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Information Journal Paper

Title

DEVELOPMENT OF BIOADHESIVE TRANSDERMAL BUPIVACAINE GELS FOR ENHANCED LOCAL ANESTHETIC ACTION

Pages

  423-431

Abstract

 Topical drug dosage forms such as ointments and creams can be easily removed through wetting, movement and contact. The new bioadhesive formulations with enhanced local anesthetic effects are needed for topical administration. The adhesive capacity of hydroxypropyl methylcellulose (HPMC) was determined by measuring the maximum detachment force and the adhesion work with an auto peeling tester. The release of drug from a HPMC gel was studied according to the drug concentration. Permeation study through the rat skin was performed at 37oC using phosphate buffer solution (pH=7.4) as a receptor medium. To increase the skin permeation of BUPIVACAINE from the HPMC GELS, PENETRATION ENHANCER such as the saturated and unsaturated fatty acids, the pyrrolidones, the propylene glycol derivatives, the glycerides, and the non-ionic surfactants were incorporated in the BUPIVACAINE-HPMC GELS. The local anesthetic effect of the formulated gel preparation was examined using a tail-flick analgesimeter. As the concentration of HPMC increased, the bioadhesive force and viscosity were increased. The rate of drug release was increased with increasing the drug concentration. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the most enhancing effects on drug permeation through the skin. In the rat tail flick test, the area under the efficacy curve of BUPIVACAINE gel containing polyoxyethylene 2-oleyl ether and tetrahydrozoline showed a 2.36-fold increase in anesthetic activity compared to control gel without any additives. The BUPIVACAINE GELS containing both PENETRATION ENHANCER and vasoconstrictor showed enhancement and prolonged efficacy compared to the control gel. To enhance the local anesthetic effects of BUPIVACAINE, the TRANSDERMAL BUPIVACAINE gel formulation containing PENETRATION ENHANCER and vasoconstrictor could be developed.

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    • Cite

    APA: Copy

    CHO, CHEONG WEON, KIM, DEOK BAE, & SHIN, SANG CHUL. (2012). DEVELOPMENT OF BIOADHESIVE TRANSDERMAL BUPIVACAINE GELS FOR ENHANCED LOCAL ANESTHETIC ACTION. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), 11(2), 423-431. SID. https://sid.ir/paper/287951/en

    Vancouver: Copy

    CHO CHEONG WEON, KIM DEOK BAE, SHIN SANG CHUL. DEVELOPMENT OF BIOADHESIVE TRANSDERMAL BUPIVACAINE GELS FOR ENHANCED LOCAL ANESTHETIC ACTION. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR)[Internet]. 2012;11(2):423-431. Available from: https://sid.ir/paper/287951/en

    IEEE: Copy

    CHEONG WEON CHO, DEOK BAE KIM, and SANG CHUL SHIN, “DEVELOPMENT OF BIOADHESIVE TRANSDERMAL BUPIVACAINE GELS FOR ENHANCED LOCAL ANESTHETIC ACTION,” IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), vol. 11, no. 2, pp. 423–431, 2012, [Online]. Available: https://sid.ir/paper/287951/en

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