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测定并对比了以Eudragit RS100或氯化铝为交联剂时聚丙烯酸钠(PAA-Na)溶液的屈服值与黏度,结果二者无显著差异。但根据绘制的流变曲线可见,以Eudragit RS100为交联剂的体系黏度较均一,有利于提高凝胶基质中药物含量的均匀性。在此基础上加入羧甲纤维素钠(CMC-Na)为增黏剂,制备空白凝胶贴膏基质,并用Box-Behnken设计-效应面法优化基质处方。所得优化处方为含PAA-Na、Eudragit RS100和CMC-Na各4.0%、0.2%和14.0%。以制川乌和白芍的提取物为模型药物制备了以Eudragit RS100或氯化铝为交联剂的乌芍凝胶贴膏,并考察了两种制品中芍药苷的透皮行为。结果两种制品中芍药苷的稳态透皮速率和释放时滞均无显著差异,提示以Eudragit RS100为交联剂并不影响该凝胶贴膏中药物的经皮渗透性能。
The yield and viscosity of sodium polyacrylate (PAA-Na) solution were measured and compared with those of Eudragit RS100 or aluminum chloride. There was no significant difference between them. However, according to the rheological curve drawn, the viscosity of the system with Eudragit RS100 as crosslinking agent is relatively uniform, which is beneficial to improve the uniformity of the drug content in the gel matrix. On this basis, CMC-Na was added as a thickening agent to prepare a blank gel adhesive matrix, and the matrix formulation was optimized by Box-Behnken design-response surface methodology. The resulting optimized formulation was 4.0%, 0.2% and 14.0% with PAA-Na, Eudragit RS100 and CMC-Na. Taking the extract of Radix Aconiti Preparata and Radix Paeoniae Alba as model drug, we prepared the Radix Ginseng paste with Eudragit RS100 or aluminum chloride as crosslinking agent, and investigated the transdermal behavior of paeoniflorin in the two products. Results There was no significant difference in steady-state transdermal rate and delayed release of paeoniflorin between the two preparations, suggesting that the use of Eudragit RS100 as the crosslinking agent did not affect the transdermal penetration of the drug in the gel patch.