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目的:考察制备工艺对盐酸噻吩诺啡微球的体外释放度的影响。方法:以乳酸羟醋酸共聚物PLGA(75/25)为载体,采用O/W型乳化溶剂挥发法制备盐酸噻吩诺啡微球。采用HPLC法测定微球的体外释放度。考察PLGA相对分子质量、理论载药量、PLGA浓度、PVA浓度、乳化搅拌速度等因素对盐酸噻吩诺啡微球体外释放度的影响。结果:PLGA相对分子质量对微球体外释放度影响较大。选择减小理论载药量、PLGA浓度和PVA浓度可以降低突释,减缓释放速度。结论:制备工艺参数的变化对盐酸噻吩诺啡微球的体外释放度影响显著。
Objective: To investigate the effect of preparation process on in vitro release of Thienorphine hydrochloride microspheres. Methods: The thienorphine hydrochloride microspheres were prepared by the emulsion method of O / W emulsification with PLGA (75/25) as the carrier. The in vitro release of microspheres was determined by HPLC. The effects of PLGA relative molecular mass, theoretical drug loading, PLGA concentration, PVA concentration, emulsifying stirring speed and other factors on in vitro release of thienone hydrochloride microspheres were investigated. Results: The relative molecular mass of PLGA greatly affected the in vitro release of microspheres. Choose to reduce the theoretical drug loading, PLGA concentration and PVA concentration can reduce the burst release, slow release rate. Conclusion: The changes of preparation parameters have significant effects on the in vitro release of thienorphine hydrochloride microspheres.