以溶媒揮發法和噴霧乾燥法開發蘭索拉唑緩釋微球劑型   全文下載

Preparation of Microparticles for Acid-labile Lansoprazole by Solvent Evaporation Method Combined with a Spray Drying Process

本研究旨在開發一緩釋微球劑型以控釋酸不安定藥物—蘭索拉唑。本實驗利用油/水溶媒揮發法製作緩釋微球，並且針對三個影響緩釋微球的因子進行評估，包括Eudragit(R) RS-100濃度、蘭索拉唑濃度及均質速度。實驗結果顯示，均質速度顯著影響緩釋微球的平均粒徑；增加Eudragit(R) RS-100或蘭索拉唑濃度可促進藥品的包覆率。蘭索拉唑從緩釋微球的釋放是藉由擴散機制並伴隨著高分子聚合物的膨脹現象。緩釋微球並進一步以腸溶膜衣包覆，以增進蘭索拉唑抗酸的效果。

The aim of this study was to develop a microparticulate delivery system for acid-labile lansoprazole. The solvent evaporation method was employed to prepare Eudragit(R) RS-100 microparticles (RS-microparticles). The effects of three parameters, including polymer concen-tration, drug concentration and homogenization rate, on microparticle performance were evaluated. The results revealed that the homogeni-zation rate played an important role on the microparticle size. Increasing the polymer concentration and decreasing the drug concentration enhanced the efficiency of drug encapsulation in RS-microparticles. The release of drug from RS-microparticles was governed by both Fickian diffusion and polymer swelling mechanisms. The RS-microparticles were further enteric coated by hydroxypropyl methyl cellulose phthalate (HPMCP) to improve the acid-resistance of lansoprazole.