Enhanced Bioavailability Of Flurbiprofen Using Gelucire 44/14 And Labrasol As Semi-Solid Dispersions

Abstract

This study was to investigated the in-vivo performance of semi-solid dispersion of flurbiprofen prepared with Gelucire 44/14 and Labrasol (F1) and pure drug (PD) filled in hard gelatin capsules. Methods: Oral bioavailability of 50 mg of semi-solid dispersion of flurbiprofen (F1) was compared with pure flurbiprofen filled into hard gelatin capsules (PD) after administration of a single oral dose to six healthy human volunteers. Two treatments were administered in crossover fashion, separated by a washout period of two weeks. Venous blood sample of 5 ml was taken immediately before dosing and after predetermined time intervals of 0, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, and 24 h. Flurbiprofen was monitored in serum by high- performance liquid chromatography. Results. The apparent rate of absorption of semi-solid dispersion of flurbiprofen from F1 was observed. The Cmax ± S.D. was found to be 50.45 ± 2.2634 µg/ml, and tmax ± S.D. was 1.5 ± 0 h and the AUC ± S.D. value was 367.47 ± 25.377 µg/ml which was significantly higher than that from PD with Cmax ± S.D. 16.06 ± 1.211 µg/ml, tmax ± S.D. was 2 ± 0 h, and AUC ± S.D. value was 201.28 ± 42.52 µg/ml . The relative bioavailability value as the ratios of mean total AUC for F1 relative to AUC for PD was 182.56 %. Conclusion. The results indicates that the bioavailability of flurbiprofen can be enhanced as semi-solid dispersions with Gelucire 44/14 and Labrasol, which would be advantageous with regards to rapid onset of action especially in various painful conditions where acute analgesic effect is desired.

Egyptian Journal of Biomedical Sciences Vol. 23 (1) 2007: pp. 15-24