Polymer blends used for the coating of multiparticulates: comparison of aqueous and organic coating techniques

• Published in: Pharmaceutical research Vol. 21; no. 5; pp. 882 - 890
• Main Authors: Lecomte, Florence, Siepmann, Juergen, Walther, Mathias, MacRae, Ross J, Bodmeier, Roland
• Format: Journal Article
• Language: English
• Published: United States Springer Nature B.V 01.05.2004
• Subjects: Adrenergic beta-Antagonists - administration & dosage; Cellulose - analogs & derivatives; Chemical Phenomena; Chemistry, Physical; Drug Compounding; Excipients; Hardness; Kinetics; Organic Chemicals; Pharmaceutical Solutions; Polymers; Polymethacrylic Acids; Propranolol - administration & dosage; Solubility; Tablets, Enteric-Coated - chemistry; Water
• ISSN: 0724-8741; 1573-904X
• DOI: 10.1023/B:PHAM.0000026443.71935.cb

The purpose of this study was to use polymer blends for the coating of pellets and to study the effects of the type of coating technique (aqueous vs. organic) on drug release. Propranolol HCl-loaded pellets were coated with blends of a water-insoluble and an enteric polymer (ethyl cellulose and Eudragit L). Drug release from the pellets as well as the mechanical properties, water uptake, and dry weight loss behavior of thin polymeric films were determined in 0.1 M HCI and phosphate buffer, pH 7.4. Drug release strongly depended on the type of coating technique. Interestingly, not only the slope, but also the shape of the release curves was affected, indicating changes in the underlying drug release mechanisms. The observed effects could be explained by the higher mobility of the macromolecules in organic solutions compared to aqueous dispersions, resulting in higher degrees of polymer-polymer interpenetration and, thus, tougher and less permeable film coatings. The physicochemical properties of the latter were of major importance for the control of drug release, which was governed by diffusion through the intact polymeric films and/or water-filled cracks. The type of coating technique strongly affects the film microstructure and, thus, the release mechanism and rate from pellets coated with polymer blends.