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Improving the Stability, Dissolution, and Bioavailability of Isotretinoin by Cocrystallization

文献类型：期刊论文

作者Cheng, Yinxiang1,2; Jiang, Yihua1,2; Zhang, Bingrui1,2; Rong, Xiaoyi2; Ding, Qiaoce2; Zhang, Zaiyong2; Wang, Jian-Rong2; Mei, Xuefeng1,2
刊名CRYSTAL GROWTH & DESIGN
出版日期2022-10-31
页码9
ISSN号1528-7483
DOI10.1021/acs.cgd.2c01043
通讯作者Mei, Xuefeng(xuefengmei@simm.ac.cn)
英文摘要Isotretinoin (13 -cis retinoic acid, ITT) is a gold standard therapy for the treatment of severe acne. However, because of its poor absorption, ITT must be taken with fatty meals to increase bioavailability. The coadministration of food could reduce the compliance of patients and increase the risk of inconsistent serum levels because of different eating habits. In this work, we designed and synthesized four cocrystals of ITT. The cocrystal between ITT and ethyl nicotinate (ENT), namely, ITT ENT, presented better chemical stability, dissolution, and absorption than ITT itself. The AUC0-10h of ITT-ENT cocrystal capsules is 2.6 times as that of the commercially available ITT capsules in the fasted state. Because of the high bioavailability in the fasted state, the food has a marginal effect on the absorption of cocrystal capsules. This work sets a good example for applying cocrystal technology to enhance the absorption and mitigate the food effect of drugs.
WOS关键词QUALITY ; ACNE ; FOOD
资助项目Natural Science Foundation of Shanghai ; Shanghai Science and Technology Innovation Action Plan ; [22ZR147390] ; [20142201800]
WOS研究方向Chemistry ; Crystallography ; Materials Science
语种英语
WOS记录号WOS:000879454300001
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/302882]  
专题中国科学院上海药物研究所
通讯作者Mei, Xuefeng
作者单位1.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, Pharmaceut Analyt & Solid State Chem Res Ctr, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Cheng, Yinxiang,Jiang, Yihua,Zhang, Bingrui,et al. Improving the Stability, Dissolution, and Bioavailability of Isotretinoin by Cocrystallization[J]. CRYSTAL GROWTH & DESIGN,2022:9.
APA Cheng, Yinxiang.,Jiang, Yihua.,Zhang, Bingrui.,Rong, Xiaoyi.,Ding, Qiaoce.,...&Mei, Xuefeng.(2022).Improving the Stability, Dissolution, and Bioavailability of Isotretinoin by Cocrystallization.CRYSTAL GROWTH & DESIGN,9.
MLA Cheng, Yinxiang,et al."Improving the Stability, Dissolution, and Bioavailability of Isotretinoin by Cocrystallization".CRYSTAL GROWTH & DESIGN (2022):9.

入库方式： OAI收割

来源：上海药物研究所

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