超声波促进盐酸利多卡因经皮渗透的研究

Enhancing Topical Delivery of Lidocaine Hydrochloride Using Sonophoresis

关键词:  盐酸利多卡因  超声波  经皮渗透

Key words:  lidocaine hydrochloride  sonophoresis  percutaneous permeation

摘要:

目的 研究低频超声波对盐酸利多卡因凝胶经皮渗透的促进作用。方法 制备2.5%盐酸利多卡因凝胶；应用单室扩散池和乳猪皮肤，测定盐酸利多卡因凝胶在20 kHz超声波作用下，利多卡因的经皮渗透性能，并以复方利多卡因乳膏作为对照品，用HPLC测定接受液中的盐酸利多卡因浓度；考察超声强度和作用持续时间等因素的影响。结果 超声波能明显促进盐酸利多卡因的经皮渗透，且随着超声强度的增加和超声作用持续时间的延长，促渗效果明显增强；功率为2.26 W·cm^-2，持续时间5 min的超声波处理皮肤，盐酸利多卡因凝胶的2 h累积经皮渗透量是被动扩散的9.3倍，是复方利多卡因乳膏的2.4倍。结论 超声波能显著促进盐酸利多卡因凝胶的经皮渗透，2 h内的体外透皮速率大于复方利多卡因乳膏，可发展成为血管穿刺止痛的新给药方法。

Abstract:

OBJECTIVE To evaluate promote efficacy of low frequency sonophoresis at 20 kHz on transdermal permeation of lidocaine hydrochloride gel. METHODS The lidocaine hydrochloride gel was preparated, permeation studies were carried out in vitro on excised suckling pig skin over a period of 2 h using one- chamber diffusion cells. The concentration of lidocaine in receptor solution was analyzed by HPLC. The permeation capability of lidocaine hydrochloride gel with and without ultrasound were determined, and compound lidocaine cream was used as a control. Parameters like ultrasound output powers and application time were tested. RESULTS Application of ultrasound could significantly promote the percutaneous permeation of lidocaine hydrochloride. With increasing ultrasonic intensity and duration, the promote effect was significantly enhanced. When ultrasound output power was 2.26 W·cm^-2 and application duration was 5 min, the cumulative amount of permeated lidocaine hydrochloride was 9.3 times higher than passive control, and 2.4 times higher than compound lidocaine cream. CONCLUSION Low frequency sonophoresis can be effectively used to enhance transdermal delivery of lidocaine hydrochloride. Sonophoresis mediated topical delivery of lidocaine hydrochloride can be developed as a drug delivery method for the prevention of pain from needle prick during the injection.