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Development of Lidocaine Gels for Enhanced Local Anesthetic Action by Sang-Chul Shin; Cheong-Weon Cho; Kyu-Ho Yang is a Pharmacology, Toxicology and Pharmaceutics article available to read on EtoBox.

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In relieving local pains, lidocaine, one of ester type local anesthetics, has been used. To develop the lidocaine gels of enhanced local anesthetic effects, hydroxypropyl methylcellulose (HPMC) based bioadhesive polymer gel containing an enhancer was formulated. As the drug concentration in the gels increased up to 3%, the permeation rate of drug linearly increased, thereafter reaching a plateau. As the temperature of surrounding solutions increased, the permeation of drug increased. The activation energy of drug permeation was 3.29 kcal/mol for lidocaine. The permeation rate of drug through skin was studied using various enhancers, such as glycols, non-ionic surfactants, and bile salts. Among the enhancers studied, diethylene glycol showed the greatest enhancing effects on drug permeation through skin. The analgesic activity was examined using a tail-flick analgesimeter. In the area under the efficacy curve (AUEC) of the rat-tail flick tests, lidocaine gel containing diethylene glycol showed about 3.89-fold increase in analgesic activity compared with the control. The addition of vasoconstrictor in the gels prolonged the analgesic effects. The result of this study supports that th

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Author

Sang-Chul Shin; Cheong-Weon Cho; Kyu-Ho Yang

Publisher

Elsevier Science; Elsevier ; Elsevier BV (ISSN 0378-5173)

Published

2004

Language

EN

Field

Pharmacology, Toxicology and Pharmaceutics (Life Sciences)