Assessment of Once Daily Sustained Release Hydrophilic Matrix Tablet of Carvedilol

Abstract

ABSTRACT:The objective of the present study was to design and evaluate once daily sustained release tablet of carvedilol, using two molecular weight grades of hydrophilic polymers (methocel ® K4M CR and methocel ® K15M CR) as release retarding materials. Two sets of formulations were prepared, where first set of four formulations (F1-F4) contained variable ratios of methocel ® K4M CR and methocel ® K15M CR (15% : 15%, 15% : 13%, 15% : 11%and 15% : 9%) to optimize the composition of polymers in the tablet matrices such that the drug and polymer interaction was sufficient for sustaining release up to 24 hours and second set of five formulations (F5-F9) contained variable percentages of sodium lauryl sulfate (SLS) (1.0, 1.25, 1.5, 1.75 and 2.0%) to enhance the dissolution rate of the drug from the tablet matrices because of its poor aqueous solubility. The tablets were prepared by direct compression method and evaluated for hardness, thickness, friability, weight variation and in vitro drug release. The in vitro dissolution studies were carried out in simulated gastric fluid (900 ml, pH 1.2) for 24 hours using USP type II apparatus operated at 100 rpm and 37 ± 0.05°C. The release profiles were explored and explained by zero order, first order, Higuchi, Korsmeyer-Peppas and Hixson-Crowell models. From this study, the drug release profiles for formulations F6 to F9 were found to be satisfactory and the release mechanism followed both diffusion and erosion.Due to lower percentage of SLS used, F6 was considered as the best formulation.

Use of Self-Assembled Colloidal Prodrug Nanoparticles for Controlled Drug Delivery of Anticancer, Antifibrotic and Antibacterial Mitomycin

“…According to Table S1 , drug release data for all the conjugated forms were fitted with the Korsmeyer–Peppas model. Based on an “n” value (diffusional exponent) ranging between 0.43 and 0.85, which correlates to an anomalous transport (non-Fickian), the drug release mechanism was dependent on both diffusion and erosion-controlled mechanisms [ 38 , 39 , 40 , 41 ].…”

“…The in vitro drug release experiments were performed for 7 days under physiological conditions (PBS, pH = 7.4) that indicated the drug-releasing process can be adjusted by variation of the cross-linking density. PVA-SA-CYS-MMC (21%) was the slowest one with maximum drug release of 33.1% compared to 62.2% for PVA-SA-CYS-MMC (3%) ( Figure 6 ), and all MMC release data for polymeric prodrugs were fitted with the Korsmeyer–Peppas model ( Table S1 ) [ 36 ] where the drug-releasing mechanism depended on both diffusion- and erosion-controlled mechanisms [ 38 , 39 , 40 , 41 ]. This means the hydrolysis reaction of the conjugated form first, followed by diffusion of the Mitomycin drug.…”

Formulation Development and Statistical Optimization of a Bilayer Tablet of Bosentan Monohydrate and Sildenafil Citrate in Management of Pulmonary Arterial Hypertension

“…The volume of medium used was 900 ml and the temperature was 37±0.5 °C. The time taken for complete disintegration of the IR layer was measured [9][10][11].…”

“…Table 2 shows the variables and their concentrations according to the design expert software trial version 11. Both the immediate and sustained release blends were evaluated for precompression parameters such as bulk density, tapped density, angle of repose and carr's compressibility index [9,10].…”

Development of Drug Customized Polymeric Carriers for Improved Therapeutic Efficiency

“…Table 2 shows that the Korsmeyer-Peppas model fits with the drug release data for all conjugated forms. The mechanism of drug release was based on both diffusion and erosion-controlled processes, according to an "n" value ranging from 0.43 to 0.85, which relates to a non-Fickian (anomalous) transport [247,248]. In other words, the conjugated form's hydrolysis process occurs first, followed by the diffusion of MMC.…”