THE SULPHAMETHOXAZOLE BIOAVAILABILITY OF POLYMORPH IIA IN RABBITS

Siti Nurasiyah; Tedjo Yuwono

doi:10.14499/indonesianjpharm0iss0pp205-210

THE SULPHAMETHOXAZOLE BIOAVAILABILITY OF POLYMORPH IIA IN RABBITS

Siti Nurasiyah, Tedjo Yuwono

Abstract

Sulphamethoxazole, a sulphonamide antibacteria, is usually combined with trimetoprime, namely cotrimoxazole, to obtain higher potency. Because of the solubility of sulphamethoxazole in water is minute, its dissolution rate would be slow. Consequently, dissolution rate become the limiting step in the absorption process. In order to overcome this problem, therefore, some polymorph forms of sulphamethoxazole were created. The previous study found a polymorph IIA crystal form, a new modified internal crystal structure of sulphamethoxazole. This study was a continuing investigation of the bioavailability of the polymorph IIA, in capsule dosage forms, in rabbits. It was evident that the bioavailability of polymorph IIA was twice of that polymorph I. The bioavailability parameter changes of polymorph I to polymorph IIA were: the AUC increased from 872 to 1,530 mg hr L-1, the peak time (tmax) increased from 2 hours to 0.9 hours, the blood plasma level peak (Cpmax) increased from 104 to 136 mg/ L-1.

Key words: bioavailability, sulphamethoxazole polymorph

Full Text:

Untitled

References

Carstensen, J. T., 1974, Theories of Dissolution Single Particulate Systems in: Leeson L.J. and Carstensen, J. T. (Ed.) Dissolution Technology, The Industrial Pharmaceutical Technology Section of the Academy Pharmaceutical Science, Washington, D.C., 1-28.

Haleblian, J. K., 1975, Characterization of Habits and Crytaline Modification of Solids and Their Pharmaceutical Applications, J Pharm. Sci, 64, 1269 - 1288.

Kaplan, S.A., 1973, Biopharmaceutics in the Preformulation Studies Stages of Drug Development in: Swarbrick, J. (Ed.), Current Concepts in Pharmaceutical Science: Dosage Form Design and Bioavailability, Chapter I, Lea & Febiger, Philadelphia, 2 - 30.

Nichols, W. K., 1995, Anti-Infectives in: Gennaro, A. R., (Ed.), The Science and practice of Pharmacy, 19th Ed., Vol. II, Mack Publishing Company, Easton, 1263 - 1336.

Richterich, R. and Colombo, L. P., 1981, Clinical Chemistry, John Wiley & Sons, New York, 467.

Ritschel, W. A., 1980, Handbook of Basic Pharmacokinetics, 2nd , Drug Intelligence Publication, Inc., Hamilton, 322- 327.

Shargel, L., and Yu, A. B. C., 1993, Applied Biopharmaceutics and Pharmacokinetics, 3rd Ed., Appleton & Lange, Norwalk, 33 -45, 193 - 223.

Turner, R.H., Mechta, C.S., and Benet, L.Z., 1970, Apparent Directional Permeability Coeficient for Drug Ions: In Vitro Intestinal Perfusion Studies, J. Pharm. Sci., 59, 590 - 595.

Yang, S. S. and Guillory, J. K., 1972, Polymorphism of Sulfonamide, j. Pharm. Sci., 61,26 - 40.

Yuwono, T., dan Namtini, S. S., 1991, Pembentukan Polimorfi Sulfametoksazol, MFI, 2, 27 - 33.

DOI: http://dx.doi.org/10.14499/indonesianjpharm0iss0pp205-210