安乃近原位凝胶的制备及体外评价

目的 制备安乃近原位凝胶,延长安乃近在体内的作用时间.方法 以泊洛沙姆407(P407)和泊洛沙姆188(P188)作为载体材料,采用冷溶法制备安乃近原位凝胶,考察P407和P188的含量、亚硫酸氢钠及安乃近浓度对胶凝温度的影响,并用透析袋法考察凝胶的体外释药情况.结果 当P407浓度为23％、P188浓度为6％、亚硫酸氢钠的浓度为0.2％时,所制得的安乃近原位凝胶注射剂的胶凝温度合适,为35.3℃时,该凝胶在1h内的平均体外累积释放率为40.57％,较安乃近水溶液同时间内的累积释放率低50.39％.结论 安乃近原位凝胶的温敏性明显,其胶凝温度适合体内给药;安乃近原位凝胶对安乃近药物的释放显示出了明显的缓释效应,可以进一步用于临床.

Preparation and in vitro evaluation of Analgin in situ gel

OBJECTIVE To prepare in situ gel of Analgin and to extend the time of Annalgin in the body.METHODS The cold soluble method was used to prepare the in situ gel Analgin,with poloxamer 407 (P407) and 188 (P188) acting as carrier materials,with dialysis bag method investigating the in vitro drug release of the gel.The effects of the concentration of poloxamer 407(P407),188(P188) sodium bisulfate and Analgin on gelation temperature were inspected at the same time.RESULTS The results showed that P407 concentration was 23％,P188 concentration was 6％,sodium bisulfite concentration was 0.2％.Such Analgin prepared in situ gel injection had appropriate gelling temperature.At 35.3 ℃,the in vitro cumulative release rate of this gel was 40.57％,which is 50.39％ lower than 2 h cumulative release time of Analgin aqueous solution.CONCLUSION The in situ gel shows apparent slow release of Analygin,and can be further used for clinical purposes.