Controlled Release of Resveratrol and Lignan by Matrix Tableting

2013 ◽  
Vol 746 ◽  
pp. 330-336
Author(s):  
Mont Kumpugdee-Vollrath ◽  
Mario Helmis
Keyword(s):  
Controlled Release ◽  
Release Kinetics ◽  
Research Work ◽  
Magnesium Stearate ◽  
Water Soluble ◽  
Matrix Tablets ◽  
Water Soluble Drug ◽  
The Matrix ◽  
Best Fitting ◽  
Model Drug

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.

scholarly journals Nanoencapsulation of Nimodipine in Novel Biocompatible Poly(propylene-co-butylene succinate) Aliphatic Copolyesters for Sustained Release

2009 ◽  
Vol 2009 ◽  
pp. 1-11 ◽  
Author(s):  
Sofia Papadimitriou ◽  
George Z. Papageorgiou ◽  
Feras I. Kanaze ◽  
Manolis Georgarakis ◽  
Dimitrios N. Bikiaris
Keyword(s):  
Chemical Interaction ◽  
Spherical Shape ◽  
Water Soluble ◽  
Degree Of Crystallinity ◽  
Butylene Succinate ◽  
Melt Polycondensation ◽  
Water Soluble Drug ◽  
The Matrix ◽  
Model Drug ◽  
Poly Propylene

Biocompatible poly(propylene-co-butylene succinate) (PPBSu) copolyesters, containing up to 50 mol% butylene succinate units, were synthesized by the two-stage melt polycondensation method (esterification and polycondensation). The copolymers were fully characterized and biocompatibility studies were also performed. They were proved to be biocompatible and they were used as polymer matrices for the preparation of drug loaded nanoparticles. Nimodipine was selected as a model hydrophobic poorly water soluble drug. From the results obtained by dynamic light scattering (DLS) and scanning electron microscopy (SEM), drug loaded copolymer nanoparticles were found to exhibit a spherical shape and their mean diameter appeared in the range of 180–200 nm. Fourier Transformation-Infrared Spectroscopy (FTIR) spectra indicated that no chemical interaction between the drug and the matrix could be justified, while Wide-Angle X-Ray Diffraction (WAXD) patterns proved a low degree of crystallinity of Nimodipine in the nanoparticles. The release behavior of the model drug from nanoparticles was also investigated in order to identify modifications and find out any possible correlation between the chemical composition of the polymer matrix and the drug release rates.

scholarly journals FORMULATION DEVELOPMENT AND EVALUATION OF HIGHLY WATER-SOLUBLE DRUG-LOADED CONTROLLED RELEASE MATRIX TABLETS

2021 ◽  
Vol 44 (1) ◽  
pp. 15-29
Author(s):  
Aqsa Siraj ◽  
Muhammad Nasiri ◽  
Syed Naqvi ◽  
Tariq Ali ◽  
Rabia Yousaf ◽  
...  
Keyword(s):  
Controlled Release ◽  
Water Soluble ◽  
Matrix Tablets ◽  
Formulation Development ◽  
Water Soluble Drug

scholarly journals Novel application of mixed solvency concept in the development of oral liquisolid system of a poorly soluble drug, cefixime and its evaluation

2018 ◽  
Vol 8 (6-s) ◽  
pp. 5-8 ◽  
Author(s):  
Rinshi Agrawal ◽  
RK Maheshwari
Keyword(s):  
Drug Loading ◽  
Research Work ◽  
Water Soluble ◽  
Dsc Studies ◽  
Water Soluble Drug ◽  
Poorly Soluble ◽  
Poorly Water Soluble ◽  
Poorly Soluble Drug ◽  
Model Drug ◽  
Poorly Water Soluble Drug

Application of mixed solvency has been employed in the present research work to develop a liquisolid system (Powder formulation) of poorly water soluble drug, cefixime (as model drug). Material and Methods: For poorly water soluble drug cefixime, combination of solubilizers such as sodium acetate, sodium caprylate and propylene glycol as mixed solvent systems were used to decrease the overall concentration of solubilizers required to produce substantial increase in solubility and thereby resulting in enhanced drug loading capacity of cefixime. The procured sample of cefixime was characterized by melting point, IR, UV and DSC studies. Stability studies of liquisolid system of cefixime were performed for two months at room temperature, 30˚C and 40˚C. All the formulations were physically, chemically, and microbiologically stable. Conclusion: Mixed solvency concept has been successfully employed for enhancing the drug loading of poorly water soluble drug, cefixime. Keywords: Solubility, cefixime, liquisolid system, mixed solvency concept.

scholarly journals PHARMACOKINETIC STUDY OF MATRIX MEMBRANE MODERATED TRANSDERMAL SYSTEM OF BOSENTAN MONOHYDRATE

2017 ◽  
Vol 10 (9) ◽  
pp. 255
Author(s):  
Revathi Mannam ◽  
Indira Muzib Yallamalli
Keyword(s):  
Controlled Release ◽  
High Performance ◽  
Release Kinetics ◽  
Research Work ◽  
Fold Increase ◽  
Oral Route ◽  
Fickian Diffusion ◽  
Pharmacokinetic Studies ◽  
The Matrix

Objective: The objective of the present research work is to carry out the pharmacokinetic studies of optimized matrix membrane moderatedtransdermal patch of bosentan monohydrate.Materials and Methods: The matrix membrane moderated transdermal system was formulated using HPMC, HPMC K4M and E RLPO. In vitrodiffusion studies were carried out using modified Franz diffusion cell and for the optimized transdermal patch, pharmacokinetic studies were carriedout using New Zealand male rabbits. Plasma samples were quantified using high-performance liquid chromatography.Results: The in vitro diffusion studies revealed that formulation F3 with HPMC K4M and E RLPO had controlled release up to 28 hrs, and a maximumof 95.02±2.68% drug was released. The release kinetics followed mixed order non-Fickian diffusion. The pharmacokinetic studies of the optimizedpatch revealed controlled release up to 45 hrs where a 2.2-fold increase in area under curve (AUC) and 3.8 times increase in mean residence time(MRT) were observed compared to oral route. The results were appeared to be significant at p≤0.05. The variation in half-life was found to be notstatistically significant when compared between oral and transdermal routes.Conclusion: The pharmacokinetic results concluded that the matrix membrane moderated transdermal system with extended AUC and MRT canenhance the bioavailability of bosentan monohydrate by minimizing the drug-related side effects in oral route.

scholarly journals Swelling and Erosion Modulation of Sterculia Foetida Gum Through Real Time Texture Probing

1970 ◽  
Vol 7 (2) ◽  
pp. 127-132 ◽  
Author(s):  
Bendgude Namdeo ◽  
Iyer Vidya ◽  
Poddar Sushilkumar
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Real Time ◽  
Microcrystalline Cellulose ◽  
Release Profile ◽  
Water Soluble ◽  
Matrix Tablets ◽  
Diltiazem Hydrochloride ◽  
Drug Release Profile ◽  
Water Soluble Drug

In the present investigation an attempt has been made to increase therapeutic efficacy, reduce frequency of administration and improve patient compliance by developing controlled release matrix tablets of diltiazem hydrochloride. Diltiazem hydrochloride was formulated as oral controlled release matrix tablets by using sterculia foetida gum. SFG fines were characterized with scanning electron microscopy. The purpose of this study was to optimize release profile of the highly water soluble drug from SFG matrix by using water soluble and swellable excipients like lactose and microcrystalline cellulose respectively. Tablets were prepared by direct compression, and their swelling behavior in presence of these excipients was assessed with the help of a Texture Analyzer. Dissolution assessment was performed using USP 26 apparatus 2 modified by insertion of a mesh to prevent sticking of the tablets to the bottom of vessel and allow them to swell three dimensionally. The interdependence of swelling front movement in relation to excipients type and progression of drug release are explained. It was concluded that unlike in conventional dosage forms insertion of excipients in hydrophilic controlled release tablets containing a water soluble drug gave the finger print information of drug release profile. In vitro drug release from these matrices was characterized and confirmed with the help of real time texture probing. Results indicated that it is possible to achieve desired modulation in the drug release profile by inclusion of lactose and microcrystalline cellulose. Key words: Diltiazem HCl, Sterculia Foetida Gum, Swelling and erosion, Lactose, Texture analysis. doi: 10.3329/dujps.v7i2.2167 Dhaka Univ. J. Pharm. Sci. 7(2): 127-132, 2008 (December)

scholarly journals Comparative Evaluation of HPMC, PVA and Gelatin as Matrices for Controlled Release Drug Delivery

1970 ◽  
Vol 2 (1) ◽  
pp. 51-55
Author(s):  
Mohammad Anwarul Basher ◽  
Abul Kalam Lutful Kabir ◽  
Mohammad Musarraf Hussain ◽  
Mir Mohammad Abdullah Al Mamun
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Diclofenac Sodium ◽  
Magnesium Stearate ◽  
Matrix Tablets ◽  
Matrix Tablet ◽  
Pharmaceutical Sciences ◽  
Drug Release Profile ◽  
Compression Process ◽  
Model Drug

The present study was undertaken to compare three different polymeric gums- HPMC, PVA and gelatin as controlled release matrices. Diclofenac sodium, a potent analgesic, was used as the model drug. Different ratio of HPMC, PVA and gelatin were incorporated into the lactose loaded Diclofenac tablet to explore their impact on drug release. Matrix tablets of Diclofenac were prepared by using individual polymer with magnesium stearate and aerosil by direct compression process at 5 ton pressure. The release of drug from these matrices was studied over 2 hrs in acidic media where insignificant release was observed. Then, the same formulations were studied over 8 hours in buffer media of pH 6.8 at a temperature of 37± 0.5°C. Statistically significant differences in drug release profile was found among the tablets prepared from different matrices. The study revealed that the average % release of drug from different types of polymer loaded matrix tablet varied with the ratio of different polymers. Among the three polymers, PVA showed best dissolution pattern. A comparison of Higuchi curve and bi-exponential curve was also performed. Key words: HPMC; PVA; Gelatin; Controlled release; Diclofenac DOI: 10.3329/sjps.v2i1.5816Stamford Journal of Pharmaceutical Sciences Vol.2(1) 2009: 51-55

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