本計畫主要目的在於開發一系列止痛藥物Nalbuphine前驅藥之Poly(lactide/glycolide)長效微球粒劑型及其生體外和生體內藥物釋放之評估研究。於生體外之藥物釋放實驗顯示不同比例之Lactide/glycolide高分子及不同親水性之前驅藥均對藥物釋放動力學有所影響。於體內之藥物動力學研究則顯示當Nalbuphine前驅藥親水性增加時其釋放速率將較快並較完全。對此系列Nalbuphine前驅藥而言,其微球粒製劑之生體外及生體內藥物釋放具有很好的相關性。 The major purpose of this project is to develop and in vitro-in vivo evaluation of poly(lactide/glycolide) based microsphere for nalbuphine prodrug controlled delivery. The in vitro release studies showed that the different poly(lactide/glycolide) ratios and the different hydrophilic prodrugs both affect the kinetics of drug release. The in vivo release studies showed that the release of more hydrophilic prodrug is faster and more complete. A good correlation can be observed from the in vivo and in vitro release studies.
