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Overcoming Poor Tabletability of Bulky Absorption Enhancers by Spray Drying Technology

文献类型：期刊论文

作者Fan, Weiwei1,2; Wang, Aohua1,2; Wu, Yue3; Water, Jorrit J.4; Buckley, Stephen T.4; Hovgaard, Lars4; Yang, Mingshi5,6; Gan, Yong1,2
刊名JOURNAL OF PHARMACEUTICAL SCIENCES
出版日期2019-06-01
卷号108期号:6页码:2128-2135
关键词absorption enhancers spray drying compaction physicochemical properties amorphism tableting
ISSN号0022-3549
DOI10.1016/j.xphs.2019.01.025
通讯作者Yang, Mingshi(mingshi.yang@sund.ku.dk) ; Gan, Yong(ygan@simm.ac.cn)
英文摘要Absorption enhancers are often a major component of solid oral peptide formulations as compared to the active pharmaceutical ingredient and excipients. This commonly results in poor tabletability that is hard to mitigate in direct compaction by addition of small amounts of excipients. To improve the tabletability of bulky absorption enhancers, the model absorption enhancers, sodium cholate and deoxycholic acid, were coespray-dried with hydroxypropyl methylcellulose E5, where the percentage of absorption enhancers was not lower than 90% (w/w). The physicochemical properties of the resulting powders were assessed by laser diffraction, scanning electron microscopy, X-ray powder diffraction, thermogravimetric analysis, and differential scanning calorimetry. The powders were compressed into tablets, and the tabletability was evaluated. Coespray drying with 10% of hydroxypropyl methylcellulose significantly improved the tabletability of the both absorption enhancers. Moreover, it was demonstrated that small particle size and amorphous state rather than high moisture content contributed to the improved tabletability of the spray-dried powders. The study suggests that spray drying technology can be promising to overcome the poor tabletability of oral peptide formulation consisting of large amounts of absorption enhancers. (c) 2019 American Pharmacists Association (R). Published by Elsevier Inc. All rights reserved.
WOS关键词COMPACTION PROPERTIES ; HYDROXYPROPYL METHYLCELLULOSE ; PARTICLE-SIZE ; ORAL DELIVERY ; BILE-SALTS ; POWDER ; INSULIN ; DRUGS ; MICROENCAPSULATION ; CRYSTALLINE
资助项目Novo Nordisk-Chinese Academy of Sciences Research Foundation[NNCAS-2015-5]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000477752600022
出版者ELSEVIER SCIENCE INC
源URL[http://119.78.100.183/handle/2S10ELR8/289065]  
专题中国科学院上海药物研究所
通讯作者Yang, Mingshi; Gan, Yong
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Pharmaceut, Shanghai 201203, Peoples R China
2.Univ Chinese Acad Sci, Sch Pharm, Beijing 100049, Peoples R China
3.Novo Nordisk Res Ctr China, Dept Pharmacol & Histopathol, Discovery Biol China, Beijing 102206, Peoples R China
4.Novo Nordisk AS, Global Res Technol, DK-2760 Malov, Denmark
5.Univ Copenhagen, Fac Hlth & Med Sci, Dept Pharm, DK-2100 Copenhagen, Denmark
6.Shenyang Pharmaceut Univ, Wuya Coll Innovat, Wenhua Rd 103, Shenyang, Liaoning, Peoples R China
推荐引用方式
GB/T 7714		 Fan, Weiwei,Wang, Aohua,Wu, Yue,et al. Overcoming Poor Tabletability of Bulky Absorption Enhancers by Spray Drying Technology[J]. JOURNAL OF PHARMACEUTICAL SCIENCES,2019,108(6):2128-2135.
APA Fan, Weiwei.,Wang, Aohua.,Wu, Yue.,Water, Jorrit J..,Buckley, Stephen T..,...&Gan, Yong.(2019).Overcoming Poor Tabletability of Bulky Absorption Enhancers by Spray Drying Technology.JOURNAL OF PHARMACEUTICAL SCIENCES,108(6),2128-2135.
MLA Fan, Weiwei,et al."Overcoming Poor Tabletability of Bulky Absorption Enhancers by Spray Drying Technology".JOURNAL OF PHARMACEUTICAL SCIENCES 108.6(2019):2128-2135.

入库方式： OAI收割

来源：上海药物研究所

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