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气溶胶-OT微乳剂作为盐酸丁卡因的透皮载体

Aerosol-OT microemulsions as transdermal carriers of tetracaine hydrochloride.

作者信息

Changez M, Varshney M

机构信息

Department of Chemistry, Faculty of Science, Hamdard University, New Delhi, India.

出版信息

Drug Dev Ind Pharm. 2000 May;26(5):507-12. doi: 10.1081/ddc-100101261.

DOI:10.1081/ddc-100101261
PMID:10789062
Abstract

The aerosol-OT (AOT)/water/isopropyl myristate microemulsion was investigated as a carrier in transdermal drug delivery of tetracaine hydrochloride. The study included in vivo analgesic studies on rats and histopathological, irritation, and oxidative stress measurements on mice. The tetracaine hydrochloride encapsulated in AOT/water/isopropyl myristate showed an eightfold enhancement in the analgesic response of drug compared to the aqueous solution of the drug as measured by the tail-flick method. The analgesic response of tetracaine hydrochloride, however, highly depended on the concentration of AOT and water of the microemulsion. The preliminary histopathological, irritation, and oxidative stress studies showed that AOT/water/isopropyl myristate microemulsion system is a safe transdermal carrier of tetracaine hydrochloride with a concentration of AOT in isopropyl myristate up to 21:79 w/w.

摘要

研究了气溶胶-OT(AOT)/水/肉豆蔻酸异丙酯微乳液作为盐酸丁卡因透皮给药载体的情况。该研究包括对大鼠的体内镇痛研究以及对小鼠的组织病理学、刺激性和氧化应激测量。与通过甩尾法测量的药物水溶液相比,包裹在AOT/水/肉豆蔻酸异丙酯中的盐酸丁卡因的镇痛反应增强了八倍。然而,盐酸丁卡因的镇痛反应高度依赖于微乳液中AOT和水的浓度。初步的组织病理学、刺激性和氧化应激研究表明,AOT/水/肉豆蔻酸异丙酯微乳液体系是一种安全的盐酸丁卡因透皮载体,其中AOT在肉豆蔻酸异丙酯中的浓度高达21:79 w/w。

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