第三届国际工业药学和临床药学研讨会.pdf

第三届国际工业药学和临床药学研讨会, 广州中山大学, 2015.12 Drug acting as a pore former in coated pellets for a zero- order release: opportunity and challenge Introduction Novel drug delivery systems (NDDS): ü Targeting ü prolonged action ü Controlled-release Oral controlled-release (CR) systems hold the major market share. Introduction Oral CR drug delivery systems can be classified two broad groups: Single unit dosage forms Multiple unit dosage forms Tablets or capsules Pellets, beads or microparticles Introduction Multiple unit CR dosage forms fall in the two categories: Matrix Coating Coating is the most popular and widely available. Introduction The essential components of coated pellets: • The drug core, which contains the active agent and/or excipients • The coating, often a polymeric material. Introduction Mechanism ：Diffusion of the dissolved drug from the core through the polymeric coating Introduction A sigmoid release profile, showing a lag phase, followed by an intense increase in the release rate Matrix Burst effect Coatin Lag-time effect Muschert et al ./ J Control. Release 135 (2009) 71–79. Introduction The common approach of reducing the lag phase + Introduction The sequential layers of drug and polymer How to easily provide zero order release of freely soluble drugs from coated pellets B. Dekyndt et al / In