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目的研究影响抗脑胶质瘤药物盐酸多柔比星缓释植入剂体外释药的因素,为动物药效学研究提供依据。方法以聚乳酸-羟基乙酸(PLGA)为载体与盐酸多柔比星混合制成缓释植入剂,采用UV测定其体外释放度。考察聚乳酸-羟基乙酸共聚物组成、聚乳酸-羟基乙酸相对分子质量(Mw)、载药量等因素对缓释植入剂体外释放度的影响。结果载药量10%的植入剂释药速度明显快于5%的植入剂;随着共聚物组成中羟基乙酸比例的增加,释药速度明显加快,LA-GA为50∶50的植入剂35d时累积释放度达90%,而75∶25的植入剂仅为60%;聚乳酸-羟基乙酸相对分子质量与释药速度成反比,Mw=20 748的植入剂释药速度明显快于Mw=30 834的植入剂。结论聚乳酸-羟基乙酸共聚物组成、聚乳酸-羟基乙酸相对分子质量、载药量是影响缓释植入剂体外释药的因素,其中共聚物组成和相对分子质量是主要的影响因素。通过调节共聚物组成和相对分子质量可以很好地控制药物的释放速度。
Objective To study the factors that affect the in vitro release of doxorubicine hydrochloride anti-glioma drug against glioma, and provide evidence for animal pharmacodynamics. Methods Polylactide - glycolic acid (PLGA) was mixed with doxorubicin hydrochloride to make sustained - release implants. The in vitro release was determined by UV. The effects of the composition of poly (DL-lactic-co-glycolic acid), the molecular weight of poly (DL-lactide-co-glycolic acid) and drug loading on the in vitro release of sustained release implants were investigated. Results The drug release rate of 10% drug delivery was significantly faster than that of 5% implants. With the increase of the proportion of glycolic acid in the copolymer, the drug release rate was significantly accelerated. The LA-GA 50:50 plant The cumulative release was 35% at 35 days compared to 60% at 75:25. The relative molecular mass of polylactic-co-glycolic acid was inversely proportional to the drug release rate and the drug release rate of Mw = 20 748 Significantly faster than implants with Mw = 30 834. CONCLUSION: The composition of poly (DL-lactic-co-glycolic acid), the relative molecular mass of poly (DL-lactic-co-glycolic acid) and drug loading are the factors that affect the in vitro release of sustained release implants. The copolymer composition and molecular weight are the main influencing factors. By adjusting the copolymer composition and molecular weight can be well controlled drug release rate.