Characterization and Evaluation of the Release Kinetics of a Model Poorly Water-Soluble and Low Dose Drug from Matrix Tablets Composed of Blends of Swellable and Erodible Polymers: Implications for Controlled and Complete Release

Author(s):  
Aiman A. Obaidat
2011 ◽  
Vol 2011 ◽  
pp. 1-10 ◽  
Author(s):  
Stephan Loew ◽  
Alfred Fahr ◽  
Sylvio May

Liposomes are frequently used as pharmaceutical nanocarriers to deliver poorly water-soluble drugs such as temoporfin, cyclosporine A, amphotericin B, and paclitaxel to their target site. Optimal drug delivery depends on understanding the release kinetics of the drug molecules from the host liposomes during the journey to the target site and at the target site. Transfer of drugs in model systems consisting of donor liposomes and acceptor liposomes is known from experimental work to typically exhibit a first-order kinetics with a simple exponential behavior. In some cases, a fast component in the initial transfer is present, in other cases the transfer is sigmoidal. We present and analyze a theoretical model for the transfer that accounts for two physical mechanisms, collisions between liposomes and diffusion of the drug molecules through the aqueous phase. Starting with the detailed distribution of drug molecules among the individual liposomes, we specify the conditions that lead to an apparent first-order kinetic behavior. We also discuss possible implications on the transfer kinetics of (1) high drug loading of donor liposomes, (2) attractive interactions between drug molecules within the liposomes, and (3) slow transfer of drugs between the inner and outer leaflets of the liposomes.


2006 ◽  
Vol 72 (12) ◽  
pp. 7531-7539 ◽  
Author(s):  
A. K. Guber ◽  
D. R. Shelton ◽  
Y. A. Pachepsky ◽  
A. M. Sadeghi ◽  
L. J. Sikora

ABSTRACT Modeling release of fecal coliforms is an important component of fate and transport simulations related to environmental water quality. Manure constituents other than fecal coliforms may serve as natural tracers of fecal contamination provided that their release from manure to runoff is similar to the fecal coliform release. The objectives of this work were to compare release of fecal coliforms (FC), chloride (Cl−), organic carbon (OC), and water-soluble phosphorus (P) from dissolving manure and to assess the performance of three models in describing the observed release. Bovine manure was applied on 0.5- by 0.3-m bare and vegetated subplots with 20% slope on sandy loam and clay loam soils. Concentrations of Cl−, FC, OC, and P were measured in runoff collected from troughs at the edges of the subplots at 5-min intervals during 1-h rainfall simulations. The one-parametric exponential model and two-parametric Vadas-Kleinman-Sharpley model and Bradford-Schijven model were fitted to the data. The Bradford-Schijven model had uncorrelated parameters, one of which was linearly related to the irrigation rate, and another parameter reflected the presence or the absence of vegetation. Kinetics of the FC release from manure was similar to the release kinetics of P and OC. The Bradford-Schijven model is recommended to simulate the release of manure constituents.


Author(s):  
Ali Asgar Dabeer ◽  
Dinesh Kumar Mishra ◽  
Nadeem Farooqui ◽  
Arpit Gawshinde

In the recent years scientific and technological advancements have been made in the research and development of oral drug delivery systems. The aim of this study was to formulate and evaluate of orodispersible tablets by direct compression for fenofibrate by using super fast disintegrating agents like croscarmellose sodium. The use of super disintegrant and excipient for preparation of fast disintegrating is highly effective and commercially feasible. In the present investigation poorly water soluble drug is one of the most important parameters of oral formulations sucessfully developed fenofibrate was using solvent evaporation method drug: PEG 6000 in (1:5 w/w). The formulation F7 was the optimized formula that showed satisfactory results with various physicochemical evaluation parameters like thickness, hardness, weight variation, friability, drug content, % drug release almost 79.98% within 15 min. and it was follow the maximum higuchi release kinetics that regression coefficient values ‘r2’= 0.995.


2016 ◽  
Vol 52 (4) ◽  
pp. 751-759 ◽  
Author(s):  
Wendy Leticia Guerra-Ponce ◽  
Sandra Leticia Gracia-Vásquez ◽  
Patricia González-Barranco ◽  
Ivonne Antonieta Camacho-Mora ◽  
Yolanda Araceli Gracia-Vásquez ◽  
...  

2002 ◽  
Vol 70 (2) ◽  
pp. 189-198
Author(s):  
Genç Lütfi ◽  
Hegazy Nahed ◽  
Arica Betül

Matrix tablets of ketorolac trometharnine (KT) were prepared by direct compression technique and Carbopol 934, 940 and 1342 have been used as polymers in different concentrations (5-15 % ). For the quality control of tablets; physical tests as crushing strength, diameter-height ratio and fkiability, KT amount assay and in vitro dissolution techniques were performed and dissolution profiles were plotted and evaluated kinetically. The in vitro release kinetics of ten different formulations of KT matrix tablet were studied at pH 1.2 and pH 7.0 using the USP dissolution technique and apparatus with basket assembly. Dissolution results were evaluated kinetically and statistically. According to our results, different types and concentrations of carbopol to tablet formulations may effect in controlled drug release.


2013 ◽  
Vol 746 ◽  
pp. 330-336
Author(s):  
Mont Kumpugdee-Vollrath ◽  
Mario Helmis

The aim of this research work was to develop the controlled release of two model drugs i.e. water insoluble drug - resveratrol and water soluble drug - lignan by matrix tableting with an eccentric tablet machine. For this purpose different kinds of polymers i.e. Metolose 90 SH-4000® (HMPC), Fetocel RT-N-100® (EC) and Eudragit RLPO® (polymethacrylate) were used. The matrix tablets containing 2 %wt of a model drug which were mixed with 5, 10, 20, 30 and 50 %wt of the polymers mentioned above. In addition, a glidant composed of 1 %wt talc and 1 %wt magnesium stearate as well as a filler Ludipress® were processed. Different physical properties of the powder mixtures (e.g. flowability) and of the tablets (e.g. hardness, uniformity of mass or drug content, drug release, etc.) were determined. Most of the tablets met the physical requirements. If the polymer content got higher the release was slower, which can be confirmed by the lower values of k. The release kinetics were described by three typical mathematic models i.e. biphasic, Noyes-Whitney and KorsmeyerPeppas. The best fitting results were ordered as follows: biphasic > Noyes-Witney > KorsmeyerPeppas.


2009 ◽  
Vol 12 (2) ◽  
pp. 261-277 ◽  
Author(s):  
Boris Baeumer ◽  
◽  
Lipika Chatterjee ◽  
Peter Hinow ◽  
Thomas Rades ◽  
...  

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