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目的研究不同内水相明胶浓度、不同微球挥干固化方法和不同pH值释放介质等对丙氨瑞林微球的体外释放趋势的影响。方法由溶剂挥发法-复乳法(W/O/W)制备丙氨瑞林微球,内水相分别采用0%、8%、16%明胶水溶液,使用室温常压挥发和低温真空挥发法固化微球。体外释放实验中,采用pH=4.5、pH=7.0、pH=10.0三种释放介质,于第1、7、14、21、28、35天取样,残余法测定体外释放微球突释量及释放度,使用电子扫描电镜记录微球释放期间各取样点的微球降解程度。结果有机溶剂挥发固化方法会影响微球的体外释放模式,含不同明胶浓度内水相的微球有不同的体外释放模式,微球中的丙氨瑞林在释放介质pH=10.0中释放速率最快,而在pH=4.5中不能完全释放,最适宜的释放介质是pH=7.0缓冲液。结论不同挥发固化方法制备会影响微球的突释量,但对微球的整体体外释放趋势没有影响,内水相浓度对体外释放的趋势有影响,释放介质的pH值对丙氨瑞林微球药物的释放有影响。
Objective To study the effects of different inner aqueous gelatin concentration, different methods of drying and curing of microspheres and different pH releasing media on the in vitro release of ararelin microspheres. Methods The ararelin microspheres were prepared by the solvent evaporation method and the double emulsion method (W / O / W). The inner aqueous phase was treated with 0%, 8% and 16% aqueous solution of gelatin, respectively. Curing microspheres. In vitro release experiment, three kinds of release media pH = 4.5, pH = 7.0, pH = 10.0 were used for sampling on the 1st, 7th, 14th, 21st, 28th and 35th days. Degree, the use of electronic scanning electron microscopy microspheres release microspheres at each sampling point during the degradation. Results Volatilization of organic solvents affected the release of microspheres in vitro. Microspheres with different gelatin concentrations in aqueous phase had different release patterns in vitro. The release rate of ararelin in microspheres was the highest in pH = 10.0 Fast, and not completely released at pH = 4.5, the most suitable delivery medium is pH = 7.0 buffer. Conclusions Different volatile solidification methods can affect the burst release of microspheres, but have no effect on the global in vitro release of microspheres. The internal aqueous phase concentration has an impact on the release trend in vitro. Ball drug release has an impact.