局部麻醉药利多卡因透皮吸收的研究

评价了局部麻醉药利多卡因的透皮吸收和制成压敏胶粘贴片皮肤局部给药麻醉的可能性。在考察利多卡因游离碱(分子型)和盐酸盐(离子型)从水和硅酮中透过无毛鼠皮肤的基础上,试制了利多卡因游离碱的橡胶型压敏胶粘贴片,对药物的体外释放和皮肤透过进行了考察,并与日本的利多卡因凝胶剂(xylocainejelly)的皮肤透过进行了比较,考察了10%～60%的利多卡因压敏胶粘贴片中药物浓度与皮肤透过之间的关系。

FEASIBILITY ASSESSMENT OF SKIN PERMEATION FOR THE LOCAL ANESTHETIC LIDOCAINE

In this paper, the feasibility of skin permeation for lidocaine and pressure sensitive adhesive(PSA)tape formulation containing lidocaine for skin local anesthetic were assessed. Firstly,in vitro skin permeation of the molecular and ionic forms of lidocaine from water and silicone fluid suspensions was measured using a side- by-side two diffusion cells and excised hairless rat skin.Secondly, PSA tape containing lidocaine was prepared by a general casting method using styrene-isoprene─styrene block copolymer. The in vitro release and skin permeation were evaluated and compared with that of Japan marketed xylocaine jelly. The effect of lidocaine concentration on the steady-state flux of skin permeation from 10%to 60%lidocaine PSA tapes was also evaluated.