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目的:以温敏性聚合物泊洛沙姆407和黏附性聚合物羟丙基甲基纤维素为载体制备阴道用塞克硝唑温敏型原位凝胶,使凝胶在阴道壁原位凝胶化并迅速黏附于黏膜表面,延长药物在黏膜表面吸收时间。方法:采用单因素考察泊洛沙姆407浓度及药物对凝胶相变温度的影响,确定最佳处方;采用冷法制备载塞克硝唑温敏型原位凝胶,考察凝胶的流变学特性;采用紫外分光光度法测定原位凝胶中药物的含量。结果:当泊洛沙姆407浓度为20%时,载塞克硝唑温敏型凝胶的胶凝相变温度为(31.7±0.5)℃,可满足阴道用药后迅速相变为凝胶的条件,流变学行为显示塞克硝唑阴道凝胶的黏度随温度的变化均呈S形曲线,相变温度与转子法测得值相近。含量测方法在4.99~24.96mg.L-1范围内线性关系良好,平均回收率为98.47%,RSD为2.73%(n=6)。结论:阴道用塞克硝唑温敏型原位凝胶制备工艺简单,能在生理温度下迅速原位凝胶化,建立的含量测定方法简便可靠。
OBJECTIVE: To prepare secoidazole thermosensitive in situ gels with temperature-sensitive polymer Poloxamer 407 and adhesive polymer hydroxypropyl methylcellulose as the carrier, Gelatinized and quickly adhered to the mucosal surface, extending the absorption of drugs in the mucosal surface. Methods: The single factor was used to investigate the effect of poloxamer 407 on the phase transition temperature of the gel, and the best prescription was determined. The gelled flow in situ gel was prepared by cold method. Variations characteristics; using UV spectrophotometry in situ gel in the drug content. Results: When the concentration of poloxamer 407 was 20%, the temperature of gelation phase of clindamycin-sensitive gels was (31.7 ± 0.5) ℃, which could meet the need of rapid phase change to gel after vaginal administration The rheological behaviors of the saxitone vaginal gel showed a S-shaped curve as a function of temperature. The phase transition temperature was similar to that measured by the rotor method. The linearity was good in the range of 4.99 ~ 24.96mg.L-1 with the average recovery of 98.47% and RSD of 2.73% (n = 6). CONCLUSION: The process of preparation of secoidazole thermo-sensitive in-situ gels for vagina is simple and can be quickly gelled in situ at physiological temperature. The established method for determination of content is simple and reliable.