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注射用利培酮微球的制备和体外性质评价

Preparation and in vitro evaluation of risperidone loaded PLGA microspheres

【作者】 张华王翔王学清张强

【Author】 ZHANG Hua;WANG Xiang;WANG Xue-qing;ZHANG Qiang;Department of Pharmaceutics,School of Pharmaceutical Sciences,Peking University;

【机构】 北京大学药学院药剂系

【摘要】 目的:制备注射用利培酮微球并进行质量评价。方法:建立HPLC方法测定利培酮的含量;以乳酸-羟基乙酸共聚物(PLGA)为载体材料,乳化-溶剂挥发法制备利培酮微球,考察药物量、载体量、乳化和固化聚乙烯醇(PVA)浓度对利培酮微球药剂学性质的影响,并对所制备的利培酮微球进行了体外释放度评价。结果:建立了利培酮含量测定的HPLC方法:采用Luna C18色谱柱,流动相为甲醇-水-三乙胺-冰醋酸(55∶45∶1∶0.5),流速为1 mL·min-1,检测波长为280 nm,柱温为25℃。根据不同因素对利培酮微球制备的影响,筛选出最佳处方:药物20 mg,载体400 mg,乳化PVA浓度为2%,固化PVA浓度为0.3%,所得的利培酮微球表面圆整,粒径为61.5μm,包封率为89.8%,载药量为6.8%。体外释放试验表明,按照最优处方制备的利培酮微球2 h内药物释放低于10%,突释效应较小;d 5药物的释放达到63%,可持续释放15 d。结论:本实验根据不同制备因素优化得到的利培酮微球,释放无滞后期,可有效缓释达两周以上。

【Abstract】 Objective: To prepare risperidone loaded PLGA microspheres and evaluate its in vitro pharmaceutical characters. Methods: An HPLC method was established to determine the concentration of risperidone. Risperidone loaded poly( lactic-co-glycolide acid)( PLGA) microspheres were prepared by emulsion-solvent evaporation method. The effects of different preparation parameters on the preparation of risperidone microspheres were investigated,and the pharmaceutical characters of risperidone microspheres were evaluated. Results: The HPLC method was established. Luna C18column was used with methanol-water-triethylamine-acetic acid( 55∶ 45∶ 1∶ 0. 5)as mobile phase. The flow rate was 1 mL·min- 1,detecting wavelength was set at 280 nm,and column temperature was set at 25 ℃. The best formulation was obtained according to the effects of different factors on the preparation of risperidone microspheres. Spherical microspheres with a smooth surface and dispersive quality were prepared based on the best formulation. The particle size of risperidone microspheres was 61. 5 μm. The encapsulation efficiency and the drug loading were 89. 8% and 6. 8%,respectively. The release of risperidone from microspheres in vitro was less than 10% in two hours and showed no burst release. The drug was released by 63% on the fifth day and could sustain for two weeks. Conclusion: Risperidone could release from PLGA microspheres constantly for two weeks,without lag phase. The prepared microspheres are helpful for improving patients’ compliance and modifying clinical dosage.

【关键词】 利培酮; 微球; 高效液相色谱法; 体外释放;

【Key words】 risperidone; microspheres; high performance liquid chromatography; in vitro release;

【分类号】R971.4;R944.9;R446.1;

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