Enhancement of dissolution and bioavailability of flurbiprofen by low molecular weight chitosans.

The dissolution behavior and absorption of flurbiprofen (FP) following oral administration from:three types of chitosans (LM chitosans), with different molecular weights and degree of acetylation, have been studied in comparison with those of the drug alone. The solubility of FP increased with concentrations of LM chitosan, especially in the case of C-III, with the highest degree of deacetylation degree among the three chitosans. This indicates that amino groups of LM chitosan play an important role in its interaction with FP. Moreover, spectroscopic studies, including NMR data, indicate that the binding involves interactions between the carboxyl group of FP and the amino group of the chitosans. The dissolution rates of FP for a C-III kneaded mixture were enhanced with increasing amounts of C-III. The oral absorption of FP from a C-III kneaded mixture was improved to a significant extent, compared to FP alone. These results suggest that FP from LM chitosan kneaded mixture increases the dissolution rate and improves the bioavailability of the drug by the formation of a water-soluble complex.

In vivo evaluation of hydrochlorothiazide liquisolid tablets in beagle dogs.

This study was carried out to evaluate the absorption characteristics of experimentally developed hydrochlorothiazide liquisolid tablets using six male beagle dogs. Comparison with reference commercial tablets was made. As no bibliographic data were found for the pharmacokinetic parameters of the drug in dogs, an intravenous drug administration was included in the study. The drug was administered orally as a single 25 mg dose of commercial and liquisolid tablets on two occasions in a randomized two-way crossover design. The pharmacokinetic parameters of the drug post intravenous dosing were reported for the first time. The results of the oral administration revealed statistically significant differences between the liquisolid and the commercial tablets in the area under the plasma concentration-time curve, the peak plasma concentration, and the absolute bioavailability. On the other hand, no significant differences were observed between the two formulations with regard to the mean residence time, the mean absorption time, and the rate of absorption. The absolute bioavailability of the drug from the liquisolid tablets was 15% higher than that from the commercial one. The parametric 90% confidence intervals for the different parameters were higher than the commonly expected intervals for bioequivalency, indicating greater bioavailability of the liquisolid tablets.