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The Cocrystal of Ubiquinol: Improved Stability and Bioavailability

文献类型：期刊论文

作者Zhang, Qi3; Xia, Mengyuan2,3; Zheng, Chenxuan1,2,3; Yang, Yinghong2,3; Bao, Junjie3; Dai, Wenjuan3; Mei, Xuefeng3
刊名PHARMACEUTICS
出版日期2023-10-01
卷号15期号:10页码:12
关键词ubiquinol cocrystal polymorph stability bioavailability
DOI10.3390/pharmaceutics15102499
通讯作者Mei, Xuefeng(xuefengmei@simm.ac.cn)
英文摘要Coenzyme Q10 (CoQ10) exists in two forms, an oxidized form and a reduced form. Ubiquinol is the fully reduced form of CoQ10. Compared to the oxidized form, ubiquinol has a much higher biological absorption and better therapeutic effect. However, ubiquinol has an important stability problem which hampers its storage and formulation. It can be easily transformed into its oxidized form-ubiquinone-even at low temperature. In this work, we designed, synthesized, and characterized a new cocrystal of ubiquinol with vitamin B3 nicotinamide (UQ-NC). Compared to the marketed ubiquinol form, the cocrystal exhibited an excellent stability, improved dissolution properties, and higher bioavailability. The cocrystal remained stable for a long period, even when stored under stressed conditions. In the dissolution experiments, the cocrystal generated 12.6 (in SIF) and 38.3 (in SGF) times greater maximum ubiquinol concentrations above that of the marketed form. In addition, in the PK studies, compared to the marketed form, the cocrystal exhibited a 2.2 times greater maximum total coenzyme Q10 concentration and a 4.5 times greater AUC than that of the marketed form.
WOS关键词COENZYME-Q10
资助项目Natural Science Foundation of Shanghai[22ZR147390]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:001095371100001
出版者MDPI
源URL[http://119.78.100.183/handle/2S10ELR8/307745]  
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.Nanchang Univ, Coll Pharm, Nanchang 330006, Peoples R China
2.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
3.Chinese Acad Sci, Pharmaceut Analyt & Solid State Chem Res Ctr, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Zhang, Qi,Xia, Mengyuan,Zheng, Chenxuan,et al. The Cocrystal of Ubiquinol: Improved Stability and Bioavailability[J]. PHARMACEUTICS,2023,15(10):12.
APA Zhang, Qi.,Xia, Mengyuan.,Zheng, Chenxuan.,Yang, Yinghong.,Bao, Junjie.,...&Mei, Xuefeng.(2023).The Cocrystal of Ubiquinol: Improved Stability and Bioavailability.PHARMACEUTICS,15(10),12.
MLA Zhang, Qi,et al."The Cocrystal of Ubiquinol: Improved Stability and Bioavailability".PHARMACEUTICS 15.10(2023):12.

入库方式： OAI收割

来源：上海药物研究所

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