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目的:采用水包油包张复乳法制备聚乙烯醇-聚乳酸羟基乙酸(PVA-g-PLGA)胰岛素微球,建立测定胰岛素PVA-g-PLGA微球药物含量的高效液相色谱法,通过考察微球的外观、粒径、载药率和包封率对微球的质量进行评价,通过比较PLGA和PVA-g-PLGA微球的体外降解pH变化来初步判断PVA-g-PLGA是否具有蛋白保护能力。方法:利用扫描电子显微镜观察胰岛素微球的表面形貌,使用激光粒度仪测定微球的粒径分布,用高效液相色谱仪测定微球的载药率和包封率。结果:所制备的胰岛素PVA-g-PLGA微球粒径均一、光滑、圆润,微球之间没有粘连,微球粒径在1800~4000 nm之间,分布相对集中;微球含量为170.8μg·mg-1,载药率为1.53%,包封率为56.51%,96 h的累积释放率为42.67%;随着时间的延长,PLGA微球体外降解的pH明显低于PVA-g-PLGA微球。结论:采用复乳法制备的微球外观光滑、圆润,微球之间无粘连,粒径均一;所建立的HPLC含量测定方法符合方法验证基本要求;PVA-g-PLGA微球具有一定的蛋白保护能力。
OBJECTIVE: To prepare PVA-g-PLGA insulin microspheres by oil-in-water-packet-double-emulsion method and establish a HPLC method for determination of the content of insulin PVA-g-PLGA microspheres. The quality of the microspheres was evaluated by examining the appearance, particle size, drug loading rate and entrapment efficiency of the microspheres. Whether PVA-g-PLGA was preliminarily judged by comparing the in vitro degradation pH changes of PLGA and PVA-g-PLGA microspheres With protein protection. Methods: The surface morphology of insulin microspheres was observed by scanning electron microscopy. The particle size distribution of the microspheres was determined by laser particle sizer. The drug loading rate and entrapment efficiency of the microspheres were determined by high performance liquid chromatography. Results: The prepared PVA-g-PLGA microspheres were uniform in size, smooth and round, with no adhesions between the microspheres. The diameters of the microspheres ranged from 1800 nm to 4000 nm with a concentration of 170.8 μg · Mg-1, drug loading rate was 1.53%, entrapment efficiency was 56.51%, the cumulative release rate of 96 h was 42.67%. With the extension of time, the in vitro degradation of PLGA microspheres was significantly lower than that of PVA-g-PLGA Microspheres. Conclusions: The microspheres prepared by the double emulsion method have a smooth and round appearance with no adhesions between the microspheres and uniform particle size. The HPLC method established by the method conforms to the basic requirements of the method validation. The PVA-g-PLGA microspheres have certain proteins Protection ability.