痛舒凝胶膏剂的制备及体外透皮研究

Preparation of Tongshu Gel Paste and study on the transdermal penetration in vitro

目的痛舒方为治疗痛经的临床常用方,为了提高治疗效果,本研究将该散剂改良为凝胶膏剂,并考察其体外透皮吸收性能,为其开发和利用提供科学依据。方法建立综合评分标准,结合单因素实验与响应面法确定凝胶膏剂的基质用量。进行体外透皮实验,以延胡索乙素、芍药苷、粉防己碱、乌药醚内酯为评价指标,考察加入不同比例氮酮促渗剂对凝胶膏剂体外透皮渗透量的影响。结果痛舒凝胶膏剂基质的最优处方为聚丙烯酸钠0.50 g、甘氨酸铝0.1 g、保湿剂8.00 g(甘油∶丙二醇=8∶2)、酒石酸0.1 g、羧甲基纤维素钠(CMC-Na)、明胶1.75 g(CMC-Na∶明胶=1∶3),体外透皮吸收实验结果表明,透皮促渗剂比例为3%时药物透皮效果最好。结论用最优处方制备的痛舒凝胶膏剂,具有骨架型缓释制剂的特性,为痛舒方外用新剂型的开发奠定了基础。

Objective Tongshu prescription is a common clinical prescription for treating dysmenorrhea.In order to improve the therapeutic effect and provide,this study improved the powder into gel ointment,and investigated its transdermal absorption performance in vitro,and provide.Methods The comprehensive evaluation standard was established,and the matrix dosage of gel paste was determined by single factor experiment and response surface method.The transdermal experiment in vitro was conducted,and the effects of different proportions of azone penetration enhancers on the transdermal penetration of gel paste in vitro were investigated with tetrahydropalmatine,paeoniflorin,tetrandrine,and linderane as evaluation indexes.Results The optimal matrixformula of Tongshu Gel Paste were as follows:sodium polyacrylate 0.50 g,aluminum glycinate 0.1 g,humectant 8.00 g(glycerol∶propylene glycol=8∶2),tartaric acid 0.1 g,sodium carboxymethyl cellulose(CMC-Na)and gelatin 1.75 g(CMC-Na∶gelatin=1∶3).The experimental results of transdermal absorption in vitro showed that the transdermal effect of drugs was the highest when the proportion of transdermal enhancers was 3%.Conclusion Tongshu Gel Paste prepared has the characteristics of skeleton sustained-release preparation,which lays a foundation for the development of new dosage forms for external use of Tongshu prescription.