复方盐酸利多卡因巴布膏剂的研制  

Preparation of compound lidocaine hydrochloride cataplasm

作　　者：胡晋红[1] 朱全刚[1] 陆松伟[1] 韩璐[1] 刘少明[1] 王景阳[2] 王天舒[2] 

机构地区：[1]第二军医大学长海医院药学部,上海200433 [2]第二军医大学长海医院麻醉科,上海200433

出　　处：《中国新药杂志》2006年第2期110-114,共5页Chinese Journal of New Drugs

基　　金：中国人民解放军医药卫生十五重点课题(01Z066)

摘　　要：目的:制备复方盐酸利多卡因巴布膏剂,并考察其黏性和体外释药特性。方法:采用盐酸利多卡因和中药三七组成复方,以水溶性高分子材料为基质制备。采用HPLC法测定制剂中盐酸利多卡因的含量,按2005年版《中华人民共和国药典》方法进行体外释放度、含膏量、赋形性及黏附性的测定,利用改良Franz扩散池研究巴布膏剂中盐酸利多卡因的透皮吸收行为。选择疱疹后神经性疼痛20例,将巴布膏剂贴于皮肤患区最痛处观察临床短期效果和不良反应。结果:复方盐酸利多卡因巴布膏剂中盐酸利多卡因含量为5 mg·cm-2,其体外释放速率为4．128 mg·cm-2·h-1。透皮吸收符合零级动力学过程,盐酸利多卡因渗透速率为0．091 mg·cm-2·h-1。每100 cm2巴布膏剂的含膏量为9．088 g,赋形性良好,初黏力能黏住13号钢球(φ9．525 mm,每个3．55 g)。止痛总有效率达85％,所有病例均未见不良反应。结论:复方盐酸利多卡因巴布膏剂为皮肤控释型透皮给药系统,对于神经性疼痛等具有显著疗效。Objective：To prepare compound lidocaine hydrochloride cataplasm and characterize its viscosity and dissolution features. Methods： The compound lidocaine hydrochloride cataplasm was composed of lidocaine hydrochloride, Radix Notoginseng powder and water-soluble matrix. The lidocaine hydrochloride in the compound was quantified by HPLC. The dissolution in vitro, ointment quantity, application feature and viscosity were assessed as per the methodologies under the China Pharmacopoeia 2005. The transdermal absorptions were characterized by using a modified Franz diffusion cell. Furthermore, the cataplasm was applied onto the most painful area of skin lesions in 20 patients with post-herpetic neuralgia to assess the short-term effects and safety. Results： The characteristics of lidocaine hydrochloride in the eataplasm were as follows： concentration of 5 mg·cm^-2; the dissolution rate in vitro of 4. 128 mg·cm^-2·h^-1 ; the permeable rate of 0. 091 mg·cm^-2·h^-1 in a zero order dynamic reaction. The cataplasm contained the ointment of 9. 088 g per 100 cm^2, and showed an adhesion to a steel ball （#13 size）. The overall effective rate of pain relief was 85%. No local or systemic adverse events were reported. Conclusion： The compound lidocaine hydrochloride cataplasm featured the transdermal controlled-release system that was effective in the relief of neuropathic pain.

关 键 词：盐酸利多卡因 三七 巴布膏剂 神经性疼痛 

分 类 号：R944.9[医药卫生—药剂学] R971.2[医药卫生—药学]