Drug-Drug Cocrystallization Simultaneously Improves Pharmaceutical Properties of Genistein and Ligustrazine

被引：25

作者：

Li, Xuejiao ^{[1
]}

Liu, Xinna ^{[1
]}

Song, Jianmin ^{[2
]}

Wang, Chenguang ^{[3
]}

Li, Jinhui ^{[1
]}

Liu, Lianchao ^{[1
]}

He, Xin ^{[1
]}

Zhao, Xinghua ^{[1
]}

Sun, Changquan Calvin ^{[3
]}

机构：

[1] Hebei Agr Univ, Coll Vet Med, Baoding 071000, Hebei, Peoples R China

[2] Hebei Agr Univ, Coll Sci, Baoding 071000, Hebei, Peoples R China

[3] Univ Minnesota, Coll Pharm, Dept Pharmaceut, Pharmaceut Mat Sci & Engn Lab, Minneapolis, MN 55455 USA

来源：

CRYSTAL GROWTH & DESIGN | 2021年 / 21卷 / 06期

基金：

中国国家自然科学基金;

关键词：

ORAL BIOAVAILABILITY; N-OXIDES; SALT; TETRAMETHYLPYRAZINE; NANOPARTICLES; CAFFEINE; FORMS; RAT;

D O I：

10.1021/acs.cgd.1c00229

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The oral delivery of genistein (GEN) is hindered by its low bioavailability. The delivery of tetramethylpyrazine (TMP or ligustrazine) is faced with physical instability challenges due to its high sublimation tendency. We tackled respective challenges of the two drugs by forming a cocrystal. The GEN-TMP cocrystal exhibits a significantly reduced sublimation tendency than TMP and a significant enhancement in both the in vitro release rate and bioavailability in rats than GEN. Thus, cocrystallization simultaneously improves pharmaceutical properties of both parent drugs.

引用

页码：3461 / 3468

页数：8