Spray dried solid dispersion of repaglinide using hypromellose acetate succinate: in vitro and in vivo characterization

Abstract

Objective

This research study attempted to develop spray-dried solid dispersion, to enhance the solubility of repaglinide, an antidiabetic drug.

Significance

Aqueous solubility plays a major role in drug delivery because any chemical entity has to be in a dissolved state at the site of absorption, in order to get absorbed. Solid dispersion (SD) is one of the widely used techniques to enhance solubility and hence dissolution rate of poorly soluble drugs.

Methods

Repagnilide, in hypromellose acetate succinate (HPMCAS) solution, was dried by spray drying to obtain spray-dried solid dispersion (SDSD). Plackett–Burman and Box–Behnken designs were used for screening formulation as well as process parameters, and optimization respectively. DSC, XRD, SEM were carried out to confirm the preparation of solid dispersion. SDSD was evaluated for in vitro dissolution, flow properties, Percentage yield and in vivo oral glucose tolerance test.

Result

Spray dried solid dispersion comprising (w/w) drug:polymer ratio of 1:3.82, 2.56% of aerosil and inlet temperature of 90 °C, corresponded to the best formulation obtained in this work. It showed t₈₅% of less than 15 min and a significant reduction in blood glucose level in rats as compared to pure drug and marketed formulation.

Conclusion

Thus, it can be concluded that spray-dried solid dispersion prepared using HPMCAS is a useful technique for solubility and dissolution enhancement of repaglinide.

Keywords:

• Spray dried solid dispersion
• bioavailability
• antidiabetic drug
• HPMCAS
• oral glucose tolerance test
• amorphization

Disclosure statement

No potential conflict of interest was reported by the author(s).