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1

Formulation and evaluation of floating matrix tablet of stavudine  

PubMed Central

Background/Aim: The purpose of the study was to prolong the gastric residence time of stavudine by designing its floating tablets and to study the influence of different polymers on its release rate. Materials and Methods: The floating mix matrix tablets of stavudine were prepared by melt granulation method. Beeswax was used as hydrophobic meltable material. Hydroxypropyl methylcellulose (HPMC), sodium bicarbonate, and ethyl cellulose were used as matrixing agent, gas generating agent, and floating enhancer, respectively. The prepared tablets were evaluated for physicochemical parameters such as hardness, weight variation, friability, floating properties (floating lag time, total floating time), drug content, stability study, and in vitro drug release. The drug- polymer interaction was studied by Differential Scanning Calorimetry (DSC) thermal analysis and Fourier transform infared (FT-IR). Results: The floating lag time of all the formulations was within the prescribed limit (<3 min). All the formulations showed good matrix integrity and retarded the release of drug for 12 h except the formulation F5.The concentration of beeswax (X1), HPMC K4M (X2), and ethyl cellulose (X3) were selected as independent variables and drug release values at 1 (Q1), at 6 (Q6) and at 12 h (Q12) as dependent variables. Formulation F7 was selected as an optimum formulation as it showed more similarity in dissolution profile with theoretical profile (similarity factor, f2 = 70.91). The dissolution of batch F7 can be described by zero-order kinetics (R2 =0.9936) with anomalous (non-Fickian) diffusion as the release mechanism (n=0.545). There was no difference observed in release profile after temperature sensitivity study at 40°C/75% relative humidity (RH) for 1 month. Conclusion: It can be concluded from this study that the combined mix matrix system containing hydrophobic and hydrophilic polymer minimized the burst release of drug from the tablet and achieved a drug release by zero-order kinetics, which is practically difficult with only hydrophilic matrix. PMID:23119237

Prajapati, Pankaj H; Nakum, Vijay V; Patel, Chhagan N

2012-01-01

2

Studies on Formulation and In Vitro Evaluation of Floating Matrix Tablets of Domperidone  

PubMed Central

Floating matrix tablets of domperidone were developed to prolong gastric residence time and thereby increased drug bioavailability. Domperidone was chosen as a model drug because it is poorly absorbed from the lower gastrointestinal tract. The tablets were prepared by wet granulation technique, using polymers such as hydroxypropylmethylcellulose K4M, carbopol 934P, and sodium alginate, either alone or in combination, and other standard excipients. Tablets were evaluated for physical characteristics viz. hardness, % friability, floating capacity, weight variation and content uniformity. Further, tablets were evaluated for in vitro release characteristics for 24 h. In vitro release mechanism was evaluated by linear regression analysis. Floating matrix tablets based on combination of three polymers namely; hydroxypropylmethylcellulose K4M, carbopol 934P and sodium alginate exhibited desired floating and prolonged drug release for 24 h. Carbopol loading showed negative effect on floating properties but were found helpful to control the release rate of drug. PMID:20177450

Prajapati, S. T.; Patel, L. D.; Patel, D. M.

2009-01-01

3

Effect of bioadhesion on initial in vitro buoyancy of effervescent floating matrix tablets of ciprofloxacin HCL  

PubMed Central

The purpose of this study was to investigate effect of bioadhesion on the initial in vitro buoyancy behaviour of effervescent matrix tablets of ciprofloxacin HCl (CIPRO). Tablets were prepared by direct compression using HPMC K4M and Carbopol 971P as hydrophilic-controlled release polymers, sodium bicarbonate (NaHCO3) as gas-generating agent, polyplasdone XL, Explotab and Ac-Di-Sol as swelling agents. Tablets were evaluated for normal and modified initial in vitro floating behavior, floating duration, swelling behavior and in vitro drug release studies. A modified buoyancy lag time for tablets was determined in order to include the effect of bioadhesion on initial buoyancy. The initial buoyancy was found depended on bioadhesion ability of tablets. The lowest modified buoyancy lag time of 20 seconds was obtained for Formulation F7 having both NaHCO3 and polyplasdone XL. The floating duration was also found dependent on concentration of NaHCO3 and swelling agents. The drug release of F7 was also sustained up to 12-hr duration with anomalous drug transport mechanism. PMID:22171304

Negi, Jeetendra Singh; Trivedi, Abhinav; Khanduri, Praveen; Negi, Vandana; Kasliwal, Nikhil

2011-01-01

4

Effect of bioadhesion on initial in vitro buoyancy of effervescent floating matrix tablets of ciprofloxacin HCL.  

PubMed

The purpose of this study was to investigate effect of bioadhesion on the initial in vitro buoyancy behaviour of effervescent matrix tablets of ciprofloxacin HCl (CIPRO). Tablets were prepared by direct compression using HPMC K4M and Carbopol 971P as hydrophilic-controlled release polymers, sodium bicarbonate (NaHCO(3)) as gas-generating agent, polyplasdone XL, Explotab and Ac-Di-Sol as swelling agents. Tablets were evaluated for normal and modified initial in vitro floating behavior, floating duration, swelling behavior and in vitro drug release studies. A modified buoyancy lag time for tablets was determined in order to include the effect of bioadhesion on initial buoyancy. The initial buoyancy was found depended on bioadhesion ability of tablets. The lowest modified buoyancy lag time of 20 seconds was obtained for Formulation F7 having both NaHCO(3) and polyplasdone XL. The floating duration was also found dependent on concentration of NaHCO(3) and swelling agents. The drug release of F7 was also sustained up to 12-hr duration with anomalous drug transport mechanism. PMID:22171304

Negi, Jeetendra Singh; Trivedi, Abhinav; Khanduri, Praveen; Negi, Vandana; Kasliwal, Nikhil

2011-04-01

5

Lornoxicam gastro retentive floating matrix tablets: Design and in vitro evaluation.  

PubMed

The objective of this present investigation is to prolong the gastric residence time of Lornoxicam by fabricating it into a floating sustained release matrix tablets. Lornoxicam, a potent oxicam group of non-steroidal anti-inflammatory drugs, suffers from relatively short half life of 2 to 3 hrs showing maximal absorption in proximal gastro intestinal tract region necessitating its need to be formulated as a floating sustained release matrix tablets. In this current investigation, hydroxyl propyl methyl cellulose K15M, a high viscous grade polymer with apparent viscosity of 15,000 cps, was kept as a variable (10-50%) and calcium carbonate (13%) was used as a gas generator. The prepared blends were subjected for its pre-formulation characterization. The directly compressed tablets were evaluated for physical parameters such as weight uniformity, hardness, friability, drug content, in-vitro buoyancy with axial and radial enlargement measurement, swelling index. From the investigation it was observed that the buoyancy lasted for up to 24 hrs. Fourier transform infra-red spectroscopy peaks assured the compatibility of the drug with excipients and confirmed the presence of pure drug in the formulation. It was supported by in-vitro dissolution studies; and the dissolution data was subjected to various release kinetic models to understand the mechanism of drug release. PMID:22171312

Sathiyaraj, S; Devi, Ramya D; Hari, Vedha B N

2011-07-01

6

Lornoxicam gastro retentive floating matrix tablets: Design and in vitro evaluation  

PubMed Central

The objective of this present investigation is to prolong the gastric residence time of Lornoxicam by fabricating it into a floating sustained release matrix tablets. Lornoxicam, a potent oxicam group of non-steroidal anti-inflammatory drugs, suffers from relatively short half life of 2 to 3 hrs showing maximal absorption in proximal gastro intestinal tract region necessitating its need to be formulated as a floating sustained release matrix tablets. In this current investigation, hydroxyl propyl methyl cellulose K15M, a high viscous grade polymer with apparent viscosity of 15,000 cps, was kept as a variable (10-50%) and calcium carbonate (13%) was used as a gas generator. The prepared blends were subjected for its pre-formulation characterization. The directly compressed tablets were evaluated for physical parameters such as weight uniformity, hardness, friability, drug content, in-vitro buoyancy with axial and radial enlargement measurement, swelling index. From the investigation it was observed that the buoyancy lasted for up to 24 hrs. Fourier transform infra-red spectroscopy peaks assured the compatibility of the drug with excipients and confirmed the presence of pure drug in the formulation. It was supported by in-vitro dissolution studies; and the dissolution data was subjected to various release kinetic models to understand the mechanism of drug release. PMID:22171312

Sathiyaraj, S.; Devi, Ramya D.; Hari, Vedha B. N.

2011-01-01

7

Floating Matrix Tablets of Domperidone Formulation and Optimization Using Simplex Lattice Design  

PubMed Central

The purpose of this research was to prepare a floating matrix tablet containing domperidone as a model drug. Polyethylene oxide (PEO) and hydroxypropyl methylcellulose (HPMC) were evaluated for matrix-forming properties. A simplex lattice design was applied to systemically optimize the drug release profile. The amounts of PEO WSR 303, HPMC K15M and sodium bicarbonate were selected as independent variables and floating lag time, time required to release 50% of drug (t50) and 80% of drug (t80), diffusion coefficient (n) and release rate (k) as dependent variables. The amount of PEO and HPMC both had significant influence on the dependent variables. It was found that the content of PEO had dominating role as drug release controlling factor, but using suitable concentration of sodium bicarbonate, one can tailor the desired drug release from hydrophilic matrixes. The linear regression analysis and model fitting showed that all these formulations followed Korsmeyer and Peppas model, which had a higher value of correlation coefficient (r). The tablets of promising formulation were found to be stable for 3 months under accelerated (40°C / 75% RH) stability testing. PMID:24250376

Prajapati, Shailesh; Patel, Laxmanbhai; Patel, Chhaganbhai

2011-01-01

8

Preparation and evaluation of novel metronidazole sustained release and floating matrix tablets.  

PubMed

In the present study, metronidazole was used for preparing floating dosage forms that are designed to retain in the stomach for a long time and have developed as a drug delivery system for better eradication of Helicobacter Pylori in peptic ulcer diseases. For this means, various formulations were designed using multi-factorial design. HPMC, psyllium and carbopol in different concentrations were used as floating agents, and sodium bicarbonate was added as a gas-forming agent. Hardness, friability, drug loading, floating ability and release profiles as well as kinetics of release were assessed. Formulations containing HPMC as filler showed prolonged lag times for buoyancy. Adding psyllium to these formulations had reduced relative lag times. Overall, selected formulations were able to float immediately and showed buoyancy for at least 8?h. Meanwhile, sustained profiles of drug release were also obtained. Kinetically, among the 10 assessed models, the release pattern of metronidazole from the tablets fitted best to Power law, Weibull and Higuchi models in respect overall to mean percentage error values of 3.8, 4.73 and 5.77, respectively, for calcium carbonate-based tablets and, 2.95, 6.39 and 3.9, respectively, for calcium silicate-based tablets. In general, these systems can float in the gastric condition and control the drug release from the tablets. PMID:20429828

Asnaashari, Solmaz; Khoei, Nazaninossadat Seyed; Zarrintan, Mohammad Hosein; Adibkia, Khosro; Javadzadeh, Yousef

2011-08-01

9

Gastric floating matrix tablets: design and optimization using combination of polymers.  

PubMed

The purpose of the present study was to develop an optimized gastric floating drug delivery system (GFDDS) containing domperidone as a model drug. Box-Behnken design was employed in formulating the GFDDS with three polymers: hydroxypropyl methylcellulose K4M (HPMC K4M) (X1), Carbopol 934P (X2) and sodium alginate (X3), as independent variables. Floating lag time (FLT), total floating time (TFT), time required to release 50% of the drug (t50) and diffusion exponent (n) were selected as dependent variables. Seventeen formulations were prepared, dissolution data obtained was fitted to the power law and floating profiles were analyzed. HPMC loading was found to be significant for floating properties. Carbopol loading had a negative effect on floating properties but was found helpful in controlling the release rate of the drug. No significant effect of sodium alginate on floating properties was observed but it was important for gel formation. The quadratic mathematical model developed could be used to predict formulations with desired release and floating properties. PMID:18515232

Prajapati, Shailesh T; Patel, Laxmanbhai D; Patel, Dasharath M

2008-06-01

10

Preparation and evaluation of gastroretentive floating tablets of acyclovir.  

PubMed

The present study performed by preparation and evaluation of floating tablets of Acyclovir as model drug for prolongation of gastric residence time. Floating effervescent tablets were formulated by various materials like hydroxypropyl methylcellulose K 4M, K 15M, psyllium husk, swelling agent as crospovidone and microcrystalline cellulose and gas generating agent like sodium bicarbonate and citric acid and evaluated for floating properties, swelling characteristics and in vitro drug release studies. Floating noneffervescent tablets were prepared by polypropylene foam powder and different matrix forming polymers like HPMC K 4M, Carbopol 934P, xanthan gum and sodium alginate. In vitro drug release studies were performed and drug release kinetics evaluated using the linear regression method was found to follow both the Higuchi and the Korsmeyer and Peppas equation. The drug release mechanism was found fickian type in most of the formulations. PMID:19751200

Garg, Rajeev; Gupta, G D

2009-10-01

11

Preparation and evaluation of gastroretentive floating tablets of Silymarin.  

PubMed

The present study performed by preparation and evaluation of floating tablets of Silymarin as model drug for prolongation of gastric residence time. Floating effervescent tablets were formulated by various materials like hydroxypropyl methylcellulose (HPMC) K 4M, K 15M, psyllium husk, swelling agent as crospovidone and microcrystalline cellulose and gas generating agent like sodium bicarbonate and citric acid and evaluated for floating properties, swelling characteristics and in vitro drug release studies. Floating noneffervescent tablets were prepared by polypropylene foam powder and different matrix forming polymers like HPMC K 4M, Carbopol 934P, xanthan gum and sodium alginate. In vitro drug release studies were performed and drug release kinetics evaluated using the linear regression method was found to follow both the Higuchi and the Korsemeyer and Peppas equation. The drug release mechanism was found fickian type in most of the formulations. The developed floating tablets of Silymarin may be used in clinic for prolonged drug release for at least 24 h, thereby improving the bioavailability and patient compliance. PMID:19483331

Garg, Rajeev; Gupta, Ghanshyam Das

2009-06-01

12

Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride.  

PubMed

Tizanidine hydrochloride is an orally administered prokinetic agent that facilitates or restores motility through-out the length of the gastrointestinal tract. The objective of the present investigation was to develop effervescent floating matrix tablets of tizanidine hydrochloride for prolongation of gastric residence time in order to overcome its low bioavailability (34-40 %) and short biological half life (4.2 h). Tablets were prepared by the direct compression method, using different viscosity grades of hydroxypropyl methylcellulose (HPMC K4M, K15M and K100M). Tablets were evaluated for various physical parameters and floating properties. Further, tablets were studied for in vitro drug release characteristics in 12 hours. Drug release from effervescent floating matrix tablets was sustained over 12 h with buoyant properties. DSC study revealed that there is no drug excipient interaction. Based on the release kinetics, all formulations best fitted the Higuchi, first-order model and non-Fickian as the mechanism of drug release. Optimized formulation (F9) was selected based on the similarity factor (f2) (74.2), dissolution efficiency at 2, 6 and 8 h, and t50 (5.4 h) and was used in radiographic studies by incorporating BaSO4. In vivo X-ray studies in human volunteers showed that the mean gastric residence time was 6.2 ± 0.2 h. PMID:21684848

Someshwar, Komuravelly; Chithaluru, Kalyani; Ramarao, Tadikonda; Kumar, K K Kalyan

2011-06-01

13

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

2010-09-01

14

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

2013-08-16

15

Formulation and evaluation of non-effervescent floating tablets of losartan potassium.  

PubMed

The aim of the work is to modify the solubility and bioavailability of Losartan potassium, by employing noneffervescent floating drug delivery (tablet dosage forms). Non-effervescent systems are a type of floating drug delivery systems, that have been used to boost the gastric residence and the floatation time in the gastro intestinal tract. The study included formulation of floating tablets using polymers like Chitosan and Karaya gum as matrix forming agents. Accurel(®) MP 1000 was used as floating agent. The tablets were prepared by direct compression technique. FTIR, DSC studies conformed that there was no incompatibility between the polymer and the drug. Tablet preformulation parameters were within the Pharmacopoeial limit. Tablet showed zero lag time, contisnuance of buoyancy for >12 h. The tablet showed good in vitro release. Drug release was through swelling and abided by the gellation mechanism. In vivo X-ray studies depicted that tablets continued to float in the GIT for 12 h. Accelerated stability showed that, tablets were stable for over 6 month. Thus the prepared non-effervescent floating tablet of Losartan potassium can be used for the treatment of hypertension for more than 12 h with single dose administration. PMID:23286884

Getyala, Anil; Gangadharappa, H V; Prasad, M Sarat Chandra; Reddy, M Praveen Kumar; Kumar, T M Pramod

2013-10-01

16

Controlled-release effervescent floating matrix tablets of ciprofloxacin hydrochloride: Development, optimization and in vitro–in vivo evaluation in healthy human volunteers  

Microsoft Academic Search

Ciprofloxacin hydrochloride has a short elimination half-life, a narrow absorption window and is mainly absorbed in proximal areas of GIT. The purpose of this study was to develop a gastroretentive controlled-release drug delivery system with swelling, floating, and adhesive properties. Ten tablet formulations were designed using hydroxypropylmethylcellulose (HPMC K15M) and\\/or sodium alginate (Na alginate) as release-retarding polymer(s) and sodium bicarbonate

Mina Ibrahim Tadros

2010-01-01

17

Controlled-release effervescent floating matrix tablets of ciprofloxacin hydrochloride: development, optimization and in vitro-in vivo evaluation in healthy human volunteers.  

PubMed

Ciprofloxacin hydrochloride has a short elimination half-life, a narrow absorption window and is mainly absorbed in proximal areas of GIT. The purpose of this study was to develop a gastroretentive controlled-release drug delivery system with swelling, floating, and adhesive properties. Ten tablet formulations were designed using hydroxypropylmethylcellulose (HPMC K15M) and/or sodium alginate (Na alginate) as release-retarding polymer(s) and sodium bicarbonate (NaHCO(3)) or calcium carbonate (CaCO(3)) as a gas former. Swelling ability, floating behaviour, adhesion period and drug release studies were conducted in 0.1 N HCl (pH 1.2) at 37+/-0.5 degrees C. The tablets showed acceptable physicochemical properties. Drug release profiles of all formulae followed non-Fickian diffusion. Statistical analyses of data revealed that tablets containing HPMC K15M (21.42%, w/w), Na alginate (7.14%, w/w) and NaHCO(3) (20%, w/w) (formula F7) or CaCO(3) (20%, w/w) (formula F10) were promising systems exhibiting excellent floating properties, extended adhesion periods and sustained drug release characteristics. Both formulae were stored at 40 degrees C/75% RH for 3months according to ICH guidelines. Formula F10 showed better physical stability. Abdominal X-ray imaging of formula F10, loaded with barium sulfate, in six healthy volunteers revealed a mean gastric retention period of 5.50+/-0.77h. PMID:19932750

Tadros, Mina Ibrahim

2010-02-01

18

Formulation and evaluation of multiple tablets as a biphasic gastroretentive floating drug delivery system for fenoverine.  

PubMed

A biphasic gastroretentive drug delivery system of fenoverine was developed to maintain constant plasma concentration. The delivery system consisted of a loading-dose tablet and a floating multiple matrix tablet prepared by the direct compression process. The drug release from biphasic GRDDS in 0.1 mol L(-1) HCl and SGF (enzyme free) was sustained over 12 h with buoyant properties. Stability studies showed no significant change in dissolution profiles (f2 value > 50). Based on the release kinetics, it can be concluded that the floating multiple matrix tablet containing HPMC was a particularly suitable gastroretentive drug delivery system with a zero-order release profile. PMID:20228043

Bandari, Suresh; Eaga, Chandra Mohan; Thadishetty, Ashok; Yamsani, Madhusudan Rao

2010-03-01

19

Floating hot-melt extruded tablets for gastroretentive controlled drug release system.  

PubMed

The purpose of this study was to investigate the influence of sodium bicarbonate on the physicochemical properties of controlled release hot-melt extruded (HME) tablets containing Eudragit RS PO and/or Eudragit E PO. Acetohydroxamic acid and chlorpheniramine maleate were used as model drugs. Sodium bicarbonate was incorporated into the tablet formulations and the drug release properties and buoyancy in media for HME tablets and directly compressed (DC) tablets were investigated. The HME tablets prepared from the powder blend containing both Eudragit RS PO and sodium bicarbonate exhibited sustained release properties and the tablets floated on the surface of the media for 24 h. The cross-sectional morphology of the HME tablets showed a porous structure since CO(2) gas was generated due to the thermal decomposition of sodium bicarbonate in the softened acrylic polymers at elevated temperature during the extrusion process. In contrast, all DC tablets prepared in this study showed no buoyancy and rapid drug release in the dissolution media. The drug release rate from floating HME tablets was controlled by both the incorporation of Eudragit E PO into the matrix tablet and the diameter of the die used in the extrusion equipment. The drug release profiles and buoyancy of the floating HME tablets were stable when stored at 40 degrees C/75%RH for 3 months. PMID:16959356

Fukuda, Mamoru; Peppas, Nicholas A; McGinity, James W

2006-10-10

20

Effect of formulation parameters on the drug release and floating properties of gastric floating two-layer tablets with acetylsalicylic acid.  

PubMed

Floating dosage forms of acetylsalicylic acid, used for its antithrombotic effect, were developed to prolong gastric residence time and increase bioavailability. In the two-layer tablet formulation, hydroxypropyl methylcellulose (HPMC) of high viscosity and an effervescent mixture of citric acid and sodium bicarbonate formed the floating layer. The release layer contained the drug, direct tableting agent and different types of matrix-forming polymers such as HPMC of low viscosity, sodium carboxymethylcellulose and chitosan. Tablets were prepared using a direct compression technique. The effect of formulation variables on physicochemical and floating properties and the drug release from tablets were investigated. Floating ability was dependent on the amount of effervescent agent and gel-forming polymer of the floating layer. Drug release was prolonged to 8 hours by changing the type and viscosity of the matrix-forming polymer in the drug-loading layer and all formulations showed a diffusion release mechanisms. PMID:21945909

Hasçiçek, Canan; Yüksel-Tilkan, Günseli; Türkmen, Berna; Ozdemir, Nurten

2011-09-01

21

Floating Tablet of Trimetazidine Dihydrochloride: An Approach for Extended Release with Zero-Order Kinetics  

Microsoft Academic Search

Trimetazidine dihydrochloride is an effective anti-anginal agent; however, it is freely soluble in water and suffers from\\u000a a relatively short half-life. To solve this encumbrance, it is a prospective candidate for fabricating trimetazidine extended-release\\u000a formulations. Trimetazidine extended-release floating tablets were prepared using different hydrophilic matrix forming polymers\\u000a including HPMC 4000 cps, carbopol 971P, polycarbophil, and guar gum. The tablets were fabricated

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

2010-01-01

22

Formulation and evaluation of floating tablets of liquorice extract  

PubMed Central

Background: Floating tablets prolong the gastric residence time of drugs, improve bioavailability, and facilitate local drug delivery to the stomach. With this objective, floating tablets containing aqueous extract of liquorice as drug was prepared for the treatment of Helicobacter pylori and gastric ulcers. Methods: The aqueous extract of liquorice was standardized by HPTLC. Tablets containing HPMC K100M (hydrophilic polymer), liquorice extract, sodium bicarbonate (gas generating agent), talc, and magnesium stearate were prepared using direct compression method. The formulations were evaluated for physical parameters like diameter, thickness, hardness, friability, uniformity of weight, drug content, buoyancy time, dissolution, and drug release mechanism. The formulations were optimized on the basis of buoyancy time and in vitro drug release. Results: The diameter of all formulations was in the range 11.166–11.933 mm; thickness was in the range 4.02–4.086 mm. The hardness ranged from 3.1 to 3.5 kg/cm2. All formulations passed the USP requirements for friability and uniformity of weight. The buoyancy time of all tablet formulations was less than 5 min and tablet remained in floating condition throughout the study. All the tablet formulations followed zero-order kinetics and Korsemeyer-Peppas model in drug release. Conclusion: The optimized formulation was found to be F6 which released 98.3% of drug in 8 h in vitro, while the buoyancy time was 3.5 min. Formulations containing psyllium husk, sodium bicarbonate and HPMC K100M in combination can be a promising for gastroretentive drug delivery systems. PMID:21589757

Ram, H. N. Aswatha; Lachake, Prachiti; Kaushik, Ujjwal; Shreedhara, C. S.

2010-01-01

23

Design, development and evaluation of clopidogrel bisulfate floating tablets  

PubMed Central

Objective: The objective of the present work was to formulate and to characterize a floating drug delivery system for clopidogrel bisulphate to improve bioavailability and to minimize the side effects of the drug such as gastric bleeding and drug resistance development. Materials and Methods: Clopidogrel floating tablets were prepared by direct compression technique by the use of three polymers xanthan gum, hydroxypropyl methylcellulose (HPMC) K15M and HPMC K4M in different concentrations (20%, 25% and 30% w/w). Sodium bicarbonate (15% w/w) and microcrystalline cellulose (30% w/w) were used as gas generating agent and diluent respectively. Studies were carried out on floating behavior and influence of type of polymer on drug release rate. All the formulations were subjected to various quality control and in-vitro dissolution studies in 0.1 N hydrochloric acid (1.2 pH) and corresponding dissolution data were fitted to popular release kinetic equations in order to evaluate release mechanisms and kinetics. Results and Discussion: All the clopidogrel floating formulations followed first order kinetics, Higuchi drug release kinetics with diffusion as the dominant mechanism of drug release. As per Korsmeyer-Peppas equation, the release exponent “n” ranged 0.452-0.654 indicating that drug release from all the formulations was by non-Fickian diffusion mechanism. The drug release rate of clopidogrel was found to be affected by the type and concentration of the polymer used in the formulation (P < 0.05). As the concentration of the polymer was increased, the drug release was found to be retarded. Conclusion: Based on the results, clopidogrel floating tablets prepared by employing xanthan gum at concentration 25% w/w (formulation F2) was the best formulation with desired in-vitro floating time and drug dissolution. PMID:24678458

Rao, K. Rama Koteswara; Lakshmi, K. Rajya

2014-01-01

24

Solid dispersions in the development of a nimodipine floating tablet formulation and optimization by artificial neural networks and genetic programming.  

PubMed

The present study investigates the use of nimodipine-polyethylene glycol solid dispersions for the development of effervescent controlled release floating tablet formulations. The physical state of the dispersed nimodipine in the polymer matrix was characterized by differential scanning calorimetry, powder X-ray diffraction, FT-IR spectroscopy and polarized light microscopy, and the mixture proportions of polyethylene glycol (PEG), polyvinyl-pyrrolidone (PVP), hydroxypropylmethylcellulose (HPMC), effervescent agents (EFF) and nimodipine were optimized in relation to drug release (% release at 60 min, and time at which the 90% of the drug was dissolved) and floating properties (tablet's floating strength and duration), employing a 25-run D-optimal mixture design combined with artificial neural networks (ANNs) and genetic programming (GP). It was found that nimodipine exists as mod I microcrystals in the solid dispersions and is stable for at least a three-month period. The tablets showed good floating properties and controlled release profiles, with drug release proceeding via the concomitant operation of swelling and erosion of the polymer matrix. ANNs and GP both proved to be efficient tools in the optimization of the tablet formulation, and the global optimum formulation suggested by the GP equations consisted of PEG=9%, PVP=30%, HPMC=36%, EFF=11%, nimodipine=14%. PMID:20934511

Barmpalexis, Panagiotis; Kachrimanis, Kyriakos; Georgarakis, Emanouil

2011-01-01

25

Design and evaluation of floating multi-layer coated tablets based on gas formation.  

PubMed

Floating multi-layer coated tablets were designed based on gas formation. The system consists of a drug-containing core tablet coated with a protective layer (hydroxypropyl methylcellulose), a gas forming layer (sodium bicarbonate) and a gas-entrapped membrane, respectively. The mechanical properties of acrylic polymers (Eudragit RL 30D, RS 30D, NE 30D) and ethylcellulose were characterized by the puncture test in order to screen a suitable film for the system. Eudragit RL 30D was chosen as a gas-entrapped membrane due to its high flexibility and high water permeability. The obtained tablets enabled to float due to the CO2-gas formation and the gas entrapment by polymeric membrane. The effect of formulation variables on floating properties and drug release was investigated. The floating tablets using direct-compressed cores had shorter time to float and faster drug release than those using wet-granulated cores. The increased amount of a gas forming agent did not affect time to float but increased the drug release from the floating tablets while increasing coating level of gas-entrapped membrane increased time to float and slightly retarded drug release. Good floating properties and sustained drug release were achieved. These floating tablets seem to be a promising gastroretentive drug delivery system. PMID:17967527

Sungthongjeen, Srisagul; Sriamornsak, Pornsak; Puttipipatkhachorn, Satit

2008-05-01

26

Release Mechanisms Behind Polysaccharides-Based Famotidine Controlled Release Matrix Tablets  

Microsoft Academic Search

Polysaccharides, which have been explored to possess gelling properties and a wide margin of safety, were used to formulate\\u000a single-unit floating matrix tablets by a direct compression technique. This work has the aim to allow continuous slow release\\u000a of famotidine above its site of absorption. The floating approach was achieved by the use of the low density polypropylene\\u000a foam powder.

Enas M. Elmowafy; Gehanne A. S. Awad; Samar Mansour; Abd El-Hamid A. El-Shamy

2008-01-01

27

Formulation and evaluation of novel coated floating tablets of bergenin and cetirizine dihydrochloride for gastric delivery.  

PubMed

A novel coated gastric floating drug-delivery system (GFDDS) of bergenin (BN) and cetirizine dihydrochloride (CET) was developed. First, the pharmacodynamic studies were performed and the results revealed that the new compounds of bergenin/cetirizine dihydrochloride had comparative efficacy as commercial products (bergenin/chlorphenamine maleate) but with fewer side effects on central nervous system (CNS). Subsequently, bergenin was formulated as an extended-release core tablet while cetirizine dihydrochloride was incorporated into the gastric coating film for immediate release. The formulation of GFDDS was optimized by CET content uniformity test, in vitro buoyancy and drug release. Herein, the effects of sodium bicarbonate (effervescent), hydroxypropyl methylcellulose (HPMC, matrix polymer) and coating weight gain were investigated respectively. The optimized GFDDS exhibited good floating properties (buoyancy lag time < 2?min; floating duration > 10?h) and satisfactory drug-release profiles (immediate release of CET in 10?min and sustained release of BN for 12?h). In vivo gamma scintigraphy proved that the optimized GFDDS could retain in the stomach with a prolonged gastric retention time (GRT) of 5?h, and the coating layer showed no side effect for gastric retention. The novel coated gastric floating drug-delivery system offers a new approach to enhance BN's absorption at its absorption site and the efficacy of both CET and BN. PMID:22206469

He, Shuang; Li, Feng; Zhou, Dan; Du, Junrong; Huang, Yuan

2012-10-01

28

Formulation and in vitro characterization of ciprofloxacin floating and bioadhesive extended-release tablets.  

PubMed

Ciprofloxacin is mainly absorbed in the proximal areas of the gastrointestinal tract. The purpose of our study was production of floating-bioadhesive tablets to lengthen the stay of drug in its absorption area. Effervescent tablets were made using sodium carboxymethyl cellulose (CMC), hydroxypropyl methylcellulose (HPMC), polyacrylic acid (AA), polymetacrylic acid (MAA), citric acid, and sodium bicarbonate. Tablets with 5% effervescent base had longer lag time than 10%. The type of polymer had no significant effect on the floating lag time. All tablets floated atop the medium for 23-24 hr. Increasing CMC caused higher mucoadhesion than AA (p < 0.05). All formulations showed a Higuchi, non-Fickian release mechanism. Tablets with 10% effervescent base, 80% CMC/20% HPMC, or 80% AA /20% MAA seemed desirable. PMID:16766469

Varshosaz, Jaleh; Tavakoli, N; Roozbahani, F

2006-01-01

29

Development and Evaluation of Gastroretentive Floating Tablets of an Antihypertensive Drug Using Hydrogenated Cottonseed Oil  

PubMed Central

The aim of the present work was to develop a gastroretentive floating tablet of Atenolol and investigate the effects of both hydrophilic and hydrophobic retardant on in vitro release. Atenolol is an antihypertensive drug with an oral bioavailability of only 50% because of its poor absorption from lower gastrointestinal tract. The floating tablets of Atenolol were prepared to increase the gastric retention, to extend the drug release, and to improve the bioavailability of the drug. The floating tablets were formulated using hydrophilic polymers as Hydroxy propyl methyl cellulose (HPMC K4M and HPMC K15M), hydrophobic retardant as a hydrogenated cottonseed oil (HCSO), and sodium bicarbonate as a gas generating agent to reduce floating lag time. The formulated tablets were evaluated for the quality control tests such as weight variation, hardness, friability, swelling index, floating lag time, and total floating time. The in vitro release study of the tablets was performed in 0.1?N HCl as a dissolution media. The results of the present study clearly indicates the promising potential of Atenolol floating system as an alternative to the conventional dosage and other sustained release formulations. The study also revealed the effectiveness of HCSO as retardant in combination with HPMC. PMID:24455312

Pawar, Harshal Ashok; Gharat, Pooja Ramchandra; Dhavale, Rachana Vivek; Joshi, Pooja Rasiklal; Rakshit, Pushpita Pankajkumar

2013-01-01

30

Design and characterization of controlled release gastro-retentive floating tablet of an atypical psychotropic agent  

PubMed Central

The purpose of the present work was to design and evaluate the once daily sustained release matrix type gastro-retentive floating tablet of Quetiapine Fumarate base on hydrophilic matrices of HPMC, sodium CMC and Carbopol. Sodium bicarbonate was incorporated as a gas-generating agent to give buoyancy. In-vitro drug release studies were performed in pH 1.2 buffer using USP type II paddle at 50 rpm. The release rate of drug decreased with increasing polymer proportion of HPMC K15M from 20 to 60 mg. Formulation with desired drug release achieved with combination of sodium CMC and K15M in ratio of 1:3. The drug release mechanism was predominantly found to be Non-Fickian diffusion and Higuchi controlled. PMID:23066221

Ukawala, Ravikumar; Singhvi, Gautam; Jain, Suresh; Shukla, Vipin; Yadav, Nilesh; Sharma, Sohiny

2012-01-01

31

Prolonged intragastric drug delivery mediated by Eudragit® E-carrageenan polyelectrolyte matrix tablets.  

PubMed

Interpolyelectrolyte (IPE) complexation between carrageenan (CG) and Eudragit E (EE) was studied in 0.1 M HCl and was used to develop floating matrix tablets aimed to prolong gastric-residence time and sustain delivery of the loaded drug. The optimum EE/CG IPE complexation weight ratio (0.6) was determined in 0.1 M HCl using apparent viscosity measurements. The IPE complex was characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry. Metronidazole matrix tablets were prepared by direct compression using EE, CG, or hybrid EE/CG with ratio optimal for IPE complexation. Corresponding effervescent tablets were prepared by including Na bicarbonate as an effervescent agent. Tablets were evaluated for in vitro buoyancy and drug release in 0.1 M HCl. Both CG and EE-CG effervescent matrices (1:2 drug to polymer weight ratio, 60 mg Na bicarbonate) achieved fast and prolonged floating with floating lag times less than 30 s and floating duration of more than 10 h. The corresponding EE effervescent matrices showed delayed floating and rapid drug release, and completely dissolved after 3 h of dissolution. CG matrices showed an initial burst drug release (48.3±5.0% at 1 h) followed by slow drug release over 8 h. EE-CG matrices exhibited sustained drug release in almost zero-order manner for 10 h (68.2±6.6%). The dissolution data of these matrices were fitted to different dissolution models. It was found that drug release followed zero-order kinetics and was controlled by the superposition of the diffusion and erosion. PMID:21302009

Bani-Jaber, Ahmad; Al-Aani, Leena; Alkhatib, Hatim; Al-Khalidi, Bashar

2011-03-01

32

Floating matrix dosage form for phenoporlamine hydrochloride based on gas forming agent: in vitro and in vivo evaluation in healthy volunteers.  

PubMed

Phenoporlamine hydrochloride is a novel compound that is used for the treatment of hypertension. The purpose of this study was to develop a sustained release tablet for phenoporlamine hydrochloride because of its short biological half-life. Three floating matrix formulations of phenoporlamine hydrochloride based on gas forming agent were prepared. Hydroxypropyl methylcellulose K4M and Carbopol 971P NF were used in formulating the hydrogel drug delivery system. Incorporation sodium bicarbonate into matrix resulted in the tablet floating over simulated gastric fluid for more than 6h. The dissolution profiles of all tablets showed non-Fickian diffusion in simulated gastric fluid. Moreover, release of the drug from these tablets was pH-dependent. In vivo evaluations of these formulations of phenoporlamine hydrochloride were conducted in six healthy male human volunteers to compare the sustained release tablets with immediate release tablets. Data obtained in these studies demonstrated that the floating matrix tablet containing more Carbopol was capable of sustained delivery of the drug for longer periods with increased bioavailability and the relative bioavailability of formulation (containing 25% Carbopol 971P NF, 8.3% HPMC K4M) showed the best bioequivalency to the reference tablet (the relative bioavailability was 1.11+/-0.19). PMID:16413710

Xu, Xiaoqiang; Sun, Minjie; Zhi, Feng; Hu, Yiqiao

2006-03-01

33

Formulation and Evaluation of Swellable and Floating Gastroretentive Ciprofloxacin Hydrochloride Tablets  

Microsoft Academic Search

Drugs that have narrow absorption window in the gastrointestinal tract (GIT) will have poor absorption. For these drugs, gastroretentive\\u000a drug delivery systems offer the advantage in prolonging the gastric emptying time. Swellable, floating, and sustained release\\u000a tablets are developed by using a combination of hydrophilic polymer (hydroxypropyl methylcellulose), swelling agents (crospovidone,\\u000a sodium starch glycolate, and croscarmelose sodium) and effervescent substance

Ramji Anil Kumar Arza; Chandra Sekhara Rao Gonugunta; Prabhakar Reddy Veerareddy

2009-01-01

34

Formulation and evaluation of swellable and floating gastroretentive ciprofloxacin hydrochloride tablets.  

PubMed

Drugs that have narrow absorption window in the gastrointestinal tract (GIT) will have poor absorption. For these drugs, gastroretentive drug delivery systems offer the advantage in prolonging the gastric emptying time. Swellable, floating, and sustained release tablets are developed by using a combination of hydrophilic polymer (hydroxypropyl methylcellulose), swelling agents (crospovidone, sodium starch glycolate, and croscarmelose sodium) and effervescent substance (sodium bicarbonate). Formulations are evaluated for percentage swelling, in vitro drug release, floating lag time, total duration of floating, and mean residence time (MRT) in the stomach. The drug release of optimized formulation follows the Higuchi kinetic model, and the mechanism is found to be non-Fickian/anomalous according to Krosmeyer-Peppas (n value is 0.68). The similarity factor (f (2)) is found to be 26.17 for the optimized formulation, which the release is not similar to that of marketed produced (CIFRAN OD). In vivo nature of the tablet at different time intervals is observed in the radiographic pictures of the healthy volunteers and MRT in the stomach is found to be 320 +/- 48.99 min (n = 6). A combination of HPMC K100M, crospovidone, and sodium carbonate shows the good swelling, drug release, and floating characters than the CIFRAN OD. PMID:19277869

Arza, Ramji Anil Kumar; Gonugunta, Chandra Sekhara Rao; Veerareddy, Prabhakar Reddy

2009-01-01

35

Prolonged Intragastric Drug Delivery Mediated by Eudragit ® E-Carrageenan Polyelectrolyte Matrix Tablets  

Microsoft Academic Search

Interpolyelectrolyte (IPE) complexation between carrageenan (CG) and Eudragit E (EE) was studied in 0.1 M HCl and was used\\u000a to develop floating matrix tablets aimed to prolong gastric-residence time and sustain delivery of the loaded drug. The optimum\\u000a EE\\/CG IPE complexation weight ratio (0.6) was determined in 0.1 M HCl using apparent viscosity measurements. The IPE complex\\u000a was characterized by Fourier transform

Ahmad Bani-Jaber; Leena Al-Aani; Hatim Alkhatib; Bashar Al-Khalidi

2011-01-01

36

Development, characterization and permeability assessment based on caco-2 monolayers of self-microemulsifying floating tablets of tetrahydrocurcumin.  

PubMed

Novel self-microemulsifying floating tablets were developed to enhance the dissolution and oral absorption of the poorly water-soluble tetrahydrocurcumin (THC). Their physicochemical properties and THC permeability across Caco-2 cell monolayers were assessed. The self-microemulsifying liquid containing THC was adsorbed onto colloidal silicon dioxide, mixed with HPMC, gas-generating agents (sodium bicarbonate and tartaric acid), lactose and silicified-microcrystalline cellulose and transformed into tablets by direct compression. The use of different types/concentrations of HPMC and sodium bicarbonate in tablet formulations had different effects on the floating characteristics and in vitro THC release. The optimum tablet formulation (F2) provided a short floating lag time (?23 s) together with a prolonged buoyancy (>12 h). About 72% of THC was released in 12 h with an emulsion droplet size in aqueous media of 33.9±1.0 nm while that of a self-microemulsifying liquid was 29.9±0.3 nm. The tablet formulation was stable under intermediate and accelerated storage conditions for up to 6 months. The THC released from the self-microemulsifying liquid and tablet formulations provided an approximately three- to fivefold greater permeability across the Caco-2 cell monolayers than the unformulated THC and indicated an enhanced absorption of THC by the formulations. The self-microemulsifying floating tablet could provide a dosage form with the potential to improve the oral bioavailability of THC and other hydrophobic compounds. PMID:23319299

Sermkaew, Namfa; Wiwattanawongsa, Kamonthip; Ketjinda, Wichan; Wiwattanapatapee, Ruedeekorn

2013-03-01

37

In vitro and in vivo sustained-release characteristics of theophylline matrix tablets and novel cluster tablets.  

PubMed

We compared the in vitro/in vivo properties of theophylline between two sustained-release preparations, which are administered once a day. Tablet A is a swelling/disintegration-type matrix tablet consisting of hydrophobic wax granules and hydrophilic polymer granules (cluster tablets). Tablet B is a matrix tablet consisting of hydrophilic polymer granules. We conducted a dissolution test with JPXIV in vitro, and compared the results between the two preparations. Neither pH nor agitation intensity influenced these preparations. After they were immersed in oleic acid, there were no marked changes in the dissolution properties in the dissolution test. After administration of Tablets A and B containing theophylline at 200mg to fasted dogs, we compared plasma level profiles of theophylline. The mean plasma level of theophylline gradually increased to a maximum (7.17microg/mL) 4h after administration of Tablet A. After administration of Tablet B, a similar finding was noted, with a maximum of 6.09microg/mL. Tablet B showed a higher coefficient of variation (CV) for the plasma level at each point. Subsequently, we administered two tablets of preparations A and B containing theophylline at 200mg to healthy volunteers who had not been fasted, and compared plasma level concentration of theophylline. The mean plasma level of theophylline gradually increased to a maximum (6.09microg/mL) 12h after administration of Tablet A, but then decreased, with a half-life of 9.10h. After administration of Tablet B, a similar finding was noted, with a maximum of 7.87microg/mL and a half-life of 7.76h. Tablet A showed a significantly higher plasma concentration 1 and 2h after administration; however, there were no significant differences at other points. The C(max) of Tablet B was significantly higher than that of Tablet A. However, there were no significant differences in other pharmacokinetic parameters between the two preparations. The T(max) of Tablet A was 10-12h after administration, relatively constant. However, that of Tablet B was 10-18h after administration. The CV for T(max) was 9.8% for Tablet A and 22.0% for Tablet B. After administration of Tablet B, the plasma level of theophylline varied at each point. Based on these results, inter-subject variations after administration of Tablet A may be less marked than those after administration of Tablet B. It is concluded that, the cluster tablets A developed in this study showed significantly less inter-subject variation of theophylline plasma levels than the conventional matrix tablets B. PMID:17512147

Hayashi, Tetsuo; Kanbe, Hideyoshi; Okada, Minoru; Kawase, Ichiro; Ikeda, Yasuo; Onuki, Yoichi; Kaneko, Tetsuo; Sonobe, Takashi

2007-08-16

38

Evaluation of roll compaction as a preparation method for hydroxypropyl cellulose-based matrix tablets  

PubMed Central

Roll compaction was applied for the preparation of hydroxypropyl cellulose (HPC)-based sustained-release matrix tablets. Matrix tablets made via roll compaction exhibited higher dosage uniformity and faster drug release than direct-compacted tablets. HPC viscosity grade, roll pressure, and milling speed affected tablet properties significantly. Roll compaction seems to be an adequate granulation method for the preparation of HPC-based matrix tablets due to the simplicity of the process, less handling difficulty from HPC tackiness as well as easier particle size targeting. Selecting the optimum ratio of plastic excipients and the particle size of starting materials can however be critical issues in this method. PMID:21687348

Jeon, Imjak; Gilli, Tiziana; Betz, Gabriele

2011-01-01

39

Application of dynamic neural networks in the modeling of drug release from polyethylene oxide matrix tablets  

Microsoft Academic Search

The main objective of this study was to demonstrate the possible use of dynamic neural networks to model diclofenac sodium release from polyethylene oxide hydrophilic matrix tablets. High and low molecular weight polymers in the range of 0.9–5×106 have been used as matrix forming materials and 12 different formulations were prepared for each polymer. Matrix tablets were made by direct

Jelena Petrovi?; Svetlana Ibri?; Gabriele Betz; Jelena Paroj?i?; Zorica ?uri?

2009-01-01

40

Research paper Pore shape in the sodium chloride matrix of tablets after the addition  

E-print Network

Research paper Pore shape in the sodium chloride matrix of tablets after the addition of starch made of sodium chloride only and tablets made of a mixture of sodium chloride (97.5% v/v) and starch (2 was developed in a research project focusing on tablets made of a binary mixture of sodium chloride and starch

van Vliet, Lucas J.

41

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

PubMed

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

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

2012-05-30

42

Modeling drug release from PVAc/PVP matrix tablets.  

PubMed

Kollidon SR-based matrix tablets containing various amounts of diprophylline were prepared and thoroughly characterized in vitro. This includes drug release measurements in 0.1M HCl and phosphate buffer pH 7.4, monitoring of changes in the tablet's height and diameter, morphology as well as dry mass upon exposure to the release media. Based on these experimental results, a mechanistic realistic mathematical theory is proposed, taking into account the given initial and boundary conditions as well as radial and axial mass transport in cylinders. Importantly, good agreement between theory and experiment was obtained in all cases, indicating that drug diffusion with constant diffusivity is the dominant mass transport mechanism in these systems. Furthermore, the proposed theory was used to quantitatively predict the effects of the initial tablet height and diameter on the resulting drug release patterns. These theoretical predictions were compared with independently measured drug release kinetics. Good agreement was observed in all cases, proving the validity of the mathematical theory and illustrating the latter's practical benefit: The model can help to significantly facilitate the recipe optimization of this type of advanced drug delivery systems in order to achieve a desired release profile. PMID:19737588

Siepmann, F; Eckart, K; Maschke, A; Kolter, K; Siepmann, J

2010-01-25

43

Floating matrix dosage form for dextromethorphan hydrobromide based on gas forming technique: in vitro and in vivo evaluation in healthy volunteers.  

PubMed

The objective of this study was to develop the dextromethorphan hydrobromide sustained-release (DMB-SR) tablets using floating technique to prolong the gastric residence time and compared their pharmacokinetic behavior with conventional sustained release tablets. DMB-SR floating tablets were prepared employing hydroxypropyl methylcellulose (HPMC) as hydrophilic gel material, sodium bicarbonate as gas-generating agent and hexadecanol as floating assistant agent. An orthogonal experiment design method was used to select the optimized formulation. The floating tablets were evaluated for uniformity of weight, hardness, friability, drug content, floating characteristics, in vitro release and in vivo bioavailability. The optimized tablets were prepared with HPMC K4M 25 mg, sodium bicarbonate 20 mg and hexadecanol 18 mg. The prepared tablets could float within 3 min and maintain for more than 24 h. The data of physical parameters were all lie within the limits. Drug release at 12 h was more than 85%. The comparative pharmacokinetic study was performed by administration of the DMB-SR floating tablets and conventional DMB-SR tablets. The area under curve of plasma concentration-time (AUC) of floating tablets was slightly higher than that of reference tablets, T(max) was prolonged apparently. The results showed the floating tablets are a feasible approach for the sustained-release preparation of drugs, which have limited absorption sites in the stomach. PMID:21050887

Hu, Liandong; Li, Li; Yang, Xun; Liu, Wei; Yang, Jianxue; Jia, Yanhong; Shang, Chuang; Xu, Hongxin

2011-01-18

44

Swelling and erosion of pectin matrix tablets and their impact on drug release behavior.  

PubMed

The aim of this study was to investigate swelling and erosion behaviors of hydrophilic matrix tablets using pectin and their impact on drug release. The matrix tablets were prepared by direct compression using different types of pectin. Swelling and erosion studies of pectin matrix tablets were carried out in various media. The pectin matrix tablets formed a continuous gel layer while in contact with the aqueous medium undergoing a combination of swelling and erosion. The swelling action of pectin matrices was controlled by the rate of its hydration in the medium. Release studies showed that the swelling and erosion of matrices influenced the drug release. The extent of matrix swelling, erosion and diffusion of drug determined the kinetics as well as mechanism of drug release from pectin-based matrix tablets. The release data showed a good fit into the power law or the Korsmeyer-Peppas equation indicating the combined effect of diffusion and erosion mechanisms of drug release. PMID:17267193

Sriamornsak, Pornsak; Thirawong, Nartaya; Weerapol, Yossanun; Nunthanid, Jurairat; Sungthongjeen, Srisagul

2007-08-01

45

Thermal sintering: a novel technique used in the design, optimization and biopharmaceutical evaluation of propranolol HCl gastric floating tablets.  

PubMed

The objective of the present investigation was to study the applicability of thermal sintering technique for the development of gastric floating tablets of propranolol HCl. Formulations were prepared using four independent variables, namely (i) polymer quantity, (ii) sodium bicarbonate concentration, (iii) sintering temperature and (iv) sintering time. Floating lag time and t95 were taken as dependent variables. Tablets were prepared by the direct compression method and were evaluated for physicochemical properties, in vitro buoyancy and dissolution studies. From the drug release studies, it was observed that drug retarding property mainly depends upon the sintering temperature and time of exposure. The statistically optimized formulation (PTSso) was characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry studies, and no significant chemical interaction between drug and polymer was observed. Optimized formulation was stable at accelerated conditions for a period of six months. PTSso was evaluated for in vivo buoyancy studies in humans for both fed and fasted states and found that gastric residence time of the floating tablets were enhanced by fed stage but not in fasted state. Optimized formulation PTSso and commercial formulation Ciplar LA 80 were subjected to bioavailability studies in healthy human volunteers by estimating pharmacokinetic parameters such as Cmax, Tmax, area under curve (AUC), elimination rate constant (Kel), biological half-life (t1/2) and mean residence time (MRT). There was a significant increase in the bioavailability of the propranolol HCl from PTSso formulation, which was evident from increased AUC levels and larger MRT values than Ciplar LA 80. PMID:23317339

Venkata Srikanth, Meka; Songa, Ambedkar Sunil; Nali, Sreenivasa Rao; Battu, Janaki Ram; Kolapalli, Venkata Ramana Murthy

2014-01-01

46

Dissolution parameters for sodium diclofenac-containing hypromellose matrix tablet.  

PubMed

Sodium diclofenac (SD) release from dosage forms has been studied under different conditions. However, no dissolution method that is discriminatory enough to reflect slight changes in formulation or manufacturing process, and which could be effectively correlated with the biological properties of the dosage form, has been reported. This study sought to develop three different formulae of SD-containing matrix tablets and to determine the effect of agitation speed in its dissolution profiles. F1, F2 and F3 formulations were developed using hypromellose (10, 20 and 30%, respectively for F1, F2 and F3) and other conventional excipients. Dissolution tests were carried out in phosphate buffer pH 6.8 at 37 degrees C using apparatus II at 50, 75 or 100 rpm. Dissolution efficiency (DE), T(50) and T(90) were determined and plotted as functions of the variables agitation speed and hypromellose concentration. Regarding DE, F2 showed more sensitivity to variations in agitation speed than F1 and F3. Increasing hypromellose concentration reduced DE values, independent of agitation speed. Analysis of T(50) and T(90) suggests that F1 is less sensitive to variations in agitation speed than F2 and F3. Most discriminatory dissolution conditions were observed at 50 rpm. Results suggest that the comparison of dissolution performance of SD matrix tablets should take into account polymer concentration and agitation conditions. PMID:19941944

Mourão, Samanta C; da Silva, Cristiane; Bresolin, Tania M B; Serra, Cristina H R; Porta, Valentina

2010-02-15

47

Thermal sintering: a novel technique in the design of gastroretentive floating tablets of propranolol HCl and its evaluation.  

PubMed

The aim of the present investigation was to formulate thermally sintered floating tablets of propranolol HCl, and to study the effect of sintering conditions on drug release, as well as their in vitro buoyancy properties. A hydrophilic polymer, polyethylene oxide, was selected as a sintered polymer to retard the drug release. The formulations were prepared by a direct compression method and were evaluated by in vitro dissolution studies. The results showed that sintering temperature and time of exposure greatly influenced the buoyancy, as well as the dissolution properties. As the sintering temperature and time of exposure increased, floating lag time was found to be decreased, total floating time was increased and drug release was retarded. An optimized sintered formulation (sintering temperature 50 degrees C and time of exposure 4 h) was selected, based on their drug retarding properties. The optimized formulation was characterized with FTIR and DSC studies and no interaction was found between the drug and the polymer used. PMID:23248967

Meka, Venkata Srikanth; Songa, Ambedkar Sunil; Nali, Sreenivasa Rao; Battu, Janaki Ram; Kukati, Latha; Kolapalli, Venkata Ramana Murthy

2012-09-01

48

Formulation and in vitro evaluation of floating tablets of hydroxypropyl methylcellulose and polyethylene oxide using ranitidine hydrochloride as a model drug.  

PubMed

The present study was carried out with an objective of preparation and in vitro evaluation of floating tablets of hydroxypropyl methyl cellulose (HPMC) and polyethylene oxide (PEO) using ranitidine hydrochloride as a model drug. The floating tablets were based on effervescent approach using sodium bicarbonate a gas generating agent. The tablets were prepared by dry granulation method. The effect of polymers concentration and viscosity grades of HPMC on drug release profile was evaluated. The effect of sodium bicarbonate and stearic acid on drug release profile and floating properties were also investigated. The result of in vitro dissolution study showed that the drug release profile could be sustained by increasing the concentration of HPMC K15MCR and Polyox WSR303. The formulation containing HPMC K15MCR and Polyox WSR303 at the concentration of 13.88% showed 91.2% drug release at the end of 24 hours. Changing the viscosity grade of HPMC from K15MCR to K100MCR had no significant effect on drug release profile. Sodium bicarbonate and stearic acid in combination showed no significant effect on drug release profile. The formulations containing sodium bicarbonate 20 mg per tablet showed desired buoyancy (floating lag time of about 2 minutes and total floating time of >24 hours). The present study shows that polymers like HPMC K15MCR and Polyox WSR303 in combination with sodium bicarbonate as a gas generating agent can be used to develop sustained release floating tablets of ranitidine hydrochloride. PMID:23493037

Gharti, Kp; Thapa, P; Budhathoki, U; Bhargava, A

2012-10-01

49

Formulation and in vitro evaluation of floating tablets of hydroxypropyl methylcellulose and polyethylene oxide using ranitidine hydrochloride as a model drug  

PubMed Central

The present study was carried out with an objective of preparation and in vitro evaluation of floating tablets of hydroxypropyl methyl cellulose (HPMC) and polyethylene oxide (PEO) using ranitidine hydrochloride as a model drug. The floating tablets were based on effervescent approach using sodium bicarbonate a gas generating agent. The tablets were prepared by dry granulation method. The effect of polymers concentration and viscosity grades of HPMC on drug release profile was evaluated. The effect of sodium bicarbonate and stearic acid on drug release profile and floating properties were also investigated. The result of in vitro dissolution study showed that the drug release profile could be sustained by increasing the concentration of HPMC K15MCR and Polyox WSR303. The formulation containing HPMC K15MCR and Polyox WSR303 at the concentration of 13.88% showed 91.2% drug release at the end of 24 hours. Changing the viscosity grade of HPMC from K15MCR to K100MCR had no significant effect on drug release profile. Sodium bicarbonate and stearic acid in combination showed no significant effect on drug release profile. The formulations containing sodium bicarbonate 20 mg per tablet showed desired buoyancy (floating lag time of about 2 minutes and total floating time of >24 hours). The present study shows that polymers like HPMC K15MCR and Polyox WSR303 in combination with sodium bicarbonate as a gas generating agent can be used to develop sustained release floating tablets of ranitidine hydrochloride. PMID:23493037

Gharti, KP; Thapa, P; Budhathoki, U; Bhargava, A

2012-01-01

50

Preparation of Coated Valproic Acid and Sodium Valproate Sustained-release Matrix Tablets.  

PubMed

The aim of this research was to investigate the technique for preparation of coated valproic acid and sodium valproate sustained-release matrix tablets. Different diluents were tested and selected as the effective absorbent for oily valproic acid. Effect of the amount of absorbent and hydroxypropylmethylcellulose on drug release from valproic acid-sodium valproate matrix tablets prepared with wet granulation technique was evaluated in pH change system. Colloidal silicon dioxide effectively adsorbed liquid valproic acid during wet granulation and granule preparation. The amounts of colloidal silicon dioxide and hydroxypropylmethylcellulose employed in tablet formulations affected drug release from the tablets. The drug release was prominently sustained for over 12 h using hydroxypropylmethylcellulose-based hydrophilic matrix system. The mechanism of drug release through the matrix polymer was a diffusion control. The drug release profile of the developed matrix tablet was similar to Depakine Chrono(®), providing the values of similarity factor (f2) and difference factor (f1) of 85.56 and 2.37, respectively. Eudragit(®) L 30 D-55 was used as effective subcoating material for core matrix tablets before over coating with hydroxypropylmethylcellulose film with organic base solvent. Drug release profile of coated matrix tablet was almost similar to that of Depakine Chrono(®). PMID:20838520

Phaechamud, T; Mueannoom, W; Tuntarawongsa, S; Chitrattha, S

2010-03-01

51

Safety, tolerability and pharmacokinetics of phenoprolamine hydrochloride floating sustained-release tablets in healthy Chinese subjects.  

PubMed

The present study was designed to assess the safety, tolerability and pharmacokinetics of phenoprolamine hydrochloride floating sustained tablets (PHFST) in healthy Chinese subjects. 116 volunteers were randomized into single- or multiple-dose groups for oral administration 30-240 mg of PHFST once or 60-120 mg twice daily. Safety and tolerability were appraised by monitoring adverse events and laboratory parameters. Pharmacokinetics was assessed by determining the plasma concentrations of phenoprolamine hydrochloride with a validated HPLC method. In single-dose studies, no severe adverse events were observed in volunteers, and all adverse events were mild; the percentages of treatment-emergent events judged to be possibly related to the drug were 3/6 in the 240 mg dose group, 1/6 in the 180-210 mg dose groups, and none in the 30-150 mg dose groups; system exposure (AUC, C(max)) increased with respect to dose at 30-120 mg, whereas AUC raised disproportionately with dose escalating from 120 to 240 mg; the absorption of phenoprolamine hydrochloride was unaffected by food. In multiple studies, no safety concerns were revealed up to 7 days; steady-state plasma concentration was achieved after approximately 4-5 days of repeated twice-daily dosing. PHFST is safe and well tolerated in healthy Chinese subjects. The mean C(max) of PHFST is proportional to dose, but not the AUC. Oral dosing regimen selected for subsequent Phase II/III clinical trials was 60 mg of PHFST, b.i.d., and dose up to 120 mg, b.i.d. - may be used to achieve better antihypertensive effect. PMID:19446622

Zhao, Libo; Yang, Xiaoyan; Xu, Rong; Wu, Jianhong; Gu, Shifen; Zhang, Li; Gong, Peili; Chen, Hui; Zeng, Fandian

2009-07-30

52

Overall mechanism behind matrix sustained release (SR) tablets prepared with hydroxypropyl methylcellulose 2910  

Microsoft Academic Search

The mechanisms of sustained release (SR) from tablet matrices prepared with hydroxypropyl methylcellulose (HPMC) 2910 polymers were investigated to define the conditions for selection of appropriate polymers for SR formulation development. It is well known that the two important parameters for the release of drug from tablet matrices are the infiltration rate of medium into the matrix, for those drugs

Koichiro Tahara; Ken Yamamoto; Toshiaki Nishihata

1995-01-01

53

Floating elementary osmotic pump tablet (FEOPT) for controlled delivery of diethylcarbamazine citrate: a water-soluble drug.  

PubMed

The present work investigates the feasibility of the design of a novel floating elementary osmotic pump tablet (FEOPT) to prolong the gastric residence of a highly water-soluble drug. Diethylcarbamazine citrate (DEC) was chosen as a model drug. The FEOPT consisted of an osmotic core (DEC, mannitol, and hydrophilic polymers) coated with a semipermeable layer (cellulose acetate) and a gas-generating gelling layer (sodium bicarbonate, hydrophilic polymers) followed by a polymeric film (Eudragit RL 30D). The effect of formulation variables such as concentration of polymers, types of diluent, and coat thickness of semipermeable membrane was evaluated in terms of physical parameters, floating lag time, duration of floatation, and in vitro drug release. The Fourier transform infrared and X-ray diffraction analysis were carried out to study the physicochemical changes in the drug excipients powder blend. The integrity of the orifice and polymeric film layer was confirmed from scanning electron microscopy image. All the developed FEOPT showed floating lag time of less than 8 min and floating duration of 24 h. A zero-order drug release could be attained for DEC. The formulations were found to be stable up to 3 months of stability testing at 40°C/75% relative humidity. PMID:21969244

Khan, Zulfequar Ahamad; Tripathi, Rahul; Mishra, Brahmeshwar

2011-12-01

54

Programmable drug release of highly water-soluble pentoxifylline from dry-coated wax matrix tablets.  

PubMed

The programmable release of pentoxifylline from a dry-coated wax matrix tablet containing behenic acid as wax matrix was investigated at 37 degrees C in Japanese Pharmacopeia XII 1st (pH 1.2) and 2nd (pH 6.8) fluids. The dry-coated tablet consisted of a low drug concentration (33% w/w) in the outer layer tablet and a high concentration (50-67% w/w) in the core. The drug release from the wax matrix significantly increased after penetrating the core; therefore, the drug release profiles showed specific biphasic curves. Because the contact angle of the wax matrix tablet increased with a decrease in the drug concentration, the fluid penetration in wax matrix tablet increased with an increase of the drug concentration. The time required for 75% drug release (T75) decreased with an increasing drug concentration in the core, and the T75 at pH 6.8 was slightly longer than that in pH 1.2. The larger core tablet had a shorter T75, indicating that the drug release rate was controlled by regulating the drug concentration and/or the weight of the core tablet. PMID:7629734

Otsuka, M; Matsuda, Y

1995-04-01

55

Design of pH-independent extended release matrix tablets of minocycline hydrochloride for the treatment of dementia  

Microsoft Academic Search

The aim of this study was to develop a pH-independent extended release matrix tablet of minocycline HCl for the treatment\\u000a of dementia. The matrix tablets were prepared by wet granulation technique using Eudragit L and S as release modifiers at\\u000a different w\\/w ratios (1:0, 1:1 and 0:1) and PEO as a matrix former. In the case of the matrix tablet

Kwang-Ho Cha; Wonkyung Cho; Dong-Geon Gu; Kihyang Jeong; Sung-Joo Hwang

2009-01-01

56

Floating hot-melt extruded tablets for gastroretentive controlled drug release system  

Microsoft Academic Search

The purpose of this study was to investigate the influence of sodium bicarbonate on the physicochemical properties of controlled release hot-melt extruded (HME) tablets containing Eudragit® RS PO and\\/or Eudragit® E PO. Acetohydroxamic acid and chlorpheniramine maleate were used as model drugs. Sodium bicarbonate was incorporated into the tablet formulations and the drug release properties and buoyancy in media for

Mamoru Fukuda; Nicholas A. Peppas; James W. McGinity

2006-01-01

57

Formulation, evaluation and optimization of sustained release matrix tablets of captopril  

PubMed Central

Sustained release matrix tablet is a delivery system by which the drug can be delivered at a controlled rate for long period of time. The present study aims at formulation, evaluation and optimization of captopril matrix tablets. A 32 full factorial design was adopted and all 9 batches were prepared by wet granulation method. Prepared granules and tablets were evaluated for precompression and postcompression characteristics respectively. Check point analysis was applied to the observations and the formula of the tablet was optimized. Optimized formula, F6 showed zero order drug release kinetics for the time period of 24 hours i.e. 17.55% release at the end of 2 hours, 53.4% release at the end of 12 hours and 100.24% release at the end of 24 hours. The results revealed that concentration of matrix forming agent and solution of granulating agent significantly affected in vitro drug release profile. PMID:23066215

Pandya, V. Pandya; Patel, Vandana B.; Patel, Prajesh

2012-01-01

58

In vitro aceclofenac release from IPN matrix tablets composed of chitosan-tamarind seed polysaccharide.  

PubMed

This communication describes the formulation and in vitro evaluation of IPN matrix tablets of aceclofenac. IPN microparticles using chitosan and tamarind seed polysaccharide blend was prepared using glutaraldehyde as cross-linker. The drug entrapment efficiency and average particle size of these microparticles was found to be 91.97±1.30% and 498.12±38.67 ?m, respectively. These IPN microparticles were characterized by scanning electron microscopy (SEM) and powder X-ray diffraction (P-XRD) study. These microparticles were compressed with tablet excipients through direct compression technique. These matrix tablets showed sustained aceclofenac release over 8 h. These matrix tablets might be helpful to minimize dosing frequency and reduction of various side effects during prolong period of treatment. PMID:24463265

Jana, Sougata; Sen, Kalyan Kumar; Basu, Sanat Kumar

2014-04-01

59

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

60

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

PubMed

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

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

2013-08-01

61

Drug release control and system understanding of sucrose esters matrix tablets by artificial neural networks.  

PubMed

Artificial neural networks (ANNs) were applied for system understanding and prediction of drug release properties from direct compacted matrix tablets using sucrose esters (SEs) as matrix-forming agents for controlled release of a highly water soluble drug, metoprolol tartrate. Complexity of the system was presented through the effects of SE concentration and tablet porosity at various hydrophilic-lipophilic balance (HLB) values of SEs ranging from 0 to 16. Both effects contributed to release behaviors especially in the system containing hydrophilic SEs where swelling phenomena occurred. A self-organizing map neural network (SOM) was applied for visualizing interrelation among the variables and multilayer perceptron neural networks (MLPs) were employed to generalize the system and predict the drug release properties based on HLB value and concentration of SEs and tablet properties, i.e., tablet porosity, volume and tensile strength. Accurate prediction was obtained after systematically optimizing network performance based on learning algorithm of MLP. Drug release was mainly attributed to the effects of SEs, tablet volume and tensile strength in multi-dimensional interrelation whereas tablet porosity gave a small impact. Ability of system generalization and accurate prediction of the drug release properties proves the validity of SOM and MLPs for the formulation modeling of direct compacted matrix tablets containing controlled release agents of different material properties. PMID:21878388

Chansanroj, Krisanin; Petrovi?, Jelena; Ibri?, Svetlana; Betz, Gabriele

2011-10-01

62

Evaluation of injection moulding as a pharmaceutical technology to produce matrix tablets  

Microsoft Academic Search

The aim of this study was to develop sustained-release matrix tablets by means of injection moulding and to evaluate the influence of process temperature, matrix composition (EC and HPMC concentration) and viscosity grade of ethylcellulose (EC) and hydroxypropylmethylcellulose (HPMC) on processability and drug release. The drug release data were analyzed to get insight in the release kinetics and mechanism. Formulations

Thomas Quinten; Thomas De Beer; Chris Vervaet; Jean Paul Remon

2009-01-01

63

Evaluation of floating and sticking extended release delivery systems: an unconventional dissolution test  

Microsoft Academic Search

The extent to which hydrophilic matrix tablets with a propensity to stick to the dissolution apparatus and\\/or float are susceptible to variations in hydrodynamic conditions during dissolution testing was investigated. Furthermore the usefulness of simple alternatives to the current compendial tests is examined. Swellable hydrocolloid (guar) matrix tablets containing verapamil HCl were evaluated using USP dissolution apparatus I and II.

Thomas Dürig; Reza Fassihi

2000-01-01

64

Evaluation of diclofenac sodium release from matrix pellets compressed into MUPS tablets.  

PubMed

The purpose of the study was to screen the effects of formulation factors on the in vitro release profile of diclofenac sodium from matrix pellets compressed into multiple unit pellet system (MUPS) tablets using design of experiment (DOE). Extended release of diclofenac sodium was accomplished using Carbopol 71G as matrix substance. According to Fractional Factorial Design FFD 2(3-1) four formulations of diclofenac sodium MUPS matrix tablets were prepared. The process of direct pelletization and subsequently compression of the pellets into tablets was applied in order to investigate a different approach in formulation of matrix systems and to achieve a better control of the process factors over the principal response - the release of the drug. The investigated factors were X1-the percentage of polymer Carbopol 71G, X2-crushing strength of the tablet and X3-different batches of the diclofenac sodium. In vitro dissolution time profiles at 6 different sampling times were chosen as responses. Results of drug release studies indicated that drug release rates vary between different formulations, with a range of 1 to 8 h to complete dissolution. The most important impact on the drug release had factor X1-the percentage of polymer Carbopol 71G. The polymer percentage is suggested as release regulator for diclofenac sodium release from MUPS matrix tablets. All other investigated factors had no significant influence on the release profile of diclofenac sodium. PMID:19881210

Ivi?, Branka; Ibri?, Svetlana; Betz, Gabriele; Djuri?, Zorica

2009-11-01

65

Effect of processing and sintering on controlled release wax matrix tablets of ketorolac tromethamine.  

PubMed

The objective of present study was to evaluate the effect of processing methods and sintering condition on matrix formation and subsequent drug release from wax matrix tablets for controlled release. Ketorolac tromethamine and compritol were processed with appropriate diluent using either dry blending, spray drying, partial melt granulation or melt granulation.The tablets were then sintered at 80 degrees . The sintered tablets were characterized by their physical parameters and in vitro dissolution tests. The micro-morphology and wettability of the tablets was also investigated. It was evident that different processing methods for identical formulation significant impact the release profile of drug. Sintering further retarded drug release and its effect was related to the manufacturing processes. Scanning electron microscopy showed that heat treatment redistributed the wax and formed a film-like structure covering drug and excipient particle. The contact angle of tablets made by dry blending, spray drying and partial melt granulation methods increased after sintering, while that of tablets made by melt granulation remained constant. Drug release from the wax tablets with or without heat treatment was best described by the Higuchi equation. Different processing methods produced different matrix structures that resulted in different drug release rates. Sintering retarded drug release mainly by decreasing the porosity of the matrix. Contact angle measurement and SEM analysis indicated that heat treatment caused the wax to melt, redistribute, coat the drug and diluents and form a network structure. Differential scanning calorimetry studies ruled out the occurrence of solid solution of the drug during sintering condition. PMID:20502573

Rao, Monica R P; Ranpise, Anuradha A; Thanki, K C; Borate, S G; Parikh, G N

2009-09-01

66

Investigation of critical polymer properties for polymer release and swelling of HPMC matrix tablets.  

PubMed

Four different HPMC batches were characterized to investigate properties related to critical functionality for their use in hydrophilic matrix tablets. In this study, the HPMC batches were chemically characterized and correlated to the behaviour of pure HPMC tablets. Parameters such as the molecular weight, viscosity, intrinsic viscosity and radius of gyration were kept in a rather limited range, which resulted in a weak correlation to polymer release and degree of swelling. The hydrophilic/hydrophobic character of the HPMC samples was elucidated by the degree of substitution and by the clouding behaviour, where an increased hydrophilicity increased the tablet swelling. This phenomenon was interpreted in a refined model for water transport into HPMC tablets. A five times slower polymer release and a considerably larger degree of swelling were found for one batch of HPMC tablets compared to the others, although the characterized average polymer parameters were in the same range. However, the conformation plot displayed a fraction with compact aggregates. In conclusion, the existence of aggregates in aqueous solution seems to perturb the functionality of HPMC tablets and it seems important to understand and characterize these aggregates to fully predict the polymer release and swelling of HPMC tablets. PMID:19038336

Viridén, Anna; Wittgren, Bengt; Larsson, Anette

2009-02-15

67

[Comparison of the characteristics of several polymer materials used in hydrophilic matrix tablets].  

PubMed

Pure and drug hydrophilic matrix tablets were prepared by direct compression method with theophylline as a model drug. The characteristics of four hydrophilic matrix polymers, hydroxypropylmethylcellulose (HPMC), polyethylene oxide (PEO), sodium alginate (NaAlg) and xanthan gum (XG), were compared by investigating the water absorption, swelling, erosion and gel layer strength. The sequence of water absorption rate was XG > NaAlg (H) > PEO > NaAlg (L) > HPMC; The sequence of swelling index was XG > PEO > HPMC > NaAlg; The sequence of erosion rate was NaAlg (L) > NaAlg (H) > PEO80 > PEO200 > PEO300 > XG approximately PEO400 approximately K4M > K15M > PEO600 approximately K100M; The sequence of the gel layer strength was PEO > HPMC > XG > NaAlg. For the PEO and HPMC matrix tablets, with the polymer molecular weight increased, the drug release mechanism was gradually transferred from mainly depending on the erosion to the diffusion; for SAL matrix tablets, the drug release mainly depends on erosion mechanism; and for XG matrix tablets, the drug release mainly depends on non-Fick diffusion mechanism. Comparison of the performance difference between the polymer materials will contribute to rational design and prediction of drug release behaviors from matrix tables and ultimately to achieve clinical needs. PMID:21626791

Nie, Shu-Fang; Liu, Hui; Liu, Yan-Li; Pan, Wei-San

2011-03-01

68

Sustained release dosage forms dissolution behavior prediction: a study of matrix tablets using NIR spectroscopy.  

PubMed

The objective of this study was to predict dissolution behavior of sustained release theophylline matrix tablets using near infrared (NIR) diffuse reflectance spectroscopy and multivariate calibration models. Eudragit NE 30D was used as a granulation binder to prepare theophylline sustained release tablets. A total of 117 tablets from 5 batches containing different proportions of Eudragit NE 30D were scanned using a NIR spectrometer. The release characteristics of the tablets were investigated in the acetate buffer for 4 h. The percentage release at 1, 2, 3 and 4 h was used to build the PLS calibration models. The Mahalanobis distance in principal component space and the 2nd derivative transformation were used for sample selection prior to building a four 4-factor partial least square (PLS) calibration models for predicting 1, 2, 3 and 4 h release rates. For PLS(1h), the standard error of calibration (SEC), and standard error of prediction (SEP) were 2.8 and 3.4%. For PLS(2h), the SEC and SEP were 2.7 and 3.5%. For PLS(3h), the SEC and SEP were 2.6 and 3.5% and for PLS(4h), the SEC and SEP were 3.0 and 3.5%, respectively. For the first time, NIR spectroscopy was successfully applied to predict drug release in the matrix tablets by correlating dissolution profile of each batch to its corresponding Eudragit NE 30D variation in tablet composition. PMID:19660535

Tabasi, Simin Hassannejad; Moolchandani, Vikas; Fahmy, Raafat; Hoag, Stephen W

2009-12-01

69

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. PMID:19555310

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

2009-01-01

70

Floating Matrix Dosage Form for Propranolol Hydrochloride Based on Gas Formation Technique: Development and In Vitro Evaluation  

PubMed Central

Gastroretentive tablets of propranolol hydrochloride were developed by direct compression method using citric acid and sodium bicarbonate as the effervescent base. Hydroxypropyl methylcellulose; HPMC K15M was used to prepare the floating tablets to retard the drug release for 12h in stomach. Na-carboxymethyl cellulose (NaCMC) or carbopol 934P was added to alter the drug release profile or the dimensional stability of the formulation. Dicalcium phosphate (DCP) was used as filler. Formulations were evaluated for floating lag time, duration of floating, dimensional stability, drug content and in vitro drug release profile. The formulations were found to have floating lag time less than 1min. It was found that the dimensional stability of the formulations increase with increasing concentration of the swelling agent. The release mechanism of propranolol hydrochloride from floating tablets was evaluated on the basis of Peppas and Higuchi model. The ‘n’ value of the formulations ranged from 0.5201 to 0.7367 (0.5

Chaturvedi, Kiran; Umadevi, S.; Vaghani, Subhash

2010-01-01

71

Floating matrix dosage form for propranolol hydrochloride based on gas formation technique: development and in vitro evaluation.  

PubMed

Gastroretentive tablets of propranolol hydrochloride were developed by direct compression method using citric acid and sodium bicarbonate as the effervescent base. Hydroxypropyl methylcellulose; HPMC K15M was used to prepare the floating tablets to retard the drug release for 12h in stomach. Na-carboxymethyl cellulose (NaCMC) or carbopol 934P was added to alter the drug release profile or the dimensional stability of the formulation. Dicalcium phosphate (DCP) was used as filler. Formulations were evaluated for floating lag time, duration of floating, dimensional stability, drug content and in vitro drug release profile. The formulations were found to have floating lag time less than 1min. It was found that the dimensional stability of the formulations increase with increasing concentration of the swelling agent. The release mechanism of propranolol hydrochloride from floating tablets was evaluated on the basis of Peppas and Higuchi model. The ânâ value of the formulations ranged from 0.5201 to 0.7367 (0.5

Chaturvedi, Kiran; Umadevi, S; Vaghani, Subhash

2010-01-01

72

Inter-grade and inter-batch variability of sodium alginate used in alginate-based matrix tablets.  

PubMed

The purpose of this study is to characterize the inter-grade and inter-batch variability of sodium alginate used in the formulation of matrix tablets. Four different grades and three batches of one grade of sodium alginate were used to prepare matrix tablets. Swelling, erosion, and drug release tests of sodium alginate matrix tablets were conducted in a USP dissolution apparatus. Substantial differences in swelling and erosion behavior of sodium alginate matrix tablets were evident among different viscosity grades. Even different batches of the same grade exhibit substantial differences in the swelling and erosion behavior of their matrix tablets. The erosion behavior of sodium alginate matrix tablets can be partly explained by their rheological properties (both apparent viscosity and viscoelasticity) in solution. Sodium alginate with higher apparent viscosity and viscoelasticity in solution show slower erosion rate and higher swelling rate. Compacts prepared from grades or batches with higher viscosity and higher viscoelasticity show slower drug release. For grades or batches with similar apparent viscosities, apparent viscosities of sodium alginate solution at low concentration alone are not sufficient to predict the functionality of sodium alginate in matrix tablets. Viscoelastic properties of sodium alginate solutions at one high concentration corresponding to the polymer gel state, may be suitable indicia of the extended release behavior of sodium alginate matrix tablets. PMID:24889735

Fu, Shao; Buckner, Ira S; Block, Lawrence H

2014-10-01

73

Design and development of polyethylene oxide based matrix tablets for verapamil hydrochloride.  

PubMed

In the present investigation an attempt has been made to increase therapeutic efficacy, reduced frequency of administration and improved patient compliance by developing controlled release matrix tablets of verapamil hydrochloride. Verapamil hydrochloride was formulated as oral controlled release matrix tablets by using the polyethylene oxides (Polyox WSR 303). The aim of this study was to investigate the influence of polymer level and type of fillers namely lactose (soluble filler), swellable filler (starch 1500), microcrystalline cellulose and dibasic calcium phosphate (insoluble fillers) on the release rate and mechanism of release for verapamil hydrochloride from matrix tablets prepared by direct compression process. Higher polymeric content in the matrix decreased the release rate of drug. On the other hand, replacement of lactose with anhydrous dibasic calcium phosphate and microcrystalline cellulose has significantly retarded the release rate of verapamil hydrochloride. Biopharmaceutical evaluation of satisfactory formulations were also carried out on New Zealand rabbits and parameters such as maximum plasma concentration, time to reach peak plasma concentration, area under the plasma concentration time curve(0-t) and area under first moment curve(0-t) were determined. In vivo pharmacokinetic study proves that the verapamil hydrochloride from matrix tablets showed prolonged release and were be able to sustain the therapeutic effect up to 24 h. PMID:24019567

Vidyadhara, S; Sasidhar, R L C; Nagaraju, R

2013-03-01

74

Design and Development of Polyethylene Oxide Based Matrix Tablets for Verapamil Hydrochloride  

PubMed Central

In the present investigation an attempt has been made to increase therapeutic efficacy, reduced frequency of administration and improved patient compliance by developing controlled release matrix tablets of verapamil hydrochloride. Verapamil hydrochloride was formulated as oral controlled release matrix tablets by using the polyethylene oxides (Polyox WSR 303). The aim of this study was to investigate the influence of polymer level and type of fillers namely lactose (soluble filler), swellable filler (starch 1500), microcrystalline cellulose and dibasic calcium phosphate (insoluble fillers) on the release rate and mechanism of release for verapamil hydrochloride from matrix tablets prepared by direct compression process. Higher polymeric content in the matrix decreased the release rate of drug. On the other hand, replacement of lactose with anhydrous dibasic calcium phosphate and microcrystalline cellulose has significantly retarded the release rate of verapamil hydrochloride. Biopharmaceutical evaluation of satisfactory formulations were also carried out on New Zealand rabbits and parameters such as maximum plasma concentration, time to reach peak plasma concentration, area under the plasma concentration time curve(0-t) and area under first moment curve(0-t) were determined. In vivo pharmacokinetic study proves that the verapamil hydrochloride from matrix tablets showed prolonged release and were be able to sustain the therapeutic effect up to 24 h. PMID:24019567

Vidyadhara, S.; Sasidhar, R. L. C.; Nagaraju, R.

2013-01-01

75

Formulation and Quality Determination of Indapamide Matrix Tablet: A Thiazide Type Antihypertensive Drug  

PubMed Central

Purpose: The present study was explored to develop a sustained release matrix tablet of Indapamide, a low-dose thiazide-type diuretic, using hydroxylpropyl methylcellulose (Methocel K15MCR) in various proportions as release controlling factor. Methods: The tablets were formulated using direct compression method. The powers for tableting were evaluated for angle of response, loose bulk density, tapped bulk density, compressibility index, total porosity and drug content etc. The tablets were subjected to thickness, weight variation test, drug content, hardness, friability, and in vitro dissolution studies. Results: The granules showed satisfactory flow properties, compressibility index, and drug content. All the formulated tablets complies pharmacopoeia specifications. The release kinetics of the drug decreased exponentially with the addition of polymer concentration. Indapamide release rate was observed to be the highest with the lowest concentration of polymer used. The release mechanism was explored with zero order, first order, Higuchi and Krosmeyer equations. Stability tests of the drug showed no notable changes in the rate of drug release, related substances and drug content. Conclusion: In the context, it can be suggested that this formulation of sustained release Indapamide tablets can be marketed to treat patients with hypertension ensuring proper healthcare. PMID:24511484

Tazri, Jannatun; Moghal, Md. Mizanur Rahman; Dewan, Syed Masudur Rahman; Noor, Wahiduzzaman; Mohammad, Nor

2014-01-01

76

Effect of Kollidon(R) SR on the release of Albuterol Sulphate from matrix tablets  

PubMed Central

The objective of this study was to evaluate Kollidon SR for the development of extended release Albuterol Sulphate matrix tablets in comparison with other polymers as Hydroxypropylmethylcellulose K15M, Carbopol 71G NF, and Eudragit L100-55. The mechanical properties of the tablets were improved as concentration of Kollidon SR or other polymers increased. It was found that Kollidon SR 30% (w/w) and HPMC 30% (w/w) tablets have f2 similarity factor of 83.5 in their Albuterol Sulphate dissolution profile. The marketed product was found to release 99.7% of drug content within 8 h, while Kollidon SR and HPMC tablets with 30% (w/w) polymer concentration level released 92.7% and 92.9% respectively of drug content within 8 h. Kollidon SR has a unique character of maintaining tablets geometric shape until the end of dissolution test, this is mainly due to the water insoluble content, polyvinyl acetate, forming 80% (w/w) of Kollidon SR, while the remaining content 20% (w/w) is the water soluble, polyvinylpyrrolidone, responsible for pore formation causing a diffusion controlled release. Drug release from all previous formulations is best described to be controlled by more than one kinetic mechanism of release. In conclusion, Kollidon SR and HPMC and Carbopol were found to be potential candidates for the development of extended release of Albuterol Sulphate tablets. PMID:24115901

Sakr, Walid; Alanazi, Fars; Sakr, Adel

2010-01-01

77

In vitro Release Kinetics Study of Ranolazine from Swellable Hydrophilic Matrix Tablets  

Microsoft Academic Search

The objective of this study was to design oral sustained release matrix tablets of Ranolazine using hydroxypropyl methylcellulose (HPMC) as the retardant polymer and to study the effect of formulation factors such as polymer proportion and polymer viscosity on the release of drug. In vitro release studies were performed using USP type II apparatus (paddle method) in 900 mL of

Mohammad Nezab Uddin; Ishtiaq Ahmed; Monzurul Amin Roni; Muhammad Rashedul Islam; Mohammad Habibur Rahman; Reza-ul Jalil

2010-01-01

78

In vitro characterization and release study of Ambroxol hydrochloride matrix tablets prepared by direct compression.  

PubMed

A series of either hydrophilic or hydrophobic polymers were used to prepare controlled release Ambroxol hydrochloride (AMX) matrix tablets by direct compression. Both the compatibility and flow properties of AMX/polymer mixtures were investigated. The effect of the amount and type of polymer on the physical properties and in vitro drug release was studied and compared to commercially available Ambroxol(®) SR capsules. A kinetic study of the release profile of AMX from the prepared matrix tablets was performed. All excipients used in the study were compatible with the model drug. AMX/drug mixtures containing sodium alginate (NA) and hydroxypropylmethyl cellulose (HPMC) showed better flow properties than other polymers used in the study. The in vitro drug release studies showed that matrix tablets formulae containing 10% HPMC (S7) or a combination of 30% NA and 5% HPMC (Ah) exhibited a higher ability to control the release of AMX. The kinetic study revealed that a diffusion controlled mechanism prevailed except when carbopol was used. Formula Ah followed a non-fickian diffusion mechanism similar to Ambroxol(®) SR capsules. Both formulae S7 and Ah could be considered as potential candidates for formulation of AMX controlled release matrix tablets. PMID:21428699

Abd-Elbary, A; Haider, M; Sayed, S

2012-01-01

79

Formulation and evaluation of sustained release matrix tablet of rabeprazole using wet granulation technique  

PubMed Central

Introduction: Rabeprazole, a member of substituted benzimidazoles, inhibits the final step in gastric acid secretions. This drug claims to cause fastest acid separation (due to higher pKa), and more rapidly converts to the active species to aid gastric mucin synthesis. The most significant pharmacological action of Rabeprazole is dose dependent suppression of gastric acid secretion; without anticholinergic or H2-blocking action. It completely abolishes the hydrochloric acid secretion as it is powerful inhibitor of gastric acid. Rabeprazole is acid labile and hence commonly formulated as an enteric coated tablet. The absorption of rabeprazole occurs rapidly as soon as tablet leaves the stomach. Aim: In the present study an attempt was made to formulate and evaluate Rabeprazole sustained release matrix tablet using wet granulation technique incorporating various polymers like HPMC-E15, Carbopol934, and sodium carboxymethyl cellulose (CMC). Materials and Methods: The Formulated tablets were evaluated for different physicochemical properties like rheological properties, weight variation, thickness, hardness, % friability, in vitro release studies and drug content. Results: Studies revealed that all the physicochemical parameters comply with the official standards. The in vitro release studies exhibits the release up to 90%, over a prolonged period of time which confirms the extended release profile of formulation, having better bioavailability as well as decreased dosing frequency with reduced doses. Conclusion: The sustained release matrix tablets of rabiprazole shown better bioavailability, efficacy and potency, when compared with official standards. PMID:25035637

Khan, Ruqaiyah; Ashraf, Md Shamim; Afzal, Muhammad; Kazmi, Imran; Jahangir, Mohammed Asadullah; Singh, Rajbala; Chandra, Ramesh; Anwar, Firoz

2014-01-01

80

Design and evaluation of matrix-based controlled release tablets of diclofenac sodium and chondroitin sulphate.  

PubMed

The purpose of the present study was to develop and characterize an oral controlled release drug delivery system for concomitant administration of diclofenac sodium (DS) and chondroitin sulfate (CS). A hydrophilic matrix-based tablet using different concentrations of hydroxypropylmethylcellulose (HPMC) was developed using wet granulation technique to contain 100 mg of DS and 400 mg of CS. Formulations prepared were evaluated for the release of DS and CS over a period of 9 hours in pH 6.8 phosphate buffer using United States Pharmacopeia (USP) type II dissolution apparatus. Along with usual physical properties, the dynamics of water uptake and erosion degree of tablet were also investigated. The in vitro drug release study revealed that HPMC K100CR at a concentration of 40% of the dosage form weight was able to control the simultaneous release of both DS and CS for 9 hours. The release of DS matched with the marketed CR tablet of DS with similarity factor (f(2)) above 50. Water uptake and erosion study of tablets indicated that swelling followed by erosion could be the mechanism of drug release. The in vitro release data of CS and DS followed Korsmeyer-Peppas and zero-order kinetics, respectively. In conclusion, the in vitro release profile and the mathematical models indicate that release of CS and DS can be effectively controlled from a single tablet using HPMC matrix system. PMID:18181548

Avachat, Amelia; Kotwal, Vikram

2007-01-01

81

Use of hydrophilic natural gums in formulation of sustained-release matrix tablets of tramadol hydrochloride  

Microsoft Academic Search

The objective of this work was to develop matrix sustained-release tablets of highly water-soluble tramadol HCl using natural\\u000a gums (xanthan [X gum] and guar [G gum]) as cost-effective, nontoxic, easily available, and suitable hydrophilic matrix systems\\u000a compared with the extensively investigated hydrophilic matrices (ie, hydroxypropyl methylcellulose [HPMC]\\/carboxymethyl cellulose\\u000a [CMC] with respect to in vitro drug release rate) and hydration rate

Jaleh Varshosaz; Naser Tavakoli; Fatemeh Kheirolahi

2006-01-01

82

Polysaccharides as potential antioxidative compounds for extended-release matrix tablets.  

PubMed

The objective of this study was to identify polysaccharides with antioxidant properties for use as potential antioxidative compounds for extended-release matrix tablets. The antioxidant properties of five different polysaccharides, high molecular weight alginate (H-ALG), low molecular weight alginate (L-ALG), high molecular weight chitosan (H-chitosan), low molecular weight chitosan (L-chitosan), and pectic acid (PA) were examined using N-centered radicals from 1,1'-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and reducing power, based on their ability to reduce Cu(2+). L-chitosan and PA had acceptable scavenging abilities and were good radical scavengers, with good reducing power, but the H-chitosan and alginate derivatives were much less effective. The results suggest that L-chitosan and PA could be useful in combating oxidative stress. A PA and L-chitosan interpolymer complex (IPC) tablet was prepared and evaluated as an extended-release tablet matrix using theophylline (TPH) as a model drug. The release of TPH from the matrix tablet (TPH/PA/L-chitosan=200 mg:150 mg:50 mg) was slower than that from PA only (TPH/PA/chitosans=200 mg:200 mg:0 mg) or L-chitosan only (TPH/PA/L-chitosan=200 mg:0 mg:200 mg) tablet. Turbidity measurements also indicated the optimum complexation ratio for IPC between PA/L-chitosan to be 1/3, indicating an acceptable relationship between the turbidity of the complex and the release ratio of TPH. These results suggest that an L-chitosan/PA complex would be potentially useful in an extended-release IPC tablet with high antioxidant activity. PMID:19931857

Tomida, Hisao; Yasufuku, Taira; Fujii, Takeshi; Kondo, Yuko; Kai, Toshiya; Anraku, Makoto

2010-01-11

83

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

PubMed

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

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

2011-07-01

84

Comparative Study of Propranolol hydrochloride Release from Matrix Tablets with Kollidon®SR or Hydroxy Propyl Methyl Cellulose  

Microsoft Academic Search

The release of propranolol hydrochloride from matrix tablets with hydroxy propyl methyl cellulose (HPMC K15M) or Kollidon®SR\\u000a at different concentrations was investigated with a view to developing twice daily sustained release dosage form. A hydrophilic\\u000a matrix-based tablet using different concentrations of HPMC K15M or Kollidon®SR was developed using direct compression technique\\u000a to contain 80 mg of propranolol hydrochloride. The resulting matrix

J. Sahoo; P. N. Murthy; S. Biswal; S. K. Sahoo; A. K. Mahapatra

2008-01-01

85

Use of hydrophilic natural gums in formulation of sustained-release matrix tablets of tramadol hydrochloride.  

PubMed

The objective of this work was to develop matrix sustained-release tablets of highly water-soluble tramadol HCl using natural gums (xanthan [X gum] and guar [G gum]) as cost-effective, nontoxic, easily available, and suitable hydrophilic matrix systems compared with the extensively investigated hydrophilic matrices (ie, hydroxypropyl methylcellulose [HPMC]/carboxymethyl cellulose [CMC] with respect to in vitro drug release rate) and hydration rate of the polymers. Matrix tablets of tramadol (dose 100 mg) were produced by direct compression method. Different ratios of 100:0, 80:20, 60:40, 20:80, 0:100 of G gum (or X):HPMC, X gum:G gum, and triple mixture of these polymers (G gum, X gum, HPMC) were applied. After evaluation of physical characteristics of tablets, the dissolution test was performed in the phosphate buffer media (pH 7.4) up to 8 hours. Tablets with only X had the highest mean dissolution time (MDT), the least dissolution efficiency (DE(8)%), and released the drug following a zero-order model via swelling, diffusion, and erosion mechanisms. Guar gum alone could not efficiently control the drug release, while X and all combinations of natural gums with HPMC could retard tramadol HCl release. However, according to the similarity factor (f(2) ), pure HPMC and H(8)G(2) were the most similar formulations to Topalgic-LP as the reference standard. PMID:16584155

Varshosaz, Jaleh; Tavakoli, Naser; Kheirolahi, Fatemeh

2006-01-01

86

Bimodal drug release achieved with multi-layer matrix tablets: transport mechanisms and device design.  

PubMed

The aim of this study was to develop new multi-layer matrix tablets to achieve bimodal drug release profiles (fast release/slow release/fast release). Hydroxypropyl methylcellulose acetate succinate (HPMCAS, type MF) was chosen as a matrix former, because it is water-insoluble at low, and water-soluble at high pH values. Studies focused on the elucidation of the drug release mechanisms from HPMCAS-MF:drug tablets. In 0.1 N HCl the resulting release kinetics can be described using Fick's second law of diffusion, taking into account axial and radial mass transfer in cylindrical geometry. As the diffusion coefficients are found to be constant and the boundary conditions to be stationary, these systems are purely drug diffusion-controlled. In contrast, the dominating mass transport phenomena in phosphate buffer pH 7.4 are more complex. Due to polymer dissolution the resulting matrix structure is time-variant, leading to increasing drug diffusion coefficients and decreasing tablet dimensions, and thus moving boundary conditions. Drug release is affected by water imbibition, drug diffusion and polymer dissolution and is faster compared to 0.1 N HCl. With knowledge of these underlying release mechanisms, multi-layer matrix tablets were developed to achieve bimodal drug release. HPMCAS-MF:drug mixtures were used as tablet cores. As expected, changing the release medium from 0.1 N HCl to phosphate buffer pH 7. 4 after 2 h, lead to a significant increase in drug release. The abruptness of this rate change could be enhanced by adding two drug-free HPMCAS-MF barrier layers (one on each side) to the system. The addition of a fourth, drug-containing and fast disintegrating initial dose layer yielded the desired bimodal drug release patterns. The process and formulation parameters affecting the resulting release rates were investigated using theophylline and acetaminophen as model drugs. PMID:11102685

Streubel, A; Siepmann, J; Peppas, N A; Bodmeier, R

2000-12-01

87

Development of enteric-coated timed-release matrix tablets for colon targeting.  

PubMed

A new oral drug delivery system for colon targeting has been developed based on enteric-coated matrix tablets which suitably exploits both pH-sensitive and time-dependent functions. Matrix-tablets were prepared by direct compression of mixtures of hydroxyethylcellulose (HEC), a hydrophilic swellable polymer, with the inert insoluble ethylcellulose (EC) or micro-crystalline cellulose (MCC) polymers, in which theophylline, selected as model drug, was dispersed. Eudragit S100, a methacrylic acid copolymer soluble at pH 7, was used as pH-sensitive coating polymer. The influence of varying the cellulose-derivative combinations and their relative ratios as well as the level of the coating polymer was investigated. Surface morphology of the tablets was monitored by SEM analysis before and after the release test. The results of release studies, performed according to the USP basket method using a sequence of dissolution media simulating the gastrointestinal physiological pH variation, indicated that the Eudragit S100 enteric-coated matrix tablets were successful in achieving gastric resistance and timed-release of the drug, assuring an adequate lag time for the intended colonic targeting, followed by a controlled-release phase. The enteric-coating level emerged as the critical factor in determining the duration of the lag-phase, whereas the release rate mainly depended on the matrix composition. Formulations with higher HEC content showed a faster drug release rate than those with greater content in inert polymer and the MCC-HEC combinations were more effective than the corresponding EC-HEC ones. The best results were given by the 27% coated 1:0.3:0.7 (w/w) drug/MCC/HEC tablets, which, after a 260 min lag time, regularly released the drug, achieving about 90% of release after 10 h. PMID:15621686

Alvarez-Fuentes, J; Fernández-Arévalo, M; González-Rodríguez, M L; Cirri, M; Mura, P

2004-01-01

88

Study of formulation variables influencing the drug release rate from matrix tablets by experimental design.  

PubMed

Experimental design was utilized to simultaneously investigate the effect of varying the type of diluent (insoluble Calcium phosphate or water-soluble arabic gum) and the diluent/matrix ratio on the drug release behaviour from both lipophilic (glyceryl behenate, Compritol) or hydrophilic (hydroxypropylmethylcellulose) matrix tablets. Ketoprofen, theophylline and sodium sulphadiazine were selected as model drugs on the basis of their respectively very low, medium and high water-solubility, in order to evaluate the influence of this parameter as well. The selected response variables were the dissolution efficiency (i.e. the area under the dissolution curve) after one and six hours and the time necessary to dissolve 10% drug. Tablets obtained by direct compression of drug-diluent-matrix ternary mixtures prepared according to the experimental plan provided for by an asymmetric screening matrix, were tested for drug release properties using a USP paddle apparatus. Graphic analysis of the effects allowed identification, for each examined drug, of the formulation factors active on the selected responses and determination of the proper level of the variables to be selected for the response improvement. The different results obtained with the three examined drugs pointed out the role of the drug solubility in determining the influence of formulation parameters on drug release rate from matrix tablets. PMID:16154333

Furlanetto, Sandra; Cirri, Marzia; Maestrelli, Francesca; Corti, Giovanna; Mura, Paola

2006-01-01

89

Effect of two hydrophobic polymers on the release of gliclazide from their matrix tablets.  

PubMed

Gliclazide is an oral hypoglycemic agent, indicated in non insulin dependent diabetes mellitus and in patients with diabetic retinopathy. It has good tolerability and is a short acting sulfonyl urea that requires large dose to maintain the blood glucose level. So development of a sustained release formulation of gliclazide (GLZ) is required for better patient compliance. This study was conducted to assess the effects of different drug polymer ratios on the release profile of gliclazide from the matrix. Oral matrix tablets of gliclazide were prepared by hot melt method, using pure and blended mixture of glyceryl monostearate (GMS) and stearic acid (SA) in different ratios. In vitro release pattern was studied for 8 h in phosphate buffer media (pH 7.4). Different kinetic models including zero order, first order, Higuchi and Peppas were applied to evaluate drug release behavior. Drug excipient compatibility was evaluated by scanning with DSC and FTIR. Higuchi model was found the most appropriate model for describing the release profile of GLZ and non-Fickian release was found predominant mechanism of drug release. The release of drug from the matrix was greatly controlled by GMS while SA appeared to facilitate the release of drug from matrix tablets. FTIR results showed no chemical interaction between drug and the polymers, and DSC results indicated amorphous state of GLZ and polymers without significant complex formation. The results indicate that matrix tablets of gliclazide using glyceryl monostearate and stearic acid showed marked sustained release properties. PMID:23923399

Hussain, Talib; Saeed, Tariq; Mumtaz, Ahmad M; Javaid, Zeeshan; Abbas, Khizar; Awais, Azeema; Idrees, Hafiz Arfat

2013-01-01

90

Solid Dispersion Matrix Tablet Comprising Indomethacin-PEG-HPMC Fabricated with Fusion and Mold Technique  

PubMed Central

The purpose of this study is to fabricate the polyethylene glycol matrix tablet by mold technique. Indomethacin and hydroxypropylmethylcellulose were used as model drug and polymer, respectively, in PEG matrix system. The physical and drug release characteristics of developed matrix tablet were studied. This inert carrier system comprising 7:3 polyethylene glycol 4000: polyethylene glycol 400 could effectively enhance the solubility of indomethacin and an addition of hydroxypropylmethylcellulose could sustain the drug release. Scanning electron microscope photomicrograph indicated the drug diffusion outward through the porous network of this developed matrix tablet into the dissolution fluid. Least square fitting the experimental dissolution data to the mathematical expressions (power law, first-order, Higuchi's and zero-order) indicated the drug release kinetics primarily as Fickian diffusion. Both the enhancement of drug dissolution and the prolongation of the drug release could be achieved for aqueous insoluble drug such as, indomethacin, by using polyethylene glycol-hydroxypropylmethylcellulose matrix system prepared with melting and mold technique. PMID:20502547

Mesnukul, A.; Yodkhum, K.; Phaechamud, T.

2009-01-01

91

Verapamil hydrochloride release characteristics from new copolymer zwitterionic matrix tablets.  

PubMed

The aim of this study was to synthesize stable copolymer (vinyl acetate-co-3-dimethyl[methacryloyloxyethyl] ammonium propane sulfinate) zwitterionic latex with different compositions for the first time by emulsifier-free emulsion copolymerization. Throughout the course of the study, a proposal was made for the explanation of the relationship between the "overshooting" phenomenon (a swelling kinetics with a maximum) and the specific self-association of the zwitterionic copolymers. The zwitterionic monomer unit mole fraction, pH, and ionic strength effects on this relationship, on the swelling kinetics of the zwitterionic copolymers, and on the sustained verapamil hydrochloride release from the model tablets were established by the study's authors. PMID:18649221

Kostova, Bistra; Kamenska, Elena; Ivanov, Ivo; Momekov, George; Rachev, Dimitar; Georgiev, George

2008-01-01

92

Optimization and characterization of a pH-independent extended-release hydrophilic matrix tablet.  

PubMed

A simple systematic optimization approach was applied to tailor the drug release profile from a hydrophilic matrix extended-release tablet. When the ratio of anionic and nonionic polymers was optimized, pH-independent in vitro release of the model drug verapamil hydrochloride was obtained. The mechanisms of drug release at the pH extremes were evaluated by graphical analysis of the dissolution data and direct examination of the tablets during dissolution. Graphical evaluation did not completely clarify the release control mechanisms involved. Direct examination of tablets during dissolution, with estimation of amounts of drug and excipients dissolved at different times, gave further insight into relative contribution of mechanisms at different pH values. The change from predominantly diffusional to predominantly erosional mechanisms as pH is increased provides for the pH-independent release observed. This understanding should help model the application of this approach to other drugs. PMID:9552428

Timmins, P; Delargy, A M; Howard, J R

1997-02-01

93

Matrix mini-tablets based on starch/microcrystalline wax mixtures.  

PubMed

Matrix mini-tablets based on a combination of microcrystalline waxes and starch derivatives were prepared using ibuprofen as a model drug. The production of mini-tablets was preferred over the production of pellets, as up-scaling of the pelletisation process seemed problematic. Prior to tabletting, melt granulation in a hot stage screw extruder and milling were required. The in vitro drug release was varied using microcrystalline waxes with a different melting range, the slowest drug release being obtained with a formulation containing a microcrystalline wax with a melting range between 68 and 72 degrees C. Generally speaking increasing the wax concentration resulted in a slower drug release. In vitro drug release profiles were also modified using different starches and mixtures of starches. Increasing the ibuprofen concentration to 70% resulted in a faster drug release rate. PMID:10802413

De Brabander, C; Vervaet, C; Fiermans, L; Remon, J P

2000-04-20

94

Influence of neutron activation factors on matrix tablets for site specific delivery to the colon.  

PubMed

The impact of the neutron activation procedure, i.e. incorporation of samarium oxide (Sm(2)O(3)) and neutron irradiation, on the compression properties (including the crushing strength) and in vitro dissolution of potential colonic delivery systems based on matrix tablets of amidated pectin (Am.P) or two types of hydroxypropyl methylcellulose (HPMC) was investigated. The neutron activation factors did not influence the compression properties of the tablets. Replacement of magnesium stearate with samarium stearate in directly compressed Am.P tablets to achieve both radiolabelling and lubrication resulted in a greater extent of concentration-dependent reduction of the crushing strength. Dissolution tests demonstrated that irradiation increased the release of the model drug ropivacaine from the tablets. The extent of this increase was unexpectedly low considering the previously observed degradation of the polymer expressed as an irradiation-induced viscosity reduction in solutions prepared from the polymers. Delayed-release coating with Eudragit L 100 protected the HPMC tablets against the release-increasing effect of irradiation until the late phases of release. Sm(2)O(3) retarded the release to a varying extent depending on particle characteristics. Incorporation of Sm(2)O(3) in the coating layer did not influence the release. However, one-third of the radioactivity leached from the coating within 60 min in 0.1 M HCl. PMID:10767600

Ahrabi, S F; Heinämäki, J; Sande, S A; Graffner, C

2000-05-01

95

FABRICATION AND IN VITRO EVALUATION OF CHITOSAN MATRIX TABLETS OF DICLOFENAC ON COLON DRUG DELIVERY SYSTEM (CODES)  

Microsoft Academic Search

The objective of this study is to fabricate and Evaluate Chitosan Matrix tablets of Diclofenac.The effect of various polymers like ethyl cellulose, cellulose acetate phthalate on the release of Diclofenac have been evaluated. Tablets were evaluated for physical and chemical parameters such as Hardness, Friability, Thickness, Weight variation, Drug Content uniformity and invitro release. All batches are complied physical and

A. ABIRAMI; S. MOHAMED HALITH; S. JAYAPRAKASH; R. SENTHIL PRABHU; K. KULATHURAN PILLAI

96

Effect of processing methods and heat treatment on the formation of wax matrix tablets for sustained drug release.  

PubMed

The objective of this study was to evaluate the effects of processing methods and heat treatment on matrix formation and subsequent drug release from wax matrix tablets for controlled release. Phenylpropanolamine hydrochloride (PPA) and Compritol were processed with appropriate diluent(s) using either dry blending (DB), wet granulation (WG), partial melt granulation (PMG), or melt granulation (MG). Then the tablets were heat-treated at 80 degrees C. Particle size distribution and compressibility, along with drug release, tablet micro-morphology, wettability, porosity, and tortuosity were investigated. The drug release was different for the four processing methods even though the tablet formulation was identical. Heat treatment further retarded drug release and its effect was related to the previous manufacturing processes. Scanning Electron Microscopy (SEM) showed that heat treatment redistributed the wax and formed a film-like structure covering drug and excipients. The contact angle of tablets made from DB, WG, and PMG methods increased after heat treatment, while that of tablets made from MG remained constant. Tablet tortuosity calculated from drug release rate constants increased dramatically after heat treatment. Drug release from the wax tablets with or without heat treatment was best described by the Higuchi equation. Different processing methods produced different matrix structures that resulted in different drug release rates. Heat treatment retarded drug release mainly by increasing tortuosity of the matrix. Contact angle measurement and SEM analysis indicated that heat treatment caused the wax to melt, redistribute, coat the drug and diluents, and form a network structure. PMID:11416986

Zhang, Y E; Tchao, R; Schwartz, J B

2001-01-01

97

Matrix tablets are drug delivery devices that release a water-soluble drug over an extended period of time. Such matrix tablets are formulated from mixtures of drug, polymer, and excipient  

E-print Network

concentrations. Our simulation tool can thus be used to streamline the formulation and production of sustained. #12;Swallowing a cellular automaton pill: predicting drug release from a matrix tablet Ezra Buchla

Hinow, Peter

98

Release of theophylline and carbamazepine from matrix tablets--consequences of HPMC chemical heterogeneity.  

PubMed

The release of theophylline and carbamazepine from matrix tablets composed of microcrystalline cellulose, lactose and hydroxypropyl methylcellulose (HPMC) was studied. The aim was to investigate the effect of different substituent heterogeneities of HPMC on the drug release from matrix tablets composed of either 35% or 45% HPMC. The release of the poorly soluble carbamazepine was considerably affected by the HPMC heterogeneity, and the time difference at 80% drug release was more than 12h between the formulations of different HPMC batches. This was explained by slower polymer erosion of the heterogeneous HPMC and the fact that carbamazepine was mainly released by erosion. In addition, results from magnetic resonance imaging showed that the rate of water transport into the tablets was similar. This explained the comparable results of the release of the sparingly soluble theophylline from the two formulations even though the polymer erosion and the swelling of the tablets were considerably different. Thus, it can be concluded that the drug release was highly affected by the substituent heterogeneity, especially in the case of carbamazepine, which was released mainly by erosion. PMID:21316446

Viridén, Anna; Abrahmsén-Alami, Susanna; Wittgren, Bengt; Larsson, Anette

2011-08-01

99

Sustained release of highly water-soluble drugs with micelle forming ability from polyionic matrix tablets.  

PubMed

The aim of present study was to evaluate the application of a hydrophilic matrix tablet capable of polyion complex (PIC-tablet) to a controlled-release device for highly water-soluble drugs. The PIC-tablet was prepared from a mixture of dextran sulfate and [2-(diethylamino)ethyl] dextran chloride, and diltiazem hydrochloride was used as a model drug. Release tests revealed that the drug release was sustained even in 50% drug loading and was influenced by ionic strength but not by pH in medium. The drug release mechanism was thus investigated from the viewpoint of drug micelle forming property. The micelle forming ability of diltiazem was examined by the conductivity method, and was found to be influenced by ionic strength but not by pH value in accordance with the release tests. The results suggested that the drug's micelle interacted with the polyionic matrix. Further studies were conducted using metoprolol tartrate and thiamine hydrochloride as cationic drugs and sodium cloxacillin and sodium salicylic acid as anionic ones. The release profiles of the micelle-forming drugs metoprolol tartrate and sodium cloxacillin were also suppressed in spite of different solubility or opposite ionic charge from diltiazem hydrochloride. These findings demonstrated that the PIC-tablet is a promising device for oral controlled release delivery of water-soluble drugs with good micelle-forming ability. PMID:17294812

Tanaka, Y; Miyazaki, Y; Yakou, S; Takayama, K

2007-01-01

100

Evaluation of injection moulding as a pharmaceutical technology to produce matrix tablets.  

PubMed

The aim of this study was to develop sustained-release matrix tablets by means of injection moulding and to evaluate the influence of process temperature, matrix composition (EC and HPMC concentration) and viscosity grade of ethylcellulose (EC) and hydroxypropylmethylcellulose (HPMC) on processability and drug release. The drug release data were analyzed to get insight in the release kinetics and mechanism. Formulations containing metoprolol tartrate (30%, model drug), EC with dibutyl sebacate (matrix former and plasticizer) and hydrophilic polymer HPMC were extruded and subsequently injection moulded into tablets (375 mg, 10 mm diameter, convex-shaped) at temperatures ranging from 110 to 140 degrees C. Tablets containing 30% metoprolol and 70% ethylcellulose (EC 4mPa s) showed an incomplete drug release within 24 h (<50%). Increasing production temperatures resulted in a lower drug release rate. Substituting part of the EC fraction by HPMC (HPMC/EC-ratio: 20/50 and 35/35) resulted in faster and constant drug release rates. Formulations containing 50% HPMC had a complete and first-order drug release profile with drug release controlled via the combination of diffusion and swelling/erosion. Faster drug release rates were observed for higher viscosity grades of EC (Mw>20 mPa s) and HPMC (4000 and 10,000 mPa s). Tablet porosity was low (<4%). Differential scanning calorimetry (DSC) and X-ray powder diffraction studies (X-RD) showed that solid dispersions were formed during processing. Using thermogravimetrical analysis (TGA) and gel-permeation chromatography no degradation of drug and matrix polymer was observed. The surface morphology was investigated with the aid of scanning electron microscopy (SEM) showing an influence of the process temperature. Raman spectroscopy demonstrated that the drug is distributed in the entire matrix, however, some drug clusters were identified. PMID:18511248

Quinten, Thomas; De Beer, Thomas; Vervaet, Chris; Remon, Jean Paul

2009-01-01

101

Effect of cogrinding time on the release of pentoxifylline from waxy matrix tablets.  

PubMed

The release of pentoxifylline from matrix tablets containing palmitic or behenic acids, as waxes, and prepared via cogrinding was investigated. X-ray powder diffraction analysis of the ground drug-wax indicated that particle size could be reduced by grinding without polymorphic transformation. After the coground mixed powder was compressed at 1000 kg/cm2, the drug-release rate from the tablet was evaluated in pH 6.8 buffer at 37 degrees C. The drug-release profiles could be fitted to the Cobby model. The release rate decreased with an increased grinding time and increased significantly with an increased proportion of the drug. The drug-release rate constant from the matrix was calculated using the Cobby equation and the drug-release profiles. Scanning electron microphotographs of the coground product after dissolution tests suggested that mechanochemical energy had been used to cover the drug particles. PMID:7965674

Otsuka, M; Matsuda, Y

1994-07-01

102

Comparative release profile of sustained release matrix tablets of verapamil HCl  

PubMed Central

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

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

2013-01-01

103

Design and evaluation of matrix-based controlled release tablets of diclofenac sodium and chondroitin sulphate  

Microsoft Academic Search

The purpose of the present study was to develop and characterize an oral controlled release drug delivery system for concomitant\\u000a administration of diclofenac sodium (DS) and chondroitin sulfate (CS). A hydrophilic matrix-based tablet using different concentrations\\u000a of hydroxypropylmethylcellulose (HPMC) was developed using wet granulation technique to contain 100 mg of DS and 400 mg of\\u000a CS. Formulations prepared were evaluated

Amelia Avachat; Vikram Kotwal

2007-01-01

104

STUDY OF PHYSICOCHEMICAL PARAMETERS AFFECTING THE RELEASE OF DICLOFENAC SODIUM FROM LIPOPHILIC MATRIX TABLETS  

Microsoft Academic Search

In the present work different parameters, which influence the release of diclofenac sodium (2-((2,6-dichlorophenyl)amino)benzeneacetic acid mono sodium salt) from lipophilic matrix prolonged release tablets, were investigated. Solubility characteristics of diclofenac sodium in aqueous media with various ionic strengths, ionic compositions and pH in the range of 1 to 10 were determined. According to the obtained results different experimental conditions of

Maja Kincl; Marija Meleh; Marjan Veber

105

Designing an extended release waxy matrix tablet containing nicardipine-hydroxy propyl ? cyclodextrin complex  

PubMed Central

Aim The current study aimed to prepare a sustained release tablet for a drug which has poor solubility in alkaline medium using complexation with cyclodextrin. Nicardipine hydrochloride (NC) a weak basic drug was chosen as a model drug for this study. Method Firstly the most suitable binary system NC-HP?CD was selected in order to improve drug solubility in the intestinal media and then embedding the complexed drug into a plastic matrix, by fusion method, consists of glycerol monostearate (GMS) as an inert waxy substance and polyethylene glycol 4000 (PEG4000) as a channeling agent, after that the final solid dispersion [(NC:HP?CD):GMS:PEG4000] which was prepared at different ratios was mixed with other excipients, avicel PH101, lactose, and talc, to get a tablet owning dissolution profile complying with the FDA and USP requirements for the extended release solid dosage forms. Results Infrared spectroscopy (IR), differential scanning colorimetry (DSC), polarized microscopy and X-ray diffractometry proved that the coevaporation technique was effective in preparing amorphous cyclodextrin complexes with NC and trapping of NC within the HP?CD cavity by dissolving both in ethanol and evaporate the solvent using a rotavapor at 65 °C. Dissolution profile of NC enhanced significantly in pH 6.8 from NC:HP?CD inclusion complex prepared by the rotavapor (t-test Student p < 0.05). The release of NC from tablet containing [(NC:HP?CD):GMS:PEG4000] [(1):0.75:0.5] (w/w/w) solid dispersion (F8) was complying with the FDA dissolution requirements for extended release dosage forms, and studying the kinetics of the release showed that the diffusional contribution is the major factor controlling the drug release from that formula. Conclusion The prepared waxy matrix tablet containing NC complexes with CD shows promising results as extended release tablets. PMID:23960765

Al-Zein, Hind; Sakeer, Khalil; Alanazi, Fars K.

2011-01-01

106

Formulation and Evaluation of Cephalexin Extended Release Matrix Tablets Using 32 Factorial Design  

PubMed Central

The aim of the present investigation was to prepare extended release film coated matrix tablets of cephalexin using binary mixture of two grades of hydrophilic polymer, hydroxypropyl methyl cellulose (HPMC), by direct compression method. Results of the preliminary trials indicated that the polymers used have significant release retarding effect on the formulation. To study the effect of concentration of polymers on drug release from matrix tablets, 32 full factorial design was applied. The concentration of HPMC K15M and HPMC 15cps were used as independent variables, while percentage drug release was selected as dependent variable. The dissolution data were fitted into zero-order, first-order, Higuchi and Korsemeyer–Peppas models to identify the pharmacokinetics and mechanism of drug release. Comparative study of dissolution profile of final batch F3 with market preparation (Sporidex AF 375) was done by similarity factor (f2) determination and it was concluded that final formulation F3 (10% HPMC K15M, 17.5% HPMC 15cps) shows good similarity with the market product. The results of the accelerated stability study of final formulation F3 for 1 month revealed that storage conditions were not found to have made any significant changes in final formulation F3. The release of cephalexin was prolonged for 6 h by using polymer combinations of HPMC and a twice daily matrix tablet was formulated. PMID:22224031

Jishnu, V; Prabhakaran, R; Gilhotra, RM

2011-01-01

107

Release from or through a wax matrix system. VI. Analysis and prediction of the entire release process of the wax matrix tablet.  

PubMed

Analysis of the entire release process of the wax matrix tablet was examined. Wax matrix tablet was prepared from a physical mixture of drug and wax powder to obtain basic or clear release properties. The release process began to deviate from Higuchi equation when the released amount reached at around the half of the initial drug amount. Simulated release amount increase infinitely when the Higuchi equation was applied. Then, the Higuchi equation was modified to estimate the release process of the wax matrix tablet. The modified Higuchi equation was named as the H-my equation. Release process was well treated by the H-my equation. Release process simulated by the H-my equation fitted well with the measured entire release process. Also, release properties from and through wax matrix well coincident each other. Furthermore, it is possible to predict an optional release process when the amount of matrix and composition of matrix system were defined. PMID:16079519

Yonezawa, Yorinobu; Ishida, Sumio; Sunada, Hisakazu

2005-08-01

108

Preparation of an extended-release matrix tablet using chitosan/Carbopol interpolymer complex.  

PubMed

A chitosan and Carbopol interpolymer complex (IPC) was formed using a precipitation method in an acidic solution. The chitosan and Carbopol IPC was characterized by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), and turbidity measurements. FT-IR demonstrated that the IPC formed a complex through an electrostatic interaction between the protonated amine (NH(3)(+)) group of chitosan and the carboxylate (COO(-)) group of Carbopol. DSC indicated the IPC to have different thermal characteristics from chitosan or Carbopol. The turbidity measurement revealed the complexation ratio of IPC between chitosan/Carbopol to be 1/4. A theophylline tablet was prepared using the IPC as a matrix material. The drug release profile from this tablet was similar to that from the HPMC tablet and showed a pH-independent release profile. The mechanisms for drug release from the IPC tablet were diffusional release at pH 6.8 and relaxational release at pH 1.2. PMID:17662544

Park, Sung-Hyun; Chun, Myung-Kwan; Choi, Hoo-Kyun

2008-01-22

109

Accessibility of solid core tablet for dissolution in an asymmetric triple-layer matrix system.  

PubMed

The importance of glassy matrix surface area to ensure constant drug release and the effect of barrier layer thickness on the duration of linear release in an asymmetric triple-layer tablet with zero-order release kinetics were investigated. Poly(ethylene oxide) of different molecular weights and hydroxypropylmethylcellulose K4M were the major polymeric constituents, and verapamil hydrochloride was used as a drug model. The contribution of diffusion and polymer relaxation towards drug release was evaluated based on drug release data using a non-linear regression analysis algorithm. The results demonstrated that application of barrier layers to the central core tablet enables polymer relaxation to be the predominant mechanism in controlling drug release and leads to the often desired zero-order release kinetics. The duration of linear release from the asymmetric triple-layer tablet depends on the barrier layer thickness and composition. It was further indicated that the magnitude of diffusion and polymer relaxation in controlling drug release is affected by the accessibility of the drug core tablet for dissolution, as well as the inherent swelling and erosion characteristics of the release rate-controlling polymer. PMID:14607013

Yang, Libo; Fassihi, Reza

2003-10-01

110

Influence of internal structure on kinetics of drug release from wax matrix tablets.  

PubMed

To examine the influence of the internal structure of a wax matrix tablet on in vitro drug release, the release rates of several tablets consisting of various proportions of drug and wax were compared with the water penetration rates from the compressed and lateral surfaces of the tablets. The penetration rates from the lateral surface were found to be much faster than those from the compressed surface in all cases. A theoretical equation involving a two-dissolving-direction was derived on the basis of the boundary retreating concept. The retreating rate constants deduced from the dissolution results were well coincident with the values directly determined by the needle penetration method, suggesting good applicability of the proposed equation. The results suggest that the tortuosity of the water channels created in a tablet during dissolution is generally smaller in the horizontal direction than that in the vertical direction. This would be caused by the drug particles or granules being elongated in the horizontal direction by compression. PMID:2092942

Ishino, R; Yoshino, H; Hirikawa, Y; Noda, K

1990-12-01

111

Assessment of xanthan gum based sustained release matrix tablets containing highly water-soluble propranolol HCl.  

PubMed

The present study was carried out to develop oral sustained release tablets of propranolol HCl by different ratios of drug : matrix. Tablets were prepared by direct compression technique using xanthan gum and lactose. All the formulations (tablets) were evaluated for thickness, diameter, hardness, friability, weight variation, content of active ingredient, in vitro dissolution using USP dissolution apparatus-II and swelling index. In case of dissolution, an inverse relationship was noted between amount of xanthan gum and release rate of propranolol HCl and the drug release was gradually enhanced as the amount of the lactose increased. The direct release was observed between swelling index and xanthan gum concentration. Significant difference in different media was observed in release profile, indicating that propranolol HCI has better solubility in HCI buffer pH 1.2. Moreover, dissolution data at differing stirring speeds was also analyzed, indicating that the drug release profile was at 50 rpm comparative to 100 rpm. The kinetic treatment showed the best fitted different mathematical models (zero order, first order, Higuchi's, Hixson-Crowell and Korsmeyer Peppas model. Most of the formulations showed linearity in Higuchi's model. The drug release from these tablets was by Fickian diffusion and anomalous (non-Fickian) mechanisms. PMID:23614284

Ali, Atif; Iqbal, Muhammad; Akhtar, Naveed; Khan, Haji Muhamad Shoaib; Ullah, Aftab; Uddin, Minhaj; Khan, Muhammad Tahir

2013-01-01

112

Formulation development of sustained-release hydrophilic matrix tablets of zileuton.  

PubMed

The purpose of this paper was to develop a hydrophilic matrix system for extended oral delivery of zileuton, and study the effects of certain formulation, processing, and dissolution variables on in vitro drug release. Tablet formulations with 60-70% drug and varying release rates were prepared by wet granulation using low and medium viscosity grades of hydroxypropylmethocellulose. In vitro drug release was evaluated using USP apparatus 1. The in vitro drug release from all formulations followed zero-order kinetics and was independent of compression force. In general, the release rate decreased with increasing drug load and higher polymer concentration or viscosity. High-shear granulation also resulted in lower release rate. Accelerated release was observed with increased agitation as well as in the dissolution media with higher surfactant concentration and/or ionic strength. No stereoselective release from the matrix system was observed. The hydrophilic matrix system effectively controlled the in vitro release of zileuton. Matrix tablets with desired release rates can be prepared by adjusting various formulation and processing parameters. The matrix system also has the advantage of simple processing and relatively low cost. PMID:9552447

Qiu, Y; Hui, H W; Cheskin, H

1997-08-01

113

Direct analysis of pharmaceutical tablet formulations using Matrix-Assisted Laser Desorption/Ionisation Mass Spectrometry Imaging.  

PubMed

Matrix-Assisted Laser Desorption/Ionisation Mass Spectrometry Imaging (MALDI MSI) has been used to directly analyse a range of tablets in order to assess the homogeneity of the active drug compound throughout the excipients contained within the tablets studied. The information gained from the imaging experiments can be used to improve and gain a greater understanding of the manufacturing process; such knowledge will enable improvements in finished product quality to make safer and more efficacious tablet formulations. Commercially available and prescription tablet formulations have been analysed, including aspirin, paracetamol, sildenafil citrate (Viagra(R)) and a batch of tablets in development (tablet X: placebo; 1 mg; 3 mg and 6 mg). MALDI MSI provides semi-quantitative information that is related to ion abundance, therefore Principal Component Analysis (PCA), a multivariate analysis technique, has been used to differentiate between tablets containing different amounts of active drug ingredient. Aspects of sample preparation have also been investigated with regard to tablet shape and texture. The results obtained indicate that MALDI MSI can be used effectively to analyse the spatial distribution of the active pharmaceutical component (API) in pharmaceutical tablet formulations. PMID:20486264

Earnshaw, Caroline J; Carolan, Vikki A; Richards, Don S; Clench, Malcolm R

2010-06-15

114

Drug release characteristics from chitosan-alginate matrix tablets based on the theory of self-assembled film.  

PubMed

The aim of this study was to better understand the underlying drug release characteristics from chitosan-alginate matrix tablets containing different types of drugs. Theophylline, paracetamol, metformin hydrochloride and trimetazidine hydrochloride were used as model drugs exhibiting significantly different solubilities (12, 16, 346 and >1000 mg/ml at 37 °C in water). A novel concept raised was that drugs were released from chitosan-alginate matrix tablets based on the theory of a self-assembled film-controlled release system. The film was only formed on the surface of tablets in gastrointestinal environment and originated from chitosan-alginate polyelectrolyte complex, confirmed by differential scanning calorimetry characterization. The formed film could decrease the rate of polymer swelling to a degree, also greatly limit the erosion of tablets. Drugs were all released through diffusion in the hydrated matrix and polymer relaxation, irrespective of the drug solubility. The effects of polymer level and initial drug loading on release depended on drug properties. Drug release was influenced by the change of pH. In contrast, the impact of ionic strength of the release medium within the physiological range was negligible. Importantly, hydrodynamic conditions showed a key factor determining the superiority of the self-assembled film in controlling drug release compared with conventional matrix tablets. The new insight into chitosan-alginate matrix tablets can help to broaden the application of this type of dosage forms. PMID:23624081

Li, Liang; Wang, Linlin; Shao, Yang; Ni, Rui; Zhang, Tingting; Mao, Shirui

2013-06-25

115

Floating Node Method and Virtual Crack Closure Technique for Modeling Matrix Cracking-Delamination Migration  

NASA Technical Reports Server (NTRS)

A novel approach is proposed for high-fidelity modeling of progressive damage and failure in composite materials that combines the Floating Node Method (FNM) and the Virtual Crack Closure Technique (VCCT) to represent multiple interacting failure mechanisms in a mesh-independent fashion. In this study, the approach is applied to the modeling of delamination migration in cross-ply tape laminates. Delamination, matrix cracking, and migration are all modeled using fracture mechanics based failure and migration criteria. The methodology proposed shows very good qualitative and quantitative agreement with experiments.

DeCarvalho, Nelson V.; Chen, B. Y.; Pinho, Silvestre T.; Baiz, P. M.; Ratcliffe, James G.; Tay, T. E.

2013-01-01

116

Floating Node Method and Virtual Crack Closure Technique for Modeling Matrix Cracking-Delamination Interaction  

NASA Technical Reports Server (NTRS)

A novel approach is proposed for high-fidelity modeling of progressive damage and failure in composite materials that combines the Floating Node Method (FNM) and the Virtual Crack Closure Technique (VCCT) to represent multiple interacting failure mechanisms in a mesh-independent fashion. In this study, the approach is applied to the modeling of delamination migration in cross-ply tape laminates. Delamination, matrix cracking, and migration are all modeled using fracture mechanics based failure and migration criteria. The methodology proposed shows very good qualitative and quantitative agreement with experiments.

DeCarvalho, N. V.; Chen, B. Y.; Pinho, S. T.; Baiz, P. M.; Ratcliffe, J. G.; Tay, T. E.

2013-01-01

117

Bioavailability of ibuprofen from matrix mini-tablets based on a mixture of starch and microcrystalline wax.  

PubMed

The bioavailability of ibuprofen from matrix mini-tablets based on microcrystalline wax and a starch derivative was tested. An oral dose of 300 mg of ibuprofen was administered to healthy volunteers (n=8) in a randomized cross-over study design either as a commercial matrix formulation (Ibu-Slow 600) or as mini-tablets (filled into hard gelatin capsules). The mini-tablets consisted of 60% ibuprofen, 15% Paracera M (wax), 22.5% DDWM (starch) and 2.5% triacetin (lubricant). t50% of the in vitro release was 4.5 and 5 h for the mini-tablet and Ibu-slow formulations, respectively. Both formulations behaved in vivo as sustained-release formulation; their HVDt50%Cmax value was determined at 5.6 and 5.1 h for the mini-tablet and Ibu-slow formulations, respectively. A significantly higher value of Cmax was seen for the mini-tablet formulation, resulting in a relative bioavailability of 116 +/- 22.6% compared to the Ibu-slow matrix. These data demonstrate that the experimental mini-tablets can be used to formulate sustained-release dosage forms. PMID:11203270

De Brabander, C; Vervaet, C; Görtz, J P; Remon, J P; Berlo, J A

2000-11-01

118

Soluble filler as a dissolution profile modulator for slightly soluble drugs in matrix tablets.  

PubMed

The purpose of this experimental work was the development of hydrophilic-lipophilic matrix tablets for controlled release of slightly soluble drug represented here by diclofenac sodium (DS). Drug dissolution profile optimization provided by soluble filler was studied. Matrix tablets were based on cetyl alcohol as the lipophilic carrier, povidone as the gel-forming agent, and common soluble filler, that is lactose or sucrose of different particle size. Physical properties of tablets prepared by melt granulation and drug release in a phosphate buffer of pH 6.8 were evaluated. In vitro studies showed that used filler type, filler to povidone ratio and sucrose particle size influenced the drug release rate. DS dissolution profile could be changed within a wide range from about 50% per 24 hours to almost 100% in 10 hours. The release constant values confirmed that DS was released from matrices by the diffusion and anomalous transport. The influence of sucrose particle size on the drug release rate was observed. As the particle size decreased, the drug release increased significantly and its dissolution profile became more uniform. Soluble fillers participated in the pore-forming process according to their solubility and particle size. Formulations containing 100 mg of the drug, 80 mg of cetyl alcohol, 40 mg of povidone, and 80 mg of either lactose or sucrose (particle size 250-125 microm) were considered optimal for 24-hour lasting dissolution of DS. PMID:19274510

Dvorácková, Katerina; Rabisková, Miloslava; Masteiková, Ruta; Muselík, Jan; Krejcová, Katerina

2009-08-01

119

The effect of chemical heterogeneity of HPMC on polymer release from matrix tablets.  

PubMed

Polymer release from hydrophilic matrix tablets, composed of hydroxypropyl methylcellulose, was studied for seven different polymer batches. A time difference of more than 80h between fully dissolved tablets was noticed although the batches were of the same pharmaceutical substituent (USP 2208) and viscosity (100 cps) grade. To find the functionality related parameters for polymer release from hydrophilic matrix tablets the polymer samples were characterised according to size and chemical composition. The size of the polymers was characterised by size-exclusion chromatography with multi-angle light scattering and refractive index detection. The average amount of substituents was measured with nuclear magnetic resonance and the distribution of the substituents along the cellulose chain was determined with high-performance anion-exchange chromatography with pulsed amperometric detection after acid and enzymatic hydrolysis. The results indicated that other types of interactions apart from entanglements were present between the polymer chains, which seemed to affect the polymer release. Most importantly, this study has shown a correlation between the polymer release and the substituent pattern, where the samples with slow release also were more heterogeneously substituted along the polymer chain. From this we can conclude that polymer release is very sensitive to alterations in chemical composition. PMID:19049865

Viridén, Anna; Wittgren, Bengt; Andersson, Thomas; Larsson, Anette

2009-03-01

120

Statistical optimization of a novel excipient (CMEC) based gastro retentive floating tablets of propranolol HCl and it's in vivo buoyancy characterization in healthy human volunteers  

PubMed Central

The objective of the present investigation is to formulate gastro retentive floating drug delivery systems (GRFDDS) of propranolol HCl by central composite design and to study the effect of formulation variables on floating lag time, D1hr (% drug release at 1?hr) and t90 (time required to release 90% of the drug). 3 factor central composite design was employed for the development of GRFDDS containing novel semi synthetic polymer carboxymethyl ethyl cellulose (CMEC) as a release retarding polymer. CMEC, sodium bicarbonate and Povidone concentrations were included as independent variables. The tablets were prepared by direct compression method and were evaluated for in vitro buoyancy and dissolution studies. From the polynomial model fitting statistical analysis, it was confirmed that the response floating lag time and D1hr is suggested to quadratic model and t90 is suggested to linear model. All the statistical formulations followed first order rate kinetics with non-Fickian diffusion mechanism. The desirability function was used to optimize the response variables, each having a different target, and the observed responses were highly agreed with experimental values. Statistically optimized formulation was characterized by FTIR and DSC studies and found no interactions between drug and polymer. The results demonstrate the feasibility of the model in the development of GRFDDS containing a propranolol HCl. Statistically optimized formulation was evaluated for in vivo buoyancy studies in healthy humans for both fed and fasted states. From the results, it was concluded that gastric residence time of the floating tablets were enhanced at fed stage but not in fasted state. PMID:23351981

2012-01-01

121

Statistical optimization of a novel excipient (CMEC) based gastro retentive floating tablets of propranolol HCl and it's in vivo buoyancy characterization in healthy human volunteers.  

PubMed

The objective of the present investigation is to formulate gastro retentive floating drug delivery systems (GRFDDS) of propranolol HCl by central composite design and to study the effect of formulation variables on floating lag time, D1hr (% drug release at 1?hr) and t90 (time required to release 90% of the drug). 3 factor central composite design was employed for the development of GRFDDS containing novel semi synthetic polymer carboxymethyl ethyl cellulose (CMEC) as a release retarding polymer. CMEC, sodium bicarbonate and Povidone concentrations were included as independent variables. The tablets were prepared by direct compression method and were evaluated for in vitro buoyancy and dissolution studies. From the polynomial model fitting statistical analysis, it was confirmed that the response floating lag time and D1hr is suggested to quadratic model and t90 is suggested to linear model. All the statistical formulations followed first order rate kinetics with non-Fickian diffusion mechanism. The desirability function was used to optimize the response variables, each having a different target, and the observed responses were highly agreed with experimental values. Statistically optimized formulation was characterized by FTIR and DSC studies and found no interactions between drug and polymer. The results demonstrate the feasibility of the model in the development of GRFDDS containing a propranolol HCl. Statistically optimized formulation was evaluated for in vivo buoyancy studies in healthy humans for both fed and fasted states. From the results, it was concluded that gastric residence time of the floating tablets were enhanced at fed stage but not in fasted state. PMID:23351981

Meka, Venkata Srikanth; Nali, Sreenivasa Rao; Songa, Ambedkar Sunil; Battu, Janaki Ram; Kolapalli, Venkata Ramana Murthy

2012-01-01

122

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

2005-01-01

123

Mechanism of drug release from an acrylic polymer-wax matrix tablet.  

PubMed

An acrylic polymer-wax matrix system was evaluated for oral sustained-release tablets of diphenhydramine HCl. A desirable release profile of diphenhydramine was achieved by incorporating Eudragit L in a carnauba wax matrix. In this polymer-wax system, carnauba wax maintained the integrity of the matrix, whereas Eudragit L slowly eroded in the matrix as the drug was released. Thus, the area-to-volume ratio of the tablet remained constant over the duration of the drug release. In vitro drug release studies were conducted at physiological pHs that exist in the gastrointestinal tract. Drug release rates decreased as the polymer:drug ratio increased from 1:2 to 2:1. The drug release rate was faster in pH 7.5 phosphate buffer than in 0.1 N HCl solution. The drug release from these polymer-wax matrices is described by a combination diffusion/erosion mechanism. Based on the typical pH encountered in intestinal fluids, complete dissolution of the drug and polymer at pH 7.5 in 8-10 h would ensure good bioavailability of the drug following oral administration. PMID:9120808

Huang, H P; Mehta, S C; Radebaugh, G W; Fawzi, M B

1994-06-01

124

Xanthan and galactomannan (from M. scabrella) matrix tablets for oral controlled delivery of theophylline.  

PubMed

Directly compressed theophylline tablets, containing commercial xanthan (X) (Keltrol) and a highly hydrophilic galactomannan (G) from the seeds of Mimosa scabrella (a brazilian leguminous tree called bracatinga) as release-controlling agents, were obtained. Gums were used at 4, 8, 12.5 and 25% (w/w), either alone or in mixture (X:G 1:1). During galactomannan extraction process, the biopolymer was dried in a scale up, by vacuum oven (VO) or spray dryer (SD). The in vitro drug release was evaluated at different time intervals during 8 h using apparatus 1 (USP 26) at 100 rpm. The pH of the dissolution medium (1.4) was changed to 4.0 and 6.8 after 2 and 3 h, respectively. Tablets containing G(SD) resulted in more uniform drug release than G(VO) ones, due to their smaller particle size. The drug release decreased with the increase of polymer concentration and all formulations at 25% w/w of gums showed excessive sustained release effect. The matrices made with alone X showed higher drug retention for all concentrations, compared with G matrices that released the drug too fast. The XG matrices were able to produce near zero-order drug release. The XG(SD) 8% tablets provided the required release rate (about 90% at the end of 8 h), with zero-order release kinetics. Tablets containing G(VO) in low concentration showed a complete erosion, while the others demonstrated fast hydration and swelling in contact with the dissolution medium. The release mechanism was a combination of diffusion and relaxation. The relative importance of these two processes varied with matrix composition. The XG(SD) 8% matrix showed higher contribution of polymer relaxation. PMID:15885450

Vendruscolo, C W; Andreazza, I F; Ganter, J L M S; Ferrero, C; Bresolin, T M B

2005-05-30

125

Drug release-modulating mechanism of hydrophilic hydroxypropylmethylcellulose matrix tablets: distribution of atoms and carrier and texture analysis.  

PubMed

Although release profiles of drug from hydrophilic matrices have been well recognized, the visual distribution of hydroxypropylmethylcellulose (HPMC) and atoms inside of internal structures of hydrophilic HPMC matrices has not been characterized. In this paper, drug release mechanism from HPMC matrix tablet was investigated based on the release behaviors of HPMC, physical properties of gelled HPMC tablet and atomic distributions of formulation components using diverse instruments. A matrix tablet consisting of hydroxypropyl methylcellulose (HPMC 6, 4,000 and 100,000 mPa·s), chlorpheniramine maleate (CPM) as a model and fumed silicon dioxide (Aerosil(®) 200) was prepared via direct compression. The distribution of atoms and HPMC imaging were characterized using scanning electron microscope (SEM)/ energy-dispersive X-ray spectroscopy (EDX), and near-infrared (NIR) analysis, respectively as a function of time. A texture analyzer was also used to characterize the thickness and maintenance of gel layer of HPMC matrix tablet. The HPMC matrix tablets showed Higuchi release kinetics with no lag time against the square root of time. High viscosity grades of HPMC gave retarded release rate because of the greater swelling and gel thickness as characterized by texture analyzer. According to the NIR imaging, low-viscosity-grade HPMC (6 mPa·s) quickly leached out onto the surface of the tablet, while the high-viscosity-grade HPMC (4000 mPa·s) formed much thicker gel layer around the tablet and maintained longer via slow erosion, resulting in retarded drug release. The atomic distribution of the drug (chlorine, carbon, oxygen), HPMC (carbon, oxygen) and silicon dioxide (silica, oxygen) and NIR imaging of HPMC corresponded with the dissolution behaviors of drug as a function of time. The use of imaging and texture analyses could be applicable to explain the release- modulating mechanism of hydrophilic HPMC matrix tablets. PMID:23855499

Park, Jun-Bom; Lim, Jisung; Kang, Chin-Yang; Lee, Beom-Jin

2013-12-01

126

Zero-order release of aspirin, theophylline and atenolol in water from novel methylcellulose glutarate matrix tablets.  

PubMed

A novel hydrocolloidal polymer, methylcellulose glutarate (MC-GA), was prepared by esterifying methylcellulose with glutaric anhydride. The formation of ester was confirmed by FTIR and NMR spectroscopy, DSC and elemental analysis. The physicochemical properties such as, rate of swelling in water, viscosity and hygroscopicity of MC-GA were determined and compared with those of methycellulose A (MC). Aspirin, theophylline and atenolol tablets were compacted on a Carver press using the wet granulation method. Each tablet contained: 200 mg active, 80 mg anhydrous lactose, 8 mg povidone, 4 mg magnesium stearate, 4 mg talc, 50mg MC or MC-GA (drug-to-polymer ratio, 4:1). Contrary to the first-order release profile of all the drugs from the MC matrix tablets, a zero-order release was obtained from the MC-GA matrix tablets in water. PMID:16621361

Khairuzzaman, A; Ahmed, S U; Savva, M; Patel, N K

2006-08-01

127

Introduction of Sustained Release Opipramol Dihydrochloride Matrix Tablets as a New Approach in the Treatment of Depressive Disorders  

PubMed Central

Opipramol 2-HCl (OP) is used for therapy of general somatoform and anxiety disorders. Conventional tablets in the market contain 50 mg OP to be used once or up to three times a day in effective treatment of depression in mild. In case of serious depressive disorders, OP may be administired up to 300 mg a day. Decrease in frequency of high dose administration via sustained drug release would reduce incidence of symptoms of intoxication in long-term use of OP. With this aim, OP matrix tablets containing 100 mg were prepared by direct compression method to be used once a day to provide patient compliance and constant blood level, consequently to decrease side effects. Two concentrations of polymers (10% and 20%): hydroxypropylcellulose (HPC) and hydroxypropyl methylcellulose (HPMC), sodium alginate (NaAlg), xanthan gum (XG) and Carbopol®941 (C941) were used in preparation of matrix tablets. Drug release study were performed in distilled water, pH1.2 HCl buffer and pH7.4 phosphate buffer solutions according to the Method II in USP 29. Two commercial tablets containing 50 mg OP available in Turkish market were used for comparison. Kinetic models of release patterns from tablets were evaluated. Drug release was displayed slower to faster pattern in order of formulations containing C941, HPMC and HPC. Drug release was significantly faster in tablets of 10% polymers than those of 20%. NaAlg and XG were insufficient to sustain drug release. The most sustaining drug release effect at the lowest polymer concentration was obtained with C941. Drug release from matrix tablets containing 10% C941 was determined as 58.2%, 52.4 and 57.0% in related dissolution mediums above after 8 hours, respectively. However, HPMC and HPC sustained drug release at 20% concentration. As a result, Carbopol® 941, HPMC and HPC can be suggested as suitable to prepare matrix tablets of OP. PMID:23675002

Gonullu, Umit; Uner, Melike; Yener, Gulgun; Alt?nkurt, Turan

2006-01-01

128

Sustained-release matrix tablets of metformin hydrochloride in combination with triacetyl-beta-cyclodextrin.  

PubMed

The low bioavailability and short half-life of metformin hydrochloride (MH) make the development of sustained-release forms desirable. However, drug absorption is limited to the upper gastrointestinal (GI) tract, thus requiring suitable delivery systems providing complete release during stomach-to-jejunum transit. This study was undertaken to develop a MH sustained-release formulation in compliance with these requirements. The strategy proposed is based on direct-compressed matrix tablets consisting of a combination of MH with the hydrophobic triacetyl-beta-cyclodextrin (TAbetaCD), dispersed in a polymeric material. Different polymers were tested as excipients, i.e. hydroxypropylmethylcellulose, xanthan gum, chitosan, ethylcellulose, Eudragit L100-55, and Precirol. Compatibility among the formulation components was assessed by DSC analysis. All the tablets were examined for drug release pattern in simulated gastric and jejunal fluids used in sequence to mimic the GI transit. Release studies demonstrated that blends of a hydrophobic swelling polymer (hydroxypropylmethylcellulose or chitosan) with a pH-dependent one (Eudragit L100-55) were more useful than single polymers in controlling drug release. Moreover, the main role played by the MH-TAbetaCD system preparation method (i.e. grinding or spray-drying) in determining the behaviour of the final formulation was evidenced. In fact, for a given matrix-tablet composition, different sustained-release effects were obtained by varying the relative amounts of MH-TAbetaCD as ground or spray-dried product. In particular, the 1:1 (w/w) blend of such systems, dispersed in a Eudragit-chitosan polymeric matrix, fully achieved the prefixed goal, giving about 30% released drug after 2h at gastric pH, and overcoming 90% released drug within the subsequent 3h in jejunal fluid. PMID:17616379

Corti, Giovanna; Cirri, Marzia; Maestrelli, Francesca; Mennini, Natascia; Mura, Paola

2008-02-01

129

Predictability of drug release from water-insoluble polymeric matrix tablets.  

PubMed

The purpose of this study was to extend the predictability of an established solution of Fick's second law of diffusion with formulation-relevant parameters and including percolation theory. Kollidon SR (polyvinyl acetate/polyvinylpyrrolidone, 80/20 w/w) matrix tablets with various porosities (10-30% v/v) containing model drugs with different solubilities (Cs=10-170 mg/ml) and in different amounts (A=10-90% w/w) were prepared by direct compression and characterized by drug release and mass loss studies. Drug release was fitted to Fick's second law to obtain the apparent diffusion coefficient. Its changes were correlated with the total porosity of the matrix and the solubility of the drug. The apparent diffusion coefficient was best described by a cumulative normal distribution over the range of total porosities. The mean of the distribution coincided with the polymer percolation threshold, and the minimum and maximum of the distribution were represented by the diffusion coefficient in pore-free polymer and in aqueous medium, respectively. The derived model was verified, and the applicability further extended to a drug solubility range of 10-1000 mg/ml. The developed mathematical model accurately describes and predicts drug release from Kollidon SR matrix tablets. It can efficiently reduce experimental trials during formulation development. PMID:23985775

Grund, Julia; Körber, Martin; Bodmeier, Roland

2013-11-01

130

Application of dynamic neural networks in the modeling of drug release from polyethylene oxide matrix tablets.  

PubMed

The main objective of this study was to demonstrate the possible use of dynamic neural networks to model diclofenac sodium release from polyethylene oxide hydrophilic matrix tablets. High and low molecular weight polymers in the range of 0.9-5 x 10(6) have been used as matrix forming materials and 12 different formulations were prepared for each polymer. Matrix tablets were made by direct compression method. Fractions of polymer and compression force have been selected as most influential factors on diclofenac sodium release profile. In vitro dissolution profile has been treated as time series using dynamic neural networks. Dynamic networks are expected to be advantageous in the modeling of drug release. Networks of different topologies have been constructed in order to obtain precise prediction of release profiles for test formulations. Short-term and long-term memory structures have been included in the design of network making it possible to treat dissolution profiles as time series. The ability of network to model drug release has been assessed by the determination of correlation between predicted and experimentally obtained data. Calculated difference (f(1)) and similarity (f(2)) factors indicate that dynamic networks are capable of accurate predictions. Dynamic neural networks were compared to most frequently used static network, multi-layered perceptron, and superiority of dynamic networks has been demonstrated. The study also demonstrated differences between the used polyethylene oxide polymers in respect to drug release and suggests explanations for the obtained results. PMID:19632323

Petrovi?, Jelena; Ibri?, Svetlana; Betz, Gabriele; Parojci?, Jelena; Duri?, Zorica

2009-09-10

131

Prolonged release matrix tablet of pyridostigmine bromide: formulation and optimization using statistical methods.  

PubMed

The aim of this study was to design and optimize a prolonged release matrix formulation of pyridostigmine bromide, an effective drug in myasthenia gravis and poisoning with nerve gas, using hydrophilic - hydrophobic polymers via D-optimal experimental design. HPMC and carnauba wax as retarding agents as well as tricalcium phosphate were used in matrix formulation and considered as independent variables. Tablets were prepared by wet granulation technique and the percentage of drug released at 1 (Y(1)), 4 (Y(2)) and 8 (Y(3)) hours were considered as dependent variables (responses) in this investigation. These experimental responses were best fitted for the cubic, cubic and linear models, respectively. The optimal formulation obtained in this study, consisted of 12.8 % HPMC, 24.4 % carnauba wax and 26.7 % tricalcium phosphate, had a suitable prolonged release behavior followed by Higuchi model in which observed and predicted values were very close. The study revealed that D-optimal design could facilitate the optimization of prolonged release matrix tablet containing pyridostigmine bromide. Accelerated stability studies confirmed that the optimized formulation remains unchanged after exposing in stability conditions for six months. PMID:22713949

Bolourchian, Noushin; Rangchian, Maryam; Foroutan, Seyed Mohsen

2012-07-01

132

Preparation and in vitro evaluation of guar gum based triple-layer matrix tablet of diclofenac sodium.  

PubMed

The objective of the present study was to design an oral controlled drug delivery system for sparingly soluble diclofenac sodium (DCL) using guar gum as triple-layer matrix tablets. Matrix tablet granules containing 30% (D1), 40% (D2) or 50% (D3) of guar gum were prepared by the conventional wet granulation technique. Matrix tablets of diclofenac sodium were prepared by compressing three layers one by one. Centre layer of sandwich like structure was incorporated with matrix granules containing DCL which was covered on either side by guar gum granule layers containing either 70, 80 or 87% of guar gum as release retardant layers. The tablets were evaluated for hardness, thickness, drug content, and drug release studies. To ascertain the kinetics of drug release, the dissolution profiles were fitted to various mathematical models. The in vitro drug release from proposed system was best explained by the Hopfenberg model indicating that the release of drug from tablets displayed heterogeneous erosion. D3G3, containing 87% of guar gum in guar gum layers and 50% of guar gum in DCL matrix granule layer was found to provide the release rate for prolonged period of time. The results clearly indicate that guar gum could be a potential hydrophilic carrier in the development of oral controlled drug delivery systems. PMID:23181081

Chavda, H V; Patel, M S; Patel, C N

2012-01-01

133

Formulation and Evaluation of Hydroxypropyl Methylcellulose-based Controlled Release Matrix Tablets for Theophylline.  

PubMed

The objectives of the study were to formulate hydroxypropyl methyl cellulose-based controlled release matrix tablets for theophylline with varying drug:polymer ratios (1:1 and 1:2) and differing tablet hardness (5, 6 and 7 kg/cm(2)), and to evaluate the tablet's physico-chemical properties such as hardness, uniformity of weight, friability, drug content and in vitro drug release. Initially, granules were made by wet granulation technique and evaluated for angle of repose, bulk density, tapped density, bulkiness, compressibility index and hausner ratio. The results indicate good flow property of the granules and thus, the evaluated tablet physical properties were within the acceptable limits. The FT-IR study for the F-6 formulation showed that there was no interaction between the drug and the polymer. In vitro release studies were performed using Disso-2000 (paddle method) in 900 ml of pH 7.4 at 50 rpm. The result indicated that at high drug:polymer ratio (1:2) and hardness value 7 kg/cm(2), prolonged drug release was observed than the low drug: polymer ratio (1:1) and hardness values (5 and 6 kg/cm(2)). The release kinetics was found to follow korsmeyers-peppas model and the mechanism of drug release was by non-fickian or anomalous diffusion. The F-6 formulation was chosen for stability studies. F-6 formulation was stable when it was kept at different temperatures for a period of 6 months. PMID:22707833

Sekharan, T Raja; Palanichamy, S; Tamilvanan, S; Shanmuganathan, S; Thirupathi, A Thanga

2011-07-01

134

Matrix tablets of carrageenans. II. Release behavior and effect of added cations.  

PubMed

Carrageenans are hydrocolloids in the rubbery state at standard conditions. They are useful excipients for controlled-release tablets. Three carrageenans, two kappa-carrageenans (Gelcarin GP-812 NF and GP-911 NF) and one iota-carrageenan (Gelcarin GP-379 NF), are analyzed regarding their release behavior in combination with sorption, swelling, and rheology. The iota-carrageenan has a higher substitution by sulfate groups. The kappa-carrageenan Gelcarin GP-812 NF contains a small amount of potassium chloride left over from processing. Water sorption of the pure materials was studied gravimetrically, and the rheology of different solutions (2% and 5% w/w) was studied by cup-cylinder rotation viscosimetry. Swelling was determined as the vertical expansion of the tablets with a specially designed swelling apparatus. Drug release from the tablets was performed by the USP paddle method for 8 hr. The data indicate that drug release increases when water sorption and swelling extent decrease and as viscosity increases. The order of release is nearly zero-order kinetics for theophylline monohydrate, a nonionic drug. Diffusion of the anionic drug diclofenac sodium is anomalous. In addition, the influence of the added salts potassium and calcium chloride on swelling and release was studied. Before tableting, physical mixtures of these salts with and without theophylline monohydrate were prepared. Swelling and release change in the same order, but this is only valid when the ionic interactions responsible for this are strong enough. Besides this, physical mixing of salts with the carrageenans can result in an increased release of drug caused by decreased cohesion of the matrix during drug release, mainly for calcium chloride. PMID:10071827

Picker, K M

1999-03-01

135

In vitro release kinetics and bioavailability of gastroretentive cinnarizine hydrochloride tablet.  

PubMed

An oral sustained release dosage form of cinnarizine HCl (CNZ) based on gastric floating matrix tablets was studied. The release of CNZ from different floating matrix formulations containing four viscosity grades of hydroxypropyl methylcellulose, sodium alginate or polyethylene oxide, and gas-forming agent (sodium bicarbonate or calcium carbonate) was studied in simulated gastric fluid (pH 1.2). CNZ release data from the matrix tablets were analyzed kinetically using Higuchi, Peppas, Weibull, and Vergnaud models. From water uptake, matrix erosion studies, and drug release data, the overall release mechanism can be explained as a result of rapid hydration of polymer on the surface of the floating tablet and formation of a gel layer surrounding the matrix that controls water penetration into its center. On the basis of in vitro release data, batch HP1 (CNZ, HPMC-K100LV, SBC, LTS, and MgS) was subjected to bioavailability studies in rabbits and was compared with CNZ suspension. It was concluded that the greater bioavailability of HP1 was due to its longer retention in the gastric environment of the test animal. Batch no. HP1 of floating tablet in rabbits demonstrated that the floating tablet CNZ could be a 24-h sustained release formulation. PMID:20182827

Nagarwal, Ramesh C; Ridhurkar, Devendra N; Pandit, J K

2010-03-01

136

Formulation and in vitro evaluation of Eudragit S-100 coated naproxen matrix tablets for colon-targeted drug delivery system  

PubMed Central

The purpose of the present investigation was to prepare matrix tablets of naproxen using a hydrophobic polymer, i.e., Eudragit RLPO, RSPO, and combination of both, by wet granulation method. The tablets were further coated with different concentrations of Eudragit S-100, a pH-sensitive polymer, by dip immerse method. In vitro drug release studies of tablets were carried out in different dissolution media, i.e., 0.1 N HCl (pH 1.2), phosphate buffers pH 6.8 and 7.4, with or without rat cecal content. The swelling studies of the optimized formulation were carried out. The physicochemical parameters of all the formulations were found to be in compliance with the pharmacopoeial standards. The effect of dissolution medium on the surface of matrix tablet was determined by using Scanning Electron Microscopy technique. The stability studies of all formulations were performed as per ICH guidelines. The results demonstrated that the tablets coated with Eudragit S-100 (2% w/v) showed a sustained release of 94.67% for 24 h, but drug release increased to about 98.60% for 24 h in the presence of rat cecal content while the uncoated tablets released the drug within 5 h. With regard to release kinetics, the data were best fitted with the Higuchi model with non-Fickian drug release kinetics mechanism. The stability studies of tablets showed less degradation during accelerated and room temperature storage conditions for 6 months. The enteric-coated Eudragit S-100 coated matrix tablets of naproxen showed promising site-specific drug delivery in the colon region. PMID:23662280

Mehta, Rohit; Chawla, Anuj; Sharma, Pooja; Pawar, Pravin

2013-01-01

137

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

138

Drug Release Kinetics and Front Movement in Matrix Tablets Containing Diltiazem or Metoprolol/?-Carrageenan Complexes  

PubMed Central

In this work we investigated the moving boundaries and the associated drug release kinetics in matrix tablets prepared with two complexes between ?-carrageenan and two soluble model drugs, namely, diltiazem HCl and metoprolol tartrate aiming at clarifying the role played by drug/polymer interaction on the water uptake, swelling, drug dissolution, and drug release performance of the matrix. The two studied complexes released the drug with different mechanism indicating two different drug/polymer interaction strengths. The comparison between the drug release behaviour of the complexes and the relevant physical mixtures indicates that diltiazem gave rise to a less soluble and more stable complex with carrageenan than metoprolol. The less stable metoprolol complex afforded an erodible matrix, whereas the stronger interaction between diltiazem and carrageenan resulted in a poorly soluble, slowly dissolving matrix. It was concluded that the different stability of the studied complexes affords two distinct drug delivery systems: in the case of MTP, the dissociation of the complex, as a consequence of the interaction with water, affords a classical soluble matrix type delivery system; in the case of DTZ, the dissolving/diffusing species is the complex itself because of the very strong interaction between the drug and the polymer. PMID:25045689

Bonferoni, Maria Cristina; Colombo, Paolo; Zanelotti, Laura; Caramella, Carla

2014-01-01

139

Formulation and Evaluation of a Novel Matrix-Type Orally Disintegrating Ibuprofen Tablet  

PubMed Central

Orally disintegrating tablets (ODTs) are capable of turning quickly into a liquid dosage form in contact with the saliva, thus possessing the advantages of both the solid dosage forms particularly stability and liquid dosage forms specially ease of swallowing and pre-gastric absorption of drug. The aim of this study was to prepare a novel matrix-type buccal fast disintegrating ibuprofen tablet formulation using special polymers, water soluble excipients, super-disintegrants and quickly soluble granules. For this purpose different tablet formulations of ibuprofen were prepared. The amount of ibuprofen in each formulation was 100 mg. Eight groups of formulation were prepared (A-H series), accounting for a total number of 45 formulations. Formulations prepared were examined in terms of different physicochemical tests including powder/granule flowability, appearance, thickness, uniformity of weight, hardness, friability and disintegration time. Results of formulation F22a (in series F), was found to be acceptable, making it the chosen formulation for further studies. Then, by adding various flavorants and sweeteners to this formulation, complementary series of formulations, named G and H, were prepared. Following the comparison of their taste with each other through asking 10 volunteers, the most suitable formulation regarding the taste, being formulation F22s, was chosen as the ultimate formulation. This formulation had PVP, ibuprofen and croscarmellose as the intra-granular components and xylitol and saccharin as the extra-granular ingredients. Formulation F22s was found to be acceptable in terms of physicochemical tests conducted, showing quick disintegration within the buccal cavity, appropriate hardness and rather low friability. Hence formulation F22s was selected as the final formulation. PMID:24250378

Tayebi, Hoda; Mortazavi, Seyed Alireza

2011-01-01

140

Impact of salt form and molecular weight of chitosan on swelling and drug release from chitosan matrix tablets.  

PubMed

Magnetic resonance imaging (MRI) and gravimetric techniques were used to assess swelling and erosion behaviors of hydrophilic matrix tablets made of chitosan. The impact of salt form, molecular weight (MW) and dissolution medium on swelling behavior and drug (theophylline) release was studied. The matrix tablets made of chitosan glycolate (CGY) showed the greatest swelling in both acid and neutral media, compared to chitosan aspartate, chitosan glutamate and chitosan lactate. MRI illustrated that swelling region of CGY in both media was not different in the first 100 min but glassy region (dry core) in 0.1N HCl was less than in pH 6.8 buffer. The tablets prepared from chitosan with high MW swelled greater than those of low MW. Moreover, CGY can delay drug release in the acid condition due to thick swollen gel and low erosion rate. Therefore, CGY may be suitably applied as sustained drug release polymer or enteric coating material. PMID:23769512

Huanbutta, Kampanart; Cheewatanakornkool, Kamonrak; Terada, Katsuhide; Nunthanid, Jurairat; Sriamornsak, Pornsak

2013-08-14

141

In Vitro Release Kinetics and Bioavailability of Gastroretentive Cinnarizine Hydrochloride Tablet  

Microsoft Academic Search

An oral sustained release dosage form of cinnarizine HCl (CNZ) based on gastric floating matrix tablets was studied. The release\\u000a of CNZ from different floating matrix formulations containing four viscosity grades of hydroxypropyl methylcellulose, sodium\\u000a alginate or polyethylene oxide, and gas-forming agent (sodium bicarbonate or calcium carbonate) was studied in simulated gastric\\u000a fluid (pH 1.2). CNZ release data from the

Ramesh C. Nagarwal; Devendra N. Ridhurkar; J. K. Pandit

2010-01-01

142

Comparative study of propranolol hydrochloride release from matrix tablets with KollidonSR or hydroxy propyl methyl cellulose.  

PubMed

The release of propranolol hydrochloride from matrix tablets with hydroxy propyl methyl cellulose (HPMC K15M) or KollidonSR at different concentrations was investigated with a view to developing twice daily sustained release dosage form. A hydrophilic matrix-based tablet using different concentrations of HPMC K15M or KollidonSR was developed using direct compression technique to contain 80 mg of propranolol hydrochloride. The resulting matrix tablets prepared with HPMC K15M or KollidonSR fulfilled all the official requirements of tablet dosage forms. Formulations were evaluated for the release of propranolol hydrochloride over a period of 12 h in pH 6.8 phosphate buffer using USP type II dissolution apparatus. Propranolol hydrochloride and pure KollidonSR or HPMC K15M compatibility interactions was investigated by using Fourier-transform infrared (FTIR) spectroscopy and differential scanning calorimetry (DSC). FTIR spectroscopic and DSC studies revealed that there was no well defined chemical interaction between propranolol hydrochloride with KollidonSR or HPMC K15M. Tablets were exposed to 40 degrees C/75% of RH in open disc for stability. The in vitro drug release study revealed that HPMC K15 at a concentration of 40% of the dosage form weight was able to control the release of propranolol hydrochloride for 12 h, exhibit non-Fickian diffusion with first-order release kinetics where as at 40% KollidonSR same dosage forms show zero-order release kinetics. In conclusion, the in vitro release profile and the mathematical models indicate that release of propranolol hydrochloride can be effectively controlled from a single tablet using HPMC K15M or KollidonSR matrix system. PMID:18459050

Sahoo, J; Murthy, P N; Biswal, S; Sahoo, S K; Mahapatra, A K

2008-01-01

143

Assay of amoxicillin sustained release from matrix tablets containing different proportions of Carbopol 971P NF.  

PubMed

The sustained release of amoxicillin is desired because of its short biological half-life. Particularly to treat Helicobacter pylori infections, the sustained release is desired to be confined to the upper gastrointestinal tract. In vitro dissolution of amoxicillin has been evaluated utilizing a direct UV-absorption method. However, UV-absorption has been reported as not useful to determine amoxicillin in acidic dissolution test medium. To clarify the suitability of the assay method, the stability and dissolution behavior of amoxicillin sustained release tablets was determined by HPLC, iodometric titration and UV-absorption. Stability of amoxicillin studied under dissolution test conditions of pH 1.2, 37 degrees C and 50 rpm and determined by HPLC and titration showed considerable degradation of amoxicillin. On the other hand, the UV-absorption increased progressively as amoxicillin degradation proceeded. Amoxicillin release curves determined by different analytical methods show different release profiles, which can be corrected for amoxicillin degradation and change in the UV-absorption to produce similar dissolution results. Release curves determined by UV-absorption and obtained from tablets containing 1017 mg amoxicillin trihydrate and Carbopol 971P NF in a range from 180 to 680 mg showed increasing values of the exponent indicative of the release mechanism (n) and decreasing release constant values (k) as the matrix polymer content increased. The release constant (k) and the exponent (n) were found to be logarithmically related. PMID:15010136

Tapia-Albarran, Manuel; Villafuerte-Robles, Leopoldo

2004-04-01

144

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

145

In vitro release of sodium diclofenac from a central core matrix tablet aimed for colonic drug delivery  

Microsoft Academic Search

The present study was aimed at developing a novel sodium diclofenac formulation for colonic release. The proposed delivery system consisted in a polymeric matrix tablet containing a drug central core purposely designed for obtaining a time-controlled release profile characterized by an initial phase of lag-time followed by a controlled release phase, according to zero order kinetics. The spheric central core

Mar??a Luisa González-Rodr??guez; Francesca Maestrelli; Paola Mura; Antonio Mar??a Rabasco

2003-01-01

146

Microenvironmental pH and microviscosity inside pH-controlled matrix tablets: An EPR imaging study  

Microsoft Academic Search

Incorporation of pH modifiers is a commonly used strategy to enhance the dissolution rate of weakly basic drugs from sustained release solid dosage forms. Electron paramagnetic resonance imaging (EPRI) was applied to spatially monitor pHM and the rotational correlation time (?R), a parameter which is closely related to the surrounding microviscosity inside HPMC (hydroxypropylmethylcellulose) matrix tablets. Fumaric, citric, and succinic

Stefanie Siepe; Werner Herrmann; Hans-Hubert Borchert; Barbara Lueckel; Andrea Kramer; Angelika Ries; Robert Gurny

2006-01-01

147

The effect of polyion complex formation on in vitro/in vivo correlation of hydrophilic matrix tablets.  

PubMed

The aim of this study was to investigate the effects of polyion complex formation on in vivo performance of hydrophilic matrix tablets. Three kinds of controlled release theophylline tablets were prepared by direct compression using carboxymethyldextran (CMD), a mixture of CMD and [2-(diethylamino)ethyl]dextran (EA), and a mixture of dextran sulfate (DS) and EA. According to a conventional dissolution test, in vitro drug release profiles of these tablets were similar to each other. In vivo absorption profiles of theophylline after oral administration to beagle dogs, however, were quite different and were not consistent with in vitro release profiles. Thus, we applied a modified in vitro release test considering destructive forces. An excellent in vitro/in vivo correlation was obtained in the cases of CMD/EA- and DS/EA-tablets. The results suggested that the drug was released constantly in the overall gastrointestinal tract, and even in the colon. Then, hydrophilic matrices were characterized by swelling rate, matrix density and strength in a wet state. DS/EA-tablets showed limited swelling, higher density and a larger value of wet strength than the others. These findings indicated that polyion complex formation in gel layer contributes to prevent over-swelling and strengthen the wetted matrices. PMID:12932710

Miyazaki, Yasunori; Yakou, Shigeru; Nagai, Tsuneji; Takayama, Kozo

2003-09-01

148

Release from or through a wax matrix system. V. Applicability of the square-root time law equation for release from a wax matrix tablet.  

PubMed

To obtain basic and clear release properties, wax matrix tablets were prepared from a physical mixture of drug and wax powder at a fixed mixing ratio. Properties of release from the single flat-faced surface, curved side surface, and/or whole surface of the wax matrix tablet were examined. Then tortuosity and the applicability of Higuchi's square-root time law equation were examined. The Higuchi equation well analyzed the release processes of different release manners. However, the region fitted to the Higuchi equation differed with the release manner. Tortuosity obtained with release from the single flat-faced surface and curved side surface was comparable with that obtained with the release from a reservoir device tablet, whereas tortuosity obtained with release from the whole surface was larger. As the wax matrix tablets were prepared at a fixed mixing ratio, their internal structures should be similar. Therefore changes in the matrix volume or volume fraction with release were examined, and an extra volume where dissolved drug stray becomes large with release time in the case of release from the whole surface. These factors should be taken into account for evaluation of applicability and release properties. Furthermore, the entire release process should be analyzed using a combination of the square-root time law and other suitable equations in accordance with release manner or condition. PMID:12913226

Yonezawa, Yorinobu; Ishida, Sumio; Sunada, Hisakazu

2003-08-01

149

Comparative in vitro and in vivo evaluation of matrix, osmotic matrix, and osmotic pump tablets for controlled delivery of diclofenac sodium  

Microsoft Academic Search

The aim of this investigation was preparation and comparative evaluation of fabricated matrix (FM), osmotic matrix (OM), and\\u000a osmotic pump (OP) tablets for controlled delivery of diclofenac sodium (DS). All formulations were evaluated for various physical\\u000a parameters, and in vitro studies were performed on USP 24 dissolution apparatus II in pH 7.4 buffer and distilled water. In\\u000a vivo studies were

Meena Rani; Brahmeshwar Mishra

2004-01-01

150

EFFECTS OF POLYMER TYPE, POLYMER:DIRECT TABLETTING AGENT RATIO AND TABLETTING METHOD ON VERAPAMIL HYDROCHLORIDE EXTENDED RELEASE FROM HYDROXYPROPYLMETHYLCELLULOSE MATRIX TABLETS POL?MER T?P?N?N, POL?MER:DO?RUDAN TABLETLEME AJANI ORANININ VE TABLETLEME YÖNTEM?N?N H?DROKS?PROP?LMET?LSELÜLOZ YAPILI MATR?S TABLETLERDEN VERAPAM?L H?DROKLORÜR`ÜN UZATILMI? SALIMI ÜZER?NE ETK?LER?  

Microsoft Academic Search

This work has focused on the effects of different hydroxypropylmethylcellulose (HPMC) types and HPMC:direct tabletting agent (DC-agent) ratio on Verapamil Hydrochloride (VRP HCl) release from monolayered and three-layered matrix tablets. Investigated polymers were Methocel K100LV, K15M, K100M and DC-agent was Ludipress® LCE. Eight formulations were prepared as monolayered matrix tablets while four formulations were prepared as three-layered matrix tablets by

Müge KILIÇARSLAN; Nilüfer YÜKSEL; Tamer BAYKARA

151

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

2007-07-18

152

Application of mixture experimental design in the formulation and optimization of matrix tablets containing carbomer and hydroxy-propylmethylcellulose.  

PubMed

Using mixture experimental design, the effect of carbomer (Carbopol((R)) 971P NF) and hydroxypropylmethylcellulose (Methocel((R)) K100M or Methocel((R)) K4M) combination on the release profile and on the mechanism of drug liberation from matrix tablet was investigated. The numerical optimization procedure was also applied to establish and obtain formulation with desired drug release. The amount of TP released, release rate and mechanism varied with carbomer ratio in total matrix and HPMC viscosity. Increasing carbomer fractions led to a decrease in drug release. Anomalous diffusion was found in all matrices containing carbomer, while Case - II transport was predominant for tablet based on HPMC only. The predicted and obtained profiles for optimized formulations showed similarity. Those results indicate that Simplex Lattice Mixture experimental design and numerical optimization procedure can be applied during development to obtain sustained release matrix formulation with desired release profile. PMID:20162406

Petrovic, Aleksandra; Cvetkovic, Nebojsa; Ibric, Svetlana; Trajkovic, Svetlana; Djuric, Zorica; Popadic, Dragica; Popovic, Radmila

2009-12-01

153

An innovative matrix controlling drug delivery produced by thermal treatment of DC tablets containing polycarbophil and ethylcellulose.  

PubMed

An innovative matrix, produced by thermal treatment on direct compression (DC) tablets containing polycarbophil (POL) and ethylcellulose (EC), identified as matrix forming polymers, and able to control the release of diltiazem hydrochloride, was developed. At pH 7.2, 72 ± 1.2% (w/w) of drug loaded was released in 25 h, mostly at constant rate. This swellable and unerodible matrix controls drug release by an anomalous transport mechanism. The modifications induced by the thermal treatment are irreversible and can be used to control and characterize the matrix. A 3-component constrained mixture design allowed the investigation of the experimental domain in which the matrix forms and the computation of a mathematical model that can be used to optimize the formulation properties. The release rate can be modulated (0.032-0.064% drug released/min) through the choice of suitable treatment conditions and tablet composition. The maximum amount of diltiazem hydrochloride released by zero-order kinetics, at the lowest release rate, occurs for POL:EC ratio in the range of 1:1-2:3 with 20-30% of diluent. The tablets are able to load up to 50% (w/w) of diltiazem hydrochloride without losing their properties. A stability study performed on a selected formulation containing DTZ showed stability for at least 2.7 years at RT conditions. PMID:24144954

Caviglioli, Gabriele; Baldassari, Sara; Cirrincione, Paola; Russo, Eleonora; Parodi, Brunella; Gatti, Paolo; Drava, Giuliana

2013-12-15

154

Effect of channeling agents on the release pattern of theophylline from kollidon SR based matrix tablets.  

PubMed

The purpose of the present study was to investigate the effect of channeling agent on the release profile of theophylline from Kollidon SR based matrix systems. Matrix tablets of theophylline using Kollidon SR which is plastic in nature were prepared by direct compression process. NaCl and PEG 1500 were used as channeling agents. Drug release study was evaluated for eight hours using USP 22 paddle-type dissolution apparatus using distilled water as the dissolution medium. The release mechanisms were explored and explained with zero order, Higuchi, first order and Korsmeyer equations. The release rate, extent and mechanisms were found to be governed by the type and content of the channeling agents. Increased rate and extent of the drug release were found by using higher content of channeling agent (42.49%) in the matrix due to increased porosity when compared with the formulation having no channeling agents. On the other hand decreased rate and extent of drug release were observed in the formulation having lower channeling agent content (19.76%). PEG 1500 ensures maximum release of drug from Kollidon SR than NaCl when other parameters were kept unchanged. It was found that type and amount of channeling agent significantly affect the time required for 50% of drug release (T50%), percentage drug release at 8 hours, release rate constant (K) and diffusion exponent (n). Kinetic modeling of dissolution profiles revealed drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport, which was mainly dependent on the type and amount of channeling agents. These studies indicate that the proper balance between a matrix forming agent and a channeling agent can produce a drug dissolution profile similar to a desired dissolution profile. PMID:19553179

Ibn Razzak, Md Shaikhul Millat; Khan, Ferdous; Hossain, Masuma; Khan, Md Ziaur Rahman; Azad, Mohammad Abul Kalam; Reza, Md Selim

2009-07-01

155

Simultaneous probing of swelling, erosion and dissolution by NMR-microimaging--effect of solubility of additives on HPMC matrix tablets.  

PubMed

Extensive studies of extended release tablets based on hydrophilic polymers have illuminated several aspects linked to their functionality. However, in some respects key factors affecting the mechanisms of release are yet unexplored. In the present study, a novel NMR-microimaging method has been used to study the influence of the solubility of additives in extended release hydroxypropyl methylcellulose (HPMC) matrix tablets. During the course of the tablet dissolution the movement of the swelling and erosion fronts were studied simultaneously to the release of both polymer and additives. Moreover, the focused beam reflectance measurement (FBRM) technology was for the first time assessed for both release and dissolution rate studies of poorly soluble particles. The studied formulations comprised solely HPMC, 40% HPMC and 60% mannitol (Cs=240 mg/ml) and 40% HPMC and 60% dicalcium phosphate (DCP) (Cs=0.05 mg/ml). The dissolution rate of the tablets was highest for the HPMC/mannitol formulation, followed by HPMC/DCP and plain HPMC tablet. A contrasting order was found regarding the degree and kinetics of swelling. The results were interpreted in light of how the mass transport in the gel layer is influenced by the solubility of additives. A mechanistic model, considering osmotic pressure gradient and the effective diffusion of the dissolution medium in the gel is proposed. PMID:19429415

Tajarobi, Farhad; Abrahmsén-Alami, Susanna; Carlsson, Anders S; Larsson, Anette

2009-05-12

156

Drug release behaviour from methyl methacrylate-starch matrix tablets: effect of polymer moisture content.  

PubMed

The aim of this work was to study the effect of the initial moisture content of the polymer on the tabletting and drug release behaviour of controlled release inert matrices elaborated with methyl methacrylate (MMA)-starch copolymers. The copolymers, obtained by free radical polymerisation and dried by two different methods (oven-drying or freeze-drying), were equilibrated at different relative humidities (0%, 25%, 50% and 75% RH) at room temperature. From these copolymers, matrix systems were directly compressed containing either a slightly water-soluble drug (anhydrous theophylline) or a freely water-soluble drug (salbutamol sulphate), and their compaction properties and in vitro dissolution profiles were evaluated. The release profiles were compared following model-independent methods, such as the Qt parameter and the similarity factor f2. Moreover, several kinetic models were employed to evaluate the possible changes in the release mechanism. For anhydrous theophylline, the initial moisture content of the copolymers did not affect the release characteristics from the inert matrices under study, and a typical Fickian diffusion mechanism was observed for the different formulations. However, in case of salbutamol sulphate, the presence of moisture might induce a fast drug dissolution, promoting the weakness of the matrix structure and hence, its partial disintegration. So, an "anomalous" mixed phenomenon of diffusion and erosion was found, influenced by the initial moisture content of the copolymer. PMID:17997292

Bravo-Osuna, I; Ferrero, C; Jiménez-Castellanos, M R

2008-05-01

157

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

2009-05-01

158

Sustained release of a water-soluble drug from alginate matrix tablets prepared by wet granulation method.  

PubMed

Alginate matrix tablet of diltiazem hydrochloride (DTZ), a water-soluble drug, was prepared using sodium alginate (SAL) and calcium gluconate (CG) by the conventional wet granulation method for sustained release of the drug. The effect of formulation variables like SAL/CG ratio, drug load, microenvironmental pH modulator, and processing variable like compression force on the extent of drug release was examined. The tablets prepared with 1:2 w/w ratio of SAL/CG produced the most sustained release of the drug extending up to 13.5 h. Above and below this ratio, the drug release was faster. The drug load and the hardness of the tablets produced minimal variation in drug release. The addition of alkaline or acidic microenvironmental modulators did not extend the release; instead, these excipients produced somewhat faster release of diltiazem. This study revealed that proper selection of SAL/CG ratio is important to produce alginate matrix tablet by wet granulation method for sustained release of DTZ. PMID:19911286

Mandal, Sanchita; Basu, Sanat Kumar; Sa, Biswanath

2009-01-01

159

Conceptuation, formulation and evaluation of sustained release floating tablets of captopril compression coated with gastric dispersible hydrochlorothiazide using 23 factorial design  

PubMed Central

Ambulatory blood pressure monitoring is regarded as the gold standard for hypertensive therapy in non-dipping hypertension patients. A novel compression coated formulation of captopril and hydrochlorothiazide (HCTZ) was developed in order to improve the efficacy of antihypertensive therapy considering the half-life of both drugs. The synergistic action using combination therapy can be effectively achieved by sustained release captopril (t1/2= 2.5 h) and fast releasing HCTZ (average t1/2= 9.5 h). The sustained release floating tablets of captopril were prepared by using 23 factorial design by employing three polymers i.e., ethyl cellulose (EC), carbopol and xanthan gum at two levels. The formulations (CF1-CF8) were optimized using analysis of variance for two response variables, buoyancy and T50%. Among the three polymers employed, the coefficients and P values for the response variable buoyancy and T50% using EC were found to be 3.824, 0.028 and 0.0196, 0.046 respectively. From the coefficients and P values for the two response variables, formulation CF2 was optimized, which contains EC polymer alone at a high level. The CF2 formulation was further compression coated with optimized gastric dispersible HCTZ layer (HF9). The compression coated tablet was further evaluated using drug release kinetics. The Q value of HCTZ layer is achieved within 20 min following first order release whereas the Q value of captopril was obtained at 6.5 h following Higuchi model, from which it is proved that rapid release HCTZ and slow release of captopril is achieved. The mechanism of drug release was analyzed using Peppas equation, which showed an n >0.90 confirming case II transportation mechanism for drug release. PMID:25006552

Sirisha, Pathuri Lakshmi; Babu, Govada Kishore; Babu, Puttagunta Srinivasa

2014-01-01

160

Conceptuation, formulation and evaluation of sustained release floating tablets of captopril compression coated with gastric dispersible hydrochlorothiazide using 2(3) factorial design.  

PubMed

Ambulatory blood pressure monitoring is regarded as the gold standard for hypertensive therapy in non-dipping hypertension patients. A novel compression coated formulation of captopril and hydrochlorothiazide (HCTZ) was developed in order to improve the efficacy of antihypertensive therapy considering the half-life of both drugs. The synergistic action using combination therapy can be effectively achieved by sustained release captopril (t1/2= 2.5 h) and fast releasing HCTZ (average t1/2= 9.5 h). The sustained release floating tablets of captopril were prepared by using 2(3) factorial design by employing three polymers i.e., ethyl cellulose (EC), carbopol and xanthan gum at two levels. The formulations (CF1-CF8) were optimized using analysis of variance for two response variables, buoyancy and T50%. Among the three polymers employed, the coefficients and P values for the response variable buoyancy and T50% using EC were found to be 3.824, 0.028 and 0.0196, 0.046 respectively. From the coefficients and P values for the two response variables, formulation CF2 was optimized, which contains EC polymer alone at a high level. The CF2 formulation was further compression coated with optimized gastric dispersible HCTZ layer (HF9). The compression coated tablet was further evaluated using drug release kinetics. The Q value of HCTZ layer is achieved within 20 min following first order release whereas the Q value of captopril was obtained at 6.5 h following Higuchi model, from which it is proved that rapid release HCTZ and slow release of captopril is achieved. The mechanism of drug release was analyzed using Peppas equation, which showed an n >0.90 confirming case II transportation mechanism for drug release. PMID:25006552

Sirisha, Pathuri Lakshmi; Babu, Govada Kishore; Babu, Puttagunta Srinivasa

2014-04-01

161

REPORT IN VITRO DISSOLUTION STUDIES OF DIFFERENT BRANDS OF SUSTAINED RELEASE DICLOFENAC SODIUM MATRIX TABLET AVAILABLE IN BANGLADESH  

Microsoft Academic Search

Commercially available national thirteen brands and three international brands of diclofenac sodium sustained release matrix tablets were studied in simulated gastric medium (pH 1.2) for 2 hours time period and simulated intestinal medium (pH 6.8) for 10 hours time period using USP reference dissolution apparatus. All the national and international brands complied with the USP in-vitro dissolution specification for drug

ABU SHARA; SHAMSUR ROUF

162

Application of mixture experimental design in the formulation and optimization of matrix tablets containing carbomer and hydroxy-propylmethylcellulose  

Microsoft Academic Search

Using mixture experimental design, the effect of carbomer (Carbopol® 971P NF) and hydroxypropylmethylcellulose (Methocel®\\u000a K100M or Methocel® K4M) combination on the release profile and on the mechanism of drug liberation from matrix tablet was\\u000a investigated. The numerical optimization procedure was also applied to establish and obtain formulation with desired drug\\u000a release. The amount of TP released, release rate and mechanism

Aleksandra Petrovic; Nebojsa Cvetkovic; Svetlana Ibric; Svetlana Trajkovic; Zorica Djuric; Dragica Popadic; Radmila Popovic

2009-01-01

163

The application of generalized regression neural network in the modeling and optimization of aspirin extended release tablets with Eudragit ® RS PO as matrix substance  

Microsoft Academic Search

The objective of this work is to use a generalized regression neural network (GRNN) in the design of extended-release aspirin tablets. As model formulations, 10 kinds of aspirin matrix tablets were prepared. Eudragit® RS PO was used as matrix substance. The amount of Eudragit® RS PO and compression pressure were selected as causal factors. In-vitro dissolution–time profiles at four different

Svetlana Ibri?; Milica Jovanovi?; Zorica Djuri?; Jelena Paroj?i?; Ljiljana Solomun

2002-01-01

164

Influence of Carbopol 71G-NF on the release of dextromethorphan hydrobromide from extended-release matrix tablets.  

PubMed

The objective of this study was to evaluate the potential of Carbopol(®) 71G-NF on the release of dextromethorphan hydrobromide (DM) from matrix tablets in comparison with hydroxypropyl methylcellulose (HPMC(®) K15M) and Eudragit(®) L100-55 polymers. Controlled release DM matrix tablets were prepared using Carbopol 71G-NF, HPMC K15M, and Eudragit L100-55 at different drug to polymer ratios by direct compression technique. The mechanical properties of the tablets as tested by crushing strength and friability tests were improved as the concentration of Carbopol, HPMC, and Eudragit increased. However, Carbopol-based tablets showed a significantly (P<0.05) higher crushing strength and a lower friability than HPMC and Eudragit tablets. No significant differences in weight uniformity and thickness values were observed between the different formulations. It was also found that Carbopol significantly (P<0.05) delayed the release of DM in comparison with HPMC K15M and Eudragit L100-55. A combination of HPMC K15M and Eudragit L100-55 in a 1:1 ratio at 20 and 30% significantly (P<0.05) delayed the release of DM than Eudragit L100-55 alone. Moreover, blends of Carbopol and HPMC at a 1:1 ratio at the 10, 20, and 30% total polymer concentration were investigated. The blend of Carbopol and HPMC at 10% level significantly (P<0.05) slowed the release of DM than Carbopol or HPMC alone, whereas blends at 20 and 30% level significantly (P<0.05) delayed the release of DM compared with HPMC or Carbopol alone. The results with these polymer blends showed that it was possible to reduce the total amount of polymers when used as a combination in formulation. PMID:21639691

Fayed, Mohamed H; Mahrous, Gamal M; Ibrahim, Mohamed A; Sakr, Adel

2013-01-01

165

pH-independent release of a weakly basic drug from water-insoluble and -soluble matrix tablets.  

PubMed

Weakly basic drugs or salts thereof demonstrate pH-dependent solubility. The resulting release from conventional matrix tablets decreases with increasing pH-milieu of the gastrointestinal tract. The aim of this study was to overcome this problem and to achieve pH-independent drug release. Two different polymers were used as matrix formers, the water-insoluble and almost unswellable ethylcellulose (EC), and the water-soluble and highly swellable hydroxypropyl methylcellulose (HPMC). Two different approaches to solve the problem of pH-dependent release of weakly basic drugs are demonstrated in this paper. The first one is based on the addition of hydroxypropyl methylcellulose acetate succinate (HPMCAS, an enteric polymer), the second one on the addition of organic acids such as fumaric, succinic or adipic acid to the drug-polymer system. The first approach failed to achieve pH-independent drug release, whereas the addition of organic acids to both matrix formers was found to maintain low pH values within the tablets during drug release in phosphate buffer (pH 6.8 or 7.4). Thus, the micro-environmental conditions for the dissolution and diffusion of the weakly basic drug were almost kept constant. The release of verapamil hydrochloride from tablets composed of ethylcellulose or HPMC and organic acids was found to be pH-independent. PMID:10773333

Streubel, A; Siepmann, J; Dashevsky, A; Bodmeier, R

2000-06-15

166

Wax-matrix tablet for time-dependent colon-specific delivery system of sophora flavescens Aiton: preparation and in vivo evaluation.  

PubMed

A wax-matrix time-dependent colon-specific tablet (WM-TDCS) was studied. Wax-matrix tablet core consisting of semi-synthetic glycerides, as a wax polymeric expanding agent, carboxymethyl starch sodium (CMS-Na), and NaCl was prepared, and Sophora flavescens Aiton (ASF, extracts of traditional Chinese medicine) was used as model drug. The wax-matrix ASF tablets core was coated with Eudragit NE 30 D as the inner coating materials and with Opadry OY-P-7171 as the outer coating materials. The in vitro release behaviors of the coated tablets were examined and then in vivo absorption kinetics of the coated tablets in dogs was further investigated. The volume of the tablet core was markedly increased at 37 degrees C because of the expand effect of polymer semi-synthetic glycerides and CMS-Na. The drug release from WM-TDCS was more stable than TDCS in vitro and in vivo. The lag time of ASF release was also controlled by the thickness of the inner coating layer. In vivo evaluation demonstrated that in vivo lag time of absorption was in a good agreement with in vitro lag time of release. ASF wax-matrix tablets coated with Eudragit NE 30 D and Opadry OY-P-7171 using the regular coating technique could be designed to achieve a lag time of 3 h in the small intestinal tract. PMID:18785039

Zou, Meijuan; Wang, Yue; Xu, Caihong; Cheng, Gang; Ren, Jungang; Wu, Gaolei

2009-02-01

167

Formulation and in vitro evaluation of theophylline matrix tablets prepared by direct compression: Effect of polymer blends  

PubMed Central

The deformation mechanism of pharmaceutical powders, used in formulating directly compressed matrix tablets, affects the characteristics of the formed tablets. Three polymers of different deformation mechanisms were tested for their impact on theophylline directly compressed tablets namely Kollidon SR (KL SR, plastic deformation), Ethylcellulose (EC, elastic deformation) and Carnauba wax (CW, brittle deformation) at different compression forces. However, tablets based mainly on KL SR, the plastically deformed polymer (TN1) exhibited the highest hardness values compared to the other formulae which are based on either blends of KL SR with CW, the very brittle deformed polymer. The upper detected force for TN formulae and the lower punch force were found to dependent mainly on the powder deformation. This difference is attributed to the work done during the compression phase as well as the work lost during the decompression phase. Furthermore, the release profiles of TN from formulae TN2 and TN4 that are based on the composition (2KL SR:1EC) and (1KL SR:2EC), respectively, were consistent with different deformation mechanisms of KL SR and EC and on the physicochemical properties like the water absorptive capacity of EC. Upon increasing the weight ratio of KL SR (TN2), the release rate was greatly retarded (39.4%, 37.1%, 35.0% and 33.6% released after 8 h at 5, 10, 15 and 20 kN. PMID:24115902

El-Bagory, Ibrahim; Barakat, Nahla; Ibrahim, Mohamed A.; El-Enazi, Fouza

2011-01-01

168

Formulation and in vitro evaluation of theophylline matrix tablets prepared by direct compression: Effect of polymer blends.  

PubMed

The deformation mechanism of pharmaceutical powders, used in formulating directly compressed matrix tablets, affects the characteristics of the formed tablets. Three polymers of different deformation mechanisms were tested for their impact on theophylline directly compressed tablets namely Kollidon SR (KL SR, plastic deformation), Ethylcellulose (EC, elastic deformation) and Carnauba wax (CW, brittle deformation) at different compression forces. However, tablets based mainly on KL SR, the plastically deformed polymer (TN1) exhibited the highest hardness values compared to the other formulae which are based on either blends of KL SR with CW, the very brittle deformed polymer. The upper detected force for TN formulae and the lower punch force were found to dependent mainly on the powder deformation. This difference is attributed to the work done during the compression phase as well as the work lost during the decompression phase. Furthermore, the release profiles of TN from formulae TN2 and TN4 that are based on the composition (2KL SR:1EC) and (1KL SR:2EC), respectively, were consistent with different deformation mechanisms of KL SR and EC and on the physicochemical properties like the water absorptive capacity of EC. Upon increasing the weight ratio of KL SR (TN2), the release rate was greatly retarded (39.4%, 37.1%, 35.0% and 33.6% released after 8 h at 5, 10, 15 and 20 kN. PMID:24115902

El-Bagory, Ibrahim; Barakat, Nahla; Ibrahim, Mohamed A; El-Enazi, Fouza

2012-07-01

169

Use of hydroxypropyl methylcellulose acetate succinate in an enteric polymer matrix to design controlled-release tablets of amoxicillin trihydrate.  

PubMed

A controlled-release table of amoxicillin trihydrate was developed by use of a matrix formulation based on the enteric polymer hydroxypropyl methylcellulose acetate succinate (HPMCAS). Sustained drug release was shown by in vitro dissolution testing; the polymer could suppress drug release in the presence of gastric pH but could enhance drug release in the presence of small intestinal pH, compared with compacts of pure drug. Grinding or physical mixing of the drug with the polymer, an alteration in normal compaction pressure, or a substitution of other enteric polymers did not markedly affect drug release from compacts. Physicochemical testing of samples confirmed that the method of mixing did not alter powder morphology. An ethanolic granulation procedure was used in the production of final tablets (21 x 10 mm) containing amoxicillin (750 mg), HPMCAS, anhydrous directly compressible lactose, and lubricants. These large tablets showed a promising sustained-release effect in vitro when a variable-pH-shift dissolution procedure was used. However, single-dose studies with a panel of fasting subjects showed that the tablets had a relative bioavailability of only 64.4%. Other pharmacokinetic parameters confirmed a lack of therapeutic advantage of these tablets over an equivalent dose of conventional capsules. PMID:8360849

Hilton, A K; Deasy, P B

1993-07-01

170

Development of enteric-coated pectin-based matrix tablets for colonic delivery of theophylline.  

PubMed

The present work was aimed at developing a new colonic drug delivery system which takes advantage of the combined approaches of a specifically colon-biodegradable pectin matrix with a pH-sensitive Eudragit S100 polymeric coating. The developed system was able to suitably retard the onset of drug release and to provide a colon-specific delivery, thus overcoming the problems of pectin solubility in the upper gastrointestinal tract and low site-specificity of simple pH-dependent systems. Due to the poor compactability properties of pectin, it was used in mixture with Emdex, a hydrophilic directly-compressible material, in order to make it possible to prepare tablets by direct compression. Theophylline (TP) was used as model drug due to its suitable pharmacokinetic properties for colonic delivery and good absorption in the large intestine. The effects of varying the type of pectin (low and high methoxylated, or amidated), the pectin:Emdex ratio and the level of the pH-dependent polymeric coating on drug release behavior were investigated. Release tests were performed using sequential liquids simulating the physiological variation of pH and the effect of the presence or not of pectinolytic enzymes into the simulated colonic medium was evaluated. Thirty percent (w/w) was the the minimum content of Emdex for obtaining directly compressible tablets with sufficient hardness to withstand the coating process and 27% (w/w) was the minimum coating amount for obtaining an adequate lag time before the onset of drug release. After lag time, linear nearly zero-order profiles were obtained whose slope (i.e. the drug release rate) depended on both the Emdex content and the pectin type. Comparison of the results obtained in the presence or not of pectynolitic enzymes allowed selection of the high methoxylated pectin as the most interesting candidate for specific colonic delivery since it was the least water-soluble and the most susceptible to enzymatic degradation, thus assuring a greater site-specificity of drug release. Finally, the importance of using appropriate dissolution test conditions to adequately characterize the drug release profiles from delivery systems endowed with a microflora-activated drug release triggering mechanism has been demonstrated. PMID:14668057

Mura, Paola; Maestrelli, Francesca; Cirri, Marzia; González Rodríguez, M Luisa; Rabasco Alvarez, Antonio M

2003-07-01

171

Preparation and in vitro/in vivo evaluation of dextran matrix tablets of budesonide in experimental ulcerative colitis in rats.  

PubMed

Budesonide is an anti-inflammatory drug of choice for treatment of ulcerative colitis which affects the rectum and a part of or the entire colon. Delivery of budesonide specifically to the colon would increase the efficacy of the drug and reduce the side-effects. The aim of this study was to develop an oral matrix system formulation for budesonide to deliver the major part of the drug to the colon for treatment of ulcerative colitis that has not been reported before. Directly compressed matrix tablets were prepared using different molecular weights of dextran and three ratios of drug-to-polymer. The physical properties of the tablets including weight variation, hardness, content uniformity, and release profile in HCl 0.1 N, phosphate buffer pH 7.4 and 6.8 containing 4% rat caecal and colonic contents were studied. The efficacy of the desired formulation was also evaluated against acetic acid-induced colitis in rats. Physical properties of the tablets were in the ranges recommended by official references. More than 10% of the drug was released in HCl 0.1 N and pH 7.4, while a very drastic increase was observed after exposure to pH 6.8 containing rat caecal contents. The efficacy of the selected formulation against rat-induced colitis was also increased in comparison to the non-targeted formulation of budesonide. In conclusion, matrix tablets with a 1:10 drug-to-dextran ratio with high molecular weight could deliver the drug specifically to the colon and are promising for treatment of ulcerative colitis. PMID:20954795

Ahmadi, Fatemeh; Varshosaz, Jaleh; Emami, Jaber; Tavakoli, Naser; Minaiyan, Mohsen; Mahzouni, Parvin; Dorkoosh, Farid

2011-02-01

172

Alginate/cashew gum floating bead as a matrix for larvicide release.  

PubMed

A polymeric floating system composed of Alginate (ALG) and Cashew gum (CG), loaded with an essential oil (Lippia sidoides-Ls) was prepared by ionotropic gelation, characterized regarding its physical-chemistry properties and evaluated on its potential as a controlled release system. The influence of process parameters on the buoyancy, loading, swelling and in vitro and in vivo release kinetics, was investigated. Results showed that beads produced with carbonate and Ls at high level contents exhibit good floatability (up to 5 days) and loading capacity (15.2-23.8%). In vitro release data showed a Fickian diffusion profile and in vivo experiments showed that ALG-CG floating system presented a superior and prolonged larvicide effect, in comparison with non-floating ones, presenting larvae mortality values of 85% and 33%, respectively, after 48 h. These results indicate that ALG-CG floating beads loaded with Ls presented enhanced oil entrapment efficiency, excellent floating ability, and suitable larvicide release pattern. PMID:24364941

Paula, Haroldo C B; de Oliveira, Erick F; Abreu, Flávia O M S; de Paula, Regina C M

2012-08-01

173

Studies on the compressibility of wax matrix granules of acetaminophen and their admixtures with various tableting bases.  

PubMed

Matrix granules of acetaminophen have been formed by a melt granulation process whereby the acetaminophen powder was triturated with the melted wax--goat wax, glyceryl monostearate or carnuba wax. The compressibility of the matrix granules and their admixture, with diluent granules (lactose, alpha-cellulose or microcrystalline cellulose) was investigated. The granules were compressed to tablets at a constant load (30 arbitrary units on the load scale) of a manesty single punch machine. Resulting tablets were evaluated for tensile strength (T) and disintegration times (DT). Granule flow was determined by measuring their angle of repose when allowed to fall freely on a level surface. Matrix granules prepared by melt granulation with goat wax or glyceryl monostearate were too sticky and therefore did not flow at all. They were also poorly compressible (T values = 0.20MN/m2). Inclusion of the diluent remarkably improved granule flow property and compressibility. The T values of the tablets (measure of compressibility) increased from about 0.24 to 0.65 MN/m2 during increase in diluent (lactose) content from 20 to 80 %w/w. Microcrystalline cellulose and alpha-cellulose were more effective than lactose in promoting compressibility of the granules. By contrast the matrix granules formed with carnuba wax were free flowing (angle of repose, 18.60). Addition of the diluent further improved flowability slightly. The matrix granules (without a diluent) were readily compressible (T value, 1.79MN/m2). Addition of the diluent (80%w/w) reduced T values (MN/m2) slightly to 1.32 (lactose), 1.48 (alpha-cellulose) and 1.74 (microcrystalline cellulose). Tablets of the matrix granules only, disintegrated rapidly within 3 minutes. DT was further reduced to <30 s by addition of any of the diluents. The indication is that the inclusion of the diluents studied can be used to improve the compressibility of the otherwise poorly compressible matrix granules. Based on the flowability, compressibility, and disintegration data, carnuba wax proved most promising in the melt granulation of the test drug for sustained release applications. PMID:16751119

Uhumwangho, M U; Okor, R S

2006-04-01

174

A novel gastro-floating multiparticulate system for dipyridamole (DIP) based on a porous and low-density matrix core: in vitro and in vivo evaluation.  

PubMed

The study was aimed to develop a novel gastro-floating multiparticulate system based on a porous and low-density matrix core with excellent floatability. The gastro-floating pellets (GFP) were composed of a porous matrix core, a drug loaded layer (DIP and HPMC), a sub-coating layer (HPMC) and a retarding layer (Eudragit(®) NE 30D). The porous matrix cores were evaluated in specific. EC was chosen as the matrix membrane for its rigidity and minimal expansion to large extent. The porous matrix core was achieved by the complete release of the bulk water soluble excipient from the EC coated beads, and mannitol was selected as the optimal water soluble excipient. SEM photomicrographs confirmed the structure of porous matrix cores. The compositions of GFP were investigated and optimized by orthogonal array design. The optimized formulation could sustain the drug release for 12h and float on the dissolution medium for at least 12h without lag time to float. The pharmacokinetic study was conducted in beagle dogs, and the relative bioavailability of the test preparation was 193.11±3.43%. In conclusion, the novel gastro-floating pellets can be developed as a promising approach for the gastro-retentive drug delivery systems. PMID:24368104

Li, Zhao; Xu, Heming; Li, Shujuan; Li, Qijun; Zhang, Wenji; Ye, Tiantian; Yang, Xinggang; Pan, Weisan

2014-01-30

175

Influence of the components of Kollicoat SR film on mechanical properties of floating pellets from the point of view of tableting.  

PubMed

The influence of pellet core ingredients on pellet behaviour, e.g. during compression, is well known. In this study the influence of components of a Kollicoat SR polymer film on mechanical properties was investigated. The aim of this study was to evaluate the influence of polymer film components on the mechanical properties of the pellet as a whole, from the point of view of tableting. Tablets should disintegrate into undeformed pellets floating in this environment for 5-6 h, releasing the model drug--verapamil hydrochloride--if possible in a controlled way. The usefulness of texture analysis and work of compression measurement was also evaluated. Kollicoat SR in the form of a 30D aqueous dispersion was chosen as the main component of the polymer film. Polyvinyl pyrrolidone K-30 as a pore former, and propylene glycol, triethyl citrate and dibutyl sebacate plasticisers were selected as typical additives. The influence of different thickness of polymer film on behaviour during stress was also evaluated. After coating the cores with a 20 microm Kollicoat SR dispersion film, an increase in mechanical strength, in comparison to the pellet core, was observed (2.74 to 3.34 mJ). Addition of porophor increased the work of compression by 50% to 5.1 mJ. The investigation of the influence of plasticiser on film properties proved that the kind of plasticiser used in the polymer film had no effect on the mechanical properties of the film or pellets. Only in the case of the film with triethyl citrate was no distinct of the pellet core found. Pellets coated both with films with triethyl citrate and with dibutyl sebacate, in contrast to pellets with a film coating with propylene glycol, showed a significant decrease of the dissolution rate of verapamil hydrochloride (20, 10 and 40% at 6 hours, respectively). It is possible to compress pellets with a 50 microm polymer film without affecting the dissolution rate, as was confirmed during release studies. When using Kollicoat SR the most appropriate plasticizer seems to be triethyl citrate, and in this case a change of behavior during compression analysis by texture analyzer was observed. But so relationship was found between the type of plasticizer and the work needed to obtain a given deformation. PMID:18972835

Lunio, R; Sawicki, W

2008-10-01

176

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

177

Response surface optimization of sustained release metformin-hydrochloride matrix tablets: influence of some hydrophillic polymers on the release.  

PubMed

The aim of the present work was designed to develop a model-sustained release matrix tablet formulation for Metformin hydrochloride using wet granulation technique. In the present study the formulation design was employed to statistically optimize different parameters of Metformin hydrochloride tablets at different drug-to-polymer ratios employing polymers Hydroxypropyl methylcellulose of two grades K4M and K100M as two independent variables whereas the dependent variables studied were X(60), X(120), T(50), T(90), n, and b values obtained from dissolution kinetics data. The in vitro drug release studies were carried out at simulated intestinal fluids, and the release showed a non-Fickian anomalous transport mechanism. The drug release was found to reveal zero order kinetics. The granules and the tablets were tested for their normal physical, morphological, and analytical parameters and were found to be within the satisfactory levels. There were no significant drug-polymer interactions as revealed by infrared spectra. It has been found out that on an optimum increased Hydroxypropyl methylcellulose K100M concentration and decreased Hydroxypropyl methylcellulose K4M concentration the formulations were elegant in terms of their release profiles and were found to be statistically significant and generable. PMID:22988527

Roy, Amitava; Roy, Kalpana; Roy, Sarbani; Deb, Jyotirmoy; Ghosh, Amitava; Ali, Kazi Asraf

2012-01-01

178

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

PubMed

The goal of this study is to develop a novel sustained-release (SR) system for poorly water-soluble drugs by applying solid dispersion (SD) technique for improving the solubility. The developed SR system, disintegration-controlled matrix tablet (DCMT), consists of hydrogenated soybean oil (HSO) as wax and SD granules containing low-substituted hydroxypropylcellulose (L-HPC) as a disintegrant. In this study, nilvadipine (NiD) was chosen as a model compound. Sustained-release profiles of NiD from DCMT were identically controlled in several dissolution mediums in spite of varying pH and agitation speed. The release of NiD from DCMT was sustained more effectively by increasing the amount of wax or by decreasing the amount of disintegrant, and supersaturation of NiD was achieved without any re-crystallization in dissolution medium. The release rate of NiD from DCMT was controlled by the disintegration rate of tablet. The release profile of NiD was described by the Hixson-Crowell's model better than zero-order kinetics, first-order kinetics and Higuchi's model, which supports that the release of NiD from DCMT is regulated by the disintegration of the tablet. From this study, it was clarified that DCMT was one of the promising SR systems applying SD for the poorly water-soluble drugs. PMID:16253377

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

2005-11-28

179

Magnetic Resonance Imaging and Image Analysis for Assessment of HPMC Matrix Tablets Structural Evolution in USP Apparatus 4  

Microsoft Academic Search

Purpose  The purpose of the study was to present a methodology for the processing of Magnetic Resonance Imaging (MRI) data for the\\u000a quantification of the dosage form matrix evolution during drug dissolution. The results of the study were verified by comparison\\u000a with other approaches presented in literature.\\u000a \\u000a \\u000a \\u000a \\u000a Methods  A commercially available, HPMC-based quetiapine fumarate tablet was studied with a 4.7T MR system.

Piotr Kulinowski; Przemys?aw Doro?y?ski; Anna M?ynarczyk; W?adys?aw P. W?glarz

2011-01-01

180

Drug release kinetics and fronts movement studies from methyl methacrylate (MMA) copolymer matrix tablets: effect of copolymer type and matrix porosity.  

PubMed

Several methyl methacrylate (MMA) copolymers have recently been proposed as an alternative for the formulation of controlled-release matrix tablets. Copolymers were synthesised by free radical copolymerisation of methyl methacrylate with starch or cellulose derivatives and were alternatively dried by oven or freeze-drying techniques. Both the chemical composition and the drying technique were demonstrated to have a considerable influence on the physical properties of the copolymers. The present investigation was focused on the elucidation of the drug release mechanism from MMA copolymer matrices, using anhydrous theophylline as model drug. Drug release experiments were performed from free tablets. Radial drug release and fronts movement were also evaluated using special devices consisting of two Plexiglass discs joined by means of four stainless steel screws. Mathematical analysis of release data was performed using Higuchi, Korsmeyer and Peppas equations and fronts movement was investigated using a colorimetric technique. The drug release rate and the relative positions of the fronts were studied as functions of the type of copolymer and the initial porosity of the tablets. Drug release was controlled mainly by diffusion and the release rate was found to be affected by the drying method and related to the area exposed to the dissolution medium. Three distinct fronts (water uptake, complete wetting, erosion) were observed during the release process and the dynamics of fronts movement confirmed the diffusional mechanism. PMID:14499186

Ferrero, C; Bravo, I; Jiménez-Castellanos, M R

2003-09-19

181

Formulation and In-vitro Characterization of Sustained Release Matrix Type Ocular Timolol Maleate Mini-Tablet  

PubMed Central

The purpose of this study was preparation and evaluation of sustained release matrix type ocular mini-tablets of timolol maleate, as a potential formulation for the treatment of glaucoma. Following the initial studies on timolol maleate powder, it was formulated into ocular mini-tablets. The polymers investigated in this study included cellulose derivatives (HEC, CMC, EC) and Carbopol 971P. Mannitol was used as the solubilizing agent and magnesium stearate as the lubricant. Mini-tablets were prepared by through mixing of the ingredients, followed by direct compression. All the prepared formulations were evaluated in terms of physicochemical tests, including uniformity of weight, thickness, crushing strength, friability and in-vitro drug release. Four groups of formulations were prepared. The presence of different amounts of cellulose derivatives or Carbopol 971P, alone, was studied in group A formulations. In group B formulations, the effect of adding Carbopol 971P alongside different cellulose derivatives was investigated. Group C formulations were made by including mannitol as the solubilizing agent, alongside Carbopol 971P and a cellulose derivative. In group D formulations, mini-tablets were made using Carbopol 971P, alongside two different cellulose derivative. The selected formulation (C1) contained ethyl cellulose, Carbopol 971P, mannitol and magnesium stearate, which showed almost 100% drug release over 5 h. Based on kinetic studies, this formulation was found to best fit the zero-order model of drug release. However, the Higuchi and Hixson -Crowell models also showed a good fit. Hence, overall, formulation C1 was chosen as the best formulation. PMID:24734053

Mortazavi, Seyed Alireza; Jafariazar, Zahra; Ghadjahani, Yasaman; Mahmoodi, Hoda; Mehtarpour, Farzaneh

2014-01-01

182

Controlled Release Matrix Tablets of Olanzapine: Influence of Polymers on the In Vitro Release and Bioavailability  

Microsoft Academic Search

Controlled-release (CR) tablet formulation of olanzapine was developed using a binary mixture of Methocel® K100 LV-CR and\\u000a Ethocel® standard 7FP premium by the dry granulation slugging method. Drug release kinetics of CR tablet formulations F1,\\u000a F2, and F3, each one suitably compressed for 9-, 12-, and 15-kg hardness, were determined in a dissolution media of 0.1 N\\u000a HCl (pH 1.5) and phosphate

Amir Badshah; Fazal Subhan; Khalid Rauf

2010-01-01

183

Formulation of controlled-release baclofen matrix tablets. II. Influence of some hydrophobic excipients on the release rate and in vitro evaluation.  

PubMed

The aim of this study was to investigate the influence of polymer level and type of some hydrophobic polymers, including hydrogenated castor oil (HCO); Eudragit RS100 (E-RS100); Eudragit L100 (E-L100), and some fillers namely mannitol [soluble filler], Dibasic calcium phosphate dihydrate (Emcompress) and anhydrous dibasic calcium phosphate [insoluble fillers] on the release rate and mechanism of baclofen from matrix tablets prepared by a hot-melt granulation process (wax tablets) and wet granulation process (E-RS100 and E-L100 tablets). Statistically significant differences were found among the drug release profile from different classes of polymeric matrices. Higher polymeric content (40%) in the matrix decreased the release rate of drug because of increased tortuosity and decreased porosity. At lower polymeric level (20%), the rate and extent of drug release was elevated. HCO was found to cause the strongest retardation of drug. On the other hand, replacement of Emcompress or anhydrous dibasic calcium phosphate for mannitol significantly retarded the release rate of baclofen, except for E-L100 (pH-dependent polymer). Emcompress surface alkalinity and in-situ increase in pH of the matrix microenvironment enhanced the dissolution and erosion of these matrix tablets. The release kinetics was found to be governed by the type and content of the excipients (polymer or filler). The prepared tablets showed no significant change in drug release rate when stored at ambient room conditions for 6 months. PMID:18500558

Abdelkader, Hamdy; Youssef Abdalla, Ossama; Salem, Hesham

2008-01-01

184

CONTROLLED RELEASE MATRIX UNCOATED TABLETS OF ENALAPRIL MALEATE USING HPMC ALONE  

PubMed Central

Hydroxy propyl methyl cellulose (HPMC) is generally combined with hydrophobic polymers in fabricating oral controlled solid dosage forms. This study evaluated the utility of diverse grades of HPMC in developing a controlled release formulation for a hydrophilic drug, enalapril maleate. Controlled release uncoated tablets were prepared by direct compression technique. Two grades of HPMC (K100 and K4M) in different proportions were used to prepare the tablets, and were evaluated for physical properties, drug content, in vitro drug release and drug release kinetics as well. All the formulations demonstrated good physical integrity and the drug content were in the official limits. The formulation with HPMC K100 (25 mg/tablet) and K4M (15 mg/tablet) have been found to release the required amount of drug (2.97 mg/h) through out the study period (14 h). The calculated regression coefficients showed higher r2 value with Higuchi model and zero order kinetics. Given the excellent release profile, the study concluded that HPMC in different grades with low concentration alone can control the enalapril maleate release over a period of time (14 h). PMID:24825968

Nair, Anroop B.; Vyas, Hiral; Kumar, Ashok

2010-01-01

185

Study on sustained-release metformin hydrochloride from matrix tablet: Influence of hydrophilic polymers and in vitro evaluation.  

PubMed

The overall objective of the present work was to develop an oral sustained-release (SR) metformin tablet prepared by the direct compression method, using hydrophilic hydroxylpropylmethylcellulose (HPMC) and Guar gum polymer alone and in combination at different concentrations. Metformin hydrochloride (HCl), a biguanide, has a relatively short plasma half-life and low absolute bioavailability. All the batches were evaluated for thickness, weight variation, hardness and drug content uniformity and in vitro drug release. Mean dissolution time is used to characterize the drug release rate from a dosage form, and indicates the drug release-retarding efficiency of the polymer. The hydrophilic matrix of HPMC alone could not control the Metformin release effectively for 12 h whereas when combined with Guar gum, it could slow down the release of drug and, thus, can be successfully employed for formulating SR matrix tablets. Fitting the data to the Korsmeyer equation indicated that diffusion along with erosion could be the mechanism of drug release. Similarity factor ƒ2 values suggest that the test and reference profiles are identical. PMID:23071938

Wadher, Kamlesh J; Kakde, Rajendra B; Umekar, Milind J

2011-07-01

186

Study on sustained-release metformin hydrochloride from matrix tablet: Influence of hydrophilic polymers and in vitro evaluation  

PubMed Central

The overall objective of the present work was to develop an oral sustained-release (SR) metformin tablet prepared by the direct compression method, using hydrophilic hydroxylpropylmethylcellulose (HPMC) and Guar gum polymer alone and in combination at different concentrations. Metformin hydrochloride (HCl), a biguanide, has a relatively short plasma half-life and low absolute bioavailability. All the batches were evaluated for thickness, weight variation, hardness and drug content uniformity and in vitro drug release. Mean dissolution time is used to characterize the drug release rate from a dosage form, and indicates the drug release-retarding efficiency of the polymer. The hydrophilic matrix of HPMC alone could not control the Metformin release effectively for 12 h whereas when combined with Guar gum, it could slow down the release of drug and, thus, can be successfully employed for formulating SR matrix tablets. Fitting the data to the Korsmeyer equation indicated that diffusion along with erosion could be the mechanism of drug release. Similarity factor ƒ2 values suggest that the test and reference profiles are identical. PMID:23071938

Wadher, Kamlesh J; Kakde, Rajendra B; Umekar, Milind J

2011-01-01

187

Design and in vitro testing of a floatable gastroretentive tablet of metformin hydrochloride.  

PubMed

Metformin hydrochloride, which is better absorbed in the upper intestine, was formulated as a floating (buoyant) matrix tablet using a gas generating agent (sodium bicarbonate) and a gel forming hydrophilic polymer (hydroxypropyl methylcellulose). The formulation was optimized on the basis of floating ability and in vitro drug release. The resulting formulation produced robust tablets with optimum hardness, consistent weight uniformity and low tablet friability. All tablets but one exhibited satisfactory (gradual and near complete) drug release and buoyancy. In vitro drug release tests of these tablets indicated controlled sustained release of metformin hydrochloride and 96-99% released at the end of 8 h. Two formulations of fabricated tablets containing metformin hydrochloride (500 mg), sodium bicarbonate (75 mg), hydroxypropyl methylcellulose-K 4M (170-180 mg), citric acid (between 15 and 20 mg) and polyvinyl pyrrolidone K90 (32-40 mg) with hardness between 6.8 to 7.5 kg/cm2 showed a floating time of more than 8 h and promising drug release results. The release followed the Higuchi kinetic model, indicating diffusion dominated drug release. PMID:17341036

Basak, S C; Rahman, J; Ramalingam, M

2007-02-01

188

Preparation and comparative evaluation of sustained release metoclopramide hydrochloride matrix tablets.  

PubMed

Metoclopramide hydrochloride (MCP) is commonly used for the management of gastrointestinal disorders. Frequent administration and the undesired side effects (extra pyramidal symptoms) of the drug on the central nervous system due to the fluctuations of its plasma concentrations may lead to patient incompliance, and hence, improper therapy. Therefore, the present work will be devoted to formulate the drug in sustained release formulations. MCP was incorporated in 12 formulae containing different polymers and/or different polymer ratios. These polymers were hydroxypropylmethyl cellulose (HPMC), carboxymethylcellulose (CMC) and ethyl cellulose (EC). Sodium starch glycolate (SSG) was added to some formulae in different amounts in order to soften and/or disintegrate the tablets. Both direct compression and granulation techniques were used to prepare the tablets. The physical properties were found to be satisfactory for all the formulae. The dissolution profiles of the tablets were constructed using the change-over method. The drug release involved a combination of both diffusion and polymer-chain relaxation mechanisms. The time required to release 50% of MCP ranged from 1.2 to more than 8 h. Direct compression and dry granulation techniques produced sufficient sustaining of the drug release. However, the pellets made by wet granulation released MCP in about 2 h, i.e., pelletization spheronization technique was not effective in sustaining the drug. PMID:23960711

Abdel-Rahman, Sayed I; Mahrous, Gamal M; El-Badry, Mahmoud

2009-10-01

189

The influence of HPMC viscosity as FRC parameter on the release of low soluble drug from hydrophylic matrix tablets.  

PubMed

The importance of functionality-related characteristics (FRC) of hydroxypropyl methylcellulose (HPMC) described in the pharmacopeia monograph can be evaluated only for selected formulation or technological process. The aim of our work was to investigate the influence of apparent viscosity as one of the FRC for two batches of the same HPMC grade on the release properties of diclofenac sodium from HPMC matrix tablets. Our results show that two batches of HPMC differ in viscosity significantly and as a consequence, the significant differences were observed in the release profiles as well. HPMC-B sample has higher viscosity and therefore higher average molecular weight, thus the erosion and drug release were slower compared to HPMC-A sample with lower apparent viscosity. It can be concluded that batch-to-batch viscosity variation of the same HPMC grade can lead to the different release profiles; therefore the specification limits of some FRC should be postulated during the development of each individual formulation. However, the viscosity interval as FRC can not be generalized, because it is different for different tablet compositions. PMID:21916601

Novak, S Devjak; Kuhelj, V; Vre?er, F; Baumgartner, S

2013-01-01

190

Influence of admixed citric acid and physiological variables on the vinpocetine release from sodium alginate compressed matrix tablets.  

PubMed

In this study, the controlled release matrix tablets of vinpocetine were prepared by direct compression using sodium alginate (SAL) as hydrophilic polymer and different amounts of citric acid as hydrosoluble acidic excipient to set up a system bringing about zero-order release of this drug in distilled water containing 0.5% sodium dodecyl sulfate. At the critical content of admixed citric acid (60 mg/tab.), the lowest drug-release rate was observed. In order to explain the effect of this critical content on drug-release rate from SAL matrices, investigation of the possibility of interaction of citric acid with SAL was performed using differential scanning calorimetric analysis and infrared analysis, which confirmed the existence of direct citric acid-SAL interaction when these two excipients came in contact with water. A zero-order drug-release system could be obtained by regulating the ratio of citric acid-to-SAL and the capacity of this system in controlling drug-release rate depended on the extent of interaction between citric acid and SAL. It is worth noticing that pH and the ionic strength of the dissolution medium were found to exert an influence on the drug-release performance of SAL tablets. PMID:21417613

Nie, Shufang; Wu, Jie; Liu, Hui; Pan, Weisan; Liu, Yanli

2011-08-01

191

Investigation of the biopharmaceutical behavior of theophylline hydrophilic matrix tablets using USP methods and an artificial digestive system.  

PubMed

This work aimed to investigate the biopharmaceutical behavior of hydrophilic matrix tablets of theophylline using different in vitro methods: USP II, USP IV, and a novel in vitro system simulating the gastrointestinal tract in man called the artificial digestive system (ADS). The potentiality of each method was evaluated by establishing in vitro/in vivo correlation. Using USP methods, the drug release was pH-independent and dependent on agitation intensity. Level A IVIVCs could be established using the different in vitro methods but one to one correlation was established only when the ADS method was used. For the prediction of in vivo drug dosage form behavior based on in vitro methods, the ADS showed a high predictability when compared to USP in vitro methods. PMID:17523011

Souliman, Sabah; Beyssac, Eric; Cardot, Jean-Michel; Denis, Sylvain; Alric, Monique

2007-04-01

192

Development and evaluation of a monolithic floating drug delivery system for acyclovir.  

PubMed

Acyclovir (ACV), a model drug for this study, is one of the most effective drugs against viruses of the herpes group. Absorption of orally administered ACV is variable and incomplete, with a bioavailability of ca. 15-30%. The drug is absorbed in the duodenum after oral administration and hence, preparation of a floating drug delivery system (FDDS) for ACV may increase oral absorption of the drug. ACV matrix tablets (200?mg) containing an effervescent base (sodium bicarbonate and citric acid) and a binary combination of hydroxypropyl methylcellulose (HPMC) K4M with carbopol or sodium carboxymethyl cellulose (Na CMC) or polyvinylpyrrolidone (PVP) and/or sodium alginate were prepared by the direct compression method. The tablets were evaluated for physicochemical properties and in vitro floating ability (floating lag-time and duration), bioadhesiveness and drug release. The drug release studies were carried out in 0.1?N HCl (pH 1.2) at 37±0.5°C. At appropriate time intervals, samples were withdrawn and assayed spectrophotometrically at ?(max)=259?nm. The floating test showed tablets containing 15% effervescent base had a floating lag time of 10-30?s and a duration of floating time of 24?h. The formulations containing HPMC-PVP, HPMC-Na CMC, HPMC-carbopol, and HPMC-sodium alginate released about 60-90% of their drug content during a 12-h period. Increasing carbopol caused slower drug release. We concluded that the proposed tablets with 15% effervescent base, 20-30% HPMC, 30% Na CMC (and/or 20% PVP or 20% sodium alginate) showed good floating and drug release properties in vitro, and should be considered as FDDS for ACV. PMID:22293475

Tavakoli, Naser; Varshosaz, Jaleh; Dorkoosh, Farid; Motaghi, Sedigheh; Tamaddon, Lana

2012-01-01

193

Report: in vitro dissolution studies of different brands of sustained release diclofenac sodium matrix tablet available in Bangladesh.  

PubMed

Commercially available national thirteen brands and three international brands of diclofenac sodium sustained release matrix tablets were studied in simulated gastric medium (pH 1.2) for 2 hours time period and simulated intestinal medium (pH 6.8) for 10 hours time period using USP reference dissolution apparatus. All the national and international brands complied with the USP in-vitro dissolution specification for drug releases in simulated gastric medium. However, four of the national brands (Code: DS-5, DS-8, DS-12, and DS-13) failed to fulfill their official requirement of 80% drug release within 8th hour in simulated intestinal medium. Drug release of those four national brands were 78.1%, 74.9%, 72.1%, and 77.8% respectively within the specified time period, however one national brand (Code: DS-2) released 83.2% drug within 6th hour in intestinal medium. Drug release profiles were analyzed for Higuchi equation, zero order, and first order to reveal the release kinetics perspective of diclofenac sodium sustained release matrix tablets. It was found that zero order release kinetics was predominant release mechanism than first order and Higuchi release kinetics for those brands (Code: DS-1, DS-3, DS-4, DS-6, DS-7, DS-9, DS-10, DS-11, DS-X, DS-Y and DS-Z) which complied with the USP in vitro dissolution specification for drug releases. On the other hand, first order release kinetics was predominant for five national substandard formulation brands (Code: DS-2, DS-5, DS-8, DS-12 and DS-13). PMID:18166523

Abdullah, M D Addnan; Bepary, Sukumar; Rouf, Abu Shara Shamsur

2008-01-01

194

Evaluation of a matrix tablet prepared with polyacrylamide-g-sodium alginate co-polymers and their partially hydrolyzed co-polymers for sustained release of diltiazem hydrochloride.  

PubMed

Diltiazem hydrochloride (DTZ) matrix tablets were prepared using polyacrylamide-grafted sodium alginate (PAam-g-SA) co-polymers having different percentages of grafting and their partially hydrolyzed products with a view to achieve sustained release of the highly water-soluble drug. PAam-g-SA co-polymers having different percentages of grafting were synthesized by free radical polymerization using acrylamide (Aam) as monomer and ammonium persulphate (APS) as initiator, and the resulting co-polymers were subjected to alkaline hydrolysis to produce their corresponding partially hydrolyzed co-polymers. Matrix tablets of DTZ were prepared by wet granulation using either PAam-g-SA co-polymers or partially hydrolyzed PAam-g-SA co-polymers. The effect of percentage grafting, drug load and calcium gluconate (CG), used as excipient, was studied in simulated gastrointestinal fluid. While the tablets prepared using the co-polymer having higher percentages of grafting provided faster drug release (100% in 5.5 h), the tablets prepared with the corresponding hydrolyzed co-polymer released the drug slowly (71% in 12 h). This behaviour in release appeared to be controlled by the relative magnitude of the viscosity and the swelling capacity of the copolymers. Moreover, increase in drug load tended to decrease the drug release from all types of tablets and increase in the amount of CG increased the drug release. FT-IR and DSC studies revealed the absence of any interaction between the drug and the co-polymers. The matrix tablet made of partially hydrolyzed graft co-polymer having the highest percentage of grafting provided the most sustained release of the drug. PMID:20557689

Mandal, Sanchita; Ray, Rajat; Basu, Sanat K; Sa, Biswanath

2010-01-01

195

Effect of formulation parameters and drug-polymer interactions on drug release from starch acetate matrix tablets.  

PubMed

The aim of this study was to determine, whether interactions between a drug and hydrophobic polymer matrix are present, and if so, how they affect the drug release. In addition, the most important formulation parameters, for example porosity or structure of the tablet, which have the greatest impact on drug release, were defined. Six different drug compounds, that is allopurinol, acyclovir, metronidazole, paracetamol, salicylamide and theophylline, were used in different formulations with hydrophobic starch acetate (DS 2.7) as a matrix forming polymer. Results indicate that the formulation parameters describing directly or indirectly the structure of the matrix, such as porosity, compaction force and the particle size fraction of the filler-binder, have the strongest impact on drug release. The contribution of drug property based variables is not as high as formulation parameters, but they cannot be overlooked. The contribution of water solubility and dissolution rate of the compound are obvious, but there are other significant parameters, which describe the hydrophobic and hydrophilic regions of the molecule, that also affect the drug release. This can be seen especially with the salicylamide: compound which appears to have a strong and sufficiently high hydrophobic region that interacts with starch acetate and impairs the drug release. PMID:19177516

Pajander, Jari; Korhonen, Ossi; Laamanen, Maria; Ryynänen, Eeva-Leena; Grimsey, Ian; van Veen, Bert; Ketolainen, Jarkko

2009-10-01

196

Regulating Drug Release Behavior and Kinetics from Matrix Tablets Based on Fine Particle-Sized Ethyl Cellulose Ether Derivatives: An In Vitro and In Vivo Evaluation  

PubMed Central

The design and fabrication of sustained/controlled release dosage forms, employing new excipients capable of extending/controlling the release of drugs from the dosage forms over prolonged periods, has worked well in achieving optimally enhanced therapeutic levels of the drugs. In this sense, the objective of this study was to investigate the suitability of selected cellulose ether derivatives for use in direct compression (DC) and as efficient drug release controlling agents. Controlled release matrix tablets of ciprofloxacin were prepared at different drug-to-polymer (D?:?P) ratios by direct compression using a fine particle sized ethylcellulose ether derivative (ETHOCEL Standard Premium 7FP) as rate controlling polymer. The tablets obtained were evaluated for various physico-chemical characteristics and in-vitro drug release studies were conducted in phosphate buffer (pH 7.4) using PharmaTest dissolution apparatus at constant temperature of 37°C ± 0.1. Similarity factor f2 was employed to the release profiles of test formulations and were compared with marketed ciprofloxacin conventional tablets. Drug release mechanism and the kinetics involved were investigated by fitting the release profile data to various kinetic models. It was found that with increasing the proportion of ethylcellulose ether derivative in the matrix, the drug release was significantly extended up to 24 hours. The tablets exhibited zero order or nearly zero order drug transport mechanism. In vivo drug release performance of the developed controlled release tablets and reference conventional tablets containing ciprofloxacin were determined in rabbit serum according to randomized two-way crossover study design using High Performance Liquid Chromatography. Several bioavailability parameters of both the test tablets and conventional tablets including Cmax?, Tmax? and AUC0-t were compared which showed an optimized Cmax? and Tmax? (P < 0.05). A good correlation was obtained between in vitro drug release and in vivo drug absorption with correlation value (R2 = 0.934). Relative bioavailability was found to be 93%. Reproducibility of manufacturing process and accelerated stability of the developed tablets were performed in stability chamber at 40 ± 2°C and 75 ± 5% relative humidity for a period of 6 months and were found to be stable throughout the stability period. PMID:22649325

Shah, Kifayat Ullah; Khan, Gul Majid

2012-01-01

197

Influence of formulation and process variables on in vitro release of theophylline from directly-compressed Eudragit matrix tablets.  

PubMed

Extended-release theophylline (TP) matrix tablets were prepared by direct compression of drug and different pH-dependent (Eudragit L100, S100 and L100-55) and pH-independent (Eudragit RLPO and RSPO) polymer combinations. The influence of varying the polymer/polymer (w/w) ratio and the drug incorporation method (simple blend or solid dispersion) was also evaluated. Drug release, monitored using the Through Flow Cell system, markedly depended on both the kind of Eudragit polymer combinations used and their relative content in the matrix. Maintaining a constant 1:1 (w/w) drug/polymers ratio, the selection of appropriate mixtures of pH-dependent and pH-independent polymers enabled achievement of a suitable control of TP release. In particular, matrices with a 0.7:0.3 w/w mixture of Eudragit L100-Eudragit RLPO showed highly reproducible drug release profiles, with an almost zero-order kinetic, and allowed 100% released drug after 360 min. As for the effect of the drug incorporation method, simple blending was better than the solid dispersion technique, which not only did not improve the release data reproducibility, but also caused, unexpectedly, a marked slowing down in drug release rate. PMID:16129436

Ceballos, A; Cirri, M; Maestrelli, F; Corti, G; Mura, P

2005-01-01

198

Characterization of physicochemical properties of hydroxypropyl methylcellulose (HPMC) type 2208 and their influence on prolonged drug release from matrix tablets.  

PubMed

The key physicochemical properties of functional excipients should be identified, and the influence of their variability on the properties of the final dosage form should be evaluated during the development phase. Excipients produced by different manufacturers and/or by different manufacturing processes should have comparable properties. Hydroxypropyl methylcellulose (HPMC) with a high molecular weight is a functional excipient often used in solid matrix systems with prolonged release of active pharmaceutical ingredients (API). This study investigates whether HPMC manufactured by two manufacturers using different chemical procedures differs in particle-size distribution, particle shape, particle morphology, chemical composition, and dissolution of diclofenac sodium as a model drug. NIR spectroscopy was introduced and calibration models were developed to detect physical differences among HPMC batches from two different origins. The physical differences between HPMC samples were additionally confirmed with scanning electron microscopy (SEM), gas chromatography (GC) measurements, and dissolution testing of hydrophilic matrix tablets. Our results prove that, even if HPMC polymers manufactured from two different sources comply with the pharmacopeial specification, they significantly differ in physicochemical properties and thus influence the properties of the formulated dosage forms. PMID:22510313

Devjak Novak, S; Šporar, E; Baumgartner, S; Vre?er, F

2012-07-01

199

Time-controlled pulse-drug release from dry-coated wax matrix tablets for colon drug delivery.  

PubMed

This study aimed to prepare a colon drug delivery system using dry-coated time-controlled disintegration wax matrix tablets. Indomethacin was used as a model drug. Behenic acid and lactose were used as coating materials. The effects of lactose content and pH of the dissolution medium on drug release were investigated. The porosity and the tortuosity of the surface matrix layer were calculated. Four formulations of wax matrices containing different percentages of lactose in the surface layer, i.e. 70, 65, 60 and 55, were prepared. The lag times of indomethacin release from the matrices in 0.05 M phosphate buffer pH 7.4 were 50, 162, 294 and 539 minutes for formulations containing 70, 65, 60 and 55% lactose, respectively. The release of drug from formulations containing lactose in the range of 60-70% in different media, i.e. 0.05 M phosphate buffer pH 7.4, 0.05 M alkaline borate buffer pH 8.5 and in the case of pH changed media from pH 1.3 to pH 7.4, was not different (p=0.1). This implies that the different environment in the gastro-intestinal tract will not affect the release of this delivery device. The required lag time period can be met by varying the amount of lactose. PMID:15299241

Peerapattana, Jomjai; Otsuka, Kuniko; Otsuka, Makoto

2004-01-01

200

Formulation and design of sustained release matrix tablets of metformin hydrochloride: Influence of hypromellose and polyacrylate polymers  

PubMed Central

Aim: The current paper was an attempt to design a sustained release dosage form using various grades of hydrophilic polymers, Hypromellose (hydroxyl-propyl methylcellulose [HPMC] K15M, HPMC K100M and HPMC K200M) and Polyacrylate polymers, Eudragit RL100 and Eudragit RS100 with or without incorporating ethyl cellulose on a matrix-controlled drug delivery system of Metformin hydrochloride. Materials and Methods: Laboratory scale batches of nine tablet formulations were prepared by wet granulation technique (Low shear). Micromeritic properties of the granules were evaluated prior to compression. Tablets were characterized as crushing strength, friability, weight variation, thickness, drug content or assay and evaluated for in-vitro release pattern for 12 h using Phosphate buffer of pH 6.8 at 37 ± 0.5°C. The in-vitro release mechanism was evaluated by kinetic modeling. Results and Discussion: The results obtained revealed that HPMC K200M at a concentration of 26% in formulation (F6) was able to sustain the drug release for 12 h and followed the Higuchi pattern quasi-Fickian diffusion. With that, combined effect of HPMC K15M as an extragranular section and Eudragit RS100 displayed a significant role in drug release. Dissolution data were compared with innovator for similarity factor (f2), and exhibited an acceptable value of ?50 Three production validation scale batches were designed based on lab scale best batch and charged for stability testing, parameters were within the limit of acceptance. There was no chemical interaction found between the drug and excipients during Fourier Transform Infrared Spectroscopy (FTIR) and Differential scanning calorimetry study. Conclusion: Hence, combinely HPMC K200M and Eudragit RS100 at a suitable concentration can effectively be used to sustain drug release. PMID:23776841

Roy, Harekrishna; Brahma, Chandan K; Nandi, Sisir; Parida, Kirti R

2013-01-01

201

Sustained-release and swelling characteristics of xanthan gum/ethylcellulose-based injection moulded matrix tablets: in vitro and in vivo evaluation.  

PubMed

Sustained-release matrix tablets were developed by injection moulding using metoprolol tartrate (MPT) and ethylcellulose (EC) as sustained-release agent. Dibutyl sebacate was selected as plasticiser. The influence of matrix composition, plasticiser concentration, and drug load on drug release was evaluated. The influence of plasticiser addition was assessed on processability and drug release: Dibutyl sebacate was added to a dichloromethane/EC solution and subsequently spray-dried, or was mixed as a liquid with EC powder. Hydrated tablets were evaluated by frequency sweep and creep rheological tests to correlate the results with drug release. Xanthan gum (XG) was added to the formulation because drug release was too slow (<50%, 24 h) from EC/MPT matrices (70%/30%, w/w). Increasing XG concentrations provided faster MPT release rates characterised by zero-order release kinetics, no burst release was observed. Lower plasticiser concentrations and higher drug loads increased drug release substantially. The plasticiser addition method did not affect drug release. Matrix composition, drug load, and plasticiser level affected the rheological properties of the swollen matrix tablets. X-ray diffraction demonstrated the formation of solid dispersions. Formulations composed of XG/EC (ratio 1:1.5) and 30% (w/w) MPT had a low relative bioavailability compared with the commercial product Lopressor®, which significantly improved at higher MPT concentration (50%, w/w). PMID:21254067

Quinten, T; De Beer, T; Onofre, F O; Mendez-Montealvo, G; Wang, Y J; Remon, J P; Vervaet, C

2011-07-01

202

Jejunal ulceration and stricture due to wax-matrix potassium chloride tablets and amitriptyline.  

PubMed

A 68-year-old woman presented with abdominal distention of several weeks duration and an acute small bowel obstruction. For several years she had been prescribed amitriptyline 150 mg/d, L-thyroxine 100 micrograms/d, and digoxin 0.25 mg/d. For the previous year she had been taking hydrochlorothiazide 50 mg/d and wax-matrix KCl 20 mEq/d for hypertension. At surgery a "napkin-ring" stricture of the midjejunum was found. It had microscopic features consistent with KCl local toxicity. It is speculated that delayed gastrointestinal motility secondary to amitriptyline predisposed this patient to wax-matrix KCl toxicity and that this potential side effect be considered when prescribing wax-matrix KCl. PMID:3429685

Bronson, D L; Gamelli, R L

1987-10-01

203

Swelling kinetics of spray-dried chitosan acetate assessed by magnetic resonance imaging and their relation to drug release kinetics of chitosan matrix tablets  

Microsoft Academic Search

Magnetic resonance imaging (MRI) was used to assess in situ swelling behaviors of spray-dried chitosan acetate (CSA) in 0.1N HCl, pH 6.8 and pH 5.0 Tris–HCl buffers. The in vitro drug releases from CSA matrix tablets containing the model drugs, diclofenac sodium and theophylline were investigated in all media using USP-4 apparatus. The effect of chitosan molecular weight, especially in

Kampanart Huanbutta; Pornsak Sriamornsak; Sontaya Limmatvapirat; Manee Luangtana-anan; Yasuo Yoshihashi; Etsuo Yonemochi; Katsuhide Terada; Jurairat Nunthanid

2011-01-01

204

Comparison of Release-Controlling Efficiency of Polymeric Coating Materials Using Matrix-type Casted Films and Diffusion-Controlled Coated Tablet  

Microsoft Academic Search

Polymeric coating materials have been widely used to modify release rate of drug. We compared physical properties and release-controlling\\u000a efficiency of polymeric coating materials using matrix-type casted film and diffusion-controlled coated tablet. Hydroxypropylmethyl\\u000a cellulose (HPMC) with low or high viscosity grade, ethylcellulose (EC) and Eudragit® RS100 as pH-independent polymers and\\u000a Eudragit S100 for enteric coatings were chosen to prepare the

Zong-Zhu Piao; Kyoung-Ho Lee; Dong-Jin Kim; Hong-Gu Lee; Jaehwi Lee; Kyung Taek Oh; Beom-Jin Lee

2010-01-01

205

Optimization of acyclovir oral tablets based on gastroretention technology: factorial design analysis and physicochemical characterization studies.  

PubMed

The purpose of this research was to prepare a floating drug delivery system of acyclovir. Floating matrix tablets of acyclovir were developed to prolong gastric residence time and increase its bioavailability. The tablets were prepared by direct compression technique, using polymers such as hydroxypropylmethylcellulose 4000, Compritol 888. Sodium bicarbonate was used as a gas-generating agent. A 3² factorial design using the Design Expert Software (version 7.1.6) was applied to optimize the drug release profile systematically. The amounts of hydroxypropylmethylcellulose 4000 (X?) and Compritol 888 (X?) were selected as independent variables and the percentage drug released in 1 (Q?), 6 (Q?), and 12 (Q??) h as dependent variables. The results of factorial design indicated that a high level of both hydroxypropylmethylcellulose 4000 (X?) and Compritol 888 (X?) favors the preparation of floating controlled-release of acyclovir tablets. Also, a good correlation was observed between predicted and actual values of the dependent variables chosen for the study. By fitting the data into zero-order, first-order, and Higuchi models, we concluded that the release followed Higuchi diffusion kinetics. Storage of the prepared formulations at 40°C/75% relative humidity for 3 months showed no significant change in drug release profiles and buoyancy of the floating tablets. We can conclude that a combination of hydroxypropylmethylcellulose 4000, Compritol 888, and sodium bicarbonate can be used to increase the gastric residence time of the dosage form up to 12?h. These floating tablets seem to be a promising gastroretentive drug delivery system. PMID:21401342

El Gamal, Safaa S; Naggar, Viviane F; Allam, Ahmed N

2011-07-01

206

Swelling kinetics of spray-dried chitosan acetate assessed by magnetic resonance imaging and their relation to drug release kinetics of chitosan matrix tablets.  

PubMed

Magnetic resonance imaging (MRI) was used to assess in situ swelling behaviors of spray-dried chitosan acetate (CSA) in 0.1N HCl, pH 6.8 and pH 5.0 Tris-HCl buffers. The in vitro drug releases from CSA matrix tablets containing the model drugs, diclofenac sodium and theophylline were investigated in all media using USP-4 apparatus. The effect of chitosan molecular weight, especially in pH 6.8 Tris-HCl, was also studied. In 0.1N HCl, the drug release from the matrix tablets was the lowest in relation to the highest swelling of CSA. The swelling kinetics in Tris-HCl buffers are Fickian diffusion according to their best fit to Higuchi's model as well as the drug release kinetics in all the media. The high swelling rate (k(s)(')) was found to delay the drug release rate (k'). The linear relationship between the swelling and fractions of drug release in Tris-HCl buffers was observed, indicating an important role of the swelling on controlling the drug release mechanism. Additionally, CSA of 200 and 800 kDa chitosan did not swell in pH 6.8 Tris-HCl but disintegrated into fractions, and the drug release from the matrix tablets was the highest. PMID:21129484

Huanbutta, Kampanart; Sriamornsak, Pornsak; Limmatvapirat, Sontaya; Luangtana-anan, Manee; Yoshihashi, Yasuo; Yonemochi, Etsuo; Terada, Katsuhide; Nunthanid, Jurairat

2011-02-01

207

Modulation of the dissolution profiles from Geomatrix multi-layer matrix tablets containing drugs of different solubility.  

PubMed

A new multi-layer tablet design has recently been proposed for constant drug release: Geomatrix Technology (Jago Pharma, Muttenz, Switzerland). It consists in the application of a drug-free barrier layer on one or both bases of an active core (hydrophilic matrix). The partial coating modulates the core hydration process and reduces the surface area available for drug release. The result is an extended release that draws close to a linear profile. The device was mainly intended for soluble drugs, while an excessive reduction of the release rate may be obtained with drugs of low solubility. In this study a new time-dependent polymeric barrier is proposed to control the release of sparingly soluble drugs. Two different barrier compositions (one swellable and one erodible) are applied on active cores containing drugs of different water solubility, Trapidil, Ketoprofen and Nicardipine hydrochlorides, and the drug dissolution patterns of the different multi-layer devices are compared. During dissolution, the swellable barrier swells and gels, but is not eroded, thus acting as a modulating membrane during the release process. The erodible barrier, instead, is progressively removed by the dissolution medium, exposing in time an increasing extent of the planar surface(s) of the core to interaction with the outer environment and to drug release. Both types of coatings are able to control drug release from the devices: the swellable barrier shows a stronger modulation efficiency and is more suitable to modify the delivery pattern of highly soluble drugs; the erodible barrier shows a time-dependent coating effect that provides better control of the dissolution profile of sparingly soluble drugs. PMID:8718934

Conte, U; Maggi, L

1996-05-01

208

Extended release of a large amount of highly water-soluble diltiazem hydrochloride by utilizing counter polymer in polyethylene oxides (PEO)/polyethylene glycol (PEG) matrix tablets.  

PubMed

The purpose of this study was to evaluate the feasibility of using a counter polymer in polyethylene oxide (PEO)/polyethylene glycol (PEG) polymeric matrices for the sustained release of a large amount of highly water-soluble drug. PEO/PEG matrix tablets (CR-A) containing four drugs with different water solubilities were prepared to investigate the effect of drug solubility on the drug-release and diffusion properties of PEO/PEG matrices. Cross-linked carboxyvinyl polymer (CVP)/PEO/PEG matrix tablets (CR-B) containing a water-soluble drug, diltiazem hydrochloride (DTZ), were also prepared, and their in vitro characteristics were compared with those of CR-A. Their in vitro drug release properties were evaluated using a dissolution test, and the polymeric erosion and drug diffusion properties of the matrices were also calculated. Drugs with higher solubility in water were released faster for the CR-A. The drug-release rate also increased with the amount of drug loaded. CR-A containing 50% DTZ (by weight) extended drug release by only 6h. This confirms the difficulty experienced when trying to formulate PEO/PEG matrices for the sustained release of a large amount of highly water-soluble drugs due to large drug diffusion. In an attempt to control this issue, a polymer bearing a charge opposite that of the drug was used to effectively decrease the diffusion of DTZ, resulting in sustained release for 24h or longer. These results suggested that including counter polymer in the PEO/PEG matrix tablet is a useful tool for achieving the sustained release of a large amount of highly water-soluble drug. PMID:18606223

Kojima, Hiroyuki; Yoshihara, Keiichi; Sawada, Toyohiro; Kondo, Hiromu; Sako, Kazuhiro

2008-10-01

209

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

2006-05-01

210

Development of Controlled-Release Matrix Tablet of Risperidone: Influence of Methocel®- and Ethocel®Based Novel Polymeric Blend on In Vitro Drug Release and Bioavailability  

Microsoft Academic Search

Controlled-release (CR) matrix tablet of 4 mg risperidone was developed using flow bound dry granulation–slugging method to\\u000a improve its safety profile and compliance. Model formulations F1, F2, and F3, consisting of distinct blends of Methocel® K100\\u000a LV-CR and Ethocel® standard 7FP premium, were slugged. Each batch of granules (250–1,000 ?m), obtained by crushing the slugs,\\u000a was divided into three portions after lubrication

Amir Badshah; Fazal Subhan; Khalid Rauf; Nadeem Irfan Bukhari; Kifayatullah Shah; Samiullah Khan; Zia Ahmed; Ihsanullah Khan

2011-01-01

211

Encapsulation of antihypertensive drugs in cellulose-based matrix microspheres: characterization and release kinetics of microspheres and tableted microspheres.  

PubMed

This study is an attempt to prepare microspheres loaded with two antihypertensive drugs viz., nifedipine (NFD) and verapamil hydrochloride (VRP) using cellulose-based polymers viz., ethyl cellulose (EC) and cellulose acetate (CA). Emulsification and solvent evaporation methods were optimized using ethyl acetate as a dispersing solvent. The particles are spherical in shape and have smooth surfaces, as evidenced by the scanning electron microscopy. The microspheres were characterized for their particle size and distribution, tapped density and encapsulation efficiency. Smaller sized particles with a narrow size distribution were produced with EC when compared to CA matrices. Molecular level drug distribution in the microspheres was confirmed by differential scanning calorimetry. The microspheres were directly compressed into tablets using different excipients. The drug release from CA was faster than EC microspheres and, also, the VRP release was faster than NFD. The excipients used in tableting showed an effect on the release as well as the physical properties of the tablets. PMID:11308229

Soppimath, K S; Kulkarni, A R; Aminabhavi, T M

2001-01-01

212

Eudragit(®) RS PO/RL PO as rate-controlling matrix-formers via roller compaction: Influence of formulation and process variables on functional attributes of granules and tablets.  

PubMed

The influence of plasticizer level, roll pressure and sintering temperature was investigated on the granule properties, tablet breaking force and theophylline release from tablets. Nine formulations using theophylline as a model drug, Eudragit(®) RL PO, Eudragit(®) RS PO, or both as a matrix former and triethyl citrate (TEC) as a plasticizer were prepared. The formulations were roller compacted and the granules obtained were evaluated for particle size distribution and flowability. These granules were compacted into tablets at a compression force of 7?kN. The tablets were thermally treated at different temperatures (50 and 75°C) for 5?h and were evaluated for breaking force and dissolution. Increase in roll pressure and TEC levels resulted in a progressive increase in the mean particle size of the granules. The flowability of the granules also improved with increasing roll pressures and TEC levels. Tablet breaking force increased with an increase in TEC levels and sintering temperatures. But these effects were significant only at the highest level of plasticizer and sintering temperature respectively. For the tablets containing Eudragit(®) RS PO, theophylline release decreased proportionately with increase in TEC levels and sintering temperatures. Tablets containing either Eudragit(®) RL PO or a mixture of RS PO and RL PO failed to impart an extended-release property to the tablets at the studied variables i.e. roll pressure, TEC levels and sintering temperature. It was clearly demonstrated that with suitable optimization of these parameters, the release-rate of a water soluble drug from the matrix tablets prepared via roller compaction can be finely controlled. PMID:22257339

Dave, Vivek S; Fahmy, Raafat M; Bensley, Dennis; Hoag, Stephen W

2012-10-01

213

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

214

Some variables affecting the characteristics of Eudragit E-sodium alginate polyelectrolyte complex as a tablet matrix for diltiazem hydrochloride.  

PubMed

Eudragit E (EE)-sodium alginate (SA) polyelectrolyte complexes (PECs) were prepared at pH 4 and 5.8 using sodium alginate of high (SAH) and low viscosity (SAL). The optimum EE-SA complexation mass ratio was determined using viscosity measurements. Interactions between EE and SA in PECs were characterized by Fourier transform infra-red spectroscopy (FT-IR) and differential scanning calorimetry (DSC). Diltiazem hydrochloride (DTZ HCl) tablets were prepared using the prepared EE-SA PECs and their physical mixtures at different ratios as matrices. Tablets were evaluated for swelling characteristics and in vitro drug release. Tablets containing EE-SAH physical mixtures of ratios (1.5:1 and 1:3) as matrices were effective in achieving sustained release of DTZ HCl, where the percent drug released was significantly (p < 0.05) decreased compared to that from tablets either containing the same ratios of EE-SAL physical mixtures or the preformed EE- -SAH and EE-SAL PECs. PMID:24670354

Yusif, Rehab Mohammad; Abu Hashim, Irhan Ibrahim; El-Dahan, Marwa Salah

2014-03-01

215

Investigation of the impact of insoluble diluents on the compression and release properties of matrix based sustained release tablets  

Microsoft Academic Search

In the present study the effect of insoluble diluents such as microcrystalline cellulose (MCC) and dibasic calcium phosphate (DCP) on the compression characteristics and release profile of sustained release tablets containing Hydroxypropylmethylcellulose (HPMC) matrices was investigated. The effect of diluents on the compression characteristics was studied using Heckel and Kawakita equations. The effect of compression forces on the release profile

M. P. Vaidya; A. M. Avachat

2011-01-01

216

Formulation and in vitro evaluation of ofloxacin-ethocel controlled release matrix tablets prepared by wet granulation method: influence of co-excipients on drug release rates.  

PubMed

Being controlled release dosage forms, tablets allow an improved absorption and release profiles of Ofloxacin. The fact that drugs with fine particles size can be compressed well after wetting, so in our research studies Ofloxacin controlled release matrix tablets were prepared by wet granulation technique. In order to investigate the potential of Ethyl cellulose ether derivatives as a matrix material, Ofloxacin formulations with different types and grades of Ethocel were prepared at several drug-to-polymer ratios. The method adopted for in vitro drug release studies was USP Method-1 (rotating Basket Method) by Pharma test dissolution apparatus using phosphate buffer 7.4 pH as a dissolution medium. Various Kinetic models were employed to the formulations for the purpose of determination of release mechanism. A comparative study was performed between the tested Ofloxacin-Ethocel formulations and a standard reference obtained from the local market. F1 dissimilarity factor and f2 similarity factor were applied to the formulations for the checking of dissimilarities and similarities between the tested formulations and reference standard. PMID:21715257

Shah, Shefaatullah; Shah, Kifayatullah; Jan, Syed Umer; Ahmad, Kamran; Rehman, Asimur; Hussain, Abid; Khan, Gul Majid

2011-07-01

217

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

PubMed

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

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

2012-04-01

218

Study the effect of formulation variables on drug release from hydrophilic matrix tablets of milnacipran and prediction of in-vivo plasma profile.  

PubMed

The objective of this study was to design oral controlled release (CR) matrix tablets of Milnacipran using hydroxypropyl methylcellulose (HPMC) as the retardant polymer and to study the effect of various formulation factors such as polymer proportion, polymer viscosity, compression force and also the pH of dissolution medium on the in-vitro release of drug. Two viscosity grade of HPMC (15?K and 100?K) were used in the proportion of 50, 100, 150 and 200?mg per CR tablet. In-vitro release rate was characterized using various model dependent approaches and model independent dissolution parameters [T50% and T80% dissolution time, mean dissolution time (MDT), mean residence time (MRT), dissolution efficiency (DE)]. The statistical analysis was performed on all the model independent approaches using student t test and ANOVA. Results were found that as polymer concentration (50?mg to 200?mg) and viscosity (15?K to 100?K) increases, the MDT, MRT, T50% and T80% extended significantly. Drug release rate was found to be significantly different at different hardness. In-vivo human plasma concentration--time profile was predicted from in-vitro release data using convolution method. Predicted human pharmacokinetic parameters shows that the design CR formulation has capability to sustained the plasma drug level of milnacipran. PMID:23931031

Singhvi, Gautam; Shah, Abhishek; Yadav, Nilesh; Saha, Ranendra N

2014-09-01

219

Hardware Acceleration for Finite Element Electromagnetics: Efficient Sparse Matrix Floating-Point Computations with Field Programmable Gate Arrays  

Microsoft Academic Search

Custom hardware acceleration of electromagnetics computations leverages favorable industry trends, which indicate reconfigurable hardware devices such as field programmable gate arrays (FPGAs) may soon outperform general purpose CPUs. We present a new striping method for efficient sparse matrix-vector multiplication implemented in a deeply pipelined FPGA design. The effectiveness of the new method is illustrated for a representative set of finite

Yousef El Kurdi; Warren J. Gross; Dennis Giannacopoulos

2006-01-01

220

Design and Optimization of Floating Drug Delivery System of Acyclovir  

PubMed Central

The purpose of the present work was to design and optimize floating drug delivery systems of acyclovir using psyllium husk and hydroxypropylmethylcellulose K4M as the polymers and sodium bicarbonate as a gas generating agent. The tablets were prepared by wet granulation method. A 32 full factorial design was used for optimization of drug release profile. The amount of psyllium husk (X1) and hydroxypropylmethylcellulose K4M (X2) were selected as independent variables. The times required for 50% (t50%) and 70% (t70%) drug dissolution were selected as dependent variables. All the designed nine batches of formulations were evaluated for hardness, friability, weight variation, drug content uniformity, swelling index, in vitro buoyancy, and in vitro drug release profile. All formulations had floating lag time below 3 min and constantly floated on dissolution medium for more than 24 h. Validity of the developed polynomial equation was verified by designing two check point formulations (C1 and C2). The closeness of predicted and observed values for t50% and t70% indicates validity of derived equations for the dependent variables. These studies indicated that the proper balance between psyllium husk and hydroxypropylmethylcellulose K4M can produce a drug dissolution profile similar to the predicted dissolution profile. The optimized formulations followed Higuchi's kinetics while the drug release mechanism was found to be anomalous type, controlled by diffusion through the swollen matrix. PMID:21694992

Kharia, A. A.; Hiremath, S. N.; Singhai, A. K.; Omray, L. K.; Jain, S. K.

2010-01-01

221

Design and optimization of floating drug delivery system of acyclovir.  

PubMed

The purpose of the present work was to design and optimize floating drug delivery systems of acyclovir using psyllium husk and hydroxypropylmethylcellulose K4M as the polymers and sodium bicarbonate as a gas generating agent. The tablets were prepared by wet granulation method. A 3(2) full factorial design was used for optimization of drug release profile. The amount of psyllium husk (X1) and hydroxypropylmethylcellulose K4M (X2) were selected as independent variables. The times required for 50% (t(50%)) and 70% (t(70%)) drug dissolution were selected as dependent variables. All the designed nine batches of formulations were evaluated for hardness, friability, weight variation, drug content uniformity, swelling index, in vitro buoyancy, and in vitro drug release profile. All formulations had floating lag time below 3 min and constantly floated on dissolution medium for more than 24 h. Validity of the developed polynomial equation was verified by designing two check point formulations (C1 and C2). The closeness of predicted and observed values for t(50%) and t(70%) indicates validity of derived equations for the dependent variables. These studies indicated that the proper balance between psyllium husk and hydroxypropylmethylcellulose K4M can produce a drug dissolution profile similar to the predicted dissolution profile. The optimized formulations followed Higuchi's kinetics while the drug release mechanism was found to be anomalous type, controlled by diffusion through the swollen matrix. PMID:21694992

Kharia, A A; Hiremath, S N; Singhai, A K; Omray, L K; Jain, S K

2010-09-01

222

Development and in vitro characterization of floating sustained-release drug delivery systems of polyphenols.  

PubMed

The aim of this study was to develop and characterize floating stomach-retentive matrix tablets that will deliver polyphenols in a controlled release manner. The tablets were prepared by direct compression. A number of polymers were examined and egg albumin was chosen in light of a better performance in terms of floating behavior and decomposition time. Dissolution studies for three representative polyphenols loaded into a number of formulations were performed using the "f?" factor in order to compare release profiles of different polyphenols and formulations. The release data showed a good fit into the power law equation and zero-order kinetics has been determined for some of the systems. Erosion and textural analysis studies revealed that higher concentration of egg albumin results in a higher gel strength that is less susceptible to erosion, potentially leading to a prolonged delivery time of drug. The ability of egg albumin-based tablets to resist high mechanical forces was also determined, while comparison to cellulose-derived polymers revealed that the latter have a much lower ability to resist the same forces. The developed delivery system has the potential to increase the efficacy of the therapy for various pathological stomach conditions and to improve patient compliance. PMID:23730744

Rosenzweig, Ohad; Lavy, Eran; Gati, Irith; Kohen, Ron; Friedman, Michael

2013-01-01

223

Artificial neural networks in the modeling and optimization of aspirin extended release tablets with eudragit L 100 as matrix substance  

Microsoft Academic Search

The purpose of the present study was to model the effects of the concentration of Eudragit L 100 and compression pressure\\u000a as the most important process and formulation variables on the in vitro release profile of aspirin from matrix tables formulated\\u000a with Eudragit L 100 as matrix substance and to optimize the formulation by artificial neural network. As model formulations,

Svetlana Ibri?; Milica Jovanovi?; Zorica Djuri?; Jelena Paroj?i?; Slobodan D. Petrovi?; Ljiljana Solomun; Biljana Stupar

2003-01-01

224

Properties of gastroretentive sustained release tablets prepared by combination of melt/sublimation actions of L-menthol and penetration of molten polymers into tablets.  

PubMed

A novel floating sustained release tablet having a cavity in the center was developed by utilizing the physicochemical properties of L-menthol and the penetration of molten hydrophobic polymer into tablets. A dry-coated tablet containing famotidine as a model drug in outer layer was prepared with a L-menthol core by direct compression. The tablet was placed in an oven at 80°C to remove the L-menthol core from tablet. The resulting tablet was then immersed in the molten hydrophobic polymers at 90°C. The buoyancy and drug release properties of tablets were investigated using United States Pharmacopeia (USP) 32 Apparatus 2 (paddle 100 rpm) and 900 ml of 0.01 N HCl. The L-menthol core in tablets disappeared completely through pathways in the outer layer with no drug outflows when placed in an oven for 90 min, resulting in a formation of a hollow tablet. The hollow tablets floated on the dissolution media for a short time and the drug release was rapid due to the disintegration of tablet. When the hollow tablets were immersed in molten hydrophobic polymers for 1 min, the rapid drug release was drastically retarded due to a formation of wax matrices within the shell of tablets and the tablets floated on the media for at least 6 h. When Lubri wax® was used as a polymer, the tablets showed the slowest sustained release. On the other hand, faster sustained release properties were obtained by using glyceryl monostearate (GMS) due to its low hydrophobic nature. The results obtained in this study suggested that the drug release rate from floating tablets could be controlled by both the choice of hydrophobic polymer and the combined use of hydrophobic polymers. PMID:21963630

Fukuda, Mamoru; Goto, Akinori

2011-01-01

225

Effect of hydrophilic natural gums in formulation of oral-controlled release matrix tablets of propranolol hydrochloride.  

PubMed

In order to develop a controlled delivery of highly water-soluble propranolol hydrochloride (PPHCl) using hydrophilic natural gums (xanthan gum [X] and locust bean gum [LBG]) as cost-effective, nontoxic, easily available. The granules of PPHCl were prepared by wet granulation method using a different ratios drug: gum ratios of X, LBG and XLBG(X and LBG in 1:1 ratios). To increase the flowability and compressibility of the granules, and to prevent its adhesion to punch and die, magnesium stearate and talc were added to the granules in 1:2 ratios before punching. The tablet was analysed to determine hardness, friability, % assay and invitro release study was carried out. The release of PPHCl from a gelatinous swollen mass, which controls the diffusion of drug molecules through the polymeric material into aqueous medium. The XLBG matrice shows precise controlled release than the X and LBG matrice because of burst effect and fast release in case of X and LBG matrice respectively and there was no chemical interaction between drug and polymer in XLBG formulation as confirmed by FTIR studies. First pass effect of PPHCl can be avoided by these formulations. Matrices with XLBG show zero-order release via swelling, diffusion and relaxation mechanism. The XLBG matrice leads to more precise result than X and LBG alone by the utilization of synergistic interaction between two biopolymers and uniformity in the hydration layer in dissolution media. However, according to the similarity factor (f(2)) XLBG3 were the most similar formulations to Lol-SR as the reference standard. PMID:19339235

Rajesh, K S; Venkataraju, M P; Gowda, D V

2009-04-01

226

Ice Floats  

NSDL National Science Digital Library

This is a lesson about displacement, buoyancy, and density. Learners will understand why ice floats. Includes background information, teacher notes, assessment criteria, and related resources; activities are differentiated for Pre-K-grade 2 and grades 3-5. This is lesson 4 of the unit Exploring Ice in the Solar System.

227

On floats and float tests  

NASA Technical Reports Server (NTRS)

The principal source of information on float resistance is the model test. In view of the insuperable difficulties opposing any attempt at theoretical treatment of the resistance problem, particularly at attitudes which tend toward satisfactory take-off, such as the transitory stage to planing, the towing test is and will remain the primary method for some time.

Seewald, Friedrich

1931-01-01

228

Effect of HPMC - E15 LV premium polymer on release profile and compression characteristics of chitosan/ pectin colon targeted mesalamine matrix tablets and in vitro study on effect of pH impact on the drug release profile.  

PubMed

The study was designed to investigate the in vitro dissolution profile and compression characteristics of colon targeted matrix tablets prepared with HPMC E15 LV in combination with pectin and Chitosan. The matrix tablets were subjected to two dissolution models in various simulated fluids such as pH 1.2, 6, 6.8, 7.2, 5.5. The fluctuations in colonic pH conditions during IBD (inflammatory bowel disease) and the nature of less fluid content in the colon may limit the expected drug release in the polysaccharide-based matrices when used alone. The Hydrophilic hydroxyl propyl methylcellulose ether premium polymer (HPMC E15 LV) of low viscosity grade was used in the formulation design, which made an excellent modification in physical and compression characteristics of the granules. The release studies indicated that the prepared matrices could control the drug release until the dosage form reaches the colon and the addition HPMC E15 LV showed the desirable changes in the dissolution profile by its hydrophilic nature since the colon is known for its less fluid content. The hydrophilic HPMC E15 LV allowed the colonic fluids to enter into the matrix and confirmed the drug release at the target site from a poorly water soluble polymer such as Chitosan and also from water soluble Pectin. The dramatic changes occurred in the drug release profile and physicochemical characteristics of the Pectin, Chitosan matrix tablets when a premium polymer HPMC E15 LV added in the formulation design in the optimized concentration. Various drug release mechanisms used for the examination of drug release characteristics. Drug release followed the combined mechanism of diffusion, erosion, swelling and polymer entanglement. In recent decade, IBD attracts many patents in novel treatment methods by using novel drug delivery systems. PMID:24597626

Newton, A M J; Lakshmanan, Prabakaran

2014-04-01

229

Preparation and in-vitro in-vivo evaluation of sustained release matrix diclofenac sodium tablets using PVP-K90 and natural gums.  

PubMed

Conventional dosage form is nowadays mostly replaced by sustained release formulation in order to increase drug efficacy and patient compliance. The sustained release properties of the PVP K90 alone and in combination with guar gum, xanthan gum and gum tragacanth were evaluated using diclofenac sodium (100 mg/tablet) as a model drug. Tablets were processed using wet granulation method and evaluated for sustained drug release properties. The drug release from the formulations was studied in relationship with Commercially available Diclofenac Sodium SR, used as a reference tablets and results were expressed as similarity (f1) and differential factor (f2). The tablets prepared using PVP K90 160 mg/tablet sustained the release of diclofenac sodium for 12 hours. Formulations where the PVP K90 was partially replaced with different gums also sustained the release of drug for 12 hours. The release of the drug from these formulations mainly followed Higuchi model and super case-II and Non-Fickian diffusion. The in-vivo drug release was studied in healthy human volunteers using non-blinded cross over, two period design using Diclofenac Sodium SR Tablets as a reference drug. The relative bioavailability of the formulation containing PVP K90 and gum tragacanth was 0.91. The studies showed that the use of the PVP K90 in combination with gum tragacanth both in-vitro and in-vivo sustained the release of the drug. PMID:21959802

Iqbal, Zafar; Khan, Raza; Nasir, Fazli; Khan, Jamshaid Ali; Rashid, Abdur; Khan, Abbas; Khan, Abad

2011-10-01

230

Preparation and in vitro evaluation of sustained release tablet formulations of diclofenac sodium  

Microsoft Academic Search

The effects of formulation variables on the release profile of diclofenac sodium (DS) from hydroxypropylmethyl cellulose (HPMC) and chitosan matrix tablets were studied. DS tablets were prepared by wet granulation and direct compression methods and different ratios of HPMC and chitosan were used. Physical properties of the prepared tablets and targeted commercial sustained release (SR) tablet and the drug release

Ayhan Sava?er; Yalç?n Özkan; A?k?n I??mer

2005-01-01

231

Matrix tablets: the effect of hydroxypropyl methylcellulose/anhydrous dibasic calcium phosphate ratio on the release rate of a water-soluble drug through the gastrointestinal tract I. In vitro tests.  

PubMed

Different hydroxypropyl methylcellulose (HPMC)/anhydrous dibasic calcium phosphate (ADCP) matrix tablets have been developed aiming to evaluate the influence of both components ratio in the control release of a water-soluble drug (theophylline). In order to characterise the matrix tablets, swelling, buoyancy and dissolution studies have been carried out in different aqueous media (demineralised water, progressive pH medium, simulated gastric fluid, simulated intestinal fluid and simulated colonic fluid). The HPMC/ADCP ratio has turned out to be the determinant in the matrix behaviour: the HPMC characteristic swelling behaviour was modulated, in some cases, by the ADCP characteristic acidic dissolution. When the HPMC/ADCP ratio was ?0.69, buoyancy, continuous swelling and low theophylline dissolution rate from the matrices (H1, H2 and H3) were observed in all dissolution media. Consequently, these formulations could be adequate as gastro-retentive drug delivery systems. Additionally, HPMC/ADCP ratio ?0.11 (H5 and H6) induces a pH-dependent drug release which could be applied to design control drug release enteric formulations (with a suitable enteric coating). Finally, a HPMC/ADCP ratio between 0.11 and 0.69 (H4) yield a gastrointestinal controlled drug release, due to its time-dependent buoyancy (7 h) and a total drug delivery in 17 h in simulated colonic fluid. PMID:22907778

Mamani, Pseidy L; Ruiz-Caro, Roberto; Veiga, María D

2012-12-01

232

Preparation of Carbopol/chitosan interpolymer complex as a controlled release tablet matrix; effect of complex formation medium on drug release characteristics.  

PubMed

Chitosan/Carbopol971NF (poly acrylic acid) interpolymer complexes were prepared in pH 3.0, 4.0, and 5.0 medium to control the ratio of chitosan and Carbopol971NF in the interpolymer complex. FT-IR analysis confirmed that the mechanism of complexation involved an electrostatic interaction between the NH3+ of chitosan and COO(-) of Carbopol971NF. An increase in the pH of the preparation medium was accompanied by an increase in the ratio of chitosan in the chitosan/Carbopol971NF complex. The maximum yield of interpolymer complexes prepared at pH 3, 4, and 5 (IPC3, IPC4, IPC 5) were obtained at ratios of 1/10, 1/5, and 1/4 (chitosan/Carbopol971NF), respectively. At pH 1.2, the overall drug release from IPC tablets did not show significant differences. However, at pH 6.8, the rate of drug release from the IPC5 tablet was higher than that from the IPC4 tablet. The release rate from the IPC3 tablet was observed to increase with time. The release mechanism was increasingly dominated by the relaxational contribution in the order of IPC3, IPC5, and IPC4 at pH 6.8. The diffusional contribution was dominated only in the early stage of drug release and the relaxational contribution gradually increased with time. PMID:18704338

Lee, Myung-Hak; Chun, Myung-Kwan; Choi, Hoo-Kyun

2008-07-01

233

Development of a Floating Dosage Form of Ranitidine Hydrochloride by Statistical Optimization Technique  

PubMed Central

The objective of this study was to evaluate the effect of formulation variables on the release properties, floating lag time, and hardness, when developing floating tablets of Ranitidine hydrochloride, by the statistical optimization technique. The formulations were prepared based on 32 factorial design, with polymer ratio (HPMC 100 KM: Xanthan gum) and the amount of aerosil, as two independent formulation variables. The four dependent (response) variables considered were: percentage of drug release at the first hour, T50% (time taken to release 50% of the drug), floating lag time, and hardness of the tablet. The release profile data was subjected to a curve fitting analysis, to describe the release mechanism of the drug from the floating tablet. An increase in drug release was observed with an increase in the polymer ratio, and as the amount of aerosil increased, the hardness of the tablet also increased, without causing any change in the floating lag time. The desirability function was used to optimize the response variables, each having a different target, and the observed responses were in accordance with the experimental values. The results demonstrate the feasibility of the model in the development of floating tablets containing Ranitidine hydrochloride. PMID:21264091

Jain, S; Srinath, MS; Narendra, C; Reddy, SN; Sindhu, A

2010-01-01

234

Evaluation of honey locust (Gleditsia triacanthos Linn.) gum as sustaining material in tablet dosage forms.  

PubMed

In this study, honey locust gum (HLG) obtained from Gleditsia triacanthos (honey locust) beans was investigated as a hydrophilic matrix material in the tablets prepared at different concentrations (5% and 10%) by wet granulation method. Theophylline was chosen as a model drug. The matrix tablets containing hydroxyethylcellulose and hydroxypropyl methylcellulose as sustaining polymers at the same concentrations were prepared and a commercial sustained release (CSR) tablet containing 200 mg theophylline was examined for comparison of HLG performance. Physical analysis on CSR tablet, matrix tablets and their granules before compression were performed. According to the results obtained from dissolution studies in distilled water, pH 1.2 HCl buffer and pH 7.2 phosphate buffer, no significant difference was found between CSR tablet and the matrix tablet containing 10% HLG in each medium (P > 0.05) and these tablets showed zero-order kinetic model in all the mediums. PMID:15231434

Uner, Melike; Altinkurt, Turan

2004-07-01

235

Direct analysis of 18 flavonol glycosides, aglycones and terpene trilactones in Ginkgo biloba tablets by matrix solid phase dispersion coupled with ultra-high performance liquid chromatography tandem triple quadrupole mass spectrometry.  

PubMed

Analysis and quality control of Ginkgo biloba have been comprehensively studied. However, little attention has been devoted to the simultaneous extraction and analysis of flavonols and terpene trilactones, especially for direct quantification of flavonol glycosides. This work described a rapid strategy for one-step extraction and quantification of the components. A matrix solid phase dispersion (MSPD) method was designed for the extraction of ginkgo ingredients and compared with the heat-reflux and ultrasonic extraction methods. An ultra-high performance liquid chromatography (UHPLC)-tandem-triple-quadrupole-mass spectrometry (QQQ-MS) method was developed for detection of the 18 components, including 10 original flavonol glycosides, 3 aglycones, and 5 lactones. Subsequently, the proposed strategy was used for the analysis of 12 G. biloba tablets. Results showed that MSPD produced comparable extraction efficiency but consumed less time and required lower solvent volumes compared with conventional methods. Without hydrolysis, the concentration detected was much closer to the original in the sample. The total flavonol glycoside contents in ginkgo tablets ranged from 3.59 to 125.21?gmg(-1), and the terpene trilactone varied from 3.45 to 57.8?gmg(-1) among different manufacturers. In conclusion, the proposed MSPD and UHPLC-QQQ-MS is rapid and sensitive in providing comprehensive profile of chemical constituents especially the genuine flavonol glycosides for improved quality control of ginkgo products. PMID:24876067

Liu, Xin-Guang; Yang, Hua; Cheng, Xiao-Lan; Liu, Lei; Qin, Yong; Wang, Qi; Qi, Lian-Wen; Li, Ping

2014-08-01

236

Bioequivalence of Clozapine Tablets  

Microsoft Academic Search

Objective To perform a bioequivalence study of clozapine tablets between Clozaril ? tablet (Novartis), the innovator product, and Clopaze ? tablet (Pharminar, Thailand). Method The study was performed in 12 healthy male volunteers for a single 100 mg dose of clozapine tablet. Randomized cross over design was used. Blood samples were collected before and after drug administration for 24 hours

Wandee Taesotikul; Sayam Kaewvichit; Chokchai Wongsinsup; Kittipong Sanichwankul; Wanida Pumpaisalchai

2000-01-01

237

Investigating the in vitro drug release kinetics from controlled release diclofenac potassium-ethocel matrix tablets and the influence of co-excipients on drug release patterns.  

PubMed

The objective of the study was to formulate and evaluate controlled release polymeric tablets of Diclofenac Potassium for the release rate, release patterns and the mechanism involved in the release process of the drug. Formulations with different types and grades of Ethyl Cellulose Ether derivatives in several drug-to-polymer ratios (D:P) were compressed into tablets using the direct compression method. In vitro drug release studies were performed in phosphate buffer (pH 7.4) as dissolution medium by using USP Method-1 (Rotating Basket Method). Similarity factor f2 and dissimilarity factor f1 were applied for checking the similarities and dissimilarities of the release profiles of different formulations. For the determination of the release mechanism and drug release kinetics various mathematical/kinetic models were employed. It was found that all of the Ethocel polymers could significantly slow down the drug release rate with Ethocel FP polymers being the most efficient, especially at D:P ratios of 10:03 which lead towards the achievement of zero or near zero order release kinetics. PMID:21454168

Shah, Shefaat Ullah; Shah, Kifayat Ullah; Rehman, Asimur; Khan, Gul Majid

2011-04-01

238

Floating microspheres: to prolong the gastric retention time in stomach.  

PubMed

A gastroretentive drug delivery system with prolong retention time in the stomach have great practical importance for drugs with an absorption window in the upper small intestine. Floating drug delivery system are expected to remain buoyant in the gastric content for prolong duration of time thus enhance the bioavailability of drugs. There are several gastroretentive drug delivery systems, which are floating microspheres, granules, tablets, powder, pills, laminated films and capsules. Floating microspheres are gaining special attention because of their wide applicability in the targeting of drug to stomach. Floating microspheres have several advantages, that they remain buoyant in the stomach and distributed uniformly to avoid the vagaries of gastric emptying and release the drug for prolong period of time. PMID:22023206

Bhadouriya, Priyanka; Kumar, Manish; Pathak, Kamla

2012-05-01

239

Wet granulation fine particle ethylcellulose tablets: Effect of production variables and mathematical modeling of drug release  

Microsoft Academic Search

In the present study, the applicability of fine particle ethylcellulose (FPEC) to produce matrix tablets by a wet granulation\\u000a technique was evaluated. The effect of various formulation and process variables, such as FPEC content, hardness of the tablet,\\u000a and solubility of the drug, on the release of drug from these tablets was examined. Tablets were prepared by wet granulation\\u000a of

Anjali M. Agrawal; Steven H. Neau; Peter L. Bonate

2003-01-01

240

Design and evaluation of sustained-release and buccal adhesive propranolol hydrochloride tablets  

Microsoft Academic Search

The release of propranolol hydrochloride incorporated into sustained-release and buccal adhesive tablets was studied in vitro. The formulation containing 20% hydroxypropyl methylcellulose (HPMC) yielded good sustained-release matrix tablets. Buccal adhesive controlled-release tablets were prepared by compression of HPMC with polycarbophil (PAA), which served as the bioactive adhesive compound. The release behaviour of buccal adhesive tablets was found to be non-Fickian.

Buket Taylan; Yilmaz Capan; Olgun Güven; Sirri Kes; A. Atilla Hincal

1996-01-01

241

An approach to formulating an oral floating drug delivery system for dexchlorpheniramine maleate using factorial design.  

PubMed

The purpose of this research was to formulate and evaluate a floating tablet formulation of dexchlorpheniramine maleate (DCPM) using full factorial design. A 32 factorial design (nine runs) was utilized to optimize the formulation, the contents of hydroxypropyl methyl cellulose (HPMC) (X1) and Carbopol 934P (X2) being taken as independent variables and t50% (Y1), % drug release after 6 h (Y2), % drug release after 12 h (Y3), and floating lag time (FLT) (Y4) as the dependent variables. The tablets showed 99.2635 to 102.4709 of the labeled amount of dexchlorpheniramine maleate indicating uniformity of content. The tablets containing DCPM released 72.28 to 99.461% of drug at the end of 12 h by an in vitro release study. Hardness, friability, floating capacity, weight variation and content uniformity were also examined. In addition,the tablets were evaluated for in vitro release characteristics for 24 h. The optimal batch (F9) was selected by regression analysis and followed Higuchi kinetics. The drug release mechanism was found to be a complex mixture of diffusion, swelling and erosion. The floating tablets of DCPM developed may be used clinically for prolonged drug release for at least 16 hrs, thereby improving bioavailability and patient compliance. PMID:22888518

Alabazi, M Y; Elzein, H

2012-07-01

242

Charge retention characteristics of silicide-induced crystallized polycrystalline silicon floating gate thin-film transistors for active matrix organic light-emitting diode.  

PubMed

In this work, non-volatile memory thin-film transistor (NVM-TFT) was fabricated by nickel silicide-induced laterally crystallized (SILC) polycrystalline silicon (poly-Si) as the active layer. The nickel seed silicide-induced crystallized (SIC) poly-Si was used as storage layer which is embedded in the gate insulator. The novel unit pixel of active matrix organic light-emitting diode (AMOLED) using NVM-TFT is proposed and investigated the electrical and optical performance. The threshold voltage shift showed 17.2 V and the high reliability of retention characteristic was demonstrated until 10 years. The retention time can modulate the recharge refresh time of the unit pixel of AMOLED up to 5000 sec. PMID:24245194

Park, Jae Hyo; Son, Se Wan; Byun, Chang Woo; Kim, Hyung Yoon; Joo, So Na; Lee, Yong Woo; Yun, Seung Jae; Joo, Seung Ki

2013-10-01

243

Clinical evaluation of sodium flouride chewable tablets in dental caries.  

PubMed

Chewable tablets containing low dosage flouride content were prepared using two varities of celluloses and their in vitro parameters were evaluated. An eighteen month clinical trial revealed that both these formulations were effective in controlling the caries. However, ethyl cellulose is proved to be superior to methylcellulose as a controlled release matrix material in controlling caries. Thus this study recommends ethylcellulose matrix tablets containing low flouride content is an efficacious and cost effective drug device in controlling dental caries. PMID:10865398

Maddi, S S; Tandon, S; Aithal, K S

1999-01-01

244

Float Zone Workshop  

NASA Technical Reports Server (NTRS)

A summary of the Analytical Float Zone Experiment System (AFZES) concept is presented. The types of experiments considered for such a facility are discussed. Reports from various industrial producers and users of float zone material are presented. Special emphasis is placed on state-of-the-art developments in low gravity manufacturing and their applications to space processing.

Naumann, R. J.

1980-01-01

245

Useful Extend-release Chitosan Tablets with High Antioxidant Activity  

PubMed Central

The antioxidant properties of different low molecular weight (LMW) chitosans (CS1; 22 kDa, CS2; 38 kDa, CS3; 52 kDa, CS4; 81 kDa) were examined for possible use in extended-release tablets. The criteria used were the ability of the chitosans to reduce Cu2+, and hydroxyl and superoxide radicals and N-centered radicals derived from 1,1'-diphenyl-2-picrylhydrazyl, via the use of ESR spectrometry. CS2 showed the highest scavenging activity. CS1 and CS3, however, were much less effective and CS4 was not a viable antioxidant. The results suggest that CS2 could be useful in combating the development of oxidative stress. A series of chitosan tablets were prepared using a spray drying method and evaluated as an extended-release matrix tablet using theophylline (TPH) as a model drug. The release of TPH from the different MW chitosan tablets increased with increasing MW of the chitosan used. CS2, CS3 and CS4 showed a reasonable release activity, but CS1 showed the shortest release activity. Moreover, the CS2-TPH tablet showed the highest scavenging activity of the three chitosan tablets (CS2-CS4) using 2,2’-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) radicals. These results suggest that a CS2-TPH tablet could be potentially useful in an extended-release matrix tablet with a high antioxidant activity.

Yasufuku, Taira; Anraku, Makoto; Kondo, Yuko; Hata, Toshiyuki; Hirose, Junzo; Kobayashi, Nobuyuki; Tomida, Hisao

2010-01-01

246

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

247

Floating emitter solar cell  

NASA Technical Reports Server (NTRS)

A front surface contact floating emitter solar cell transistor is provided in a semiconductor body (n-type), in which floating emitter sections (p-type) are diffused or implanted in the front surface. Between the emitter sections, a further section is diffused or implanted in the front surface, but isolated from the floating emitter sections, for use either as a base contact to the n-type semiconductor body, in which case the section is doped n+, or as a collector for the adjacent emitter sections.

Chih, Sah (inventor); Cheng, Li-Jen (inventor)

1987-01-01

248

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

2006-01-01

249

Micromechanisms with floating pivot  

DOEpatents

A new class of tilting micromechanical mechanisms have been developed. These new mechanisms use floating pivot structures to relieve some of the problems encountered in the use of solid flexible pivots.

Garcia, Ernest J. (Albuquerque, NM)

2001-03-06

250

Floating Magnet Demonstration.  

ERIC Educational Resources Information Center

A room-temperature demonstration of a floating magnet using a high-temperature superconductor is described. The setup and operation of the apparatus are described. The technical details of the effect are discussed. (CW)

Wake, Masayoshi

1990-01-01

251

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

252

Formulation and evaluation of dextromethorphan hydrobromide sustained release tablets.  

PubMed

Sustained release (SR) matrix tablets of dextromethorphan hydrobromide were prepared by wet granulation using hydroxypropyl methyl cellulose (HPMC-K-100 CR) as the hydrophilic rate controlling polymer. The effect of the concentration of the polymer and different fillers on the in vitro drug release rate was studied. The studies indicated that the drug release can be modulated by varying the concentration of the polymer and the fillers. A complete cross-over bioavailability study of the optimized formulation of the developed sustained tablets and marketed immediate release tablets was performed on six healthy male volunteers. The extent of absorption of drug from the SR tablets was significantly higher than that for the marketed dextromethorphan hydrobromide tablet because of lower elimination rate and longer half-life. PMID:18712620

Meyyanathan, Subramania Nainar; Rajan, Sekar; Muralidaharan, Selvadurai; Siddaiah, Mahesh Kumar; Krishnaraj, Kaliaperumal; Suresh, Bhojraj

2008-09-01

253

Design and in vitro evaluation of effervescent gastric floating drug delivery systems of propanolol HCl.  

PubMed

Abstract. The purpose of this research was to develop and evaluate effervescent gastric floating tablets of propranolol HCl. The oral delivery of antihypertensive propranolol HCl was facilitated by preparing an effervescent floating dosage form which could increase its absorption in the stomach by increasing the drug's gastric residence time. In the present work, effervescent floating tablets were prepared with a hydrophilic carrier such as polyethylene oxide (PEO WSR N 60K and PEO WSR 303) as a release retarding agent and sodium bicarbonate as a gas generating agent. The prepared tablets were evaluated for all their physicochemical properties, in vitro buoyancy, drug release and rate order kinetics. From the results, P9 was selected as an optimized formulation based on their 12 h drug release, minimal floating lag time and maximum total floating time. The optimized formulation followed first order rate kinetics with erosion mechanism. The optimized formulation was characterized with FTIR studies and no interaction between the drug and the polymers were observed. PMID:22524109

Meka, Venkata Srikanth; Songa, Ambedkar Sunil; Nali, Sreenivasa Rao; Battu, Janaki Ram; Kolapalli, Venkata Ramana Murthy

2012-03-01

254

The influence of hydroxypropyl methylcellulose (HPMC) molecular weight, concentration and effect of food on in vivo erosion behavior of HPMC matrix tablets.  

PubMed

Four different hydrophilic matrix formulations based on hydroxypropyl methylcellulose (HPMC) were investigated for erosion properties in vivo. Three formulations contained a fixed amount of HPMC (40%) with varying proportions of two HPMC grades with different molecular weights (Methocel K100LV and K4M), and a fourth formulation contained a lower amount of the HPMC of lower molecular weight (20%). The effect of food on the in vivo erosion behavior was investigated on two formulations containing different contents of the same HPMC grade. The in vivo erosion behavior and gastrointestinal transit were investigated using magnetic marker monitoring (MMM). The in vitro and in vivo erosion-time profiles show that the erosion was strongly dependent on the composition of the formulation. The formulations containing a larger proportion of high molecular weight HPMC or higher content of HPMC exhibit relatively slower erosion rate and vice versa. In vivo erosion rates were significantly higher under postprandial administration as compared to fasted state administration. No rapid disintegration of any of the formulations (i.e. formulation failure that can potentially cause dose dumping) was observed. PMID:24818771

Jain, Arun Kumar; Söderlind, Erik; Viridén, Anna; Schug, Barbara; Abrahamsson, Bertil; Knopke, Christian; Tajarobi, Farhad; Blume, Henning; Anschütz, Maria; Welinder, Anette; Richardson, Sara; Nagel, Stefan; Abrahmsén-Alami, Susanna; Weitschies, Werner

2014-08-10

255

Molecular dynamic simulations of ocular tablet dissolution.  

PubMed

Small tablets for implantation into the subconjunctival space in the eye are being developed to inhibit scarring after glaucoma filtration surgery (GFS). There is a need to evaluate drug dissolution at the molecular level to determine how the chemical structure of the active may correlate with dissolution in the nonsink conditions of the conjunctival space. We conducted molecular dynamics simulations to study the dissolution process of tablets derived from two drugs that can inhibit fibrosis after GFS, 5-fluorouracil (5-FU) and the matrix metalloprotease inhibitor (MMPi), ilomastat. The dissolution was simulated in the presence of simple point charge (SPC) water molecules, and the liquid turnover of the aqueous humor in the subconjunctival space was simulated by removal of the dissolved drug molecules at regular intervals and replacement by new water molecules. At the end of the simulation, the total molecular solvent accessible surface area of 5-FU tablets increased by 60 times more than that of ilomastat as a result of tablet swelling and release of molecules into solution. The tablet dissolution pattern shown in our molecular dynamic simulations tends to correlate with experimental release profiles. This work indicates that a series of molecular dynamic simulations can be used to predict the influence of the molecular properties of a drug on its dissolution profile and could be useful during preformulation where sufficient amounts of the drug are not always available to perform dissolution studies. PMID:24073784

Ru, Qian; Fadda, Hala M; Li, Chung; Paul, Daniel; Khaw, Peng T; Brocchini, Steve; Zloh, Mire

2013-11-25

256

In vivo drug release from hydrophilic dextran tablets capable of forming polyion complex.  

PubMed

The aim of this comparative study was to investigate the in vivo drug release property of hydrophilic dextran tablets with or without swelling in the upper gastrointestinal tract (GIT) in humans. Two kinds of theophylline (TH) tablets were prepared by direct compression from a mixture of carboxymethyldextran and [2-(diethylamino)ethyl]dextran as a matrix capable of forming polyion complex (PIC-tablet), and a mixture of low and medium molecular weight hydroxypropylcellulose as a representative hydrophilic matrix (HPC-tablet). In these tablets, in vitro drug release behaviors and saliva TH level profiles after oral administration to humans were similar to each other, indicating equivalent AUC value. The tablets were then coated with Eudragit S100, enteric-coating polymer, by a dipping method in order to reveal drug release without full swelling in the upper GIT. Although the two enteric-coated tablets showed a similar in vitro release pattern, saliva level profiles were quite different as reflected in AUC values of 16.4 and 4.68 microg h/ml for enteric-coated PIC- and enteric-coated HPC-tablet, respectively. These results demonstrated that HPC-tablet could not release sufficiently without swelling in the upper GIT. In contrast, enteric-coated PIC-tablet showed an equivalent AUC value to PIC-tablet, indicating that TH was released well even in the lower GIT. PMID:16824636

Miyazaki, Yasunori; Tanaka, Yoichi; Yakou, Shigeru; Takayama, Kozo

2006-08-10

257

Development of press-coated, floating-pulsatile drug delivery of lisinopril.  

PubMed

Lisinopril is an angiotensin-converting enzyme (ACE) inhibitor, primarily used for the treatment of hypertension, congestive heart failure, and heart attack. It belongs to BCS class III having a half-life of 12 hrs and 25% bioavailability. The purpose of the present work was to develop a press-coated, floating-pulsatile drug delivery system. The core tablet was formulated using the super-disintegrants crosprovidone and croscarmellose sodium. A press-coated tablet (barrier layer) contained the polymer carrageenan, xanthan gum, HPMC K4M, and HPMC K15M. The buoyant layer was optimized with HPMC K100M, sodium bicarbonate, and citric acid. The tablets were evaluated for physical characteristics, floating lag time, swelling index, FTIR, DSC, and in vitro and in vivo behavior. The 5% superdisintgrant showed good results. The FTIR and DSC study predicted no chemical interactions between the drug and excipients. The formulation containing xanthan gum showed drug retaining abilities, but failed to float. The tablet containing HPMC K15M showed a high swelling index. The lag time for the tablet coated with 200 mg carrageenan was 3±0.1 hrs with 99.99±1.5% drug release; with 140 mg HPMC K4M, the lag time was 3±0.1 hrs with 99.71±1.2% drug release; and with 120 mg HPMC K15M, the lag time was 3±0.2 hrs with 99.98±1.7% drug release. The release mechanism of the tablet followed the Korsmeyer-Peppas equation and a first-order release pattern. Floating and lag time behavior have shown good in vitro and in vivo correlations. PMID:24959410

Jagdale, Swati C; Suryawanshi, Vishnu M; Pandya, Sudhir V; Kuchekar, Bhanudas S; Chabukswar, Aniruddha R

2014-06-01

258

Development of Press-Coated, Floating-Pulsatile Drug Delivery of Lisinopril  

PubMed Central

Lisinopril is an angiotensin-converting enzyme (ACE) inhibitor, primarily used for the treatment of hypertension, congestive heart failure, and heart attack. It belongs to BCS class III having a half-life of 12 hrs and 25% bioavailability. The purpose of the present work was to develop a press-coated, floating-pulsatile drug delivery system. The core tablet was formulated using the super-disintegrants crosprovidone and croscarmellose sodium. A press-coated tablet (barrier layer) contained the polymer carrageenan, xanthan gum, HPMC K4M, and HPMC K15M. The buoyant layer was optimized with HPMC K100M, sodium bicarbonate, and citric acid. The tablets were evaluated for physical characteristics, floating lag time, swelling index, FTIR, DSC, and in vitro and in vivo behavior. The 5% superdisintgrant showed good results. The FTIR and DSC study predicted no chemical interactions between the drug and excipients. The formulation containing xanthan gum showed drug retaining abilities, but failed to float. The tablet containing HPMC K15M showed a high swelling index. The lag time for the tablet coated with 200 mg carrageenan was 3±0.1 hrs with 99.99±1.5% drug release; with 140 mg HPMC K4M, the lag time was 3±0.1 hrs with 99.71±1.2% drug release; and with 120 mg HPMC K15M, the lag time was 3±0.2 hrs with 99.98±1.7% drug release. The release mechanism of the tablet followed the Korsmeyer-Peppas equation and a first-order release pattern. Floating and lag time behavior have shown good in vitro and in vivo correlations. PMID:24959410

Jagdale, Swati C.; Suryawanshi, Vishnu M.; Pandya, Sudhir V.; Kuchekar, Bhanudas S.; Chabukswar, Aniruddha R.

2014-01-01

259

Tablet Splitting: A Risky Practice  

MedlinePLUS

... practice of splitting tablets, the Food and Drug Administration (FDA), the American Medical Association, and other medical organizations advise against it unless it's specified in the drug's labeling. Tablet splitting often involves buying higher strength tablets and then breaking the tablets in ...

260

Floating microspheres as drug delivery system: newer approaches.  

PubMed

A controlled drug delivery system with prolonged residence time in the stomach can be of great practical importance for drugs with an absorption window in the upper small intestine. The main limitations are attributed to the inter- and intra-subject variability of gastro-intestinal (GI) transit time and the non-uniformity of drug absorption throughout the alimentary canal. Floating drug delivery systems (FDDSs) are expected to remain buoyant in a lasting way upon the gastric contents and consequently to enhance the bioavailability of drugs. The various buoyant preparations include hollow microspheres, granules, powders, tablets, capsules, pills and laminated films. Floating microspheres are specially gaining attention due to their wide applicability in the targeting of drugs to stomach. These floating microspheres have the advantage that they remain buoyant and distributed uniformly over the gastric fluid to avoid the vagaries of gastric emptying and release the drug for prolonged period of time. A major drawback of low-density floating drug delivery systems is that their performance is strongly dependent upon the gastric emptying process of stomach. Multiparticulate low-density particles can successfully prolong the gastric retention time of drugs. This article is a review of two important approaches utilized to prepare and improve the performance of floating microspheres. PMID:18673266

Jain, Sunil K; Agrawal, Govind P; Jain, Narendra K

2008-07-01

261

Design and study of lamivudine oral controlled release tablets.  

PubMed

The objective of this study was to design oral controlled release matrix tablets of lamivudine using hydroxypropyl methylcellulose (HPMC) as the retardant polymer and to study the effect of various formulation factors such as polymer proportion, polymer viscosity, and compression force on the in vitro release of drug. In vitro release studies were performed using US Pharmacopeia type 1 apparatus (basket method) in 900 mL of pH 6.8 phosphate buffer at 100 rpm. The release kinetics were analyzed using the zero-order model equation, Higuchi's square-root equation, and the Ritger-Peppas empirical equation. Compatibility of the drug with various excipients was studied. In vitro release studies revealed that the release rate decreased with increase in polymer proportion and viscosity grade. Increase in compression force was found to decrease the rate of drug release. Matrix tablets containing 60% HPMC 4000 cps were found to show good initial release (26% in first hour) and extended the release up to 16 hours. Matrix tablets containing 80% HPMC 4000 cps and 60% HPMC 15,000 cps showed a first-hour release of 22% but extended the release up to 20 hours. Mathematical analysis of the release kinetics indicated that the nature of drug release from the matrix tablets was dependent on drug diffusion and polymer relaxation and therefore followed non-Fickian or anomalous release. No incompatibility was observed between the drug and excipients used in the formulation of matrix tablets. The developed controlled release matrix tablets of lamivudine, with good initial release (20%-25% in first hour) and extension of release up to 16 to 20 hours, can overcome the disadvantages of conventional tablets of lamivudine. PMID:18181522

Ravi, Punna Rao; Ganga, Sindhura; Saha, Ranendra Narayan

2007-01-01

262

Direct molding of tablets with prolonged drug release  

Microsoft Academic Search

Auxiliary components have been selected and optimum production technology has been developed for matrix tablets of diclofenac\\u000a sodium. Physicochemical properties of the parent drug, polymer matrix (delay release factor), and auxiliary components of\\u000a a mixture used in the direct molding technology have been studied.

S. V. Emshanova; O. Yu. Lashcheva; N. P. Sadchikova; A. P. Zuev

2006-01-01

263

Imperatorin sustained-release tablets: In Vitro and pharmacokinetic studies  

Microsoft Academic Search

We prepared and evaluated imperatorin (IMP) sustained-release tablets. IMP is an active compound in Angelica dahuricae, a\\u000a Chinese herbal medicine. We used different polymers, such as hydroxypropyl methylcellulose (HPMC K4M, K15M, and K100M), carbopol\\u000a 934P, sodium carboxymethyl cellulose (CMC-Na), and their combinations to prepare the matrix tablets and achieve the desired\\u000a sustained release profile. The in vitro release profiles of

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

2010-01-01

264

What Floats Your Boat?  

NSDL National Science Digital Library

Students use modeling clay, a material that is denser than water and thus ordinarily sinks in water, to discover the principle of buoyancy. They begin by designing and building boats out of clay that will float in water, and then refine their designs so that their boats will carry as great a load (metal washers) as possible. Building a clay boat to hold as much weight as possible is an engineering design problem. Next, they compare amount of water displaced by a lump of clay that sinks to the amount of water displaced by the same lump of clay when it is shaped so as to float. Determining the masses of the displaced water allows them to arrive at Archimedes' principle, whereby the mass of the displaced water equals the mass of the floating clay boat.

Engineering K-Phd Program

265

Ketorolac tromethamine floating beads for oral application: Characterization and in vitro/in vivo evaluation.  

PubMed

The floating beads have been employed to make a sustained release of the drug in the stomach and to decrease the dose of the drug and hence overcome its side effects. The common benefits of the floating beads were it is easy preparation, without the need of a high temperature, and high percentage of the drug entrapment. In the present work, the Ketorolac tromethamine (KT) floating beads were prepared by extrusion congealing method utilizing calcium carbonate as a gas forming agent. The physical characters of the produced beads were investigated such as KT yield, KT loading, and entrapment efficiency of the drug. In addition, floating behavior, swelling, particle size, morphology and KT stability were also evaluated. In vitro drug release study was carried out, and the kinetics of the release was evaluated using the linear regression method. Furthermore, the in vivo analgesic effect of KT after oral administration of the selected formula of floating beads (F10) was carried out using hot plate and tail flick methods. Oral commercial KT tablets and KT solution were used for the comparison. The prepared beads remained floated for more than 8 h. The optimized formulation (F10) exhibited prolonged drug release (more than 8 h) and the drug release follows the Higuchi kinetic model, with a Fickian diffusion mechanism according to Korsmeyer-Peppas (n = 0.466). Moreover, F10 showed a sustained analgesic effect as compared to the commercial tablet. PMID:25161380

Abou El Ela, Amal El Sayeh F; Hassan, Maha A; El-Maraghy, Dalia A

2014-09-01

266

Ketorolac tromethamine floating beads for oral application: Characterization and in vitro/in vivo evaluation  

PubMed Central

The floating beads have been employed to make a sustained release of the drug in the stomach and to decrease the dose of the drug and hence overcome its side effects. The common benefits of the floating beads were it is easy preparation, without the need of a high temperature, and high percentage of the drug entrapment. In the present work, the Ketorolac tromethamine (KT) floating beads were prepared by extrusion congealing method utilizing calcium carbonate as a gas forming agent. The physical characters of the produced beads were investigated such as KT yield, KT loading, and entrapment efficiency of the drug. In addition, floating behavior, swelling, particle size, morphology and KT stability were also evaluated. In vitro drug release study was carried out, and the kinetics of the release was evaluated using the linear regression method. Furthermore, the in vivo analgesic effect of KT after oral administration of the selected formula of floating beads (F10) was carried out using hot plate and tail flick methods. Oral commercial KT tablets and KT solution were used for the comparison. The prepared beads remained floated for more than 8 h. The optimized formulation (F10) exhibited prolonged drug release (more than 8 h) and the drug release follows the Higuchi kinetic model, with a Fickian diffusion mechanism according to Korsmeyer-Peppas (n = 0.466). Moreover, F10 showed a sustained analgesic effect as compared to the commercial tablet. PMID:25161380

Abou el Ela, Amal El Sayeh F.; Hassan, Maha A.; El- Maraghy, Dalia A.

2013-01-01

267

Preparation of rosiglitazone maleate sustained-release floating microspheres for improved bioavailability.  

PubMed

The object of this study was to prepare rosiglitazone maleate (RM) sustained-release floating microspheres and investigate their pharmacokinetics. RM microspheres were prepared with ethyl cellulose (EC) and octadecyl alcohol as the carrier materials by an emulsion-solvent diffusion method, and the properties of morphology in vitro floating capability, drug loading (DL), entrapment efficiency (EE), in vitro release and in vivo pharmacokinetics were investigated. The prepared microspheres had a completely spherical shape. The percentage of microspheres floating after 12 h was (91.45 +/- 1.62)%, and the DL and EE were (9.31 +/- 0.31)% and (89.55 +/- 1.65)% respectively. Pharmacokinetic studies demonstrated that the RM floating microspheres were superior to commercial tablets in terms of the decrease in peak plasma concentration and maintenance of RM concentration in plasma. The area under the curve of plasma concentration-time (AUC) of the floating microspheres was equivalent to that of reference tablets. The results showed that floating microspheres are a feasible approach for the sustained-release preparation of drugs which have limited absorption sites in the upper small intestine. PMID:20662314

Hu, Lian-Dong; Xing, Qian-Bin; Shang, Chuang; Liu, Wei; Liu, Ci; Luo, Zhao-Liang; Xu, Hong-Xin

2010-07-01

268

Novel chitosan-magnesium aluminum silicate nanocomposite film coatings for modified-release tablets.  

PubMed

Chitosan (CS), a positively charged polysaccharide, and magnesium aluminum silicate (MAS), a negatively charged clay with silicate layers, can electrostatically interact to form nanocomposite films. In this study, CS-MAS nanocomposite films were evaluated for use in tablet film coating. Effects of CS-MAS ratio and coating level on water uptake and drug release from the coated tablets were investigated. Surface and film matrix morphology of the coated film and the effect of enzymes in the simulated gastro-intestinal fluid on drug release were also examined. The results demonstrated that the CS-MAS coated tablets had a rough surface and a layered matrix film, whereas a smooth surface and dense matrix film on the CS coated tablets was found. However, the CS-MAS coated tablets provided fewer film defects than the CS coated tablets. Nanocomposite formation between CS and MAS could retard swelling and erosion of CS in the composite films in acidic medium. The higher MAS ratio of the CS-MAS coated tablets gave lower water uptake and slower drug release when compared with the CS coated tablets. Moreover, the CS-MAS films on the tablets presented good stability towards enzymatic degradation in simulated intestinal fluid. The release of drug from the CS-MAS coated tablets could be modulated by varying CS-MAS ratios and coating levels. Additionally, drug solubility also influenced drug release characteristics of the CS-MAS coated tablets. These findings suggest that the CS-MAS nanocomposites displays a strong potential for use in tablet film coating intended for modifying drug release from tablets. PMID:21291977

Khunawattanakul, Wanwisa; Puttipipatkhachorn, Satit; Rades, Thomas; Pongjanyakul, Thaned

2011-04-01

269

Can flexibility help you float?  

E-print Network

We consider the role of flexibility in the weight-bearing characteristics of bodies floating at an interface. Specifically, we develop a theoretical model for a two-dimensional thin floating plate that yields the maximum ...

Burton, Lisa Janelle

270

Corona from floating electrodes  

Microsoft Academic Search

It is not unusual to have insulated conducting objects located close to the conductors of a Lightning Protection System. However, the separation of these objects from the Lightning Protection System could vary from a few millimetres to some centimetres. When the system is exposed to thunderstorm electric fields, discharge could be initiated between the Lightning Protection System and the floating

Francisco Roman; Vernon Cooray; Viktor Scuka

1996-01-01

271

Float My Boat  

NSDL National Science Digital Library

In this activity, learners use tinfoil to build and test their own boats - which designs will float, and which will sink? Learners must adjust many variables in their boat design to maximize stability and flotation, in order for the boat to support a heavy load of pennies. This activity is great used with lessons on engineering or design.

Wgbh

2006-01-01

272

Compound floating pivot micromechanisms  

DOEpatents

A new class of tilting micromechanical mechanisms have been developed. These new mechanisms use compound floating pivot structures to attain far greater tilt angles than are practical using other micromechanical techniques. The new mechanisms are also capable of bi-directional tilt about multiple axes.

Garcia, Ernest J. (Albuquerque, NM)

2001-04-24

273

Floating Paper Clip  

NSDL National Science Digital Library

In this activity, challenge learners to float a paper clip in a cup of water. Learners discover that a paper clip will sink in a cup of water, except when it is placed on a piece of paper towel. Use this activity to demonstrate the principles of surface tension, adhesion/cohesion, and gravity.

Boston, Wgbh

2002-01-01

274

Floating platform with monolithically formed float members and platform  

SciTech Connect

Floating platforms for various offshore facilities are formed of float members monolithically connected to a superposed platform. The float members are spherically shaped and are formed of reinforced or prestressed concrete. The platform can be a hollow planar member or it can be curved in one or two directions, and the platforms are formed of prestressed concrete. Cylindrical shafts can be used to connect the spherically shaped floats and the platform. Individual floating platforms can be connected by expansion joints and used as a runway. The float members can be constructed at the shoreline, launched into the water and held in a regular pattern while decked over with the platform. After completion of the construction procedure, the floating platform can be moved to an offshore location for use.

Finsterwalder, U.

1981-06-30

275

Effect of tablet integrity on the dissolution rate of sustained-release preparations.  

PubMed

The objective of this study was to evaluate the effect of tablet integrity on the dissolution rate. The model drug used for this study was aspirin. A dissolution study was performed with three commercially-available aspirin tablets (ZORprin, Bayer 8-h aspirin and Bayer aspirin), two of which were sustained-release tablets. For ZORprin, the average dissolution data indicated that the in vitro release rate of aspirin was consistent with the intended design of the sustained-release wax matrix tablets only when the tablets were intact. The split tablets showed a consistently higher release profile over time, with a 50% higher release at 6 h. However, the Bayer 8-h aspirin and plain aspirin tablet data showed that tablet integrity had no significant impact on the dissolution rate, because the intact and split tablets showed similar drug release profiles over time. In conclusion, care should be taken to administer sustained-release tablets, avoiding any breaking or crushing of the tablets unless this is directed by the manufacturer. PMID:8873848

Mandal, T K

1996-06-01

276

Microstructural investigation of tablet compaction and tablet pharmacological properties  

E-print Network

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

Mao, Kangyi

2010-01-01

277

Desktop 3D printing of controlled release pharmaceutical bilayer tablets.  

PubMed

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

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

2014-01-30

278

Compressibility of floating pellets with verapamil hydrochloride coated with dispersion Kollicoat SR 30 D.  

PubMed

The purpose of this study was to work out a method of compression of floating pellets with verapamil hydrochloride (VH) in a dose of 40 mg. It was assumed that this form should reside in the stomach floating for several hours and gradually release the drug in a controlled way. Compression of pellets into tablets, being a modern technological process, is much more perfect than enclosing them in a hard gelatin capsule. Kollicoat SR 30 D was selected for coating. In experiments three plasticizers were examined-propylene glycol, triethyl citrate and dibuthyl sebecate (all at concentration of 10%). It was found that VH release from pellets coated by the films of the same thickness (70 microm), however, containing plasticizers is considerably different. Pellets were prepared by wet granulation of powder mixture, spheronization of the granulated mass and coating of the cores with a sustained release film. Two kinds of cellulose, microcrystalline and powdered, and sodium hydrocarbonate were the main components of pellet core. Proper pellet coating film thickness, ensuring obtaining desirable VH release profile and flotation effect, was defined. X compositions of tablets with pellets were examined in order to obtain formulation, from which VH release would mostly approximate pellets before compressing. The best formulation was evaluated taking into account the effect of compression force an tablet hardness and friability, and pellet agglomeration and flotation. Tablet cross-section photographs were taken confirming necessary coating film thickness preventing their deformation caused by compressing into tablets. PMID:15848067

Sawicki, Wies?aw; Lunio, Rafa?

2005-05-01

279

Gum odina: a novel matrix forming material for sustained drug delivery  

Microsoft Academic Search

The study concerns the evaluation of natural gum odina as novel sustained release matrix forming material in tablet formulation.\\u000a Matrix tablets were prepared by wet granulation technique. Diclofenac sodium was used as model drug. The tablet weight (250 mg)\\u000a and diameter (9 mm) was kept constant. The tablets were evaluated for physicochemical properties, drug content uniformity\\u000a and in vitro drug release kinetics.

Subas Chandra Dinda; Biswajit Mukherjee; Amalesh Samanta

280

Physical characterizations and sustained release profiling of gastroretentive drug delivery systems with improved floating and swelling capabilities.  

PubMed

The aim was to develop gastroretentive drug delivery systems (GRDDSs) by combining floating and swelling. GRDDS tablets formulated with hydroxyethylcellulose (HEC), chitosan (CS) and sodium bicarbonate (SB) for evaluating floating capacity (floating lag time and duration) and swelling characteristics. CS was used because it was swellable in acidic media and biocompatible. Losartan was incorporated into the optimized formulations for sustained release profiling. Results demonstrated that for those formulations at HEC:CS ratio of 5:5 containing CS, both the floating lag time and floating duration were optimal and reached the preferred swelling effect and sustain for 24h. Adding SB improved the floating capabilities for all ratios of HEC:CS, but reduced the swelling ability for those formulations containing a higher portion of low viscosity grade CS. Sustained release profiles for losartan in those formulations were achievable, using all viscosity grades of CS at all examined HEC:CS ratios; however, it is more adjustable at different HEC:CS ratios when using a lower viscosity grade of CS. Optimized GRDDS formulations for losartan composed of an equivalent ratio of HEC to CS with 20mg SB resulted in the tablets floating for more than 16 h and an adjustable sustained release profile. PMID:23237874

Chen, Ying-Chen; Ho, Hsiu-O; Lee, Tzu-Yu; Sheu, Ming-Thau

2013-01-30

281

Serial floating point formatter  

SciTech Connect

A floating point formatter for changing fixed point serial digital data, such as that received by a seismic data acquisition system, is disclosed wherein fixed point serial digital data is received and scaled to remove any bias added by preamplification. The scaled data is shifted a predetermined number of bits and a resulting exponent is calculated. The shifted data signal and corresponding exponent are combined and further scaled to permit stacking the data without exceeding the system capacity.

Peterson, R. D.; Penner, W. A.

1985-11-12

282

Fabrication and Evaluation of Bi-layer Tablet Containing Conventional Paracetamol and Modified Release Diclofenac Sodium.  

PubMed

The objectives of present investigation were to achieve immediate release of paracetamol and tailored release of diclofenac sodium from bi-layer tablets. A 2(3) full factorial design was adopted using the amount of polyethylene glycol, microcrystalline cellulose and crospovidone as independent variables for fabricating paracetamol tablets. Diclofenac sodium tablets were prepared using hydroxypropyl methylcellulose as a matrixing agent. The results of analysis of variance showed that the friability of paracetamol was distinctly influenced by the formulation variables. The in vitro drug release behaviour of diclofenac tablets was compared with a marketed formulation. The optimized formulations of paracetamol and diclofenac sodium were used for manufacturing of bi-layer tablets. The bi-layer tablets showed immediate release of paracetamol and modified release of diclofenac. PMID:20838522

Gohel, M C; Parikh, R K; Nagori, S A; Jethwa, B A

2010-03-01

283

[Tablets and tablet production - with special reference to Icelandic conditions].  

PubMed

Modern tablet compression was instituted in England in 1844 by William Brockedon (1787-1854). The first tablets made according to Brockedon´s procedures contained watersoluble salts and were most likely compressed without expedients. In USA a watershed occurred around 1887 when starch (amylum maydis) was introduced to disperse tablets in aqueous milieu in order to corroborate bioavailability of drugs in the almentary canal. About the same time great advances in tablet production were introduced by the British firm Burroughs Wellcome and Co. In Denmark on the other hand tablet production remained on low scale until after 1920. As Icelandic pharmacies and drug firms modelled themselves mostly upon Danish firms tablet production was first instituted in Iceland around 1930. The first tablet machines in Iceland were hand-driven. More efficent machines came after 1945. Around 1960 three sizeable tablet producers were in Iceland; now there is only one. Numbers of individual tablet species (generic and proprietary) on the market rose from less than 10 in 1913 to 500 in 1965, with wide variations in numbers in between. Tablets have not wiped out other medicinal forms for peroral use but most new peroral drugs have been marketed in the form of tablets during the last decades. PMID:23695970

Skaftason, Jóhannes F; Jóhannesson, Thorkell

2013-04-01

284

Advanced formulation design of venlafaxine hydrochloride coated and triple-layer tablets containing hypromellose.  

PubMed

The purpose of this research work was to develop venlafaxine hydrochloride-coated and layered matrix tablets using hypromellose adopting wet granulation technique. The granules and the tablets were characterized. The monolithic tablets were coated with different ratios of ethyl cellulose and hypromellose. The in vitro dissolution study was performed in distilled water. In the layered tablets, the middle layer containing drug was covered with barrier layers containing high viscosity grade hypromellose. Simplex lattice design was used for formulating the layered tablets. The dissolution study of the optimized batches and a reference product was carried out in 0.1 N HCl, phosphate buffer and hydroalcoholic solution. Burst drug release was exhibited by the uncoated tablets, probably due to high aqueous solubility of venlafaxine HCl. The coated tablets showed sustained drug release without burst effect. The drug release was best explained by Weibull model. A unified Weibull equation was evolved to express drug release from the coated tablets. The layered tablets also exhibited sustained release without burst effect due to effective area reduction. The optimized batches showed identical drug release in 0.1 N HCl, phosphate buffer and 10% v/v aqueous alcohol. Layered tablets may well be adopted by the industry due to the possibility of achieving a high production rate. PMID:19883254

Gohel, Mukesh; Bariya, Shital H

2009-01-01

285

Absence of effect of food on alprazolam absorption from sustained release tablets.  

PubMed

This study examined the effect of food on alprazolam absorption from a mixed polymeric matrix sustained release (SR) tablet in 21 healthy adults. Each subject received each of three treatments according to a crossover design: 1 mg alprazolam SR tablet while fasting; 1 mg alprazolam SR tablet immediately after a standardized breakfast; 1 mg alprazolam conventional tablet while fasting. The breakfast contained approximately 33 g protein, 55 g fat, and 58 g carbohydrate (850 calories). Serial blood samples were obtained and plasma alprazolam levels determined by HPLC. Results indicate that the SR tablet was minimally affected by food. Relative bioavailabilities of the SR tablet while fasting and with food were 100 per cent and 97 per cent, respectively. Although statistically significant, differences in mean Cmax values between SR tablets administered with and without food were small (12 per cent increase with food). Rates of absorption as measured by mean tmax values were also nearly the same: 7.2 h while fasting and 7.0 h with food. Absorption was relatively uniform with the SR tablets. Coefficients of variation for Cmax, tmax, and AUC were somewhat smaller with the SR tablet than with the conventional tablet. PMID:2322635

Eller, M G; Della-Coletta, A A

1990-01-01

286

Tablet Process Simulator  

NSDL National Science Digital Library

The North Carolina Community College System BioNetwork's interactive eLearning tools (IETs) are reusable chunks of training that can be deployed in a variety of courses or training programs. IETs are designed to enhance, not replace hands-on training. Learners are able to enter a hands-on lab experience better prepared and more confident. This particular IET is a Tablet Process Simulator in which visitors set up and run a tablet press in a virtual 3D environment. The tool requires the program to be downloaded and installed, and gives helpful installation instructions. Users will start by downloading a zip file to their computer.

2013-07-23

287

40 CFR 65.45 - External floating roof converted into an internal floating roof.  

Code of Federal Regulations, 2010 CFR

... 2010-07-01 false External floating roof converted into an internal floating roof. 65.45...Storage Vessels § 65.45 External floating roof converted into...material emissions by using an external floating roof converted...

2010-07-01

288

Understanding and Predicting Drug Delivery from Hydrophilic Matrix  

E-print Network

and diclofenac sodium was studied in phosphate buffer (pH 7.4) and 0.1 M HCl, respectively. The initial drugUnderstanding and Predicting Drug Delivery from Hydrophilic Matrix Tablets Using the "Sequential phenomena which are involved in the swelling and drug release from hydrophilic matrix tablets using

Peppas, Nicholas A.

289

Will It Float?  

NSDL National Science Digital Library

Student preconceptions are one of the greatest challenges we face as science teachers. This Predict, Explain, Observe, and Explain (PEOE) activity challenges students? preconceived notions about why matter floats or sinks when placed in a liquid. The idea behind this model is to do a demonstration that first confirms student's conceptions followed by a second, similar demonstration that provides discrepant information creating cognitive dissonance. Learning happens as students are forced to modify their conceptions so that their view of how things work is not in conflict with what they are seeing.

Major, Jeff

2006-01-01

290

CES 2011: Tablet Crazy  

ERIC Educational Resources Information Center

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

Rapp, David

2011-01-01

291

Floating offshore structure  

SciTech Connect

A floating offshore structure which is moored at a fixed position on the sea by means of mooring hawsers and anchors connected to the ends thereof respectively for conducting a submarine excavating operation from a deck of the structure. The structure includes a moorage hull part provided with a vertical through-hole formed therein for receiving an excavating drill pipe and the mooring hawsers and a movable hull part connected to the moorage hull part so as to be rotatable within a horizontal plane. The movable hull part is constituted as a hull defining the outer wall of the floating offshore structure and connected with the moorage hull part by inserting it into a moorage hull part receiving hole formed at a position closer to the bow thereof. The movable hull part has near its water plane a horizontal section with a substantially oval shape formed by a fore draft part in a substantially circular or polygonal shape, with the moorage hull part receiving hole as a center and an after draft part taperingly projecting aft from the fore draft part.

Oshima, M.; Narita, H.; Tabuchi, H.; Yashima, N.

1985-05-28

292

What Makes a Boat Float?  

NSDL National Science Digital Library

Whether or not a boat floats is determined by its shape and density. In this activity, students discover how and why boats float by designing different hull shapes and finding which design holds the most weight. Students record, calculate, and interpret data as they learn about buoyancy in this hands-on activity.

Eichinger, John

2009-05-01

293

Formulation Variables Influencing Drug Release from Layered Matrix System Comprising Chitosan and Xanthan Gum  

Microsoft Academic Search

The purpose of this study was to investigate the formulation variables influencing the drug release from the layered tablets\\u000a containing chitosan and xanthan gum as matrix component. Increasing the amount of lactose could diminish pH sensitive release\\u000a behavior of these matrix tablets. Effect of formulation variables on drug release from the prepared three-layered matrix tablets\\u000a was investigated. The amount of

Thawatchai Phaechamud; Garnpimol C. Ritthidej

2008-01-01

294

Formulation and Evaluation of Floating Oral In Situ Gelling System of Amoxicillin  

PubMed Central

Purpose. Effective Helicobacter pylori eradication requires delivery of the antibiotic locally in the stomach. High dose of amoxicillin (750 to 1000?mg) is difficult to incorporate in floating tablets but can easily be given in liquid dosage form. Keeping the above facts in mind, we made an attempt to develop a new floating in situ gelling system of amoxicillin with increased residence time using sodium alginate as gelling polymer to eradicate H. pylori. Methods. Floating in situ gelling formulations were prepared using sodium alginate, calcium chloride, sodium citrate, hydroxypropyl methyl cellulose K100, and sodium bicarbonate. The prepared formulations were evaluated for solution viscosity, floating lag time, total floating time, and in vitro drug release. The formulation was optimized using a 32 full factorial design. Dissolution data were fitted to various models to ascertain kinetic of drug release. Regression analysis and analysis of variance were performed for dependent variables. Results. All formulations (F1–F9) showed floating within 30?s and had total floating time of more than 24?h. All the formulations showed good pourability. It was observed that concentration of sodium alginate and HPMC K100 had significant influence on floating lag time, cumulative percentage drug release in 6?h and 10?h. The batch F8 was considered optimum since it showed more similarity in drug release (f2 = 74.38) to the theoretical release profile. Conclusion. Floating in situ gelling system of amoxicillin can be formulated using sodium alginate as a gelling polymer to sustain the drug release for 10 to 12?h with zero-order release kinetics. PMID:22389849

Patel, Dasharath M.; Patel, Divyesh K.; Patel, Chhagan N.

2011-01-01

295

Quantification, mechanism, and mitigation of active ingredient phase transformation in tablets.  

PubMed

Model tablet formulations containing thiamine hydrochloride [as a nonstoichiometric hydrate (NSH)] and dicalcium phosphate dihydrate (DCPD) were prepared. In intact tablets, the water released by dehydration of DCPD mediated the transition of NSH to thiamine hydrochloride hemihydrate (HH). The use of an X-ray microdiffractometer with an area detector enabled us to rapidly and simultaneously monitor both the phase transformations. The spatial information, gained by monitoring the tablet from the surface to the core (depth profiling), revealed that both DCPD dehydration and HH formation progressed from the surface to the tablet core as a function of storage time. Film coating of the tablets with ethyl cellulose caused a decrease in both the reaction rates. There was a pronounced lag time, but once initiated, the transformations occurred simultaneously throughout the tablet. Thus the difference in the phase transformation behavior between the uncoated and the coated tablets could not have been discerned without the depth profiling. Incorporation of hydrophilic colloidal silica as a formulation component further slowed down the transformations. By acting as a water scavenger it maintained a very "dry" environment in the tablet matrix. Finally, by coating the NSH particles with hydrophobic colloidal silica, the formation of HH was further substantially decelerated. The microdiffractometric technique not only enabled direct analyses of tablets but also provided the critical spatial information. This helped in the selection of excipients with appropriate functionality to prevent the in situ phase transformations. PMID:23869937

Thakral, Naveen K; Ragoonanan, Vishard; Suryanarayanan, Raj

2013-08-01

296

Application of Design of Experiment for Floating Drug Delivery of Tapentadol Hydrochloride  

PubMed Central

The aim of the present study was to apply design of experiment (DOE) to optimize floating drug delivery of tapentadol hydrochloride. Tapentadol hydrochloride is a synthetic opioid used as a centrally acting analgesic and effective in both experimental and clinical pain. The half-life of the drug is about 4 hours and oral dose is 50 to 250?mg twice a day. For optimization 32 full factorial design was employed for formulation of tapentadol hydrochloride tablets. Sodium bicarbonate was incorporated as a gas-generating agent. Combination of polymers Xanthan gum and Locust bean gum was used to achieve controlled release effect. The concentration of polymers was considered as the independent variables and dependent variables were floating lag time and swelling index of the tablets. From the factorial batches, it was observed that formulation containing combination of 20% sodium bicarbonate and 10% citric acid shows optimum floating ability whereas the formulation containing 20% Xanthan gum and 28% Locust bean gum shows optimum sustained drug release pattern with adequate floating. PMID:23878616

Jagdale, Swati C.; Patil, Somnath; Kuchekar, Bhanudas S.

2013-01-01

297

Application of design of experiment for floating drug delivery of tapentadol hydrochloride.  

PubMed

The aim of the present study was to apply design of experiment (DOE) to optimize floating drug delivery of tapentadol hydrochloride. Tapentadol hydrochloride is a synthetic opioid used as a centrally acting analgesic and effective in both experimental and clinical pain. The half-life of the drug is about 4 hours and oral dose is 50 to 250?mg twice a day. For optimization 3(2) full factorial design was employed for formulation of tapentadol hydrochloride tablets. Sodium bicarbonate was incorporated as a gas-generating agent. Combination of polymers Xanthan gum and Locust bean gum was used to achieve controlled release effect. The concentration of polymers was considered as the independent variables and dependent variables were floating lag time and swelling index of the tablets. From the factorial batches, it was observed that formulation containing combination of 20% sodium bicarbonate and 10% citric acid shows optimum floating ability whereas the formulation containing 20% Xanthan gum and 28% Locust bean gum shows optimum sustained drug release pattern with adequate floating. PMID:23878616

Jagdale, Swati C; Patil, Somnath; Kuchekar, Bhanudas S

2013-01-01

298

[Sanhuang tablets research].  

PubMed

Sanhuang tablets is one of common traditional Chinese patent preparation, it has effects of clear fever, detoxifcation, dispel inflammation, purgation. It was contained in the ministerial standards of Ministry of Health in 1997, and was contained in Chinese pharmacopoeia version 1 of 2000 and 2005. Its improvement of dosage form, preparation technique, quality analysis, pharmacology and clinical usage were reviewed in this paper. PMID:17993010

Liu, Cui-zhe; Chen, Da-wei

2007-09-01

299

Floating Cities, Islands and States  

E-print Network

Many small countries are in need of additional territory. They build landfills and expensive artificial islands. The ocean covers 71 per cent of the Earth surface. Those countries (or persons of wealth) starting the early colonization of the ocean may obtain advantages through additional territory or creating their own independent state. An old idea is building a big ship. The best solution to this problem, however, is the provision of floating cities, islands, and states. The author idea is to use for floating cities, islands, and states a cheap floating platform created from a natural ice field taken from the Arctic or Antarctic oceans. These cheap platforms protected by air-film (bottom and sides) and a conventional insulating cover (top) and having a cooling system can exist for an unlimited time. They can be increased in number or size at any time, float in warm oceans, travel to different continents and countries, serve as artificial airports, harbors and other marine improvements, as well as floating cities and industrial bases for virtually any use. Author researches and computes parameters of these ice floating platforms, other methods of building such floating territory, compares them and shows that the offered method is the most cheap and efficient means of ocean colonization.

Alexander Bolonkin

2008-04-04

300

Organic molecular floating gate memories  

E-print Network

Flash memory devices dominate the non-volatile memory market, with device structures that utilize charge storage in polysilicon floating gates imbedded in insulating silicon oxide films'. As demands for high storage density, ...

Paydavosi, Sarah

2011-01-01

301

Control development for floating wind  

NASA Astrophysics Data System (ADS)

Control of a floating wind turbine has proven to be challenging, but essential for lowering the cost of floating wind energy. Topic of a recent joint R&D project by GustoMSC, MARIN and ECN, is the concept design and verification with coupled simulations and model tests of the GustoMSC Tri-Floater. Only using an integral design approach, including mooring and control design, a cost effective system can be obtained. In this project, ECN developed a general floating wind turbine control strategy and applied this in a case study to the GustoMSC Tri-Floater and the OC3Hywind spar, both equipped with the NREL 5MW RWT. The designed controller ensures stable operation, while maintaining proper speed and power regulation. The motions of the floating support are reduced and substantial load reduction has been achieved.

Savenije, Feike; Peeringa, Johan

2014-06-01

302

Chitosan and sodium sulfate as excipients in the preparation of prolonged release theophylline tablets.  

PubMed

The major objectives of this study were to monitor the effect of cross-linking of cationic chitosan in acidic media with sulfate anion during granules preparation by wet granulation method prior to tableting using theophylline (TPH) as a model drug. The prepared granules and the compressed tablets were subjected to in vitro evaluation. The properties of the prepared matrix granules and the compressed tablets were dependent on chitosan:sodium sulfate weight ratios, chitosan content, and molecular weight of chitosan. The prepared granules of all batches showed excellent to passable flowability and were suitable for compression into tablets. Most of the granules were hard and expected to withstand handling during the subsequent compression into tablets. Granules with high friabilities were only those prepared with a high amount of sodium sulfate or low amount of chitosan. Compression of granule batches yield nondisintegrating tablets that showed a decrease in tensile strength with the increase of sodium sulfate content at high chitosan:sodium sulfate weight ratio or with decrease of chitosan content. On the other hand, friability of tablets was increased in the presence of an excessive amount of sodium sulfate and low chitosan content as observed with granules. Slow TPH release from the formulated tablets was achieved at 1:0.5 and 1:1 chitosan:sodium sulfate weight ratios where all or most of the cationic chitosan and sulfate anions were used in a cross-linking reaction during wet granulation. Ratios of 1:2 and 1:3 showed fast drug release, which support the hypothesis that excessive unreacted water-soluble sodium sulfate might increase the porosity of the nondesintegrating tablets during dissolution. Slow drug release was also obtained with high molecular weight chitosan, whereas changing the hardness of the tablets did not significantly change the release profile of the drug as long as the tablets are intact during dissolution. Furthermore, slow drug release was observed as the total amount of chitosan was increased in the formulated tablets. A comparative in vivo study between the chosen formulated tablets (1:1 chitosan:sodium sulfate ratio that contains 10% high molecular weight chitosan) and the commercial Quibron tablets indicated prolonged appearance of the drug in dogs' plasma for both formulations with no significant differences (p > 0.05) in rate and extent of drug absorption. The formulated tablets showed 103.16% bioavailability relative to that of the commercial tablets. PMID:16093204

Alsarra, Ibrahim A; El-Bagory, Ibrahim; Bayomi, Mohsen A

2005-05-01

303

An osmotic bioequivalent nifedipine tablet  

Microsoft Academic Search

A new osmotic nifedipine tablet with a controlled release profile of 24 hours, was developed. It is composed of a core containing nifedipine, a polymeric membrane and a laser drilled orifice to allow the release of the drug. The aim of the study was to assess the bioequivalency between the osmotic nifedipine tablet and the innovator Procardia® XL (nifedipine extended

E. C. Feleder; M. Befumo; M. A. Ricci; M. A. Coppari; J. Faour

2004-01-01

304

Review of bilayer tablet technology.  

PubMed

Therapeutic strategies based on oral delivery of bilayer (and multilayer) tablets are gaining more acceptance among brand and generic products due to a confluence of factors including advanced delivery strategies, patient compliance and combination therapy. Successful manufacturing of these ever more complex systems needs to overcome a series of challenges from formulation design to tablet press monitoring and control. This article provides an overview of the state-of-the-art of bilayer tablet technology, highlighting the main benefits of this type of oral dosage forms while providing a description of current challenges and advances toward improving manufacturing practices and product quality. Several aspects relevant to bilayer tablet manufacturing are addressed including material properties, lubrication, layer ordering, layer thickness, layer weight control, as well as first and final compression forces. A section is also devoted to bilayer tablet characterization that present additional complexities associated with interfaces between layers. The available features of the manufacturing equipment for bilayer tablet production are also described indicating the different strategies for sensing and controls offered by bilayer tablet press manufacturers. Finally, a roadmap for bilayer tablet manufacturing is advanced as a guideline to formulation design and selection of process parameters and equipment. PMID:24370841

Abebe, Admassu; Akseli, Ilgaz; Sprockel, Omar; Kottala, Niranjan; Cuitiño, Alberto M

2014-01-30

305

Floating into Thin Air  

SciTech Connect

On May 18, 2005, a giant helium balloon carrying the High Energy Focusing Telescope (HEFT) sailed into the spring sky over the deserts of New Mexico. The spindly steel and aluminum gondola that houses the optics, detectors, and other components of the telescope floated for 25 hours after its launch from Fort Sumner, New Mexico. For 21 of those hours, the balloon was nearly 40 kilometers above Earth's surface--almost four times higher than the altitude routinely flown by commercial jet aircraft. In the upper reaches of Earth's atmosphere, HEFT searched the universe for x-ray sources from highly energetic objects such as binary stars, galaxy clusters, and supermassive black holes. Before landing in Arizona, the telescope observed and imaged a dozen scientific targets by capturing photons emitted from these objects in the high-energy (hard) x-ray range (above 10 kiloelectronvolts). Among these targets were the Crab synchrotron nebula, the black hole Cygnus X-1 (one of the brightest x-ray sources in the sky), and the blazar 3C454.3. The scientific data gathered from these targets are among the first focused hard x-ray images returned from high altitudes.

Hazi, A U

2007-02-06

306

Floating wind turbine system  

NASA Technical Reports Server (NTRS)

A floating wind turbine system with a tower structure that includes at least one stability arm extending therefrom and that is anchored to the sea floor with a rotatable position retention device that facilitates deep water installations. Variable buoyancy for the wind turbine system is provided by buoyancy chambers that are integral to the tower itself as well as the stability arm. Pumps are included for adjusting the buoyancy as an aid in system transport, installation, repair and removal. The wind turbine rotor is located downwind of the tower structure to allow the wind turbine to follow the wind direction without an active yaw drive system. The support tower and stability arm structure is designed to balance tension in the tether with buoyancy, gravity and wind forces in such a way that the top of the support tower leans downwind, providing a large clearance between the support tower and the rotor blade tips. This large clearance facilitates the use of articulated rotor hubs to reduced damaging structural dynamic loads. Major components of the turbine can be assembled at the shore and transported to an offshore installation site.

Viterna, Larry A. (Inventor)

2009-01-01

307

Tests find hammering, fluid cutting, erosion cause float shoe failures  

Microsoft Academic Search

The results of a systematic test program to evaluate float equipment performance are presented. The testing has destroyed, over an eightmonth period, 160 float valves, float shoes and float collars. A new float valve design with greater resistance to failure has been developed as a result of the testing. New float collars and float shoes are expected to provide the

Stringfellow

1985-01-01

308

A floating multiparticulate system for ofloxacin based on a multilayer structure: In vitro and in vivo evaluation.  

PubMed

The purpose of this research was to develop a novel gastroretentive multiparticulate system with floating ability. This system was designed to provide drug-loaded pellets coated with three successive coatings-the retarding film (ethyl cellulose), the effervescent layer (sodium bicarbonate) and the gas-entrapped polymeric membrane (Eudragit RL 30D). The floating pellets were evaluated for SEM, floating characteristic parameters, in vitro release and bioavailability in New Zealand rabbits. The zero-order release theory model is designed to interpret the release processes. Due to the swelling property, high flexibility and high water permeability, Eudragit RL 30D was used as a gas-entrapped polymeric membrane. The obtained pellets exhibit excellent floating ability and release characteristics. Analysis of the release mechanism showed a zero-order release for the first 8h because of the osmotic pressure of the saturated solution inside of the membrane, which was in accordance with that predicted. Abdominal X-ray images showed that the gastroretention period of the floating barium sulfate-labeled pellets was no less than 6h. The relative bioavailability of the floating pellets compared with reference tablets was 113.06 ± 23.83%. All these results showed that the floating pellets are a feasible approach for the gastroretentive drug delivery system. PMID:22525085

Zhang, Chungang; Xu, Ming; Tao, Xiaoguang; Tang, Jingya; Liu, Zitong; Zhang, Yu; Lin, Xia; He, Haibing; Tang, Xing

2012-07-01

309

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

310

Design and in vitro evaluation of zidovudine oral controlled release tablets prepared using hydroxypropyl methylcellulose.  

PubMed

Oral controlled release matrix tablets of zidovudine were prepared using different proportions and different viscosity grades of hydroxypropyl methylcellulose. The effect of various formulation factors like polymer proportion, polymer viscosity and compression force on the in vitro release of drug were studied. In vitro release studies were carried out using United States Pharmacopeia (USP) type 1 apparatus (basket method) in 900 ml of pH 6.8 phosphate buffer at 100 rpm. The release kinetics were analyzed using Zero-order model equation, Higuchi's square-root equation and Ritger-Peppas' empirical equation. Compatibility of drug with various formulations excipients used was studied. In vitro release studies revealed that the release rate decreased with increase in polymer proportion and viscosity grade. Increase in compression force was found to decrease the rate of drug release. Matrix tablets containing 10% hydroxypropyl methylcellulose (HPMC) 4000 cps were found to show a good initial drug release of 21% in the first hour and extended the release upto 16 h. Matrix tablets containing 20% HPMC 4000 cps and 10% HPMC 15000 cps showed a first hour release of 18% and extended the release upto 20 h. Mathematical analysis of the release kinetics indicated that the nature of drug release from the matrix tablets followed non-Fickian or anomalous release. No incompatibility was observed between the drug and excipients used in the formulation of matrix tablets. The developed controlled release matrix tablets of zidovudine, with good initial release (17-25% in first hour) and which extend the release upto 16-20 h, can overcome the disadvantages of conventional tablets of zidovudine. PMID:18379101

Ravi, Punna Rao; Ganga, Sindhura; Saha, Ranendra Narayan

2008-04-01

311

Bioadhesive mini-tablets for vaginal drug delivery.  

PubMed

Different non-ionic cellulose ethers (methyl cellulose, MC; hydroxyethyl cellulose, HEC; hydroxypropyl cellulose, HPC; hydroxypropylmethyl cellulose, HPMC) and microcrystalline cellulose (MCC) were investigated as matrix formers for preparation of mini-tablets targeting vaginal drug delivery. Hexyl aminolevulinat hydrochloridum (HAL) was used as a model drug. The mini-tablets were characterized with respect to their mechanical strength, bioadhesion towards cow vaginal tissue in two independent tests (rotating cylinder test, detachment test using texture analyzer), and dissolution rate in two media mimicking the pH levels of fertile, healthy and post-menopausal women (vaginal fluid simulant pH 4.5, phosphate buffer pH 6.8). Mini-tablets with a matrix of either HPMC or HPC were found to possess adequate mechanical strength, superior bioadhesive behavior towards vaginal tissue, and pH independent controlled release of the model drug, suggesting that both systems would be suited for the treatment of women regardless of age, i.e., respective of their vaginal pH levels. Bioadhesive mini-tablets offer a potential for improved residence time in the vaginal cavity targeting contact with mucosal tissue and prolonged release of the drug. PMID:25166286

Hiorth, Marianne; Nilsen, Susanne; Tho, Ingunn

2014-01-01

312

Bioadhesive Mini-Tablets for Vaginal Drug Delivery  

PubMed Central

Different non-ionic cellulose ethers (methyl cellulose, MC; hydroxyethyl cellulose, HEC; hydroxypropyl cellulose, HPC; hydroxypropylmethyl cellulose, HPMC) and microcrystalline cellulose (MCC) were investigated as matrix formers for preparation of mini-tablets targeting vaginal drug delivery. Hexyl aminolevulinat hydrochloridum (HAL) was used as a model drug. The mini-tablets were characterized with respect to their mechanical strength, bioadhesion towards cow vaginal tissue in two independent tests (rotating cylinder test, detachment test using texture analyzer), and dissolution rate in two media mimicking the pH levels of fertile, healthy and post-menopausal women (vaginal fluid simulant pH 4.5, phosphate buffer pH 6.8). Mini-tablets with a matrix of either HPMC or HPC were found to possess adequate mechanical strength, superior bioadhesive behavior towards vaginal tissue, and pH independent controlled release of the model drug, suggesting that both systems would be suited for the treatment of women regardless of age, i.e., respective of their vaginal pH levels. Bioadhesive mini-tablets offer a potential for improved residence time in the vaginal cavity targeting contact with mucosal tissue and prolonged release of the drug. PMID:25166286

Hiorth, Marianne; Nilsen, Susanne; Tho, Ingunn

2014-01-01

313

Study on jelly fig extract as a potential hydrophilic matrix for controlled drug delivery.  

PubMed

The principal component of aqueous extract of jelly fig (Ficus awkeotsang Makino) seeds is a pectin-type polysaccharide, gelling even at room temperature without adding any sugars, acids or ions. The objective of this study was to evaluate jelly fig extract (JF) as a matrix base for sustained release tablets. Drug release profile from JF tablet was examined using theophylline as a model drug, compared with those from USP graded pectin (USP-P). Release profile from JF tablet was a sustained release pattern and not affected by pH of medium. USP-P tablet showed a similar release profile of JF tablet, however, the release mechanisms differed. Matrix erosion studies revealed that the percentage of drug released from USP-P tablet was proportional to that of matrix eroded. On the other hand, JF tablet was eroded up to 50% of matrix for 4h and showed a constant value thereafter. According to water uptake studies, JF tablet showed an initial burst swelling followed by slow water uptake, suggesting diffusion-controlled kinetics in later phase. Moreover, theophylline release rate from JF tablet was modified by drug content in the tablet, increasing with decrease in drug amount. These findings indicated JF was a potential hydrophilic matrix for controlled drug delivery. PMID:15541910

Miyazaki, Yasunori; Yakou, Shigeru; Takayama, Kozo

2004-12-01

314

Evaluation of porous carrier-based floating orlistat microspheres for gastric delivery.  

PubMed

The purpose of this research was to prepare floating microspheres consisting of (1) calcium silicate as porous carrier; (2) orlistat, an oral anti-obesity agent; and (3) Eudragit S as polymer, by solvent evaporation method and to evaluate their gastro-retentive and controlled-release properties. The effect of various formulation and process variables on the particle morphology, micromeritic properties, in vitro floating behavior, percentage drug entrapment, and in vitro drug release was studied. The gamma scintigraphy of the optimized formulation was performed in albino rabbits to monitor the transit of floating microspheres in the gastrointestinal tract. The orlistat-loaded optimized formulation was orally administered to albino rabbits, and blood samples collected were used to determine pharmacokinetic parameters of orlistat from floating microspheres. The microspheres were found to be regular in shape and highly porous. Microsphere formulation CS4, containing 200 mg calcium silicate, showed the best floating ability (88% +/- 4% buoyancy) in simulated gastric fluid as compared with other formulations. Release pattern of orlistat in simulated gastric fluid from all floating microspheres followed Higuchi matrix model and Peppas-Korsmeyer model. Prolonged gastric residence time of over 6 hours was achieved in all rabbits for calcium silicate-based floating microspheres of orlistat. The enhanced elimination half-life observed after pharmacokinetic investigations in the present study is due to the floating nature of the designed formulations. PMID:17233542

Jain, Sunil K; Agrawal, Govind P; Jain, Narendra K

2006-01-01

315

Development and optimization of press coated floating pulsatile drug delivery of sumatriptan succinate.  

PubMed

Floating pulsatile is combined approach designed according to circadian rhythm to deliver the drug at right time, in right quantity and at right site as per pathophysiological need of disease with prolong gastric residence and lag phase followed by burst release. As the migraine follows circadian rhythm in which headache is more painful at the awakening time, the dosage form should be given during night time to release drug when pain get worsen. Present work deals with formulation and optimization of floating pulsatile tablet of sumatriptan succinate. Core tablet containing crospovidone as superdisintegrant (10%) showed burst release. Lag time was maintained using swellable polymer as polyoxN12K and xanthum gum. 3(2) experimental design was carried out. Developed formulations were evaluated for physical characteristics, in vitro and in vivo study. Optimized batch F2 with concentration of polyox N12K (73.43%) and xanthum gum (26.56%) of total polymer weight showed floating lag time 15±2 sec, drug content 99.58±0.2 %, hardness 6±0.2 Kg/cm(2) and drug release 99.54±2% with pulsatile manner followed lag period of 7±0.1h. In vivo x-ray study confirms prolong gastric residence of system. Programmable pulsatile release has been achieved by formulation F2 which meet demand of chronotherapeutic objective of migraine. PMID:24893996

Jagdale, Swati C; Pawar, Chandrakala R

2014-01-01

316

Optimization studies on compression coated floating-pulsatile drug delivery of bisoprolol.  

PubMed

The purpose of the present work was to design and optimize compression coated floating pulsatile drug delivery systems of bisoprolol. Floating pulsatile concept was applied to increase the gastric residence of the dosage form having lag phase followed by a burst release. The prepared system consisted of two parts: a core tablet containing the active ingredient and an erodible outer shell with gas generating agent. The rapid release core tablet (RRCT) was prepared by using superdisintegrants with active ingredient. Press coating of optimized RRCT was done by polymer. A 3² full factorial design was used for optimization. The amount of Polyox WSR205 and Polyox WSR N12K was selected as independent variables. Lag period, drug release, and swelling index were selected as dependent variables. Floating pulsatile release formulation (FPRT) F13 at level 0 (55?mg) for Polyox WSR205 and level +1 (65?mg) for Polyox WSR N12K showed lag time of 4?h with >90% drug release. The data were statistically analyzed using ANOVA, and P < 0.05 was statistically significant. Release kinetics of the optimized formulation best fitted the zero order model. In vivo study confirms burst effect at 4?h in indicating the optimization of the dosage form. PMID:24367788

Jagdale, Swati C; Bari, Nilesh A; Kuchekar, Bhanudas S; Chabukswar, Aniruddha R

2013-01-01

317

Tablet PC and Computing Curriculum Initiative Evaluation of Tablet PC Supported Pedagogy  

E-print Network

Tablet PC and Computing Curriculum Initiative 2006 Evaluation of Tablet PC Supported Pedagogy http holders react to the technology? Does the student submissions pedagogy increase engagement? Which types

Anderson, Richard

318

Design and evaluation of hydrophobic coated buoyant core as floating drug delivery system for sustained release of cisapride.  

PubMed

An inert hydrophobic buoyant coated-core was developed as floating drug delivery system (FDDS) for sustained release of cisapride using direct compression technology. Core contained low density, porous ethyl cellulose, which was coated with an impermeable, insoluble hydrophobic coating polymer such as rosin. It was further seal coated with low viscosity hydroxypropyl methyl cellulose (HPMC E15) to minimize moisture permeation and better adhesion with an outer drug layer. It was found that stable buoyant core was sufficient to float the tablet more than 8 h without the aid of sodium bicarbonate and citric acid. Sustained release of cisapride was achieved with HPMC K4M in the outer drug layer. The floating lag time required for these novel FDDS was found to be zero, however it is likely that the porosity or density of the core is critical for floatability of these tablets. The in vitro release pattern of these tablets in simulated gastric fluid showed the constant and controlled release for prolonged time. It can be concluded that the hydrophobic coated buoyant core could be used as FDDS for gastroretentive delivery system of cisapride or other suitable drugs. PMID:24825997

Jacob, Shery; Nair, Anroop B; Patil, Pandurang N

2010-12-01

319

Design and evaluation of hydrophobic coated buoyant core as floating drug delivery system for sustained release of cisapride  

PubMed Central

An inert hydrophobic buoyant coated–core was developed as floating drug delivery system (FDDS) for sustained release of cisapride using direct compression technology. Core contained low density, porous ethyl cellulose, which was coated with an impermeable, insoluble hydrophobic coating polymer such as rosin. It was further seal coated with low viscosity hydroxypropyl methyl cellulose (HPMC E15) to minimize moisture permeation and better adhesion with an outer drug layer. It was found that stable buoyant core was sufficient to float the tablet more than 8 h without the aid of sodium bicarbonate and citric acid. Sustained release of cisapride was achieved with HPMC K4M in the outer drug layer. The floating lag time required for these novel FDDS was found to be zero, however it is likely that the porosity or density of the core is critical for floatability of these tablets. The in vitro release pattern of these tablets in simulated gastric fluid showed the constant and controlled release for prolonged time. It can be concluded that the hydrophobic coated buoyant core could be used as FDDS for gastroretentive delivery system of cisapride or other suitable drugs. PMID:24825997

Jacob, Shery; Nair, Anroop B; Patil, Pandurang N

2010-01-01

320

14 CFR 27.753 - Main float design.  

...2014-01-01 false Main float design. 27.753 Section 27...DEPARTMENT OF TRANSPORTATION AIRCRAFT AIRWORTHINESS STANDARDS: NORMAL CATEGORY ROTORCRAFT Design and Construction Floats and Hulls § 27.753 Main float design. (a) Bag floats....

2014-01-01

321

14 CFR 27.753 - Main float design.  

Code of Federal Regulations, 2012 CFR

...2012-01-01 false Main float design. 27.753 Section 27...DEPARTMENT OF TRANSPORTATION AIRCRAFT AIRWORTHINESS STANDARDS: NORMAL CATEGORY ROTORCRAFT Design and Construction Floats and Hulls § 27.753 Main float design. (a) Bag floats....

2012-01-01

322

14 CFR 29.753 - Main float design.  

...2014-01-01 false Main float design. 29.753 Section 29...DEPARTMENT OF TRANSPORTATION AIRCRAFT AIRWORTHINESS STANDARDS: TRANSPORT CATEGORY ROTORCRAFT Design and Construction Floats and Hulls § 29.753 Main float design. (a) Bag floats....

2014-01-01

323

14 CFR 27.753 - Main float design.  

Code of Federal Regulations, 2011 CFR

...2011-01-01 false Main float design. 27.753 Section 27...DEPARTMENT OF TRANSPORTATION AIRCRAFT AIRWORTHINESS STANDARDS: NORMAL CATEGORY ROTORCRAFT Design and Construction Floats and Hulls § 27.753 Main float design. (a) Bag floats....

2011-01-01

324

14 CFR 25.753 - Main float design.  

Code of Federal Regulations, 2011 CFR

...2011-01-01 false Main float design. 25.753 Section 25...DEPARTMENT OF TRANSPORTATION AIRCRAFT AIRWORTHINESS STANDARDS: TRANSPORT CATEGORY AIRPLANES Design and Construction Floats and Hulls § 25.753 Main float design. Each main float must...

2011-01-01

325

14 CFR 25.753 - Main float design.  

Code of Federal Regulations, 2010 CFR

...2010-01-01 false Main float design. 25.753 Section 25...DEPARTMENT OF TRANSPORTATION AIRCRAFT AIRWORTHINESS STANDARDS: TRANSPORT CATEGORY AIRPLANES Design and Construction Floats and Hulls § 25.753 Main float design. Each main float must...

2010-01-01

326

14 CFR 27.753 - Main float design.  

Code of Federal Regulations, 2010 CFR

...2010-01-01 false Main float design. 27.753 Section 27...DEPARTMENT OF TRANSPORTATION AIRCRAFT AIRWORTHINESS STANDARDS: NORMAL CATEGORY ROTORCRAFT Design and Construction Floats and Hulls § 27.753 Main float design. (a) Bag floats....

2010-01-01

327

14 CFR 25.753 - Main float design.  

Code of Federal Regulations, 2013 CFR

...2013-01-01 false Main float design. 25.753 Section 25...DEPARTMENT OF TRANSPORTATION AIRCRAFT AIRWORTHINESS STANDARDS: TRANSPORT CATEGORY AIRPLANES Design and Construction Floats and Hulls § 25.753 Main float design. Each main float must...

2013-01-01

328

14 CFR 25.753 - Main float design.  

Code of Federal Regulations, 2012 CFR

...2012-01-01 false Main float design. 25.753 Section 25...DEPARTMENT OF TRANSPORTATION AIRCRAFT AIRWORTHINESS STANDARDS: TRANSPORT CATEGORY AIRPLANES Design and Construction Floats and Hulls § 25.753 Main float design. Each main float must...

2012-01-01

329

14 CFR 25.753 - Main float design.  

...2014-01-01 false Main float design. 25.753 Section 25...DEPARTMENT OF TRANSPORTATION AIRCRAFT AIRWORTHINESS STANDARDS: TRANSPORT CATEGORY AIRPLANES Design and Construction Floats and Hulls § 25.753 Main float design. Each main float must...

2014-01-01

330

14 CFR 29.753 - Main float design.  

Code of Federal Regulations, 2010 CFR

...2010-01-01 false Main float design. 29.753 Section 29...DEPARTMENT OF TRANSPORTATION AIRCRAFT AIRWORTHINESS STANDARDS: TRANSPORT CATEGORY ROTORCRAFT Design and Construction Floats and Hulls § 29.753 Main float design. (a) Bag floats....

2010-01-01

331

14 CFR 29.753 - Main float design.  

Code of Federal Regulations, 2013 CFR

...2013-01-01 false Main float design. 29.753 Section 29...DEPARTMENT OF TRANSPORTATION AIRCRAFT AIRWORTHINESS STANDARDS: TRANSPORT CATEGORY ROTORCRAFT Design and Construction Floats and Hulls § 29.753 Main float design. (a) Bag floats....

2013-01-01

332

14 CFR 27.753 - Main float design.  

Code of Federal Regulations, 2013 CFR

...2013-01-01 false Main float design. 27.753 Section 27...DEPARTMENT OF TRANSPORTATION AIRCRAFT AIRWORTHINESS STANDARDS: NORMAL CATEGORY ROTORCRAFT Design and Construction Floats and Hulls § 27.753 Main float design. (a) Bag floats....

2013-01-01

333

14 CFR 29.753 - Main float design.  

Code of Federal Regulations, 2012 CFR

...2012-01-01 false Main float design. 29.753 Section 29...DEPARTMENT OF TRANSPORTATION AIRCRAFT AIRWORTHINESS STANDARDS: TRANSPORT CATEGORY ROTORCRAFT Design and Construction Floats and Hulls § 29.753 Main float design. (a) Bag floats....

2012-01-01

334

14 CFR 29.753 - Main float design.  

Code of Federal Regulations, 2011 CFR

...2011-01-01 false Main float design. 29.753 Section 29...DEPARTMENT OF TRANSPORTATION AIRCRAFT AIRWORTHINESS STANDARDS: TRANSPORT CATEGORY ROTORCRAFT Design and Construction Floats and Hulls § 29.753 Main float design. (a) Bag floats....

2011-01-01

335

Flexible dynamics of floating wind turbines  

E-print Network

This work presents Tower Flex, a structural dynamics model for a coupled analysis of offshore floating wind turbines consisting of a tower, a floating platform and a mooring system. In this multi-body, linear frequency-domain ...

Luypaert, Thomas (Thomas J.)

2012-01-01

336

32 CFR 935.165 - Floating objects.  

...INSULAR REGULATIONS WAKE ISLAND CODE Public Safety § 935.165 Floating objects. No person may anchor, moor, or beach any boat, barge, or other floating object on Wake Island in any location or manner other than as prescribed by the...

2014-07-01

337

Have Floating Rates Been a Success?  

ERIC Educational Resources Information Center

Floating exchange rates have not lived up to all expectations, but neither have they performed as badly as some critics have suggested. Examined are the impact of floating rates on balance of payments adjustment, domestic economic policy, and inflation and the claim that floating rates have displayed excessive fluctuations. (Author/RM)

Higham, David

1983-01-01

338

Dragging a floating horizontal cylinder  

Microsoft Academic Search

A cylinder immersed in a fluid stream experiences a drag, and it is well known that the drag coefficient is a function of the Reynolds number only. Here we study the force exerted on a long horizontal cylinder that is dragged perpendicular to its axis while floating on an air-water interface with a high Reynolds number. In addition to the

Duck-Gyu Lee; Ho-Young Kim

2010-01-01

339

Suminagashi: Floating Ink Paper Marbling  

NSDL National Science Digital Library

In this activity, learners try to float ink on the surface of water to create a pattern and then capture it with absorbent paper. This technique, called Suminagashi, is an ancient Japanese style of decorating paper with inks and believed to be the oldest form of marbling. This art activity can introduce learners to fluid mechanics, viscosity, and surface tension.

Henricks, Jessica

2012-06-26

340

21 CFR 520.1510 - Nitenpyram tablets.  

Code of Federal Regulations, 2010 CFR

...DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ...Conditions of use —(1) Dogs —(i) Amount —(A) One 11.4-mg tablet for dogs weighing less than 25 pounds...or one 57-mg tablet for dogs weighing more than 25...

2010-04-01

341

21 CFR 520.312 - Carnidazole tablets.  

Code of Federal Regulations, 2013 CFR

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

2013-04-01

342

21 CFR 520.312 - Carnidazole tablets.  

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

2014-04-01

343

21 CFR 520.312 - Carnidazole tablets.  

Code of Federal Regulations, 2012 CFR

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

2012-04-01

344

Formulation and evaluation of mixed matrix gastro-retentive drug delivery for famotidine  

PubMed Central

Introduction: Present investigation describes an influence of ratio of Gelucire 43/01(hydrophobic) to hydroxypropyl methylcellulose K4M (HPMC K4M) (hydrophilic) and different fillers on release of famotidine from gastro-retentive tablets using 32 full factorial design. Ratio of Gelucire 43/01 to HPMC K4M (X1) and the type of filler (X2) were selected as independent variables while buoyancy lag time (BLT), drug release at 1h (Q1), 6h (Q6), and the 12h (Q12) were selected as dependent variables. Materials and Methods: Gastro-retentive tablets of famotidine were prepared by a solvent free melt granulation technique using Gelucire 43/01 as a hydrophobic meltable binder. HPMC K4M and sodium bicarbonate were used as matrixing agent and gas-generating agent, respectively. Prepared tablets were evaluated for in vitro dissolution, in vitro buoyancy, friability, hardness, drug content and weight variation. Dissolution data were fitted to various models to ascertain kinetics of drug release. The data were analyzed using regression analysis and analysis of variance. Results: All formulations (F1-F9) showed floating within 3min and had total floating time of more than 12h. It was observed that a type of filler and the ratio of Gelucire 43/01 to HPMC K4M had significant influence on buoyancy lag time (P = 0.037) and Q6 (P = 0.011), respectively without significant influence on Q1 and Q12. Conclusion: Formulation F5 was selected as an optimum formulation as it showed more similarity in dissolution profile with theoretical profile (Similarity factor, f2 = 83.01). The dissolution of batch F5 can be described by zero order kinetics (r2 = 0.9914) with anomalous (non-Fickian) diffusion as a release mechanism (n = 0.559). The difference observed in in vitro release profile after temperature sensitivity study at 40°C for 1 month was insignificant. PMID:23071951

Patel, Dasharath M; Patel, Mehul J; Patel, Ankit N; Patel, Chhagan N

2011-01-01

345

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

PubMed

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

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

2008-06-01

346

Scaffolding Equals Success in Teaching Tablet PCs  

ERIC Educational Resources Information Center

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

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

2009-01-01

347

Mathematics Instruction and the Tablet PC  

ERIC Educational Resources Information Center

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 to write on…

Fister, K. Renee; McCarthy, Maeve L.

2008-01-01

348

Touch Screen Tablets and Emergent Literacy  

ERIC Educational Resources Information Center

The use of touch screen tablets by young children is increasing in the home and in early childhood settings. The simple tactile interface and finger-based operating features of tablets may facilitate preschoolers' use of tablet application software and support their educational development in domains such as literacy. This article reviews…

Neumann, Michelle M.; Neumann, David L.

2014-01-01

349

Sugar end-capped poly-D,L-lactides as excipients in oral sustained release tablets.  

PubMed

Sugar end-capped poly-D,L-lactide (SPDLA) polymers were investigated as a potential release controlling excipient in oral sustained release matrix tablets. The SPDLA polymers were obtained by a catalytic ring-opening polymerization technique using methyl alpha-D-gluco-pyranoside as a multifunctional initiator in the polymerization. Polymers of different molecular weights were synthesized by varying molar ratios of monomer/catalyst. The matrix tablets were prepared by direct compression technique from the binary mixtures of SPDLA and microcrystalline cellulose, and theophylline was used as a model drug. The tablet matrices showed in vitro reproducible drug release profiles with a zero-order or diffusion-based kinetic depending on the SPDLA polymer grade used. Further release from the tablet matrices was dependent on the molecular weight of the SPDLA polymer applied. The drug release was the fastest with the lowest molecular weight SPDLA grade, and the drug release followed zero-order rate. With the higher molecular weight SPDLAs, more prolonged dissolution profiles for the matrix tablets (up to 8-10 h) were obtained. Furthermore, the prolonged drug release was independent of the pH of the dissolution media. In conclusion, SPDLAs are a novel type of drug carrier polymers applicable in oral controlled drug delivery systems. PMID:19430908

Vuorinen, Sirpa; Heinämäki, Jyrki; Antikainen, Osmo; Lahcini, Mohammed; Repo, Timo; Yliruusi, Jouko

2009-01-01

350

A floating type holographic display.  

PubMed

A floating image type holographic display which projects an electronically generated holographic image together with a background image displayed on a monitor/TV to enhance the visual effects of the former image is introduced. This display can display a holographic image with a spatial volume floating in the front space of the display with use of PDLC sheets as the focused plane of the image. This display can preserve and enhance the main property of holographic image from a display chip, i.e., a spatial image with a volume. This property had not been appealed by the previous holographic displays due to the much brighter active surface image accompanied with the reconstructed image and the diffuser used for viewing the image. PMID:24105588

Son, Jung-Young; Lee, Chun-Hae; Chernyshov, Oleksii O; Lee, Beom-Ryeol; Kim, Sung-Kyu

2013-08-26

351

Development and optimization of a novel sustained-release dextran tablet formulation for propranolol hydrochloride.  

PubMed

A novel oral controlled delivery system for propranolol hydrochloride (PPL) was developed and optimized. The in vitro dissolution profiles of sustained-release matrix tablets of racemic PPL were determined and compared with the United States Pharmacopeia (USP) tolerance specifications for Propranolol Hydrochloride Extended-Release Capsules. The influence of matrix forming agents (native dextran, hydroxypropyl methylcellulose (HPMC), cetyl alcohol) and binary mixtures of them on PPL release in vitro was investigated. A central composite design was applied to the optimization of a sustained-release tablet formulation. The sustained-release matrix tablets with good physical, mechanical and technological properties were obtained with a matrix excipient:PPL ratio of 60:40 (w/w), with a dextran:HPMC ratio of 4:1 (w/w) and with a cetyl alcohol amount of 15% (w/w). A comparative kinetic study of the present matrix tablets and commercial SUMIAL RETARD capsules (Spain) was established. The value for the similarity factor (f(2)=69.6) suggested that the dissolution profile of the present two sustained-release oral dosage forms are similar. Higuchi (diffusion) and Hixon-Crowell (erosion) kinetic profiles were achieved and this codependent mechanism of drug release was established. PMID:16584856

Gil, Eddy Castellanos; Colarte, Antonio Iraizoz; Bataille, Bernard; Pedraz, José Luis; Rodríguez, Fernand; Heinämäki, Jyrki

2006-07-01

352

Silicone adhesive matrix of verapamil hydrochloride to provide pH-independent sustained release.  

PubMed

Providing pH-independent oral release of weakly basic drugs with conventional matrix tablets can be challenging because of the pH-dependent solubility characteristics of the drugs and the changing pH environment along the gastrointestinal tract. The aim of the present study was to use a hydrophobic polymer to overcome the issue of pH-dependent release of weakly basic model drug verapamil hydrochloride from matrix tablets without the use of organic buffers in the matrix formulations. Silicone pressure-sensitive adhesive (PSA) polymer was evaluated because of its unique properties of low surface energy, hydrophobicity, low glass transition temperature, high electrical resistance, and barrier to hydrogen ion diffusion. Drug release, hydrogen ion diffusion, tablet contact angle, and internal tablet microenvironment pH with matrix tablets prepared using PSA were compared with those using water-insoluble ethyl cellulose (EC). Silicone PSA films showed higher resistance to hydrogen ion diffusion compared with EC films. Verapamil hydrochloride tablets prepared using silicone PSA showed higher hydrophobicity and lower water uptake than EC tablets. Silicone PSA tablets also showed pH-independent release of verapamil and decreased in dimensions during drug dissolution. By contrast, verapamil hydrochloride tablets prepared using EC did not achieve pH-independent release. PMID:24022347

Tolia, Gaurav; Li, S Kevin

2014-02-01

353

Dragging a floating horizontal cylinder  

NASA Astrophysics Data System (ADS)

A cylinder immersed in a fluid stream experiences a drag, and it is well known that the drag coefficient is a function of the Reynolds number only. Here we study the force exerted on a long horizontal cylinder that is dragged perpendicular to its axis while floating on an air-water interface with a high Reynolds number. In addition to the flow-induced drag, the floating body is subjected to capillary forces along the contact line where the three phases of liquid/solid/gas meet. We first theoretically predict the meniscus profile around the horizontally moving cylinder assuming the potential flow, and show that the profile is in good agreement with that obtained experimentally. Then we compare our theoretical predictions and experimental measurement results for the drag coefficient of a floating horizontal cylinder that is given by a function of the Weber number and the Bond number. This study can help us to understand the horizontal motion of partially submerged objects at air-liquid interface, such as semi-aquatic insects and marine plants.

Lee, Duck-Gyu; Kim, Ho-Young

2010-11-01

354

Sustained release phenylpropanolamine hydrochloride from ATO 888 matrix.  

PubMed

Sustained release phenylpropanolamine HCl tablets were prepared with compritol as a retardant material. The effects of varying wax levels and methods of matrix formation on drug release were investigated. Also the compaction profiles were recorded for all formulations. The amount of drug in the formula was held constant (10% w/w), while the wax level was varied from 10% to 50% w/w. Two methods were used for the preparation of drug: wax systems; physical mixture and solid dispersion. The drug release from tablets containing 10% Compritol and prepared by solid dispersion was 97% after six hours of testing dissolution. Tablets prepared with 30% wax released 72% of the drug, while tablets containing 50% wax released only 30% of the drug after six hours. Tablets prepared by physical mixture gave higher drug release than tablets prepared by solid dispersion method. The incorporation of Compritol decreased the ejection forces of tablets during compaction. The drug release from tablets prepared by solid dispersion followed the diffusion controlled model described by Higuchi for inert porous matrix. PMID:8140204

Perez, M A; Ghaly, E S; Marti, A

1993-12-01

355

Real-time tablet formation monitoring with ultrasound measurements in eccentric single station tablet press.  

PubMed

A real-time ultrasound measurement system for tablet compression monitoring is introduced. The measurement system was tested in actual manufacturing environment and found to be capable of measuring the ultrasound response of the tabletting process from bulk to tablet. The tablet sets were compressed and the ultrasound measurements were conducted as implemented in eccentric single station tabletting apparatus in through transmission geometry. The speed of sound and ultrasound spectrum was measured during dynamic compression for microcrystalline cellulose/paracetamol tablets. The ultrasound system introduced in this study was found to be suitable for tabletting process monitoring as the mechanical properties of compressed tablets can be estimated during compression using the ultrasound system. In addition, it was found that the ultrasound was sensitive to the mixing time of magnesium stearate and the concentration of paracetamol. Thus, ultrasound measurements made during the compression can be used to monitor the tablet formation process. PMID:22985771

Leskinen, Jari T T; Simonaho, Simo-Pekka; Hakulinen, Mikko; Ketolainen, Jarkko

2013-02-14

356

The impact on seaplane floats during landing  

NASA Technical Reports Server (NTRS)

In order to make a stress analysis of seaplane floats, and especially of the members connecting the floats with the fuselage, it is of great importance to determine the maximum pressure acting on the floats during landing. Here, the author gives a formula for maximum pressures during landing that permits one to apply experimental results to different bodies and different velocities. The author notes that the formula checks very well with experimental results.

Von Karman, TH

1929-01-01

357

Clustering of Floating Particles by Surface Waves  

Microsoft Academic Search

We study experimentally and theoretically how waves affect the distribution of particles floating on a liquid surface. According\\u000a to the Archimedes’ law the weight of floating particle is equal to the weight of displaced liquid. This law is not quite precise\\u000a for small floating objects. An additional force generating by surface tension pulls a hydrophilic particle deeper into the\\u000a water

Sergei Lukaschuk; Petr Denissenko; Gregory Falkovich

2006-01-01

358

Condition and Error Estimates in Numerical Matrix Computations  

SciTech Connect

This tutorial paper deals with sensitivity and error estimates in matrix computational processes. The main factors determining the accuracy of the result computed in floating--point machine arithmetics are considered. Special attention is paid to the perturbation analysis of matrix algebraic equations and unitary matrix decompositions.

Konstantinov, M. M. [University of Architecture, Civil Engineering and Geodesy, 1046 Sofia (Bulgaria); Petkov, P. H. [Technical University of Sofia, 1000 Sofia (Bulgaria)

2008-10-30

359

Dissolution profile of 24 levofloxacin (100 mg) tablets.  

PubMed

Although there are 23 generic levofloxacin (100 mg) tablets (LVFX tablets) and 1 brand name LVFX tablet (supply now discontinued) in Japan, there have been no reports that have evaluated and compared the dissolution profiles of LVFX tablets using the same dissolution method. We studied the dissolution profile of LVFX tablets by the Paddle method, a standard dissolution test method. Among 23 generic LVFX tablets, 2 LVFX tablets had lower dissolution rates and 14 had higher dissolution rates than the brand name LVFX tablet. It is suggested that LVFX tablets have different dissolution profiles, which could cause different pharmacokinetic profiles. PMID:23380968

Maezawa, Kayoko; Yajima, Ryo; Terajima, Tomoko; Kizu, Junko; Hori, Seiji

2013-10-01

360

Design and Characterization of Diclofenac sodium tablets containing Tamarind seed polysaccharide as Release retardant  

Microsoft Academic Search

Polysaccharides are the choice of materials among the hydrophilic polymers used as they are nontoxic and most acceptable by the regulating authorities. The tamarind seed polysaccharide (TSP) was isolated from tamarind kernel powder and this polysaccharide was utilized in the formulation of matrix tablets containing Diclofenac Sodium by wet granulation technique and evaluated for its drug release characteristics. Hardness of

R. Deveswaran; Sindhu Abraham; S. Bharath; B. V. Basavaraj; Sharon Furtado; V. Madhavan

361

Floating-Point Matrix Multiplication in a Polymorphic Processor  

E-print Network

and of the applications using it. In this paper, we address a reconfigurable coprocessor extension of a General Purpose, proposed in [1], with the major difference that we consider a tightly coupled co-processor architectural multiplier with 9 process- ing elements, organized in a CCU running at 100 MHz on an XC2VP30­6 FPGA. Our

Kuzmanov, Georgi

362

Floating Ice-Algal Aggregates below Melting Arctic Sea Ice  

PubMed Central

During two consecutive cruises to the Eastern Central Arctic in late summer 2012, we observed floating algal aggregates in the melt-water layer below and between melting ice floes of first-year pack ice. The macroscopic (1-15 cm in diameter) aggregates had a mucous consistency and were dominated by typical ice-associated pennate diatoms embedded within the mucous matrix. Aggregates maintained buoyancy and accumulated just above a strong pycnocline that separated meltwater and seawater layers. We were able, for the first time, to obtain quantitative abundance and biomass estimates of these aggregates. Although their biomass and production on a square metre basis was small compared to ice-algal blooms, the floating ice-algal aggregates supported high levels of biological activity on the scale of the individual aggregate. In addition they constituted a food source for the ice-associated fauna as revealed by pigments indicative of zooplankton grazing, high abundance of naked ciliates, and ice amphipods associated with them. During the Arctic melt season, these floating aggregates likely play an important ecological role in an otherwise impoverished near-surface sea ice environment. Our findings provide important observations and measurements of a unique aggregate-based habitat during the 2012 record sea ice minimum year. PMID:24204642

Assmy, Philipp; Ehn, Jens K.; Fernandez-Mendez, Mar; Hop, Haakon; Katlein, Christian; Sundfjord, Arild; Bluhm, Katrin; Daase, Malin; Engel, Anja; Fransson, Agneta; Granskog, Mats A.; Hudson, Stephen R.; Kristiansen, Svein; Nicolaus, Marcel; Peeken, Ilka; Renner, Angelika H. H.; Spreen, Gunnar; Tatarek, Agnieszka; Wiktor, Jozef

2013-01-01

363

Optimization of primaquine diphosphate tablet formulation for controlled drug release using the mixture experimental design.  

PubMed

A tablet formulation based on hydrophilic matrix with a controlled drug release was developed, and the effect of polymer concentrations on the release of primaquine diphosphate was evaluated. To achieve this purpose, a 20-run, four-factor with multiple constraints on the proportions of the components was employed to obtain tablet compositions. Drug release was determined by an in vitro dissolution study in phosphate buffer solution at pH 6.8. The polynomial fitted functions described the behavior of the mixture on simplex coordinate systems to study the effects of each factor (polymer) on tablet characteristics. Based on the response surface methodology, a tablet composition was optimized with the purpose of obtaining a primaquine diphosphate release closer to a zero order kinetic. This formulation released 85.22% of the drug for 8 h and its kinetic was studied regarding to Korsmeyer-Peppas model, (Adj-R(2) = 0.99295) which has confirmed that both diffusion and erosion were related to the mechanism of the drug release. The data from the optimized formulation were very close to the predictions from statistical analysis, demonstrating that mixture experimental design could be used to optimize primaquine diphosphate dissolution from hidroxypropylmethyl cellulose and polyethylene glycol matrix tablets. PMID:22670808

Duque, Marcelo Dutra; Kreidel, Rogério Nepomuceno; Taqueda, Maria Elena Santos; Baby, André Rolim; Kaneko, Telma Mary; Velasco, Maria Valéria Robles; Consiglieri, Vladi Olga

2013-01-01

364

14 CFR 23.753 - Main float design.  

Code of Federal Regulations, 2013 CFR

...2013-01-01 false Main float design. 23.753 Section 23...DEPARTMENT OF TRANSPORTATION AIRCRAFT AIRWORTHINESS STANDARDS...COMMUTER CATEGORY AIRPLANES Design and Construction Floats and Hulls § 23.753 Main float design. Each seaplane main...

2013-01-01

365

14 CFR 23.753 - Main float design.  

Code of Federal Regulations, 2012 CFR

...2012-01-01 false Main float design. 23.753 Section 23...DEPARTMENT OF TRANSPORTATION AIRCRAFT AIRWORTHINESS STANDARDS...COMMUTER CATEGORY AIRPLANES Design and Construction Floats and Hulls § 23.753 Main float design. Each seaplane main...

2012-01-01

366

14 CFR 23.753 - Main float design.  

...2014-01-01 false Main float design. 23.753 Section 23...DEPARTMENT OF TRANSPORTATION AIRCRAFT AIRWORTHINESS STANDARDS...COMMUTER CATEGORY AIRPLANES Design and Construction Floats and Hulls § 23.753 Main float design. Each seaplane main...

2014-01-01

367

14 CFR 23.753 - Main float design.  

Code of Federal Regulations, 2011 CFR

...2011-01-01 false Main float design. 23.753 Section 23...DEPARTMENT OF TRANSPORTATION AIRCRAFT AIRWORTHINESS STANDARDS...COMMUTER CATEGORY AIRPLANES Design and Construction Floats and Hulls § 23.753 Main float design. Each seaplane main...

2011-01-01

368

14 CFR 23.753 - Main float design.  

Code of Federal Regulations, 2010 CFR

...2010-01-01 false Main float design. 23.753 Section 23...DEPARTMENT OF TRANSPORTATION AIRCRAFT AIRWORTHINESS STANDARDS...COMMUTER CATEGORY AIRPLANES Design and Construction Floats and Hulls § 23.753 Main float design. Each seaplane main...

2010-01-01

369

Used float shoe recovered and tested  

Microsoft Academic Search

A cement float valve has been recovered after it was circulated through and cemented downhole. It was retrieved by coring as part of an investigation into a cementing failure. The float equipment was then analyzed for downhole performance. This is believed to be the first instance of intact recovery of full-scale cementing hardware after it has been cemented in place.

Colvard

1986-01-01

370

14 CFR 23.757 - Auxiliary floats.  

...and Hulls § 23.757 Auxiliary floats. Auxiliary floats must be arranged so that, when completely submerged in fresh water, they provide a righting moment of at least 1.5 times the upsetting moment caused by the seaplane or amphibian...

2014-01-01

371

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

2012-02-28

372

Floating plant dominance as a stable state  

PubMed Central

Invasion by mats of free-floating plants is among the most important threats to the functioning and biodiversity of freshwater ecosystems ranging from temperate ponds and ditches to tropical lakes. Dark, anoxic conditions under thick floating-plant cover leave little opportunity for animal or plant life, and they can have large negative impacts on fisheries and navigation in tropical lakes. Here, we demonstrate that floating-plant dominance can be a self-stabilizing ecosystem state, which may explain its notorious persistence in many situations. Our results, based on experiments, field data, and models, represent evidence for alternative domains of attraction in ecosystems. An implication of our findings is that nutrient enrichment reduces the resilience of freshwater systems against a shift to floating-plant dominance. On the other hand, our results also suggest that a single drastic harvest of floating plants can induce a permanent shift to an alternative state dominated by rooted, submerged growth forms. PMID:12634429

Scheffer, Marten; Szabo, Sandor; Gragnani, Alessandra; van Nes, Egbert H.; Rinaldi, Sergio; Kautsky, Nils; Norberg, Jon; Roijackers, Rudi M. M.; Franken, Rob J. M.

2003-01-01

373

21 CFR 520.88f - Amoxicillin trihydrate tablets.  

Code of Federal Regulations, 2010 CFR

...2010-04-01 false Amoxicillin trihydrate tablets. 520.88f ...ANIMAL DRUGS § 520.88f Amoxicillin trihydrate tablets. (a) Specifications... Each tablet contains amoxicillin trihydrate equivalent to 50,...

2010-04-01

374

[Preparation of ondansetron hydrochloride sustained-release tablet evaluation of its and drug release behavior in vitro].  

PubMed

For the purpose of preparing the ondansetron hydrochloride sustained-release tablets and studying the influencing factors, we prepared the ondansetron hydrochloride sustained-release tablets, using hydroxypropylmethylcellose (HPMC) as the matrix material. Then we investigated the effects of the viscosity and amount of HPMC,the sort of fillers, the preparation methods, the alcohol content in adhesives, and the pH of the dissolving solution on the release of ondansetron hydrochloride from sustained-release tablets. On the basis of pharmaceutical preformulation studies,the best formulation and preparation methods were screened out according to orthogonal experiment design method. The release behavior of the tablets followed the Higuchi equation. The viscosity of HPMC,the sort of fillers and the rotation speed had no significant effects on the release of ondansetron hydrochloride sustained-release tablets,while the preparation methods, the alcohol content in adhesives and the pH of the dissolving solution influcenced the release of ondansetron hydrochloride sustained-release tablets significantly. Ondansetron hydrochloride sustained-release tablets had good drug relase behavior for in 12 h in vitro. PMID:16856397

Zhang, Yuhong; Huang, Guihua; Yu, Yanling; Han, Jingbin; Yu, Ping

2006-06-01

375

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

2010-09-01

376

Formulation and optimization of mucoadhesive bilayer buccal tablets of atenolol using simplex design method  

PubMed Central

Introduction: In the present study, mucoadhesive buccal bilayer tablets of atenolol were fabricated with the objective of avoiding first pass metabolism and to improve its bioavailability with reduction in dosing frequency. Hence, the aim of this work was to design oral controlled release mucoadhesive tablets of atenolol and to optimize the drug release profile and bioadhesion. Materials and Methods: Bilayer buccal tablets of atenolol were prepared by direct compression method using simplex method of optimization to investigate the combined effect of hydroxypropyl methylcellulose 15 cps (X1), Carbopol (X2) and mannitol (X3); the in vitro drug release (Y1) and mucoadhesive strength (Y2) were taken as responses. The designed tablets were evaluated for various physical and biological parameters like drug content uniformity, in vitro drug release, short-term stability, and drug- excipient interactions (FTIR). Results: The formulation C containing hydroxypropyl methylcellulose 15 cps (10% w/w of matrix layer), Carbopol 934p (10% w/w of matrix layer) and mannitol (channeling agent, 40% w/w of matrix layer) was found to be promising. This formulation exhibited an in vitro drug release of 89.43% in 9 h along with satisfactory bioadhesion strength (7.20 g). Short-term stability studies on the promising formulation indicated that there are no significant changes in drug content and in vitro dissolution characteristics (P<0.05). IR spectroscopic studies indicated that there are no drug-excipient interactions. PMID:23071958

Shirsand, SB; Suresh, Sarasija; Keshavshetti, GG; Swamy, PV; Reddy, P Vijay Prakash

2012-01-01

377

Evaluation of named binders in Rauwolfia vomitoria root tablets.  

PubMed

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

Onunkwo, G C

2000-01-01

378

WindWaveFloat Final Report  

SciTech Connect

Principle Power Inc. and National Renewable Energy Lab (NREL) have completed a contract to assess the technical and economic feasibility of integrating wave energy converters into the WindFloat, resulting in a new concept called the WindWaveFloat (WWF). The concentration of several devices on one platform could offer a potential for both economic and operational advantages. Wind and wave energy converters can share the electrical cable and power transfer equipment to transport the electricity to shore. Access to multiple generation devices could be simplified, resulting in cost saving at the operational level. Overall capital costs may also be reduced, provided that the design of the foundation can be adapted to multiple devices with minimum modifications. Finally, the WindWaveFloat confers the ability to increase energy production from individual floating support structures, potentially leading to a reduction in levelized energy costs, an increase in the overall capacity factor, and greater stability of the electrical power delivered to the grid. The research conducted under this grant investigated the integration of several wave energy device types into the WindFloat platform. Several of the resulting system designs demonstrated technical feasibility, but the size and design constraints of the wave energy converters (technical and economic) make the WindWaveFloat concept economically unfeasible at this time. Not enough additional generation could be produced to make the additional expense associated with wave energy conversion integration into the WindFloat worthwhile.

Alla Weinstein, Dominique Roddier, Kevin Banister

2012-03-30

379

Development of optimization program for single point mooring floating production system  

SciTech Connect

The Floating Production Systems (FPS) or the Floating, Storage and Offloading Systems (FPSO) have been applied to marginal oil fields or early production systems since late `70 in view of less capital and short delivery. There are two types of floating production systems: semi-submersible based spread mooring type and tanker-based single point mooring. This paper describes the analysis method, the technical development of optimization programs and the model experiments for the Single Point Mooring (SPM) systems for FPSO, which have been carried out as a joint research project by Japan National Oil Corporation, Akishima Laboratories Inc. and MODEC Inc. The detailed analysis program is developed based on the constraint matrix method in frequency and time domains and is capable of calculating the motions and constraint forces of SPM in wind, current and random waves. Outline of calculation method is presented.

Nakagawa, H.; Kanda, M. Mikami, T. [Mitsui Zosen, Inc., Akishima (Japan); Kamishohara, A. [MODEC, Inc., Tokyo (Japan). Dept. of Offshore Terminal and Floating Production; Kojima, T.; Yoshizawa, M. [Japan National Oil Corp., Chiba (Japan)

1995-12-31

380

The reality of in-line tablet coating.  

PubMed

The possibility of continuous processing in pharmaceutical tablet manufacturing is hampered by the viscoelastic recovery of tablets post-compaction. Compacted tablets are typically aged before coating to allow complete viscoelastic recovery so as to avoid subsequent coating defects. There has been little attempt to overcome tablet recovery in order to enable continuous processing and improve manufacturing efficiency. However, with the introduction of improved or newly developed types of tablet-coating equipment, there is renewed interest in the coating of tablets in-line. In-line tablet coating is defined as the coating of tablets immediately after compaction. It is a one-step highly integrated system that circumvents the delay in processing time typically given to allow viscoelastic recovery of tablets. This review aims to summarize the requirements of an in-line tablet-coating system. The possibility of carrying out in-line tablet coating in the near future will also be discussed. PMID:21649557

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

2013-02-01

381

Development of a prolonged-release gastroretentive tablet formulation of ciprofloxacin hydrochloride: pharmacokinetic characterization in healthy human volunteers.  

PubMed

The fluroquinolone anti-biotic ciprofloxacin is primarily dissolved and absorbed from the upper part of the GI tract. We, therefore, aimed to develop a prolonged release gastroretentive (GT) formulation of ciprofloxacin that could be administered once daily with a conventional tablet (CT). A variety of polymers and effervescent properties were utilized to optimize the desired disposition profile. Tablets were prepared by the direct compression technique and evaluated for physical properties, swelling, floating, and drug release. In vivo studies were also carried out on the optimized GT formulation and CT in healthy volunteers. A very sensitive and reliable HPLC method was developed to measure plasma concentration of ciprofloxacin. The duration of floating times were predominantly >24 h and floating lag times <20 s. The drug release mechanism followed zero order kinetics. C(max), T(max), and AUC(0-?) of GT vs CT were 0.945±0.29 vs 2.1±0.46 ?g/ml, 6.0±1.42 vs 1.42±0.59 h and 8.54±1.87 vs 9.45±2.12 ?g/ml/h, respectively. Pharmacokinetic parameters indicate that the developed GT formulation extended the pharmacokinetic profile achieved with CT. The C(max)/MIC and AUC(0-?)/MIC, which are indicative of eradication of pathogens, following co-administration of GT with CT were comparable to those of twice-daily administration of CT alone. PMID:21371548

Mostafavi, Abolfazl; Emami, Jaber; Varshosaz, Jaleh; Davies, Neal M; Rezazadeh, Mahboubeh

2011-05-16

382

Effect of hydrodynamic environment on tablet dissolution using flow-through dissolution apparatus.  

PubMed

The main objective of this research is to investigate the principles underlying the dissolution process, study the phenomena of drug release in laminar flow, and better understand the effect of hydrodynamic condition on drug dissolution, in order to predict drug dissolution from a solid dosage form. Two drug models were selected, theophylline (Class I) and naproxen (Class II), and were formulated into conventional tablets containing 105 mg theophylline or 300 mg naproxen using wet granulation method. Additionally theophylline (105 mg) and naproxen (300 mg) matrices containing 30% hydroxypropylmethylcellulose (HPMC) polymer were prepared by direct compression and tested for dissolution using both USP II and IV dissolution apparatus. Tablets were tested for dissolution (USP IV) using different cell diameter, flow rate, and different position of the tablet inside the cell. In general, the drug dissolution at a given time is a direct function of the flow rate, increasing the flow rate increases drug release. The use of a small cell resulted in faster drug dissolution and higher Reynold's Number than using a large cell. Tablet position in the cell, also has an effect on drug dissolution, inserting the tablet in a horizontal position inside the cell gave faster dissolution than a vertical position. The hydrodynamic conditions did not affect the drug dissolution from HPMC controlled release tablets indicating that the drug dissolution is controlled by the matrix. An equation to predict drug dissolution from conventional tablets was established: Sh=-21.36+10.58Re(1/2) where R2=0.98. This study demonstrated that hydrodynamic conditions, and type of dissolution testing apparatus used have an effect on dissolution rate, mass transfer rate, and film thickness underlying dissolution process. PMID:16883682

Wu, Yan; Ghaly, Evone S

2006-03-01

383

14 CFR 25.751 - Main float buoyancy.  

Code of Federal Regulations, 2012 CFR

...2012-01-01 2012-01-01 false Main float buoyancy. 25.751 Section 25.751 Aeronautics...Floats and Hulls § 25.751 Main float buoyancy. Each main float must have— (a) A buoyancy of 80 percent in excess of that...

2012-01-01

384

14 CFR 23.751 - Main float buoyancy.  

Code of Federal Regulations, 2011 CFR

... 2011-01-01 false Main float buoyancy. 23.751 Section 23.751 Aeronautics...Floats and Hulls § 23.751 Main float buoyancy. (a) Each main float must have— (1) A buoyancy of 80 percent in excess of the...

2011-01-01

385

14 CFR 29.751 - Main float buoyancy.  

Code of Federal Regulations, 2011 CFR

...2011-01-01 2011-01-01 false Main float buoyancy. 29.751 Section 29.751 Aeronautics...Floats and Hulls § 29.751 Main float buoyancy. (a) For main floats, the buoyancy necessary to support the maximum weight...

2011-01-01

386

14 CFR 25.751 - Main float buoyancy.  

Code of Federal Regulations, 2011 CFR

...2011-01-01 2011-01-01 false Main float buoyancy. 25.751 Section 25.751 Aeronautics...Floats and Hulls § 25.751 Main float buoyancy. Each main float must have— (a) A buoyancy of 80 percent in excess of that...

2011-01-01

387

14 CFR 27.751 - Main float buoyancy.  

Code of Federal Regulations, 2012 CFR

...2012-01-01 2012-01-01 false Main float buoyancy. 27.751 Section 27.751 Aeronautics...Floats and Hulls § 27.751 Main float buoyancy. (a) For main floats, the buoyancy necessary to support the maximum weight...

2012-01-01

388

14 CFR 27.751 - Main float buoyancy.  

Code of Federal Regulations, 2011 CFR

...2011-01-01 2011-01-01 false Main float buoyancy. 27.751 Section 27.751 Aeronautics...Floats and Hulls § 27.751 Main float buoyancy. (a) For main floats, the buoyancy necessary to support the maximum weight...

2011-01-01

389

14 CFR 23.751 - Main float buoyancy.  

Code of Federal Regulations, 2012 CFR

... 2012-01-01 false Main float buoyancy. 23.751 Section 23.751 Aeronautics...Floats and Hulls § 23.751 Main float buoyancy. (a) Each main float must have— (1) A buoyancy of 80 percent in excess of the...

2012-01-01

390

14 CFR 29.751 - Main float buoyancy.  

Code of Federal Regulations, 2012 CFR

...2012-01-01 2012-01-01 false Main float buoyancy. 29.751 Section 29.751 Aeronautics...Floats and Hulls § 29.751 Main float buoyancy. (a) For main floats, the buoyancy necessary to support the maximum weight...

2012-01-01

391

14 CFR 29.751 - Main float buoyancy.  

Code of Federal Regulations, 2010 CFR

...2010-01-01 2010-01-01 false Main float buoyancy. 29.751 Section 29.751 Aeronautics...Floats and Hulls § 29.751 Main float buoyancy. (a) For main floats, the buoyancy necessary to support the maximum weight...

2010-01-01

392

14 CFR 23.751 - Main float buoyancy.  

Code of Federal Regulations, 2010 CFR

... 2010-01-01 false Main float buoyancy. 23.751 Section 23.751 Aeronautics...Floats and Hulls § 23.751 Main float buoyancy. (a) Each main float must have— (1) A buoyancy of 80 percent in excess of the...

2010-01-01

393

14 CFR 25.751 - Main float buoyancy.  

Code of Federal Regulations, 2010 CFR

...2010-01-01 2010-01-01 false Main float buoyancy. 25.751 Section 25.751 Aeronautics...Floats and Hulls § 25.751 Main float buoyancy. Each main float must have— (a) A buoyancy of 80 percent in excess of that...

2010-01-01

394

14 CFR 27.751 - Main float buoyancy.  

Code of Federal Regulations, 2010 CFR

...2010-01-01 2010-01-01 false Main float buoyancy. 27.751 Section 27.751 Aeronautics...Floats and Hulls § 27.751 Main float buoyancy. (a) For main floats, the buoyancy necessary to support the maximum weight...

2010-01-01

395

14 CFR 25.751 - Main float buoyancy.  

Code of Federal Regulations, 2013 CFR

...2013-01-01 2013-01-01 false Main float buoyancy. 25.751 Section 25.751 Aeronautics...Floats and Hulls § 25.751 Main float buoyancy. Each main float must have— (a) A buoyancy of 80 percent in excess of that...

2013-01-01

396

14 CFR 27.751 - Main float buoyancy.  

Code of Federal Regulations, 2013 CFR

...2013-01-01 2013-01-01 false Main float buoyancy. 27.751 Section 27.751 Aeronautics...Floats and Hulls § 27.751 Main float buoyancy. (a) For main floats, the buoyancy necessary to support the maximum weight...

2013-01-01

397

14 CFR 29.751 - Main float buoyancy.  

Code of Federal Regulations, 2013 CFR

...2013-01-01 2013-01-01 false Main float buoyancy. 29.751 Section 29.751 Aeronautics...Floats and Hulls § 29.751 Main float buoyancy. (a) For main floats, the buoyancy necessary to support the maximum weight...

2013-01-01

398

14 CFR 23.751 - Main float buoyancy.  

Code of Federal Regulations, 2013 CFR

... 2013-01-01 false Main float buoyancy. 23.751 Section 23.751 Aeronautics...Floats and Hulls § 23.751 Main float buoyancy. (a) Each main float must have— (1) A buoyancy of 80 percent in excess of the...

2013-01-01

399

14 CFR 25.751 - Main float buoyancy.  

...2014-01-01 2014-01-01 false Main float buoyancy. 25.751 Section 25.751 Aeronautics...Floats and Hulls § 25.751 Main float buoyancy. Each main float must have— (a) A buoyancy of 80 percent in excess of that...

2014-01-01

400

Program Converts VAX Floating-Point Data To UNIX  

NASA Technical Reports Server (NTRS)

VAX Floating Point to Host Floating Point Conversion (VAXFC) software converts non-ASCII files to unformatted floating-point representation of UNIX machine. This is done by reading bytes bit by bit, converting them to floating-point numbers, then writing results to another file. Useful when data files created by VAX computer must be used on other machines. Written in C language.

Alves, Marcos; Chapman, Bruce; Chu, Eugene

1996-01-01

401

Tablet PCs: A Physical Educator's New Clipboard  

ERIC Educational Resources Information Center

Computers in education have come a long way from the abacus of 5,000 years ago to the desktop and laptop computers of today. Computers have transformed the educational environment, and with each new iteration of smaller and more powerful machines come additional advantages for teaching practices. The Tablet PC is one. Tablet PCs are fully…

Nye, Susan B.

2010-01-01

402

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

403

Inulin-based tablet in capsule device for variable multipulse delivery of aceclofenac: optimization and in vivo roentgenography.  

PubMed

The aim of the study was to develop single-unit tablet in capsule system of aceclofenac for the treatment of late night pain and morning stiffness associated with rheumatoid arthritis. The system was conceptualized as a three-component design (1) a hard gelatin enteric-coated capsule (for carrying two pulses), (2) first-pulse granules (for rapid release in intestine), and (2) second-pulse matrix tablet (for slow release in colon). An appropriate integration of pH-sensitive (Eudragit S100) and bacteria-responsive (inulin) functions, on the basis of 3(2) factorial design, led to formulation of TICS 1-9 that were screened for in vitro release. TICS 2 with biphasic drug release of 98.64% from first-pulse granules in simulated intestinal fluid (12 h) and 97.82% from second-pulse matrix tablet in simulated colonic fluid (24 h) was the optimized formulation that exhibited Fickian diffusion of drug (n=0.363). In vivo fluoroscopy in rats traced the intact tablet to colon in 7.5 h that got eroded at the tenth hour. This demonstrated the colon-specific delivery of the matrix tablet affirming the potential of the system to obviate the need for two-time administration of drug at odd hours. The experimental design was validated by extra design check point, and diffuse reflectance spectroscopy and DSC revealed absence of chemical interaction between the formulation excipients. PMID:23615771

Sharma, Puja; Pathak, Kamla

2013-06-01

404

The development and in vitro evaluation of sustained release tablet formulations of benzydamine hydrochloride and its determination.  

PubMed

A novel oral controlled delivery system for benzydamine hydrochloride (BN) was developed and optimized. Hydrophilic matrix tablets of B