Modeling drug release from PVAc/PVP matrix tablets

Siepmann, Florence; Eckart, K.; Maschke, Angelika; Kolter, Karl; Siepmann, Juergen

doi:10.1016/j.jconrel.2009.08.027

Cited by 63 publications

(40 citation statements)

References 19 publications

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“…11,12 For the present study, a computational fluid dynamic (CFD) based model was developed to quantitatively describe the drug transport in the matrix of the capsule and the drug release process. The following assumptions were made:…”

Section: Mathematical Modelingmentioning

confidence: 99%

Fatty Acid and Water-Soluble Polymer-Based Controlled Release Drug Delivery System

Desai

Kothari

Chen

et al. 2011

Journal of Pharmaceutical Sciences

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Section: Mathematical Modelingmentioning

confidence: 99%

Fatty Acid and Water-Soluble Polymer-Based Controlled Release Drug Delivery System

Desai

Kothari

Chen

et al. 2011

Journal of Pharmaceutical Sciences

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“…Several mathematical models have been proposed to characterize the drug release (10,11). For the present study, a CFD-based model was developed to quantitatively describe the drug transport in the matrix of the tablet and the drug release process.…”

Section: Resultsmentioning

confidence: 99%

Mathematical Model-Based Accelerated Development of Extended-release Metformin Hydrochloride Tablet Formulation

Chen

Desai²,

Good³

et al. 2015

AAPS PharmSciTech

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Abstract. A computational fluid dynamic (CFD) model was developed to predict metformin release from a hydroxypropylmethylcellulose (HPMC) matrix-based extended-release formulation that took into consideration the physical and chemical properties of the drug substance, composition, as well as size and shape of the tablet. New high dose strength (1000 mg) tablet geometry was selected based on the surface area/volume (SA/V) approach advocated by Lapidus/Lordi/Reynold to obtain the desired equivalent metformin release kinetics. Maintaining a similar SA/V ratio across all extended-release metformin hydrochloride (Met XR) tablet strengths that had different geometries provided similar simulations of dissolution behavior. Experimental dissolution profiles of three lots of high-strength tablets agreed with the simulated release kinetics. Additionally, a pharmacokinetic absorption model was developed using GastroPlus™ software and known physicochemical, pharmacokinetic, and in vitro dissolution properties of metformin to predict the clinical exposure of the new high strength (1000 mg) tablet prior to conducting a human clinical bioequivalence study. In vitro metformin release kinetics were utilized in the absorption model to predict exposures in humans for new 1000-mg Met XR tablets, and the absorption model correctly projected equivalent in vivo exposure across all dose strengths. A clinical bioequivalence study was pursued based on the combined modeling results and demonstrated equivalent exposure as predicted by the simulations.

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“…This effect might be assigned to the fact that KSR delayed the disintegration of tablets by virtue of their lower porosity of the matrices. [44][45][46] It was evident that KSR gave remarkable effect on the increase in D.T. of the prepared tablets accompanied with the increase in KSR concentration.…”

Section: Physical Characteristics Of At Matrix Tabletsmentioning

confidence: 99%

“…These findings were in agreement with other investigators. 44,46,52) Stability of AT Matrix Tablet Formulations Two formulae namely; F4 and F12 were selected for the stability study owing to their excellent flow characteristic and best release profile. They were subjected to the stability study by storing them for three months at two different temperatures and humidity; 30±1°C/atmospheric RH and 40±1°C/75% RH.…”

Section: 12)mentioning

confidence: 99%

Potential Use of Polyvinyl Acetate–Polyvinylpyrrolidone Mixture for the Development of Atenolol Sustained Release Matrix Tablets: Optimization of Formulation through <i>in Vitro</i>–<i>in Vivo</i> Assessment Study

2017

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The objective of this study was to develop sustained release matrix tablets of atenolol (AT) using different concentrations of polyvinyl acetate-polyvinylpyrrolidone mixture (KSR) (20, 30, or 40%) with various types of fillers such as spray dried lactose (SP.D.L), avicel pH 101 (AV), and emcompress (EMS). The physical characteristics of the prepared tablets were evaluated. Characterization of the optimized formulation was performed using Fourier transform (FT)-IR spectroscopy and differential scanning calorimetry (DSC). Moreover, the in vitro release profiles of AT formulations were investigated in different pH dissolution media. Drug release kinetics and mechanisms were also determined. The results revealed that there was no potential incompatibility of the drug with the polymer. The release profiles of AT were affected by the concentration of KSR, fillers used, and pH of the dissolution media. The drug release kinetic from most of the formulations obeyed Higuchi diffusion model. The selected formulae were investigated for their stability by storage at 30 and 40°C with atmospheric humidity and 75% relative humidity (RH), respectively. The results demonstrated that no change in the physicochemical properties of the tablets stored at 30°C/atmospheric RH in comparison with some changes at 40°C/75% RH. Finally, the in vivo study provided an evidence that the optimized AT tablet containing 40% KSR and SP.D.L exhibited prominent higher oral bioavailability and more efficient sustained-release effect than the drug alone or the commercial tablet product. It is noteworthy that KSR could be considered as a promising useful release retardant for the production of AT sustained release matrix tablets.Key words polyvinyl acetate-polyvinylpyrrolidone mixture; atenolol; sustained; tablet; stability; bioavailability Atenolol (AT) is a selective β1 receptor blocker that decreases blood pressure primarily by reducing cardiac output. It may also reduce sympathetic outflow from the central nervous system (CNS) and prevent the release of renal renin, thus reducing angiotensin II formation and aldosterone secretion. 1)About 50% of an oral dose of AT is absorbed. Peak plasma concentrations are reached in 2 to 4 h. The plasma half-life is about 6 to 7 h. AT has little or no hepatic metabolism and the renal system is considered the main site of its excretion. 2)Administration of conventional tablets of AT has been reported to show fluctuations in the plasma drug concentration leading to the increase in its side effects or decrease in its concentration at receptor site. [3][4][5] To overcome such problems, sustained release matrix tablets containing AT were developed in order to maintain proper blood level for a long time without fluctuation. [6][7][8]

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Modeling drug release from PVAc/PVP matrix tablets

Cited by 63 publications

References 19 publications

Fatty Acid and Water-Soluble Polymer-Based Controlled Release Drug Delivery System

Fatty Acid and Water-Soluble Polymer-Based Controlled Release Drug Delivery System

Mathematical Model-Based Accelerated Development of Extended-release Metformin Hydrochloride Tablet Formulation

Potential Use of Polyvinyl Acetate–Polyvinylpyrrolidone Mixture for the Development of Atenolol Sustained Release Matrix Tablets: Optimization of Formulation through <i>in Vitro</i>–<i>in Vivo</i> Assessment Study

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