丹酚酸B原位眼用凝胶剂的制备及体外释放

Research on Preparation and in Vitro Release of pH Sensitive Gel for Eye Cornea of Salvianolic Acid B

目的筛选丹酚酸B原位眼用凝胶剂处方,完成相关体外释放研究.方法通过离体角膜透过实验、刺激性实验、角膜水化值测定、凝胶粘度、胶凝能力、流动性等评价方法,筛选丹酚酸B药物浓度、促透剂、増粘剂等辅料的种类及用量.结果确定该凝胶剂的成分组成为:0.5%丹酚酸B、0.14%卡波姆、0.05%氮酮、0.3%羟丙甲基纤维素、0.1%羟苯乙酯和0.2%维生素C.角膜水化值(77.32±1.88).该凝胶在15 min时释放率27.21%的药物,6 h后累计释放率达到97.44%.经过240 min的角膜透过实验,丹酚酸B凝胶的累积释放量大于生理盐溶液的释放量(P<0.05).结论该原位凝胶剂处方设计合理,制备简单,无刺激性,延长药物在角膜的滞留时间,增加药物角膜透过释放量.

Objective To prepare pHsensitive gel for eye cornea of salvianolic acid B and accomplish in vitro release study.Methods We used corneal permeability,eye irritation in rabbits,hydration of the cornea,viscosity,gel capacity,transparency,liquidity as index,to select pH sensitive gel matrix composition.Results The gel composition was:0.5%of salvianolic acid B,0.14%Carbomer,0.3%HPMC,0.05%Azone,0.1%ethylparaben and 0.2%Vc.The corneal hydration level was 77.32±1.88.The gel released 27.21%drug in 15 min,and released 97.44%drug in 6 h.By research of corneal permeability,the cumulative release of gel was bigger than the one of saline(<0.05).Conclusions The selection of the gel matrix prescription is reasonable in design,simple in process,not harsh to eyes,and can prolong the retention time of drug in corneas and improve the corneal penetration.