摘要
The sinomenine hydrochloride （SH） patch, a topical drug delivery system, was prepared and characterized. The in vitro release was studied according to the paddle-over-disk method in the appendix of Chinese Pharmacopeia （appendix XD, 2005）. Stability of SH patch was evaluated at accelerated testing conditions （40 ℃, 75% RH）. Pharmacological and pharmacokinetics study were also performed. It was found that the release of SH from patches depended on pH value of the release medium. There were no significant differences between SH patches stored for 6 mon and those stored for 0 mon in the drug content, initial adhesion, lasting stickiness, peeling strength and in vitro release. SH patches exhibited better anti-inflammatory activity as well as analgesic efficacy. More importantly, primary pharmacokinetic parameters of SH patch, such as Cmax and AUC, were much lower than those of SH solution dosed orally. In conclusion, the patch might be a promising delivery system for SH, which bypassed the gastrointestinal tract and was a convenient, efficacious, safe and non-invasive delivery method.
本文目的在于制备和评价一种盐酸青藤碱的局部给药系统——盐酸青滕碱贴剂。按中国药典(2005版)附录XD规定,采用管碟法测定该贴剂的体外释放度;以加速实验条件(40℃,75%RH)考察贴剂的稳定性;另外还对贴剂的药效学和药动学特性进行评价。结果表明,盐酸青藤碱贴剂的体外释放度依赖于释放介质的pH值;加速实验条件下放置6个月,药物含量、初粘力、持粘力、剥离强度和体外释放特性没有发生明显变化;该贴剂还显示出较好的抗炎和镇痛活性。更重要的是,贴剂的主要药代动力学参数均低于盐酸青滕碱的口服溶液。通过这些实验表明,盐酸青藤碱贴剂有希望成为更方便用药、安全有效、非损伤的给药系统,尤其适用于长期给药以及有胃肠道疾病的关节炎患者。
