止痛凝胶膏剂的制备及体外释放考察

Preparation and in vitro Release Properties Investigation of Zhitong Gel Ointments

目的:优选止痛凝胶膏剂的基质处方并考察其体外释放特性。方法:以初黏力、持黏力、膜残留为评价指标,通过星点设计-效应面法优选止痛凝胶膏剂基质中NP-700、铝化合物、酒石酸、甘油的比例。采用改良的Franz扩散池法,以微孔滤膜代替筛网,阿魏酸为指标,进行体外释放试验。结果:优选的基质配方为NP-700-铝化合物-酒石酸-甘油(1.5∶0.16∶8.8∶0.12),止痛凝胶膏剂中阿魏酸于12 h内累积释放率(86.31±6.73)%。结论:优选的基质配方载药量高,涂展性、保湿性、黏着力良好。止痛凝胶膏剂中阿魏酸体外释放接近零级方程,具有扩散和溶蚀的双重机制,但以扩散为主。

Objective： To optimize matrix formulation of Zhitong gel ointments and investigate its in vitro release properties.Method： With initial bonding strength,endurance bonding strength and film residual as indexes,optimal proportion of matrix formulation（NP-700,aluminum compounds,glycerin and tartaric acid） was selected by central composite design-response surface methodology.Modified Franz diffusion cell and millipore membrane were used to investigate in vitro release properties of ferulic acid in Zhitong gel ointments.Result： Optimum matrix formulation was NP-700-aluminum compounds-glycerin-tartaric acid（1.5 ∶ 0.16 ∶ 8.8 ∶ 0.12）.Cumulative release rate of ferulic acid in Zhitong gel ointments was（86.31 ± 6.73） % in 12 h.Conclusion： This optimized matrix formulation had high drug loading and good spreadability,moisture resistance and adhesion.In vitro release behavior of ferulic acid in Zhitong gel ointments was close to the zero-order equation with a dual mechanism of diffusion and dissolution,but mainly by diffusion.