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目的 :研究紫杉醇微乳的制备 ,稳定性和静注、口服的生物利用度。方法 :聚乙二醇 (EPC) ,紫杉醇和PEG DSPE的氯仿溶液在氮气流下减压成膜 ,加入经水化超声处理的玉米油 ,进一步超声处理后 ,通过微流化器使其微乳化。结果 :粒径 5 0～1 0 0nm ,包封率≥ 99.2 % ,兔绝对生物利用度 :静注 1 0 7.7% ,口服 2 2 .4%。结论 :本实验研究为开发紫杉醇新型静注和口服制剂提供了科学依据。
Objective: To study the preparation of paclitaxel microemulsion, stability and intravenous injection, oral bioavailability. METHODS: Polyethylene glycol (EPC), paclitaxel and PEG DSPE in chloroform were decompressed to form a membrane under a stream of nitrogen. The hydrous sonicated corn oil was added to further sonicate and then microemulsified through a microfluidizer. Results: The particle size ranged from 50 nm to 100 nm. The entrapment efficiency was 99.2%. The absolute bioavailability of rabbits was 10.7% intravenously and 22.4% orally. Conclusion: This experimental study provides a scientific basis for the development of new intravenous and oral formulations of paclitaxel.