Acta Univ. Palacki. Olomuc., Fac. Med. Volume 141, 1998

PERCUTANEOUS ABSORPTION OF DISOPYRAMIDE, LIDOCAINE AND TRIMECAINE

Jan Příborskýa,b, Katsuya Kikuchic, Kozo Takayamac, Tsuneji Nagaic
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

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Příborský, J., Kikuchi, K., Takayama, K., & Nagai, T. (1998). PERCUTANEOUS ABSORPTION OF DISOPYRAMIDE, LIDOCAINE AND TRIMECAINE. Biomedical papers141(1), 
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References

  1. 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...
  2. 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...
  3. 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...
  4. 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.
  5. 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...
  6. 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.
  7. Flavouring Extract Manufacturers Association (1965) Survey of flavouring ingredient usage levels. No. 2633. Fd. Technol. Champaign 19, part 2, p. 155.
  8. 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.
  9. Thomas, A. F., Bessiere, Y. (1989) Limonene. Natural Product Reports 6, 291-309. Go to original source...
  10. 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...
  11. 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.
  12. Sarpotdar, P. P. (1985) UK Patent application. GB 2158355 A.
  13. 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.
  14. 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...
  15. 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.
  16. 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...