滋肾凝胶贴膏剂的制备及其体外透皮吸收研究  

Preparation and Transdermal Absorption Study In Vitro of Zishen Gel Plaster

作　　者：张成 王杰 卫禹辰 孙晓熙 卢昊 许汉林 ZHANG Cheng;WANG Jie;WEI Yuchen;SUN Xiaoxi;LU Hao;XU Hanlin(School of Pharmacy,Hubei University of Traditional Chinese Medicine,Wuhan 430065,China)

机构地区：[1]湖北中医药大学药学院,武汉430065

出　　处：《医药导报》2024年第12期2013-2020,共8页Herald of Medicine

摘　　要：目的将滋肾丸按照处方制成凝胶贴膏剂,探讨其体外透皮特性。方法在预实验的基础上,以初黏力、持黏力、感官评分为评价指标,采用单因素试验和Box-Behnken响应面法来优化凝胶贴膏剂的基质处方用量。采用改良的Franz扩散池,以新芒果苷、盐酸黄柏碱、芒果苷、盐酸小檗碱透过量为评价指标,考察促渗剂对凝胶贴膏剂体外透皮特性的影响。结果滋肾凝胶贴膏剂基质的处方用量为聚丙烯酸钠NP-7002.55 g,甘油11.04 g,聚乙烯吡咯烷酮K901.13 g,酒石酸0.1 g,甘羟铝0.1 g,高岭土0.3 g,蒸馏水15 g;不同类型和浓度的促渗剂中,5%氮酮的促渗性能最佳,新芒果苷、盐酸黄柏碱、芒果苷、盐酸小檗碱的渗透速率依次为1.5338、1.7809、2.3247、20.0899μg·(cm^(2))^(-1)·h^(-1),增渗倍速则为2.4319、1.9408、1.9604、1.4701;药物经皮吸收曲线符合零级动力学方程。结论所得凝胶贴膏剂的制备工艺稳定可行,膏体性能良好,释药持续,有着良好的体外经皮渗透性,具备一定的临床应用价值。Objective To prepare Zishen pills as gel plaster according to the prescription,and investigate its transdermal absorption characteristics in vitro.Methods Based on preliminary experiments,the matrix prescription of the gel plaster was optimized by single-factor tests and the Box-Behnken design.Evaluation indicators included initial viscosity,viscosity retention and sensory scores.The modified Franz diffusion cell was used to investigate the effect of penetration enhancers on the transdermal characteristics of gel plaster in vitro,with the permeability of neomangiferin,phellodendrine hydrochloride,mangiferin and berberine hydrochloride as evaluation indicators.Results The prescription dosage of the preferred matrix for the Zishen gel plaster was sodium polyacrylate NP7002.55 g,glycerin 11.04 g,polyvinylpyrrolidone K901.13 g,tartaric acid 0.1 g,glycyrrhizin 0.1 g,kaolin 0.3 g,and distilled water 15 g.Among different types and concentrations of permeation enhancers,5%aminoketone showed the best permeation performance.The permeation rates for neomangiferin,phellodendrine hydrochloride,mangiferin,and berberine hydrochloride were 1.5338,1.7809,2.3247 and 20.0899μg·(cm^(2))^(-1)·h^(-1),and the penetration rates were 2.4319,1.9408,1.9604 and 1.4701,respectively.The percutaneous absorption curve of the drug conformed to the zero-order kinetic equation.Conclusion The preparation process of the obtained gel plaste is stable and feasible,with good adhesive properties,sustained drug release,and favorable in vitro percutaneous permeability,indicating potential clinical application value.

关 键 词：滋肾凝胶贴膏 处方优化 响应面 含量测定 透皮吸收 

分 类 号：R932[医药卫生—生药学] R944.2[医药卫生—药学]