摘要
目的:制备硫酸软骨素眼用温敏凝胶,并考察其体外释放度和房水动力学。方法:选用泊洛沙姆407(P407)、泊洛沙姆188(P188)和聚卡波菲为凝胶基质,正交试验L9(34)确定处方组成,通过含量测定、胶凝温度(T1)、人工泪液稀释后的胶凝温度(T2)、凝胶黏度(P)、眼部刺激性试验考察其质量,体外释放度和房水动力学考察其体内疗效。结果:最佳处方组成为硫酸软骨素3%,P40716%,P1883%,聚卡波菲1%。凝胶制剂的T1为27.38℃,T2为34.28℃,P为740 cpa,眼部刺激性符合要求,体外释放度和房水动力学均优于溶液剂。结论:所制备的硫酸软骨素眼用温敏凝胶各项质量指标符合要求。
Objective: To prepare chondroitin sulfate ophthalmic thermosensitive gels,and study the in vitro drug release and pharmacokinetic parameters in aqueous humor. Methods: The ophthalmic thermosensitive gels were prepared with poloxamer 407,poloxamer 188 and polycarbophil as the gel bases,the formulation was optimized by L9( 34) orthogonal design,and the quality was evaluated with the content determination,gelation temperature( T1),gelation temperature( T2) after diluted by simulated tear,gelation viscosity( P) and irritation as the indices. The curative effect in vivo was studied by using the drug release in vitro and pharmacokinetic parameters in aqueous humor as the indices. Results: The best formulation of chondroitin sulfate ophthalmic thermosensitive gels contained 3% chondroitin sulfate,16% Poloxamer 407( P407),3% Poloxamer 188( P188) and 1% propylene glycol. The gelation temperature( T1) was 27.38℃,gelation temperature( T2) after diluted by simulated tear was 34.28℃,the gelation viscosity was 740 cpa,the results of irritation experiment met the requirements,and the drug release in vitro and pharmacokinetic parameters in aqueous humor of the gels were superior to those of the eye drops. Conclusion: The quality evaluation indices of chondroitin sulfate ophthalmic thermosensitive gels all meet the requirements.
作者
崔颖
赵瑛
Cui Ying;Zhao Ying(Tianyou Hospital Affiliated to Wuhan University of Science and Technology,Wuhan 430064,China)
出处
《中国药师》
CAS
2020年第4期651-654,共4页
China Pharmacist
关键词
硫酸软骨素
眼用温敏凝胶
胶凝温度
体外释放
Chondroitin sulfate
Ophthalmic thermosensitive gels
Gelation temperature
Drug release in vitro
