微孔洞控釋錠的開發與動物體內藥動研究   全文下載

Development of Micropore-Controlled Release Tablet and In Vivo Pharmacokinetic Study

本研究旨在開發一種微孔洞控釋錠。微孔洞控釋錠的組成包括藥物核心錠和包覆其外圍的微孔洞薄膜兩部份。微孔洞薄膜是利用二種不互溶的高分子聚合物組合而成，其中作為薄膜主體的高分子聚合物是具有半透特性的醋酸纖維素；另一種則是作為孔洞形成劑的水溶性高分子聚合物—聚乙二醇。薄膜組成及藥物核心錠所添加的賦形劑對藥物釋離的影響於文中加以探討。體外溶離結果顯示微孔洞控釋錠可以持續釋放藥物達24-36小時，添加乳糖於藥物核心錠可以促進藥物的釋放速率；動物試驗結果顯示微孔洞控釋錠可以降低藥物的最高血中濃度並延長藥物於體內的滯留時間。

The aim of this work was to develop a micropore-controlled release tablet for theophylline. The tablets were composed of a drug core surrounded by a microporous film. The major components of coating film included a biocompatible semipermeable polymer, cellulose acetate, and a water-soluble pore-forming agent, poly(ethylene glycol). The effect of the coating film composition and the type of excipient incorporated in the drug core on drug release were demonstrated via an in vitro release study. The optimized formulation was further investigated in vivo of rabbits. The results showed that micropore-controlled release tablets continuously released drug for 24-36 hours depending on the type of excipient in the drug core and the coating film composition. Incorporation of lactose in the drug core enhanced drug release from micropore-controlled release tablets. In vivo animal study revealed that the micropore-controlled release tablets reduced the maximum concentration and prolonged the mean residence time of drug.