Preparation and Characterization of Aprepitant Solid Dispersion with HPMCAS-LF

Jinwen Liu; Yongji Li; Wuliji Ao; Yingge Xiao; Meirong Bai; Shuyan Li

doi:10.1021/acsomega.2c04021

Preparation and Characterization of Aprepitant Solid Dispersion with HPMCAS-LF

ACS Omega. 2022 Oct 24;7(44):39907-39912. doi: 10.1021/acsomega.2c04021. eCollection 2022 Nov 8.

Authors

Jinwen Liu^{1

2}, Yongji Li², Wuliji Ao³, Yingge Xiao¹, Meirong Bai⁴, Shuyan Li¹

Affiliations

¹ College of Traditional Mongolian Medicine, Inner Mongolia Minzu University, Tongliao 028000, China.
² School of Pharmacy, Heilongjiang University of Traditional Chinese Medicine, Harbin 150040, China.
³ Inner Mongolia Research Institute of Traditional Mongolian Meweight ratios ofdicine Engineering, Tongliao 028000, China.
⁴ Key Laboratory of Monglian Medicine Research and Development Engineering, Ministry of Education, Tongliao 028000, china.

Abstract

This study focused on improving the physicochemical characteristics of aprepitant with poor water solubility by preparing solid dispersion (SD). To prepare the SD with HPMCAS-LF, the solvent evaporation method was applied. Based on dissolution analysis, the dissolution rate of SD increased by five times compared with aprepitant. In addition, scanning electron microscopy (SEM), X-ray powder diffraction (XRPD), and differential scanning calorimetry (DSC) results suggested the presence of amorphous-form aprepitant inside SD. According to Fourier transform infrared (FTIR) spectroscopy, intermolecular hydrogen bonds were detected between polymer and aprepitant. The Caco-2 cell experiment proved that SD did not lower the transepithelial electrical resistance (TEER) values but improved the permeation amount of aprepitant. Additionally, the SD of aprepitant displayed excellent stability.