Optimizing the Formulation for Ginkgolide B Solid Dispersion

Open Life Sci. 2018 Aug 21:13:253-262. doi: 10.1515/biol-2018-0031. eCollection 2018 Jan.

Abstract

The main purpose of our study is to optimize the formulation for Ginkgolide B (GB) solid dispersion in order to improve its dissolution in water. For the preparation of GB solid dispersion, we use a solvent method. The optimized formulation consists of GB : PVPK30 = 1:10, PVPK30 as the carrier, and ethanol : dichloromethane = 1:1 as the solvent. They were treated ultrasonically for 10 min at 60°C. The results from scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD), and particle size analysis show that the morphological appearance of GB changed significantly in solid dispersion. The original crystal form of GB no longer existed, but it was uniformly dispersed within PVPK30 in a non-crystalline form. It is probably because the -C=O in GB forms hydrogen bonds with the -OH of PVPK30 or urea; this produces a nice solid dispersion and significantly improves the dissolution of GB in water. When GB is in a solid dispersion system, GB's dissolution in water could be enhanced from 30% to 80%. Furthermore, it may even be produced as a solid agent.

Keywords: Crystal; Ginkgolide B; Rate of dissolution; Solid dispersion.