枸橼酸西地那非凝胶剂基质考察及体外溶出度测定

A Study on the Optimization of Matrix for Sildenafil Citrate Gel and the Determination for Its Dissolution In Vitro

目的:考察枸橼酸西地那非凝胶剂的基质,并对其体外溶出度进行测定。方法:建立枸橼酸西地那非含量测定高效液相色谱法,筛选了该凝胶剂的处方工艺。结果:HPLC法以pH 3.0三乙胺-甲醇-乙腈(58∶25∶17,V∶V∶V)作为流动相;采用ZORBAX SB-C_(18)色谱柱(4.6 mm×250 mm,5μm),在5~100μg·mL^(-1)的浓度范围内枸橼酸西地那非线性关系良好,线性方程为Y=25.58X-2.9823,r^(2)=0.9997;通过单因素实验考察,以10%明胶-3%蔗糖作为凝胶基质的处方;通过药物含量及溶出度测定,在1~3 mg·mL^(-1)药物浓度范围内,药物回收与投药量存在线性关系,Y=0.823X+0.053(r^(2)=0.9989),可作为凝胶剂药物含量设定的参考;且在pH 1.0盐酸介质中,3种药物浓度的凝胶剂均有较好的溶出行为。结论:筛选出枸橼酸西地那非凝胶剂优化处方,有利于小儿服用。

Objective:To optimize the matrix of sildenafil citrate gel preparation and determinate its dissolution in vitro.Methods:An assay method based on high performance liquid chromatography for sildenafil citrate was established,the formulation process of sildenafil citrate gel was optimized.Results:The mobile phase consisted of triethylamine,methanol and acetonitrile(58∶25∶12,V/V/V,pH 3.0).The separation was carried out on a ZORBAX SB serial C_(18) column and the method showed well linearity for sildenafil citrate in the range of 5-100μg·mL^(-1)(linear equation Y=25.58X-2.9823,r^(2)=0.9997).According to the results of the single factor test,10%gel and 3%sucrose was applied as the optimized matrix formulation.According to the results of assay and dissolution,the dosing quantity of sildenafil citrate also showed good linearity with the recovery in the range of 1-3 mg·mL^(-1)(Y=0.823X+0.053,r^(2)=0.9989),and all three gel preparations at different concentrations showed good dissolution in the pH=1.0 hydrochloric acid medium.Conclusion:The study has screened out the optimal formulation of sildenafil citrate gel.