A COMPARATIVE BIOAVAILABILITY OF FUROSEMIDE IN SOLID DISPERSIONS FORMS

Yandi Syukri, Lukman Hakim, Tedjo Yuwono

Abstract


Furosemide is a poorly soluble diuretic drug, the solubility of which can be enhanced by solid dispersion with polyvinylpirolidon (PVP). The solid dispersion system was prepared by a solvent method in various ratios of 1 : 5 and 1 : 7 of the drug and PVP, respectively, in order to improve furosemide bioavailability. The bioavailability of furosemide - PVP solid dispersion was compared with pure furosemide (control) and Lasix (reference). The study was done in a cross over design with a single-dose peroral that administered to the white male rabbits (n = 6). Furosemide blood levels were determined spectrofluorometrically by an extraction method. The area under the blood concentration-time curve AUC0 - , peak blood concentration Cmax and time to reach peak blood concentration Tmax were used to compare their bioavailabilities. The solid dispersion systems produced a higher extent of bioavailability than pure furosemide (P < 0,05). On the contrary, no statistically significant difference about the extent of bioavailability between solid dispersion and Lasix (P > 0,05). Finally, furosemide – PVP solid dispersion (1 : 7) was the best formulation with the highest extent of bioavailability and bioequivalence with the Lasix formula.

Key Word : Solid dispersion, solubility, dissolution, bioavailability, furosemide.


Full Text:

Untitled

References


Akbuga, J., Gursoy, A., and Kendi, E., 1988, The Preparation and Stability of Fast Release Furosemide – PVP Solid Dispersion, Drug-Dev. Ind. Pharm, 14 (10), 1439-1464

Chiou, W.L., and Riegelman, S., 1971, Pharmaceutical Application of Solid Dispersion System, J. Pharm. Sci., 60 (9), 1281-1301

Hakim, L., 1996, Eksresi Urin Furosemida pada Kelinci setelah Pra-Perlakuan dengan Bunga Kubis, Laporan Penelitian Universitas Gadjah Mada, Yogyakarta, halaman 8 – 10.

Kelly, M.R., Cutler, R.E., Forrey, A.W., and Kimpel, B.M., 1974, Pharmacokinetics of Orally Administered Furosemide, Clin. Pharmacol. Ther., 15, 178-186

Santoso, S., 2000, SPSS, Mengolah Data Statistika secara Profesional, Gramedia, Jakarta, halaman 371 – 380.

Shargel, L., and Yu, A.B.C., 1993, Applied Biopharmaceutics and Pharmacokinetics, Appleton-Century-Crofts, Norwalk, halaman 193 – 211.




DOI: http://dx.doi.org/10.14499/indonesianjpharm0iss0pp28-32

Refbacks

  • There are currently no refbacks.




Copyright (c) 2017 INDONESIAN JOURNAL OF PHARMACY

Creative Commons License
This work is licensed under a Creative Commons Attribution-ShareAlike 4.0 International License.

Indonesian J Pharm indexed by:

web
analytics View My Stats