Development of lidocaine gels for enhanced local anesthetic action.
作者： Sang-Chul Shin , Cheong-Weon Cho , Kyu-Ho Yang
DOI: 10.1016/J.IJPHARM.2004.08.012
关键词:
摘要: In relieving local pains, lidocaine, one of ester type anesthetics, has been used. To develop the lidocaine gels enhanced anesthetic effects, hydroxypropyl methylcellulose (HPMC) based bioadhesive polymer gel containing an enhancer was formulated. As drug concentration in increased up to 3%, permeation rate linearly increased, thereafter reaching a plateau. temperature surrounding solutions increased. The activation energy 3.29 kcal/mol for lidocaine. through skin studied using various enhancers, such as glycols, non-ionic surfactants, and bile salts. Among enhancers studied, diethylene glycol showed greatest enhancing effects on skin. analgesic activity examined tail-flick analgesimeter. area under efficacy curve (AUEC) rat-tail flick tests, about 3.89-fold increase compared with control. addition vasoconstrictor prolonged effects. result this study supports that efficient effect could be developed HPMC combination vasoconstrictor.
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