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Journal ArticleDOI

Investigation of drug release from solids*. I. Some factors influencing the dissolution rate

TL;DR: The velocity constant for the conditons employed in the procedure and the dissolution rate of compressed benzoic acid tablets were determined and it was found that when neutral ionic and nonionic organic compounds were employed as additives the dissolved rate was linearly dependent upon the solubility of benzosic acid in the particular solvent system.
Abstract: A method for determining the dissolution rate and the underlying physical‐chemical theories are presented. The velocity constant for the conditons employed in the procedure and the dissolution rate of compressed benzoic acid tablets were determined. In the density range investigated the dissolution rate was essentially independent of the tablet density. When neutral ionic and nonionic organic compounds were employed as additives the dissolution rate was linearly dependent upon the solubility of benzoic acid in the particular solvent system.
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TL;DR: The re-interpreted, in terms of the heterogeneity of the reaction and/or diffusion space topology, the conventional Eq.
Abstract: release. We re-interpreted, in terms of the heterogeneity of the reaction and/or diffusion space topology, the conventional Eq. 3 has a classical exponential form concaving downwards parameters of the current models using experimental data from throughout the time course of the process approaching the in vitro studies. Data from in vivo studies indicate that a time plateau level Cs /V asymptotically. Although Eq. 3 has been dependent rate coefficient governing dissolution kinetics oper- used widely, it has been proven inadequate in modeling either ates in the gastrointestinal (GI) tract too. These observations S-shaped experimental data or data with a steeper initial slope. provide a physically based interpretation for one of the major Therefore, a more general function, based on the Weibull distrisources of high variability of the sparingly soluble drugs and bution (12), was proposed (5) and applied (5,13) empirically imply the need to reconsider the current as well as the proposed but successfully in all types of dissolution curves: changes for the assessment of bioequivalence studies for spar

84 citations


Cites background from "Investigation of drug release from ..."

  • ...995 26 Carbamazepineg Suspension — Human (1) 20....

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  • ...dt 5 K(Cs 2 C ) (1) M 5 K1t (6) where K1 is a kinetic constant characteristic of the drug/polymer Later on, Eq....

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Journal ArticleDOI
TL;DR: Characterisation techniques included X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, thermomicroscopy, Karl Fischer titration, FT-IR spectroscopy and elemental analysis, and reasonable correlation was found between the free base melting point and the salt melting point.

79 citations

Journal ArticleDOI
TL;DR: In this paper, the dissolution of diclofenac sodium from Voltaren SR and hydroxypropylmethylcellulose (HPMC) based matrix tablets was studied in a medium which simulates the changing pH of the pathway followed by the drug as it passes from the stomach to the intestine.

60 citations

References
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Journal ArticleDOI
TL;DR: In this paper, the effect of the concentration on the rate at which a solid substance dissolves in its own solution, has not heretofore been investigated, probably due to the experimental difficulties in the way of keeping the surface of the dissolving substance constant during the solution.
Abstract: As far as we know, the effect of the concentration on the rate at which a solid substance dissolves in its own solution, has not heretofore been investigated. This is probably due to the experimental difficulties in the way of keeping the surface of the dissolving substance constant during the solution.

1,653 citations

Journal ArticleDOI
TL;DR: Eleven Mannich bases derived from 5‐nitro‐2‐acetylfuran and 5-nitro-2‐furfuralacetone have been prepared using various dialkyl and heterocyclic secondary amines to be screened for possible pharmacodynamic activity.
Abstract: Eleven Mannich bases derived from 5‐nitro‐2‐acetylfuran and 5‐nitro‐2‐furfuralacetone have been prepared using various dialkyl and heterocyclic secondary amines. These β‐aminoketones are to be screened for possible pharmacodynamic activity.

9 citations