Formulation and pharmacokinetics of gelucire solid dispersions of flurbiprofen

Abstract

Context: Development of solid dispersions is to improve the therapeutic efficacy by increasing the drug solubility, dissolution rate, bioavailability as well as to attain rapid onset of action.

Objective: The present research deals with the development of solid dispersions of flurbiprofen which is poorly water soluble to improve the solubility and dissolution rate using gelucires.

Materials and methods: In this study, solid dispersions were prepared following solvent evaporation method using gelucire 44/14 and gelucire 50/13 as carriers in different ratios. Then the formulations were evaluated for different physical parameters, solubility studies, DSC, FTIR studies and in vitro dissolution studies to select the best formulation that shows rapid dissolution rate and finally subjected to pharmacokinetic studies.

Results and discussion: From the in vitro dissolution study, formulation F3 showed the better improvement in solubility and dissolution rate. From the pharmacokinetic evaluation, the control tablets produced peak plasma concentration (C_max) of 9140.84 ± 614.36 ng/ml at 3 h T_max and solid dispersion tablets showed C_max = 11 445.46 ± 149.23 ng/ml at 2 h T_max. The area under the curve for the control and solid dispersion tablets was 31 495.16 ± 619.92 and 43 126.52 ± 688.89 ng h/ml and the mean resident time was 3.99 and 3.68 h, respectively.

Conclusion: From the above results, it is concluded that the formulation of gelucire 44/14 solid dispersions is able to improve the solubility, dissolution rate as well as the absorption rate of flurbiprofen than pure form of drug.

• Control tablet
• dissolution rate
• peak plasma concentration
• solvent evaporation method
• solubility studies

Acknowledgements

The authors acknowledge the FDC Limited, Mumbai, India, Gattefosse and Matrix laboratories, Hyderabad, India for gift samples. The authors also thank to Management, Sri Shivani College of Pharmacy and Chaitanya College of Pharmacy Education and Research for providing facilities and thanks to Management of Vagdevi College of Pharmacy for providing ethical approval.

Declaration of interest

The authors report no conflicts of interest.