Antihistamine Effects of Triprolidine from the Transdermal Administration of the TPX Matrix in Rats

  • 발행 : 2005.01.01

초록

The antihistamine effects of the triprolidine were studied in rats to determine the feasibility of their enhanced transdermal delivery from the poly (4-methyl-1-pentene) (TPX) matrix system containing penetration enhancer and plasticizer. The antihistamine effects were determined by the Evans blue dye procedure by comparing the changes in vascular permeability increase following the transdermal administration. The vascular permeability increase was significantly reduced by transdermal administration of the triprolidine-TPX system containing triethyl citrate (TEC) and polyoxyethylene-2-oleyl ether (POE). Both the plasticizer and penetration enhancer played an important role in the skin permeation of triprolidine and increased the antihistamine effects. These results showed that the triprolidine-TPX matrix system containing plasticizer and penetration enhancer could be a transdermal delivery system providing the increased antihistamine effects.

키워드

참고문헌

  1. Chien, Y. W., 'Transdermal controlled systemic medications', Marcel Dekker, Inc., New York and Basel, pp. 132-137 (1987)
  2. Gennaro, A. R., Remington (Eds.). The science and practice of pharmacy. 19th ed., Mack publishing company, Easton, PA, pp. 1207-1218 (1995)
  3. Hadgraft, J., 'Transdermal drug delivery', Marcel Dekker, Inc., New York and Basel, pp. 298-300 (1987)
  4. Holgate, S. T., The mast cell and its function in allergic disease. Clin. Exp. Allergy, 21, 11-16 (1991) https://doi.org/10.1111/j.1365-2222.1991.tb01758.x
  5. Inagaki. N., Miura, T., Nagai, H., Ono, Y., and Koda, A., Inhibition of vascular permeability increase in mice - An addition anti-allergic mechanism of glucocorticoids. Int. Arch. Allergy Appl. Immunol., 87, 254-259 (1998)
  6. Katayama, S., Shionoya. H., and Ohtake, S., A new method for extraction of extravasated dye in the skin and the influence of fasting stress on passive cutaneous anaphylaxis in guinea pigs and rats. Microbiol. Immunol., 22, 89-101 (1978)
  7. Morimoto, Y., Seki, T., Sugibayashi, K., Juni, K., and Miyazaki, S., Basic studies on controlled transdermal delivery of nicardipine hydrochloride using ethylene-vinyl acetate and ethylene-vinyl alcohol copolymer membranes. Chem. Pharm. Bull., 36, 2633-2641 (1988) https://doi.org/10.1248/cpb.36.2633
  8. Ocak, F. and Agabeyoglu, I., Development of a membranecontrolled transdermal therapeutic system containing isosorbide dinitrate. Int. J. Pharm., 180, 177-183 (1999) https://doi.org/10.1016/S0378-5173(99)00005-8
  9. Shin, S. C. and Yoon, M. K., Application of TPX polymer membranes for the controlled release of triprolidine. Int. J. Pharm., 232, 131-137 (2002) https://doi.org/10.1016/S0378-5173(01)00906-1
  10. Shin, S. C. and Choi, J. S., Enhanced bioavailability of triprolidine from the transdermal TPX matrix. Int. J. Pharm., 234, 67-73 (2002) https://doi.org/10.1016/S0378-5173(01)00960-7
  11. Shin, S. C., Kim, J., Yoon, M. K., Oh, I. J., and Choi, J. S., Transdermal delivery of triprolidine using TPX polymer membrane. Int. J. Pharm., 235, 141-147 (2002) https://doi.org/10.1016/S0378-5173(01)00996-6
  12. Stevens, R. L. and Austen, J. F., Recent advances in the cellular and molecular biology of mast cells. Immunol. Today, 10, 381-386 (1989) https://doi.org/10.1016/0167-5699(89)90272-7