安乃近原位凝胶的制备及体外评价

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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1 h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。 Objective To prepare analgin in situ gel to prolong the effect of metamizole in vivo. Methods Poloxamer 407 (P407) and poloxamer 188 (P188) were used as the carrier materials, and the in situ gel was prepared by cold dissolving method. The content of P407 and P188, Concentration on the gelation temperature, and with the dialysis bag study gel in vitro release. Results When the concentration of P407 was 23%, the concentration of P188 was 6% and the concentration of sodium bisulfite was 0.2%, the gelation temperature of the prepared in situ gel injections was suitable at 35.3 ° C The average in vitro cumulative release rate of gum in 40 days was 40.57%, which was 50.39% lower than the cumulative release rate of amphotericin in the same time. Conclusion The in situ gels of Amphenol gel have obvious thermo-sensitivities and their gelation temperature is suitable for in vivo administration. The release of metamizole gel in situ shows obvious sustained-release effect and can be used in clinical.
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