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目的:考察处方和制备工艺对氟尿嘧啶(5-FU)3种原位形成植入体释药速度的影响。方法:以单甲基聚乙二醇-羟基乙酸共聚物(mPEG-PLGA)为材料制备温敏性凝胶,以聚乙二醇/乳酸羟基乙酸共聚物(PLGA-PEG-PLGA)为材料制备原位形成凝胶剂,原位形成微球分别以PLGA-PEG-PLGA、聚乳酸(PLA)、端羧基聚乳酸-羟基乙酸共聚物(PLGA-C00H)为材料制备。采用UV法通过透析袋法测定体外释放度。结果:聚合物的浓度是影响原位植入体体外释放度的主要因素。除此外对于原位微球剂来说,N-甲基吡咯烷酮(NMP)和油相的比例也是影响体外释放度的重要因素之一。3种原位形成植入体主要通过扩散机制释药,其中温敏性凝胶的释药速度最快,原位微球剂与原位形成凝胶剂相比,突释减小,释药速度降低。结论:原位微球剂的控释效果最理想,值得进一步研究。
OBJECTIVE: To investigate the effect of prescription and preparation process on the release rate of three kinds of in-situ implantable fluorouracil (5-FU). Methods: The temperature-sensitive gels were prepared from monomethyl polyethylene glycol-co-glycolic acid (mPEG-PLGA). Polyethylene glycol / lactic acid glycolic acid (PLGA-PEG-PLGA) The gels were formed in situ and the in-situ microspheres were prepared by PLGA-PEG-PLGA, PLA and PLGA-C00H. Determination of in vitro release by dialysis bag method by UV method. Results: The concentration of polymer was the main factor affecting the in vitro release of in situ implants. In addition to the in situ microsphere agents, N-methylpyrrolidone (NMP) and the oil phase ratio is also one of the important factors affecting the in vitro release. The three kinds of implants formed by in situ release were mainly through diffusion mechanism, in which thermo-sensitive gel released the fastest, the in situ microspheres decreased compared with in situ gel formation, Slow down. Conclusion: The controlled release of in situ microspheres is the best and worthy of further study.