Overcoming Poor Tabletability of Bulky Absorption Enhancers by Spray Drying Technology

doi:10.1016/j.xphs.2019.01.025

	Overcoming Poor Tabletability of Bulky Absorption Enhancers by Spray Drying Technology
	Fan, Weiwei 1,2; Wang, Aohua 1,2; Wu, Yue 3; Water, Jorrit J.4; Buckley, Stephen T.4; Hovgaard, Lars 4; Yang, Mingshi 5,6; Gan, Yong 1,2
刊名	JOURNAL OF PHARMACEUTICAL SCIENCES
	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
DOI	10.1016/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.
资助项目	Novo Nordisk-Chinese Academy of Sciences Research Foundation[NNCAS-2015-5]
WOS关键词	COMPACTION PROPERTIES ; HYDROXYPROPYL METHYLCELLULOSE ; PARTICLE-SIZE ; ORAL DELIVERY ; BILE-SALTS ; POWDER ; INSULIN ; DRUGS ; MICROENCAPSULATION ; CRYSTALLINE
WOS研究方向	Pharmacology & Pharmacy ; Chemistry
语种	英语
出版者	ELSEVIER SCIENCE INC
WOS记录号	WOS:000477752600022
内容类型	期刊论文
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.