Acta Univ. Palacki. Olomuc., Fac. Med. Volume 141, 1998
PERCUTANEOUS ABSORPTION OF DISOPYRAMIDE, LIDOCAINE AND TRIMECAINE
- a Glaxo Wellcome s.r.o., K Žižkovu 4, 190 00 Prague, Czech Republic
- b Institute of Pharmacology, Faculty of Medicine, Palacký University, Hněvotínská 3, 77 515 Olomouc, Czech Republic
- c Department of Pharmaceutics, Hoshi University, Ebara 2-4-41, Shinagawa-ku, Tokyo 142, Japan
Promoting effect of cyclic monoterpenes on percutaneous absorption of antiarrhytmic drugs disopyramide, lidocaine andtrimecaine was investigated in the rats. Laurocapram (Azone) was used as a standard comparator of penetration enhancement.The absorption of trimecaine was significantly enhanced by addition of limonene, trans-p-menthane and Azone in1% concentration. Lidocaine and disopyramide penetrated across the skin only when 1% of limonene was used. Othercyclic monoterpenes showed no effect on percutaneous absorption of examined drugs.
Keywords: Antiarrhytmic drugs, Penetration enhancer, Cyclic monoterpenes
Published: July 1, 1998 Show citation
References
- Akitoshi, Y., Takayama, K., Machida, Y., Nagai, T. (1988) Effect of cyclohexanone derivatives of percutaneous absorption of ketoprofen and indomethacin. Drug Design and Delivery, 2, 239-245.
Go to PubMed...
- Okabe, H., Takayama, K., Ogura, A., Nagai, T. (1989) Effect of limonene and related compounds on the percutaneous absorption of indomethacin. Drug Design and Delivery 4, 313-321.
Go to PubMed...
- Sugibayashi, K., Nemoto, M., Morimoto, Y. (1988) Effect of several penetration enhancers on the percutaneous absorption of indomethacin in hairless rats. Chem. Pharm. Bull. 34, 1519-1528.
Go to original source...
Go to PubMed...
- Marty, J. P., Dervault, A. M., Chanez, J. F., Doucet, O., Samour, C. M. (1989) Effect of dioxolanes on indomethacin in vitro percutaneous absorption enhancement. Proceed. Intern. Symp. Control. Rel. Bioact. Mater 16, 179.
- Williiams, A. C., Barry, B. W. (1989) Essential oils as novel human skin penetration enhancers. Int. J. Pharm. 57, R7-R9.
Go to original source...
- Barry, B. W., Williams, A. C. (1989) Human skin penetration enhancement: The synergy of propylene glycol with terpenes. Proceed. Intern. Symp. Control. Rel. Bioact. Mater. 16, 33-34.
- Flavouring Extract Manufacturers Association (1965) Survey of flavouring ingredient usage levels. No. 2633. Fd. Technol. Champaign 19, part 2, p. 155.
- Council of Europe (1974) Natural Flavourin Substances, Their Sources and Added Artificial Flavouring Substances. Partial Agreement in the Social and Public Health Field. List 1 no. 491, p. 227. Strasbourg.
- Thomas, A. F., Bessiere, Y. (1989) Limonene. Natural Product Reports 6, 291-309.
Go to original source...
- Proelss, F. H., Towsend, T. B. (1986) Simultaneous liquid-chromatographic determination of five antiarrhythmic drugs and their major active metabolites in serum. Clin. Chem. 32, 1311-1317.
Go to original source...
- Příborský, J., Takayama, K., Nagai, T., Waitzová, D., Elis, J. (1987) Combination effect of penetration enhancers and propylene glycol on in vitro transdermal absorption of insulin. Drug Design Delivery 2, 91-97.
- Sarpotdar, P. P. (1985) UK Patent application. GB 2158355 A.
- Das, S. K., Chattaraj, S. C., Gupta, B. K. (1989) Development and optimisation of verapamil transdermal patch. Proceed. Intern. Symp. Control. Rel. Bioact. Mater 16, 288-289.
- Siddiqui, O., Roberts, M. S., Polack, A. E. (1985) The effect of iontophoresis and vehicle pH on the in vitro permeation of lignocaine through human stratum corneum. J. Pharm. Pharmacol. 37, 732-735.
Go to original source...
Go to PubMed...
- Sage, B. H., Riviere, J. E. (1989) Optimisation of iontophoretic flux of lidocaine using the isolated perfused porcine skin flap. Proceed. Intern. Symp. Control. Rel. Bioact. Mater. 16, 49.
- Miller I. I., K. J., Rao, I. K., Goldwin, S. R., Westermann-Clark, G. B., Shah, D. O. (1993) Solubility and in vitro percutaneous absorption of tetracaine from solvents of propylene glycol and saline. Int. J. Pharm. 98, 101-111.
Go to original source...