notoginseng saponins  

PubMed Central

Panax notoginseng saponin (PNS) is the main active gradient of Chinese traditional medicine Panax notoginseng. Although its prominent therapeutic efficacy has been demonstrated by various researchers, the broader application is restricted by the low bioavailability of PNS. This article aims to discuss PNS's plasma pharmacokinetics after oral administration of bio-adhesive tablet of PNS to beagle dogs and improve its bioavailability in comparison with normal tablet. The bio-adhesive tablet was prepared according to our previous patent, using chitosan as main excipient. A simple and sensitive LC-MS/MS combined with solid-phase extraction (SPE) method for the analysis of PNS in dog's plasma was developed in our previous study, and was validated to apply in the pharmacokinetics study in this work. Three ingredients: Notoginsenoside R1 (R1), Ginsenoside Rg1 (Rg1) and Ginsenoside Rb1 (Rb1) (Figure 1), were chosen as indicators of PNS to analyze it in vivo. Statistically significant increase (P < 0.05) in pharmacokinetic parameters of PNS including AUC and Tmax for R1, Rg1 and Rb1, Cmax for R1 and Rb1, MRT for Rg1 were obtained after oral administration of bio-adhesive tablet of PNS comparing with its normal tablet. The formulation modification of using chitosan to prepare bio-adhesive tablet for oral administration is effective in improving the bioavailability of PNS, thereby enhancing its potential therapeutic effect and broadening its clinical application.

2011-01-01

346

Comparison of febantel tablets and Vercom paste against gastrointestinal nematodes of dogs.  

PubMed

Thirty adult dogs with naturally acquired gastrointestinal nematode infections were assigned at random to ten replicates and treated daily for 3 days with either a combination febantel/praziquantel (Vercom) paste, febantel tablets or placebo tablets. Numbers of hookworm and whipworm eggs after treatment were reduced similarly for both drug formulations when compared with pretreatment egg counts, whereas these counts increased in the controls. Vercom paste reduced the hookworm egg count by 99.9% and the whipworm egg count by 99.6%. The febantel tablet decreased the hookworm egg count by 99.9% and the whipworm egg count by 100%. As determined at necropsy, the controlled test efficacy against adult hookworms and whipworms was similar for the Vercom paste and the febantel tablets. The controlled test efficacies of Vercom paste against Ancylostoma caninum, Ancylostoma braziliense, and Trichuris vulpis were, respectively, 99.7%, 100% and 95.8% and those of febantel tablets were 98.2%, 100% and 99.7%. These results indicate that the nematocidal efficacy of febantel against these nematodes remains unchanged in these two formulations. No adverse reactions to either febantel tablets or to Vercom paste were observed. PMID:1561756

Greiner, E C; Brenner, D G; Cox, D D; Heaton-Jones, D L

1992-02-01

347

[Barbital buffer in tablets as a solvent for complement fixation test (CFT)].  

PubMed

The purpose of this paper was to develop a tableting technology of barbital buffer as a standard diluent easy in use for complement fixation test (CFT). As starting point, barbital (veronal) buffer after Alton et al. [1] was assumed. Among 4 solubilizers polyvinyl pyrrolidone (PVP 10 000) was chosen, which provided a good solubility of the barbital in distilled water at 20 degrees C and it affected favourably the complement activity (C'). PVP 10 000 added to the components of barbital buffer at an amount of 0.275 per 10 tablets, in the form of solution for granulation, provided the required physical properties of the tablets. As compared with the barbital buffer after Alton et al. [1], the tablets produced affected favourably C' activity, decreased the range of spontaneous haemocyte lysis, and they did not effect CFT titers of two anti-Brucella abortus standard sera as well as 77 sera of cattle infected with brucellosis under natural conditions. The described physical and biological properties of the barbital buffer tablets with PVP addition indicate their usability as diluent for CFT. A standard diluent used in the form of tablets in all Poland's laboratories should provide a better reproducibility of CFT results in diagnostic examinations towards brucellosis as well as other infectious diseases in men and animals. PMID:7167394

Królak, M; Janicki, S; Starostka, K; B?aszczyk, B

1982-01-01

348

Controlled-Release Carbamazepine Matrix Granules and Tablets Comprising Lipophilic and Hydrophilic Components  

PubMed Central

The objective of this study was to investigate the effect of lipophilic (Compritol® 888 ATO) and hydrophilic components (combination of HPMC and Avicel) on the release of carbamazepine from granules and corresponding tablet. Wet granulation followed by compression was employed for preparation of granules and tablets. The matrix swelling behavior was investigated. The dissolution profiles of each formulation were compared to those of Tegretol® CR tablets and the mean dissolution time (MDT), dissolution efficiency (DE%), and similarity factor (f2 factor) were calculated. It was found that increase in the concentration of HPMC results in reduction in the release rate from granules and achievement of zero-order is difficult from the granules. The amount of HPMC plays a dominant role for the drug release. The release mechanism of CBZ from matrix tablet formulations follows non-Fickian diffusion shifting to Case II by the increase of HPMC content, indicating significant contribution of erosion. Increasing in drug loading resulted in acceleration of the drug release and in anomalous controlled-release mechanism due to delayed hydration of the tablets. These results suggest that wet granulation followed by compression could be a suitable method to formulate sustained release CBZ tablets.

Barakat, Nahla S.; Elbagory, Ibrahim M.; Almurshedi, Alanood S.

2009-01-01

349

Formulation, Release Characteristics and Bioavailability Study of Oral Monolithic Matrix Tablets Containing Carbamazepine  

PubMed Central

This study examined the release of carbamazepine (CBZ) from hydrophobic (Compritol® 888 ATO) and hydrophilic-hydrophobic matrix combination (Compritol® 888 ATO-hydroxpropyl methylcellulose, HPMC). Hydrophobic matrix tablets were prepared by hot fusion technique, while hydrophilic-hydrophobic matrix tablets were prepared by wet granulation technique. The properties of the compressed matrix tablets were determined according to the US Pharmacopoeia. Both matrix formulations displayed a controlled-release profile when compared to the reference formulation (Tegretol® CR 200). The bioavailability of CBZ formulations and Tegretol® CR 200 were evaluated in beagle dogs. Carbamazepine presented a significant higher bioavailability from matrix tablets containing hydrophilic polymer (HPMC) than that obtained from Tegretol® CR200. The average inter-subject plasma concentration variability CV% was the least with tablet containing hydrophilic polymer (HPMC) and was the highest with Tegretol® CR 200 (33.8 and 54.1, respectively). Analysis of variance applied to log \\documentclass[12pt]{minimal} \\usepackage{amsmath} \\usepackage{wasysym} \\usepackage{amsfonts} \\usepackage{amssymb} \\usepackage{amsbsy} \\usepackage{mathrsfs} \\usepackage{upgreek} \\setlength{\\oddsidemargin}{-69pt} \\begin{document}$${\\text{AUC}}_{0 - \\alpha } $$\\end{document} and log C max showed statistical significant differences among the three formulations (P?tablets examined.

Elbagory, Ibrahim M.; Almurshedi, Alanood S.

2008-01-01

350

Controlled-Release Carbamazepine Granules and Tablets Comprising Lipophilic and Hydrophilic Matrix Components  

PubMed Central

The objective of this study was to investigate the effect of lipophilic (Compritol® 888 ATO) and hydrophilic components (combination of HPMC and Avicel) on the release of carbamazepine from granules and corresponding tablet. Wet granulation followed by compression was employed for preparation of granules and tablets. The matrix swelling behavior was investigated. The dissolution profiles of each formulation were compared to those of Tegretol® CR tablets and the mean dissolution time (MDT), dissolution efficiency (DE %) and similarity factor (f2 factor) were calculated. It was found that increase in the concentration of HPMC results in reduction in the release rate from granules and achievement of zero-order is difficult from the granules. The amount of HPMC plays a dominant role for the drug release. The release mechanism of CBZ from matrix tablet formulations follows non-Fickian diffusion shifting to case II by the increase of HPMC content, indicating significant contribution of erosion. Increasing in drug loading resulted in acceleration of the drug release and in anomalous controlled-release mechanism due to delayed hydration of the tablets. These results suggest that wet granulation followed by compression could be a suitable method to formulate sustained release CBZ tablets.

Elbagory, Ibrahim M.; Almurshedi, Alanood S.

2008-01-01

351

IHF-independent assembly of the Tn10 strand transfer transpososome: implications for inhibition of disintegration  

PubMed Central

The frequency of DNA transposition in transposition systems that employ a strand transfer step may be significantly affected by the occurrence of a disintegration reaction, a reaction that reverses the strand transfer event. We have asked whether disintegration occurs in the Tn10 transposition system. We show that disintegration substrates (substrates constituting one half of the strand transfer product) are assembled into a transpososome that mimics the strand transfer intermediate. This strand transfer transpososome (STT) does appear to support an intermolecular disintegration reaction, but only at a very low level. Strikingly, assembly of the STT is not dependent on IHF, a host protein that is required for de novo assembly of all previously characterized Tn10 transpososomes. We suggest that disintegration substrates are able to form both transposon end and target type contacts with transposase because of their enhanced conformational flexibility. This probably allows the conformation of DNA within the complex that prevents the destructive disintegration reaction, and is responsible for relaxing the DNA sequence requirements for STT formation relative to other Tn10 transpososomes.

Stewart, Barry J.; Wardle, Simon J.; Haniford, David B.

2002-01-01

352

Preparation and characterization of novel fast disintegrating capsules (Fastcaps) for administration in the oral cavity.  

PubMed

The objective of this study was to prepare novel capsule-based fast disintegrating dosage forms for the oral cavity (Fastcaps). First, cast films were prepared from various additive-containing gelatin solutions and evaluated with respect to disintegration time and mechanical properties in order to identify suitable formulations for the capsule preparation. The disintegration time of films decreased with decreasing bloom strength and could be further decreased by the addition of sugars or PEGs. Fast disintegrating capsules were successfully prepared by a dipping process, whereby parameters such as the viscosity and temperature of the dipping solution and the dipping velocity of the steel pins were optimized. The required viscosity range of the dipping solution for Fastcap manufacturing was 500-600 cP. The addition of the hydrophilic additives (xylitol, sorbitol or PEG 1500) did not significantly affect the viscosity and gelation temperature of the dipping solution. The in vitro disintegration of Fastcaps (30-45 s) was twice as rapid as the one of regular hard gelatin capsules. In vivo, Fastcaps disintegrated rapidly (9-13 s) and their content was spread throughout the oral cavity within seconds. Lactose and/or microcrystalline cellulose were suitable fillers for Fastcaps. The mechanical properties of Fastcaps were similar to commercially available gelatin capsules, which assures good processability and handling. PMID:16111845

Ciper, Mesut; Bodmeier, Roland

2005-10-13

353

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.

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

2009-01-01

354

Properties of lipophilic matrix tablets containing phenylpropanolamine hydrochloride prepared by hot-melt extrusion.  

PubMed

The objective of the present study was to investigate the influence of formulation factors on the physical properties of hot-melt extruded granules and compressed tablets containing wax as a thermal binder/retarding agent, and to compare the properties of granules and tablets with those prepared by a high-shear melt granulation (MG) method. Powder blends containing phenylpropanolamine hydrochloride, Precirol and various excipients were extruded in a single-screw extruder at open-end discharge conditions. The extrudates were then passed through a 14-mesh screen to form granules. The extrusion conditions and the optimum amount of wax to function as the thermal binder were dependent on the properties of the filler excipients. At the same wax level, drug release from tablets decreased in the order of using microcrystalline cellulose (MCC), lactose and Emcompress as the filler excipient. The observed differences in the dissolution properties of the tablets were due to the differences in the solubility, swellability and density of the filler excipients. Replacing Precirol with Sterotex K, a higher melting point wax, resulted in slightly increased dissolution rates, when the extrusion was performed at the same temperature conditions. Hot-melt extruded granules were observed to be less spherical than high-shear melt granules and showed lower values of bulk/tap densities. However, tablets containing MCC or lactose granules prepared by hot-melt extrusion (HME) exhibited higher hardness values. Slower drug release rates were found for tablets containing MCC by HME compared with MG. Analysis of the hot-melt extruded granules showed better drug content uniformity among granules of different size ranges compared with high-shear melt granules, resulting in a more reproducible drug release from the corresponding tablets. PMID:11522484

Liu, J; Zhang, F; McGinity, J W

2001-09-01

355

Optimization and in vivo pharmacokinetic study of a novel controlled release venlafaxine hydrochloride three-layer tablet.  

PubMed

Several matrix tablet formulations (hydrophilic-based, wax-based, and three-layer tablets) were designed for controlling the release of the highly water soluble drug, venlafaxine hydrochloride (VenHCl) for once-daily administration. The three-layer tablets consist of non-swellable, compritol-based middle layers containing the drug to which hydrophilic top and bottom barrier layers were applied. A 2(3) full-factorial design was employed for optimization and to explore the effect of different variables on the release rate of the drug from the three-layer tablets. The optimized levels of each independent variable were based on the criterion of desirability. The calculated values of f(1) and f(2) were 4.131 and 79.356, respectively; indicating that the release profile of the optimized PEO layered tablet formulation is comparable to that of the target release model. The pharmacokinetic parameters of VenHCl from the optimized three-layer tablet was compared to the marketed extended release capsule as a reference in healthy human subjects using a randomized crossover design. In this study, the 90% confidence interval for AUC(0-24) and AUC(0-?) are within (0.8-1.25), which satisfied the bioequivalence criteria. It could be concluded that a promising once-daily extended-release three-layer tablet of the highly water soluble drug, VenHCl, was successfully designed. PMID:20532709

Aboelwafa, Ahmed A; Basalious, Emad B

2010-06-08

356

Optimization and In vivo Pharmacokinetic Study of a Novel Controlled Release Venlafaxine Hydrochloride Three-Layer Tablet  

PubMed Central

Several matrix tablet formulations (hydrophilic-based, wax-based, and three-layer tablets) were designed for controlling the release of the highly water soluble drug, venlafaxine hydrochloride (VenHCl) for once-daily administration. The three-layer tablets consist of non-swellable, compritol-based middle layers containing the drug to which hydrophilic top and bottom barrier layers were applied. A 23 full-factorial design was employed for optimization and to explore the effect of different variables on the release rate of the drug from the three-layer tablets. The optimized levels of each independent variable were based on the criterion of desirability. The calculated values of f1 and f2 were 4.131 and 79.356, respectively; indicating that the release profile of the optimized PEO layered tablet formulation is comparable to that of the target release model. The pharmacokinetic parameters of VenHCl from the optimized three-layer tablet was compared to the marketed extended release capsule as a reference in healthy human subjects using a randomized crossover design. In this study, the 90% confidence interval for AUC0–24 and AUC0?? are within (0.8–1.25), which satisfied the bioequivalence criteria. It could be concluded that a promising once-daily extended-release three-layer tablet of the highly water soluble drug, VenHCl, was successfully designed.

Basalious, Emad B.

2010-01-01

357

Chitosan-kaolin coprecipitate as disintegrant in microcrystalline cellulose-based pellets elaborated by extrusion-spheronization.  

PubMed

The usefulness of a coprecipitate of chitosan and kaolin as disintegrant in the pellets of microcrystalline cellulose (MCC) and hydrochlorothiazide (HCT) (as a model of poorly water-soluble drug) produced by extrusion-spheronization was evaluated in this study. The effectiveness of chitosan-kaolin coprecipitate to increase the dissolution rate was compared with that of kaolin and chitosan. A possible synergy effect was also evaluated between the coprecipitate, kaolin or chitosan and sorbitol, added to the pellets as a very water-soluble diluent. The chitosan-kaolin coprecipitate, the kaolin or the chitosan allowed pellets to be obtained of adequate size, roundness, mechanical strength and flow properties. Furthermore, the incorporation of chitosan-kaolin coprecipitate or chitosan significantly increased the dissolution rate of HCT independently of the sorbitol content. The effects on the dissolution of HCT derived from the incorporation of coprecipitate to the pellets can be attributed to its content of chitosan. However, the addition of kaolin into the pellets did not significantly affect the HCT dissolution process. The pellets incorporating coprecipitated chitosan-kaolin or chitosan and the maximum proportion of sorbitol (50%) led to the highest HCT dissolution rate and experienced a rapid and complete disintegration in the dissolution medium. PMID:22309024

Goyanes, Alvaro; Souto, Consuelo; Martínez-Pacheco, Ramón

2012-02-07

358

21 CFR 520.804 - Enalapril tablets.  

Code of Federal Regulations, 2013 CFR

...HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.804 Enalapril tablets...maleate is administered as conjunctive therapy with furosemide and digoxin in...

2013-04-01

359

21 CFR 520.1380 - Methocarbamol tablets.  

Code of Federal Regulations, 2013 CFR

...HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1380 Methocarbamol tablets...administered to dogs and cats as an adjunct to therapy for acute inflammatory and...

2013-04-01

360

21 CFR 520.531 - Cythioate tablets.  

Code of Federal Regulations, 2013 CFR

...tablet. (c) Special considerations. Cythioate is a cholinesterase inhibitor. Do not use this product in animals simultaneously...a few days before or after treatment with or exposure to cholinesterase-inhibiting drugs, insecticides, pesticides, or...

2013-04-01

361

21 CFR 520.812 - Enrofloxacin tablets.  

Code of Federal Regulations, 2013 CFR

...CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.812 Enrofloxacin tablets... Dogs and cats for management of diseases associated with bacteria susceptible to enrofloxacin. (3) Limitations...

2013-04-01

362

Fentanyl Buccal Tablets (marketed as Fentora) Information  

Center for Drug Evaluation (CDER)

... Fentora (fentanyl buccal tablets) is a an opioid pain medication used for the treatment of breakthrough pain in cancer patients receiving opioid ... More results from www.fda.gov/drugs/drugsafety/postmarketdrugsafetyinformationforpatientsandproviders

363

Chocolate Tablet Aspects of Cytherean Meshkenet Tessera.  

National Technical Information Service (NTIS)

Meshkenet Tessera structures were mapped from Magellan data and several resemblances to chocolate tablet boudinage were found. The complex fault sets display polyphase tectonic sequences of a few main deformation phases. Shear and tension have contributed...

J. Raitala

1993-01-01

364

Workshop - tablet PCs in engineering education & research  

Microsoft Academic Search

Tablet PCs are one of the newest innovations in computing and communications tools, offering an opportunity to positively impact the way in which students and faculty use technology to support teaching and learning. In this three hour workshop faculty will receive a hands-on introduction to the use of several tablet-based software tools including OneNote, Classroom Presenter, WriteOn, ChemPad, VectorPad and

J. G. Tront; J. C. Prey

2007-01-01

365

Mechanical and geometric property characterization of dry-coated tablets with contact ultrasonic techniques.  

PubMed

A dry-coated tablet is a solid dosage form with a controlled drug-release system, which consists of a core and an outer layer. The accuracy of its geometric (e.g. the outer layer wall and core thicknesses) and mechanical properties (e.g. Young's moduli and mass densities of associated materials) could be crucial to its therapeutic and structural functions. The objective of current study is to develop a non-destructive technique for determining the geometric and mechanical properties of dry-coated tablets. Two contact ultrasonic techniques (i.e. pitch-catch and pulse-echo measurement modes) are employed and the properties of all the structural components of a set of experimental tablets are measured and reported. The thicknesses of the outer layers of the sample tablets are used to obtain the eccentricity of the core tablets. The two approaches are compared for their effectiveness in obtaining these properties of the sample dry-coated tablets. The thicknesses of the outer layers obtained with the proposed approach and with the direct (destructive) measurements are also compared. A good agreement is found; there is an approximately 2% difference. The eccentricity and concentricity of a set of tablets are determined and it is concluded that the observed consistent anomaly in eccentricity can be attributed to the same root cause and its correction can be achieved by control input based on monitoring data. Potential of the approach for in-die real-time monitoring of compaction presses and its PAT (Process Analytical Technology) applications for the pharmaceutical manufacturing are also discussed. PMID:20363299

Liu, Jingfei; Cetinkaya, Cetin

2010-04-02

366

The natural history of somatic morbidity in disintegrative psychosis and infantile autism: a validation study.  

PubMed

In order to study the validity of disintegrative psychosis (DP) as defined in ICD-9, we compared the natural history of somatic morbidity of 13 patients given this diagnosis in childhood with a control group of 39 patients with infantile autism (IA) matched for gender, age, IQ and social class. Average follow-up time was 22 and 23 (11-33) years, respectively. Significantly more DP patients (85 versus 41%) had been admitted to a non-psychiatric hospital during the follow-up period. They also had significantly more admissions (3.6 versus 1.0) and stayed longer in hospital (78 versus 4 days) than patients with IA. Three of the DP individuals had an associated medical disorder and made extensive use of somatic services during the follow-up period. Altogether the DP group had utilised the medical health care system more than patients with IA suggesting that they had more medical symptoms than the IA group. On the whole our findings suggest that individuals with DP and IA should be conceptualised as essentially distinct and should be studied separately as regards aetiology, pathophysiology, course and treatment. PMID:10522520

Mouridsen, S E; Rich, B; Isager, T

1999-10-01

367

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.

2010-01-01

368

Tablet computer use by medical students in the United States.  

PubMed

The value of tablet computer use in education is an area of considerable interest. Preliminary investigations shows that medical students feel that tablet computers were a positive addition to the preclinical curriculum. To better understand how and why medical students use tablet computers, we conducted an online survey of medical students in the United States This study shows frequent tablet computer use by medical students. Students in clinical years of medical school are the most frequent users of tablet computers. The high frequency of tablet computer use suggest that this may be an important area for medical educators to explore. PMID:23832806

Robinson, Robert L; Burk, Martha S

2013-07-07

369

Day-long reduction of oral malodor by a palatal mucoadhesive tablet containing herbal formulation.  

PubMed

Previous research has shown the oral malodor reducing abilities of an herbal formulation delivered using a palatal mucoadhesive tablet. The aim of the present study was to test the day-long effect of this preventive treatment on oral malodor reduction as compared with placebo and commercial mouthwash. Forty young healthy subjects (mean age, 25.8 ± 1.8 yrs, 19 females) presenting with oral malodor were randomly assigned to use one of the three tested products: herbal mucoadhesive tablets, placebo mucoadhesive tablets and a commercial mouthwash. Following baseline measurements, subjects were instructed to use the products in the evening of the same day and the following morning. Baseline and follow-up measurements were conducted in the afternoon and included odor judge scores (two judges), volatile sulfide compounds (VSC) levels using a sulfide monitor (Halimeter™) and saliva sample for ?-galactosidase activity assay. The herbal mucoadhesive tablet caused a significant reduction in malodor scores (p = 0.004), VSC levels (p = 0.002) and ?-galactosidase assay (p = 0.02) as compared to the placebo, and reduced malodor level to below the clinical threshold (mean odor judge score of 1.7). These results demonstrate the efficacy of the herbal formulation delivered using a mucoadhesive tablet for day-long prevention of oral malodor. PMID:23519054

Sterer, N; Ovadia, O; Weiss, E I; Perez Davidi, M

2013-03-22

370

Impaired oesophageal transit of capsule versus tablet formulations in the elderly.  

PubMed Central

Drug induced oesophageal injury is an important and preventable cause of iatrogenic injury. In most cases the injury is considered to be due to mucosal contact from formulations lodged in the oesophagus. A scintigraphic study was performed comparing the oesophageal transit of enteric coated tablets with similar sized and shaped gelatin capsules, using a population of elderly healthy volunteers similar in age (50-79 years) to the population most likely to be receiving regular treatment. Twenty three volunteers injected the radiolabelled tablet or capsule with 50 ml of water while sitting on two separate occasions according to a randomisation schedule. Oesophageal transit was assessed by gamma scintigraphy. Gastric residence was also assessed in 11 of 23 subjects. While the tablet was readily cleared from the oesophagus, mean transit time 4.3 seconds (range 1.0-14.0), the capsule often showed a comparatively prolonged holdup, mean transit time 20.9 seconds (range 1.5-174.5). Ten of 11 tablets emptied from the stomach intact, while all 11 capsules broke up in the stomach. Gelatin capsules showed a clear tendency to remain within the oesophagus of healthy elderly volunteers, while similar sized enteric coated tablets did not. These studies show the importance of assessing oesophageal transit when designing the formulation of drugs with a potential for oesophageal injury. Images Figure 2 Figure 3

Perkins, A C; Wilson, C G; Blackshaw, P E; Vincent, R M; Dansereau, R J; Juhlin, K D; Bekker, P J; Spiller, R C

1994-01-01

371

Characterization of khaya gum as a binder in a paracetamol tablet formulation.  

PubMed

The influence of khaya gum, a binding agent obtained from Khaya grandifolia (Meliaceae family), on the bulk, compressional, and tabletting characteristics of a paracetamol tablet formulation was studied in comparison with the effects of two standard binders: polyvinylpyrrolidone (PVP; molecular weight 40,000) and gelatin. The relative ability of khaya gum to destroy any residual microbial contamination in the binder or in the formulation during tabletting was also studied using Bacillus subtilis spores as a model. Formulations containing khaya gum exhibited more densification than formulations containing PVP and gelatin during die filling, but less densification due to rearrangement at low pressures. The mean yield pressure of the formulation particles obtained from Heckel plots, and another pressure term, also inversely related to plasticity, obtained from Kawakita plots, showed dependence on the nature and concentration of the binder, with formulations containing khaya gum exhibiting the lowest and highest values respectively. The values of the pressure terms suggest that the yield pressure relates to the onset of plastic deformation during compression, while the Kawakita pressure relates to the total amount of plastic deformation occurring during the compression process. Tablets made from formulations containing khaya gum had the lowest tensile strength values but also the lowest tendency to laminate or cap, as indicated by their lowest brittleness. All the tablets had friability values < 1% at higher concentrations of the three binders. In addition, khaya gum demonstrated a comparable ability to destroy microorganisms in the formulation during tabletting as the two binders. The characterization of the formulations suggests that khaya gum can be developed into a commercial binding agent for particular tablets. PMID:12026225

Odeku, O A; Itiola, O A

2002-03-01

372

Reduction of tobacco withdrawal symptoms with a sublingual nicotine tablet: a placebo controlled study.  

PubMed

Many smokers are unable to use gum as a cessation aid due to fillings, bridgework and dyspepsia or they reject it for esthetic reasons. The nicotine sublingual tablet is a new alternative to the nicotine polacrilex chewing gum that does not necessitate chewing. Twenty subjects used 2-mg sublingual nicotine tablets and placebo in a double-blind randomized crossover study of 2-day smoke-free periods. Craving and other withdrawal symptoms were rated on 100-mm visual analog scales (VAS) nine times over each 2-day period. Plasma nicotine concentrations in the afternoon of each study day were determined. A blood sample was also taken in the afternoon of a 2-day period with normal smoking. The mean number of nicotine tablets was 10 and seven on days 1 and 2, respectively. The corresponding number for placebo tablets was six and five. No subject used less than five tablets on any study day. The degree of nicotine substitution, defined as the quotient between the plasma levels achieved with the sublingual tablet and smoking, was 43, 30 and 23% for smokers with FTQ < or = 6, FTQ = 7 and FTQ > or = 8 (Fagerström Tolerance Questionnaire), respectively. Active treatment was significantly superior in decreasing craving and other withdrawal symptom scores compared to placebo treatment. Mean total scores were reduced by approximately 50%. Adverse events were mainly symptoms of local irritation such as a burning sensation in the throat or under the tongue, a lump in the throat and heartburn. These results demonstrate partial relief of the tobacco withdrawal syndrome with use of the sublingual tablet similar to that achieved from other forms of nicotine replacement. PMID:11072457

Molander, L; Lunell, E; Fagerström, K O

2000-05-01

373

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

2013-01-17

374

Determination of sunset yellow in multi-vitamin tablets by photoacoustic spectroscopy and a comparison with alternative methods  

Microsoft Academic Search

Photoacoustic (PA) spectroscopy in the visible wavelength region was shown to be suitable for a direct (no preparatory steps involved) quantification of sunset yellow (E110) colour in effervescent multi-vitamin tablets. Measurements on powdered tablets containing E110 were performed at 480?nm at which wavelength this synthetic colour shows appreciable absorbance. The PA data obtained were compared to the results acquired by

Dóka Ottó; Dane Bicanic; Zsolt Ajtony; R. B. M. Koehorst

2005-01-01

375

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

Microsoft Academic Search

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

Salim Abdulla; Baraka Amuri; Abdunoor M Kabanywanyi; David Ubben; Christine Reynolds; Steve Pascoe; Serge Fitoussi; Ching-Ming Yeh; Marja Nuortti; Romain Séchaud; Günther Kaiser; Gilbert Lefèvre

2010-01-01

376

Pharmaceutical applications of shellac: moisture-protective and taste-masking coatings and extended-release matrix tablets.  

PubMed

Shellac is a natural polymer, which is used as enteric coating material in pharmaceutical applications. The major objective of the present study was to investigate the potential of shellac for other purposes, namely to provide moisture-protective and taste-masking coatings as well as extended-release matrix tablets. The efficiency of shellac to achieve moisture protection and taste masking was compared with that of hydroxypropyl methylcellulose (HPMC), which is most frequently used for these purposes. Shellac-coated tablets showed lower water uptake rates than HPMC-coated systems at the same coating level. The stability of acetylsalicylic acid was higher in tablets coated with shellac compared with HPMC-coated systems, irrespective of the storage humidity. Therefore, lower shellac coating levels were required to achieve the same degree of drug protection. Shellac coatings effectively masked the unpleasant taste of acetaminophen tablets. Compared to HPMC, again lower coating levels were required to achieve similar effects. The resulting drug release in simulated gastric fluid was not significantly altered by the thin shellac coatings, which rapidly ruptured due to the swelling of the coated tablet core. In addition, shellac was found to be a suitable matrix former for extended-release tablets. The latter could be prepared by direct compression or via wet granulation using ethanolic or ammoniated aqueous shellac binder solutions. The resulting drug-release patterns could effectively be altered by varying different formulation and processing parameters. PMID:14570313

Pearnchob, N; Siepmann, J; Bodmeier, R

2003-09-01

377

21 CFR 520.1200 - Ivermectin, fenbendazole, and praziquantel tablets.  

Code of Federal Regulations, 2010 CFR

...false Ivermectin, fenbendazole, and praziquantel tablets. 520.1200 Section 520...1200 Ivermectin, fenbendazole, and praziquantel tablets. (a) Specifications ...fenbendazole, and 57 milligrams (mg) praziquantel; or (2) 27 µg ivermectin,...

2009-04-01

378

21 CFR 520.1200 - Ivermectin, fenbendazole, and praziquantel tablets.  

Code of Federal Regulations, 2013 CFR

...false Ivermectin, fenbendazole, and praziquantel tablets. 520.1200 Section 520...1200 Ivermectin, fenbendazole, and praziquantel tablets. (a) Specifications ...fenbendazole, and 57 milligrams (mg) praziquantel; or (2) 27 µg ivermectin,...

2013-04-01

379

21 CFR 520.1199 - Ivermectin, pyrantel, and praziquantel tablets.  

Code of Federal Regulations, 2010 CFR

...false Ivermectin, pyrantel, and praziquantel tablets. 520.1199 Section 520...1199 Ivermectin, pyrantel, and praziquantel tablets. (a) Specifications ...mg) pyrantel pamoate, and 28.5 mg praziquantel; (2) 68 mcg ivermectin, 57...

2009-04-01

380

21 CFR 520.1409 - Methylprednisolone, aspirin tablets.  

Code of Federal Regulations, 2010 CFR

...2009-04-01 false Methylprednisolone, aspirin tablets. 520.1409 Section 520... § 520.1409 Methylprednisolone, aspirin tablets. (a) Specifications. ...methylprednisolone and 300 milligrams of aspirin. (b) Sponsor. See No....

2009-04-01

381

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.

Prajapati, Shailesh T; Mehta, Anant P; Modhia, Ishan P; Patel, Chhagan N

2012-01-01

382

Effects of Orally Administered Lactoferrin and Lactoperoxidase-Containing Tablets on Clinical and Bacteriological Profiles in Chronic Periodontitis Patients  

PubMed Central

This study was undertaken to evaluate the effect of oral administration of lactoferrin (LF) and lactoperoxidase-(LPO-)containing tablet on periodontal condition. Seventy-two individuals with chronic periodontitis were randomly assigned to take either bovine LF and LPO-containing tablets (test group, n = 37) or control tablets (control group, n = 35) every day for 12 weeks. Periodontal parameters and levels of subgingival plaque bacteria, human and bovine LF, and endotoxin in gingival crevicular fluid (GCF) were evaluated at baseline, 1 week, 4 weeks, and 12 weeks. Significant differences were observed in GCF levels of bovine LF between the test and control groups throughout the study (P < .05). However, clinical and bacteriological parameter values proved comparable between the two groups at 1 week to 12 weeks. Therefore, the effect of oral administration of LF and LPO-containing tablets might be weak on periodontal and bacteriological profile in this study.

Shimizu, Eiju; Kobayashi, Tetsuo; Wakabayashi, Hiroyuki; Yamauchi, Koji; Iwatsuki, Keiji; Yoshie, Hiromasa

2011-01-01

383

Effects of orally administered lactoferrin and lactoperoxidase-containing tablets on clinical and bacteriological profiles in chronic periodontitis patients.  

PubMed

This study was undertaken to evaluate the effect of oral administration of lactoferrin (LF) and lactoperoxidase-(LPO-)containing tablet on periodontal condition. Seventy-two individuals with chronic periodontitis were randomly assigned to take either bovine LF and LPO-containing tablets (test group, n = 37) or control tablets (control group, n = 35) every day for 12 weeks. Periodontal parameters and levels of subgingival plaque bacteria, human and bovine LF, and endotoxin in gingival crevicular fluid (GCF) were evaluated at baseline, 1 week, 4 weeks, and 12 weeks. Significant differences were observed in GCF levels of bovine LF between the test and control groups throughout the study (P < .05). However, clinical and bacteriological parameter values proved comparable between the two groups at 1 week to 12 weeks. Therefore, the effect of oral administration of LF and LPO-containing tablets might be weak on periodontal and bacteriological profile in this study. PMID:21747858

Shimizu, Eiju; Kobayashi, Tetsuo; Wakabayashi, Hiroyuki; Yamauchi, Koji; Iwatsuki, Keiji; Yoshie, Hiromasa

2011-04-03

384

Formulation and in vivo evaluation of omeprazole buccal adhesive tablet  

Microsoft Academic Search

For the development of omeprazole buccal adhesive tablets, we studied the release and bioavailability of omeprazole delivered by buccal adhesive tablets composed of sodium alginate, hydroxypropylmethylcellulose (HPMC), magnesium oxide and croscarmellose sodium. Croscarmellose sodium enhanced the release of omeprazole from the tablets. The analysis of the release mechanism showed that croscarmellose sodium changed the release profile of omeprazole from first-

Han-Gon Choi; Jac-Hee Jung; Chul Soon Yong; Chong-Dal Rhee; Mi-Kyung Lee; Jeong-Hee Han; Kyung-Mi Park; Chong-Kook Kim

2000-01-01

385

Adhesive tablet effective for treating canker sores in humans  

Microsoft Academic Search

A new mucoadhesive tablet, which releases natural active agents for pain reduction and rapid healing of canker sores, has been prepared and characterized. Adhesive tablets were prepared by compression molding of mixed powders of crosslinked polyacrylic acid and hydroxypropyl cellulose, absorbed with citrus oil and magnesium salt. The rate of tablet erosion and the rates of citrus oil and magnesium

Boaz Mizrahi; Jacob Golenser; Joseph S. Wolnerman; Abraham J. Domb

2004-01-01

386

Issues and techniques in touch-sensitive tablet input  

Microsoft Academic Search

Touch-sensitive tablets and their use in human-computer interaction are discussed. It is shown that such devices have some important properties that differentiate them from other input devices (such as mice and joysticks). The analysis serves two purposes: (1) it sheds light on touch tablets, and (2) it demonstrates how other devices might be approached. Three specific distinctions between touch tablets

William Buxton; Ralph Hill; Peter Rowley

1985-01-01

387

The Tablet PC For Faculty: A Pilot Project  

Microsoft Academic Search

This paper describes a pilot project with the purpose of evaluating the usefulness of tablet PCs for university professors. The focus is on the value of tablets primarily with respect to teaching and learning (and not for research or administrative work). Sixty-four professors, distributed across the various schools of a university, were provided with tablet PCs and were trained in

Rob R. Weitz; Bert Wachsmuth; Danielle Mirliss

2006-01-01

388

Granular disintegration of marble in nature: A thermal-mechanical origin for a grus and corestone landscape  

Microsoft Academic Search

Here we document for the first time in detail a natural landscape dominated by granular disintegration of marble and the associated production of marble grus sediment and corestones. We provide several lines of evidence for a thermal-mechanical origin for the observed granular disintegration and resulting corestones. In the San Bernardino Mountains of southern California, calcite marble outcrops whose average grain

Martha Cary Eppes; David Griffing

2010-01-01

389

Comparative bioavailability and tolerability of a single 20-mg dose of two fluoxetine hydrochloride dispersible tablet formulations in fasting, healthy Chinese male volunteers: An open-label, randomized-sequence, two-period crossover study  

Microsoft Academic Search

Background: The proprietary formulation of fluoxetine hydrochloride is an antidepressant of the selective serotonin reuptake inhibitor class. Pharmacokinetic studies investigating the bioequivalence of generic and branded formulations are needed to market generic fluoxetine in China.Objective: The aim of this study was to compare the bioavailability and tolerability of the proposed generic formulation with the established reference formulation of fluoxetine hydrochloride

Shaojun Shi; Yani Liu; Jianhong Wu; Zhongfang Li; Yan Zhao; Dafang Zhong; Fandian Zeng

2010-01-01

390

Spectrophotometric Estimation of Azithromycin in Tablets  

PubMed Central

The present manuscript describes a simple, sensitive, accurate, precise and economical visible spectrophotometric method for the estimation of azithromycin from tablet formulation. The method is based on the reduction of potassium permanganate in alkaline medium with azithromycin. The measurement of decrease in absorbance of potassium permanganate at 547 nm was done, as it decolourises upon reduction by azithromycin. The method was used to determine between 2 and 20 ?g/ml of azithromycin in the final measured solution. There is no interference from the ingredients commonly found in azithromycin tablets with this method. The results for the determination of azithromycin in tablets were in good agreement with the labelled quantities and related analytical parameters are calculated.

Jayanna, B. K.; Nagendrappa, G.; Arunkumar; Gowda, N.

2012-01-01

391

Mapped Submarine Landforms in Pine Island Bay, West Antarctica, Indicate Past Ice Shelf Disintegration and Grounding line Retreat  

NASA Astrophysics Data System (ADS)

Swath bathymetry images from the inner part of Pine Island Bay reveal a well-organized subglacial drainage system carved into bedrock and the termination of a cross-shelf trough has been mapped on the outer shelf. The middle part of Pine Island Bay has, however, only been sparsely mapped due to persistent sea ice cover in the area. During the 2009/2010 austral summer the bay was virtually ice free, allowing detailed swath bathymetry mapping with the Swedish Icebreaker Oden covering 4,140 km2 of the middle part of the trough. When the ice sheet was grounded in Pine Island Trough (PIT), several common glacigenic landforms were produced including mega-scale glacial lineations (MSGL), indicating paleo-ice stream flow direction, and grounding line wedges marking the location where the ice stream's grounding line remained for a longer period. In addition, the multibeam data reveal two other landforms previously not described from this setting. The first of these are ridges oriented transverse the ice flow direction. They are on the order of 1-2 m from trough-to-peak and separated by about 60-200 m. They extend virtually across the entire width of PIT, but individual sets are separated by lineations that are spaced 50 to 500 m apart. The second feature comprises sediment mounds that terminate linear to curvilinear sets of ridges and furrows that are aligned parallel to the axis of the trough, similar to MSGL. These two feature sets are interpreted to indicate the disintegration of a former ice shelf in Pine Island Bay that extended from the paleo-ice stream in the PIT. The ridges mapped in PIT are referred to as “fishbone moraines” and the proposed formation model is that a former ice shelf in Pine Island Bay disintegrated, similarly as happened with Larsen A and B ice shelves, back to the grounding line where it breaks off, tilts landward and begins to drift seaward. With each tidal cycle the ice shelf remnant was lifted, moved seaward and then settling, squeezing sediment out to form a small ridge just behind the grounded edge of the ice shelf. The armada of icebergs from the disintegrated ice shelf moves seaward and ground in the outer trough, where they form sediment mounds, referred to as “plough moraines”. To test the fishbone moraine formation model, we examined the possible influence of spring/neap versus diurnal tides in regulating iceberg movement by comparing a tidal model with ridge spacing and height. Consistent with the tidal model, quasi-periodic fluctuations in ridge heights are observed, assuming fishbone ridges are formed daily, with higher ridges forming roughly every two weeks.

Jakobsson, M.; Anderson, J. B.; Nitsche, F. O.; Dowdeswell, J. A.; Gyllencreutz, R.; Kirchner, N.; O'Regan, M. A.; Alley, R. B.; Anandakrishnan, S.; Mohammad, R.; Eriksson, B.; Fernandez-Vasquez, R. A.; Kirshner, A. E.; Minzoni, R. L.; Stolldorf, T. D.; Majewski, W.

2010-12-01

392

Hypocitraturia despite potassium citrate tablet supplementation.  

PubMed

Citrate supplementation is widely used in the prevention of recurrent nephrolithiasis with hypocitraturia. Potassium citrate is the most commonly used citrate agent for this indication. In patients with chronic diarrheal syndromes, the absorption of potassium citrate can be affected. We describe a patient who presented with recurrent nephrolithiasis and chronic diarrhea and was found to have severe hypocitraturia despite citrate supplementation with potassium citrate tablets, likely due to inadequate gastrointestinal absorption of citrate from the slow-release wax-matrix tablets. PMID:17406150

Shenoy, Chetan

2006-07-13

393

Dabrowski without the Theory of Positive Disintegration Just Isn't Dabrowski  

ERIC Educational Resources Information Center

Dabrowski's theory of positive disintegration (K. Dabrowski, 1964, 1967, 1970, 1972, 1973) has been the subject of a number of research projects in the gifted field over the past 20 or so years. Most of this research has focused on Dabrowski's idea of overexcitability and has not discussed the broader context or implications of his theory or…

Tillier, William

2009-01-01

394

Brief Report: Childhood Disintegrative Disorder--A Brief Examination of Eight Case Studies  

ERIC Educational Resources Information Center

|Childhood disintegrative disorder (CDD) is a rare condition characterized by distinct regression of developmental and behavioral functioning following a period of apparently normal development for at least 2 years. The purpose of this article is to present the developmental, behavioral, psychosocial, and medical histories of eight children who…

Homan, Kendra J.; Mellon, Michael W.; Houlihan, Daniel; Katusic, Maja Z.

2011-01-01

395

Ultrasonic treatment of biological sludge: Floc disintegration, cell lysis and inactivation  

Microsoft Academic Search

The aim of this work was to study the effect of ultra sound treatment on the solid content of sludge and biological activity, and the increase in the soluble chemical oxygen demand (SCOD), proteins and nucleic acids concentrations during sonication. The results showed that sonication effectively degraded and inactivated the sludge. The sludge disintegration and cell lysis occurred continuously while

Panyue Zhang; Guangming Zhang; Wei Wang

2007-01-01

396

Adult Education and (Dis)integration Processes in Yugoslavia. Uppsala Reports on Education 22.  

ERIC Educational Resources Information Center

|This report is a synopsis of a study that dealt with the dominant problem in Yugoslavian society, namely the phenomenon of social and economic crisis, and with the role of adult education within the disintegration processes. In addition to an introduction, the report consists of five sections concerning the following issues: (1) the country in a…

Bron, Michal, Jr.

397

Anomalous Distribution of Nuclear Disintegration in Photographic Emulsions Exposed to Cosmic Rays: Double Stars  

Microsoft Academic Search

IN making systematic exploration of 640 cm.2 of Ilford plates of 100µ thickness exposed vertically to cosmic rays for three to six weeks at a height of 3,600 m., we have observed 2,250 nuclear disintegrations and have noticed an anomaly in their distribution.

L. Leprince-Ringuet; J. Heidmann

1948-01-01

398

Knowledge DisIntegration: A neglected process in the Organizational Knowledge Debate?  

Microsoft Academic Search

Abstract This paper introduces a fresh ,perspective to ,the current Knowledge ,Management debate by exploring ,Knowledge ,Integration and ,Dis-integration practices. These issues are relatively under-researched in ,studies of organisational knowledge ,even though,issues of integration ,seem ,to underpin ,most of the ,knowledge ,processes

Elena P. Antonacopoulou; Stephanie Geary; Efrosyni Konstantinou

2008-01-01

399

Imaging of odor perception delineates functional disintegration of the limbic circuits in mesial temporal lobe epilepsy  

Microsoft Academic Search

Metabolic and neuro-receptor abnormalities within the extrafocal limbic circuits are established in mesial temporal lobe epilepsy (MTLE). However, very little is known about how these circuits process external stimuli. We tested whether odor activation can help delineate limbic functional disintegration in MTLE, and measured cerebral blood flow with PET during birhinal smelling of familiar and unfamiliar odors, using smelling of

Carolina Ciumas; Per Lindström; Bernard Aoun; Ivanka Savic

2008-01-01

400

The role of East Timor's security institutions in national integration – and disintegration  

Microsoft Academic Search

This article examines the interplay between security sector developments and national unity in East Timor since the Indonesian occupation ended in 1999. Particular attention is paid to the regional distinction between Loromonu and Lorosae – people from the west and east of East Timor, respectively. In 2006, East Timor experienced a crisis that saw the disintegration of the military and

Sven Gunnar Simonsen

2009-01-01