Reza-ul Jalil

Formulation and in vitro Evaluation of Alfuzosin Extended Release Tablets Using Directly Compressible Eudragit

The aim of the present study was the determination of formulation factors and the in vitro evaluation of an extended release dosage form of a freely soluble weakly basic drug (alfuzosin hydrochloride). Binary mixer of one hydrophilic polymer (hydroxypropylmethylcellulose) and one directly compressible Eudragit (RS PO) was used in tablets prepared by direct compression. The amounts of both polymers were taken as independent variables for the 32 Factorial design. The percent drug releases at 1, 6, 12 and 20 h were selected as responses. The main effect and interaction terms were quantitatively evaluated using mathematical model. Dissolution data were fitted to zero order, first order, and Higuchis release kinetics to evaluate kinetic data. Both the diffusion and erosion mechanisms were responsible for drug release as shown by the power law. The release of Alfuzosin was prolonged for 20 h by binary mixer indicating the usefulness of the formulations for once daily dosage forms.

Systematic development of self-emulsifying drug delivery systems of atorvastatin with improved bioavailability potential.

The aim of this study was to prepare and characterize a self-emulsifying drug delivery system (SEDDS) with a high drug load of poorly water-soluble atorvastatin for the enhancement of dissolution and oral bioavailability. Solubility of atorvastatin in oil, surfactant, and cosurfactant was determined. Pseudo-ternary phase diagrams were constructed by the aqueous titration method, and formulations were developed based on the optimum excipient combinations. A high drug load (10% w/w) was achieved with a combination of oleic acid, Tween 80, and polyethylene glycol 400, ensuring the maximum dissolution property (in the case of SES6). Effects of lipids and surfactants on physical properties of SEDDS such as in vitro emulsification efficiency in terms of self-emulsification time, emulsion droplet size, and percent transmittance were measured. Multiple regression analysis revealed that a higher amount of surfactants significantly increased dissolution of ATV while decreasing emulsion droplet size and emulsification time. About a four-fold increase in dissolution was achieved by SEDDS compared to pure ATV powder. Overall, this study suggests that dissolution and oral bioavailability of ATV could be improved by SEDDS technology.

Formulation and Evaluation of Release Kinetics of Diltiazem Hydrochloride from Kollicoat SR 30 D Coated Pellets Prepared by Air Suspension Technique

The purpose of the present study is to investigate the effect of polyvinyl acetate on the release kinetics of diltiazem hydrochloride from coated pellets prepared by solution and suspension layering technique. Kollicoat SR 30 D, an aqueous dispersion of polyvinyl acetate with different weight ratios was chosen to sustain the release of the drug. Drug was loaded with hydroxypropyl methyl cellulose on nonpareil seeds then coated with the Kollicoat SR 30 D. In vitro dissolution studies were carried out using USP dissolution apparatus Type-2. No significant difference was found in drug release from uncoated pellets and the pellets coated with 5% polymer load. With 10% polymer load, the initial release was minimized but from 2nd hour the release was quick-tempered. Better sustaining effect was found from 1520% polymer loaded pellets. The mean dissolution time was 2.5h and 4h while the polymer load was 15% and 20% respectively. Also these two cases 80% drug was released at 6h and 9h respectively. The physical parameters of the prepared pellets were also compared in this study. The release of drug from the coated pellets appeared to follow Higuchi’s release kinetics.