Chana R. Kowarski

Preparation and Evaluation of Eudragit® Acrylic Resin for Controlled Drug Release of Pseudoephedrine Hydrochloride

AbstractThe preparation of a sustained release dosage form for pseudoephedrine hydrochloride was evaluated. Beadlets (PS) containing pseudoephedrine hydrochloride were prepared by spraying a slurry of pseudoephedrine hydrochloride, Eudragit® S-100, dibutyl sebacate and alcohol onto non-pariel seeds via the Wurster column process. The oven-dried PS beadlets were coated with different levels of Eudragit® RS (poorly water permeable) and Eudragit® S-100 (enteric resin). In-vitro dissolution

The Effect of Polymer Coating Systems on the Preparation, Tableting, and Dissolution Properties of Sustained-Release Drug Pellets

AbstractThe preparation of sustained-release (SR) drug pellets and their tablets was evaluated. Pellets containing indomethacin, pseudoephedrine hydrochloride (P-HCl), or pseudoephedrine (P) base were prepared by spraying a mixture of drug, Eudragit S-100 resins, dibutyl sebacate, and alcohol onto nonpareil seeds via the Wurster-column process. The oven-dried drug/Eudragit S-100 (DS) pellets were coated with different levels of Eudragit RS and Eudragit S-100 acrylic resins. Tablets containing P-HCl or P-base SR pellets, microcrystalline cellulose, and Methocel K4M were compressed. The solubility of the drug entity in the polymer solution was found to be the most critical factor affecting the yield and the physical properties of the resultant DS pellets. Dissolution studies of Eudragit RS coated drug pellets demonstrated that the release profiles depended not only on the physicochemical properties of the drug, particularly aqueous solubility, but also on the coating levels. The release rate profiles of the...

Preparation of a controlled release drug delivery system of indomethacin: Effect of process equipment, particle size of indomethacin, and size of the nonpareil seeds

AbstractIndomethacin pellets (IS) were prepared by spraying a slurry of indomethacin, Eudragit® S-100, dibuty1 sebacate and alcohol onto an appropriate mesh fraction of nonpareil seeds using appropriate processing equipment. Factors affecting this layering process were studied and identified. The average particle diameter and the overall particle size distribution of the indomethacin powder were found to be critical factors influencing the physical properties of the IS pellets. Micronized indomethacin powder, having an average particle diameter of four microns and a particle size distribution ranging from one to thirteen microns, was found to be the optimum for this layering process. Altering the mesh fraction of the starting nonpareil seeds for the layering process was found to greatly affect the release characteristics of the drug from the beadlets. The Wurster column process was found to be better than a fluid-bed granulator process for the manufacture of IS beadlets.

Preparation of a Controlled Release Drug Delivery System of Indomethacin

The preparation of a sustained release dosage form for indomethacin was studied. Pellets (I) containing indomethacin were prepared by spraying a slurry of indomethacin, Eudragit® S-100, dibutyl sebacate and alcohol onto non-pareil seeds via Wurster column processing. The resultant pellets were further coated with various combinations of EudragitrG RS (poorly water permeable) and EudragitrG RL polymers (readily water permeable) also using the Wurster column. In-vitro dissolution tests were conducted in a USP dissolution apparatus containing 900 ml of phosphate buffer at either pH 6.5 or 7.2. The in-vitro release studies of pellets (I) at pH 6.5 phosphate buffer exhibited a T dependence indicating a diffusion controlled process from a matrix formulation. At pH 7.2 phosphate buffer, pellets coated with EudragitrG RS showed the most retardation in the release rate of drug. As expected, the total amount of drug released from the coated pellets increased as the concentration of EudragitrG RL increased in the ba...