生物等效性和生物利用度杂志

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Formulation and Pharmacokinetics of Vitamin E TPGS Melt Dispersion Granules: An Approach to Improve Oral Delivery of Flurbiprofen

Abdul Bari Mohd and Sateesh Kumar Vemula

Formulation of solid dispersions using BCS class II drugs is one of the fruitful technologies to improve the drug solubility and dissolution rate to improve the bioavailability, but suffers from poor flowability and stability. To overcome the above problems, present research was intended to prepare the solid dispersions using combination of melt dispersion and surface adsorption methods. In the present study flurbiprofen melt dispersion granules were prepared by incorporating vitamin E TPGS as the carrier material and lactose as an adsorbent to improve the dissolution rate and flowability. Melt dispersion granules were evaluated for angle of repose, solubility studies, differential scanning calorimetry, in vitro dissolution studies, stability studies and finally subjected to pharmacokinetic studies. From the differential scanning calorimetry studies, change in the drug peak in formulation revealed the change in drug crystallinity. F4 formulation showed not only good flowability but also complete drug release in 15 min when compared to other formulations and pure drug. From the pharmacokinetic evaluation, F4 formulation showed 1.38- fold higher bioavailability and 1.32-fold higher Cmax compared to plain flurbiprofen. Hence, the formulated vitamin E TPGS melt dispersion granules were able to improve the dissolution rate as well as the bioavailability of flurbiprofen.