肛肠科外用凝胶剂的制备及其体外透皮性能考察

摘要

Objective To study the preparation method of a topical gel formulation for anorectal diseases, and investigate the topical gel formulation's drug performance and characteristics in topical transdermal drug delivery. Methods The study time was from September to November 2016. Carbomer was used as the matrix. An appearance/quality test, centrifugation and heat/cold resistance test were performed. The optimal concentration of the matrix was determined by a comprehensive scoring method. The rutin content was measured by a modified Franz diffusion cell technique and ultra-high performance liquid chromatography. The drug performance and characteristics of the transdermal delivery of the topical gel formulation were evaluated. Results The optimal concentration of carbomer was determined to be 1.5% by appearance/quality test, centrifugation and heat/cold resistance test. In vitro transdermal delivery test showed that the apparent permeability coefficient (Papp) and steady state flow rate (Jss) of the gel formula were both significantly higher than those of the solution formula (tPapp=0.001, P<0.01; tJss=0.001, P<0.01). Conclusion The topical gel formulation is more convenient and the gel is less irritating than the original fuming-washing lotion. It is significantly increases the transdermal permeability of active compounds. Our results can be a reference to guide the subsequent study of the topical gel formulation and lay a foundation for the clinical application of the formulation.%目的 探讨肛肠科外用凝胶剂的制备方法,并考察其体外透皮给药的性能与特点.方法 2016年9—11月,以卡波姆为基质,以外观性状、离心实验、耐热耐寒实验为观察指标,采用综合评分法考察基质的最佳浓度,制备肛肠科外用凝胶剂.采用改良Franz扩散池,超高效液相色谱(UPLC)测定芦丁的含量,评价肛肠科外用凝胶剂的体外透皮给药性能与特点.结果 通过外观性状、离心实验、耐热耐寒实验,确定1.5%的卡波姆为最佳浓度.体外透皮实验显示,制剂组的表观渗透系数(Papp)与稳态流量(Jss)均高于溶液组,差异有统计学意义(tPapp=0.001, P<0.01;tJss=0.001,P<0.01).结论 中药制备成外用凝胶剂后,较原中药熏洗汤剂使用更加方便,刺激性小,且能显著提高透皮渗透性.此结果可进一步应用于该制剂的后续研究中,为其临床应用奠定基础.