文献类型：期刊文献

英文题名：Drug-Drug Cocrystals Provide Significant Improvements of Drug Properties in Treatment with Progesterone

作者：Guo, Chunyang[1,2];Zhang, Qi[3];Zhu, Bingqing[3];Zhang, Zaiyong[3];Ma, Xiaoyu[3,4];Dai, Wenjuan[3];Gong, Xiaoyi[3];Ren, Guobin[1,2];Mei, Xuefeng[3]

机构：[1]East China Univ Sci & Technol, Lab Pharmaceut Crystal Engn & Technol, Sch Pharm, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Shanghai Key Lab New Drug Design, Sch Pharm, Shanghai 200237, Peoples R China;[3]Chinese Acad Sci, Shanghai Inst Mat Med, Pharmaceut Analyt & Solid State Chem Res Ctr, Shanghai 201203, Peoples R China;[4]Univ Chinese Acad Sci, Beijing 100049, Peoples R China

年份：2020

卷号：20

期号：5

起止页码：3053

外文期刊名：CRYSTAL GROWTH & DESIGN

收录：;EI(收录号：20202108705558);WOS:【SCI-EXPANDED(收录号:WOS:000535174000027)】；

基金：We acknowledge the support from the National Natural Science Foundation of China (Grant Nos. 21576080 and 21776073), Shanghai Natural Science Foundation (Grant No. 18ZR1447900), Youth Innovation Promotion Association of CAS (Grant No. 2016257), CAS Key Technology Talent Program, and SANOFI-SIBS Scholarship for funding.

语种：英文

外文关键词：Pelletizing - Solubility - Stability - Differential scanning calorimetry

摘要：Progesterone (Prog), a natural steroid hormone, is widely used in birth control pills and menopausal hormone replacement therapies. Phloroglucinol (SPF) and resveratrol (RSV) are also two kinds of active products that can be used during pregnancy. Drug-drug cocrystals of Prog with SPF and RSV were designed and successfully synthesized for purpose of bringing improvements of drug properties, including solubility, hydroscopic stability, and color stability. The cocrystals and their hydrate structures were systematically characterized by X-ray diffraction, differential scanning calorimetry, and thermogravimetric analysis. In addition, powder dissolution experiments of Prog, Prog-SPF, and Prog-RSV were conducted in aqueous solutions with the presence of different surfactants, and the result revealed that the Prog-SPF cocrystal exhibits a superior solubility compared with Prog and Prog-RSV. Furthermore, the Prog-SPF cocrystal also enhances the hydroscopic stability and color stability of SPF. Those findings may provide a promising formulation to overcome some weaknesses of the parent drugs.