New Cocrystals of Antipsychotic Drug Aripiprazole: Decreasing the Dissolution Through Cocrystallization

Overview

Journal Molecules

Publisher MDPI

Specialty Biology

Date 2021 Apr 30

PMID 33919175

Citations 3

Authors

Wenwen Liu

Ru Ma

Feifei Liang

Chenxin Duan

Guisen Zhang

Yin Chen

Chao Hao

Affiliations

Soon will be listed here.

Abstract

Cocrystallization is an important route to tuning the solubility in drugs development, including improving and reducing. Five cocrystals of aripiprazole (ARI) with resveratrol (RSV) and kaempferol (KAE), ARI-RSV, ARI-RSV·MeOH, ARI-KAE, ARI-KAE·EtOH, ARI-KAE·IPA, were synthesized and characterized. The single crystal of ARI-RSV·MeOH, ARI-KAE·EtOH, and ARI-KAE·IPA were analyzed by single crystal X-ray diffraction (SCXRD). The SCXRD showed multiple intermolecular interactions between API and the coformers, including hydrogen bond, halogen bond, and π-π interactions. Dissolution rate of the two nonsolvate ARI-RSV and ARI-KAE cocrystals were investigated through powder dissolution experiment in pH = 4.0 acetate buffer and pH = 6.8 phosphate buffer. The result showed that RSV could reduce the dissolution rate and solubility of ARI in both medium through cocrystallization. However, KAE improved the dissolution rate and solubility of ARI in pH = 4.0 medium, on the contrary, the two solubility indicators of ARI were both reduced for ARI-KAE cocrystal.

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