苄达赖氨酸眼用温敏凝胶的制备

Preparation of the ophthalmic thermosensitive gel of bendazac lysine

目的制备苄达赖氨酸眼用温敏凝胶并考察其性能。方法采用冷溶法制备温敏凝胶;试管倒转法考察凝胶浓度、药物含量对相转变温度的影响;无膜溶出法模拟眼部生理环境,考察凝胶的体外溶蚀和药物释放行为。结果转变温度随凝胶溶液浓度而发生变化;含药量对相变温度无影响;优化处方为泊洛沙姆407浓度17.33%、药物的含量为1 mg·mL-1、溶剂为pH7.4的磷酸缓冲溶液、温敏凝胶转变温度为25.82℃。结论制备的苄达赖氨酸眼用温敏凝胶满足眼部用药的要求,可延长药物在眼部的作用时间。

OBJECTIVE To prepare and investigate the ophthalmic thermosensitive gel of bendazac lysine.METHODS Preparation of thermosensitive gel used cold-dissolve method.The influence on phase transition temperature of the gel concentration and the drug content by tube reversal method was investigated.Without membrane release method were used to investigate the gel release behavior in the simulate eye physiological environment.RESULTS The phase transition temperature was related to the gel solution concentration.But it was nothing to do with drug dosage.The optimized the prescription was composed of 17.33% poloxamer 407,1 mg·mL-1 drug content,pH7.4 phosphate buffer solution.Phase transition temperature of the thermosensitive gel was 25.82 ℃.CONCLUSION The preparation of ophthalmic thermosensitive gel of bendazac lysine contented the requirements of eyes medicine.It was favorable to prolong the drug duration in the eyes.