论文部分内容阅读
目的:筛选马来酸噻吗洛尔眼用温敏型凝胶优化处方,并对其体外释放进行评价。方法:选用泊洛沙姆P407、P188为载体材料制备眼用温敏凝胶,测定不同处方的凝胶前体溶液分别在未经处理和经人工泪液稀释条件下,从溶液态转变为凝胶态的胶凝温度,通过星点设计-效应面法筛选优化处方,并考察胶凝时间和释放行为。结果:根据温敏凝胶保存和使用的温度要求,筛选出优化处方为P407∶P188(24.25%∶1.56%)。前体溶液能够在34℃人工泪液中迅速形成凝胶,并在体外缓慢释放6 h以上。结论:经过筛选并制备出的噻吗洛尔温敏型凝胶具有良好的载药能力、稳定性及释放性能,满足眼用制剂质量要求和实际应用要求。
OBJECTIVE: To screen timolol maleate ophthalmic thermosensitive gel and to evaluate its in vitro release. Methods: The ophthalmic thermosensitive gels were prepared by using poloxamer P407 and P188 as carrier materials. The gel precursor solutions of different prescriptions were determined to be changed from solutions to gels under the conditions of untreated and artificial tear dilution Gelation temperature, through the star design - response surface method to optimize the prescription, and study the gelling time and release behavior. Results: Based on the temperature requirements for the preservation and use of temperature-sensitive gels, the optimized prescription was selected as P407: P188 (24.25%: 1.56%). The precursor solution was able to rapidly gel in artificial tears at 34 ° C and release slowly over 6 h in vitro. Conclusion: The timolol-sensitive gels prepared by screening have good drug-loading capacity, stability and release properties, and meet the requirements of ophthalmic preparations quality and practical application.