Amino acids as co-amorphous excipients for tackling the poor aqueous solubility of valsartan

doi:10.3109/10837450.2016.1163390

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 药物质量控制与固体化学研究中心

	Amino acids as co-amorphous excipients for tackling the poor aqueous solubility of valsartan
	Huang, Ying; Zhang, Qi; Wang, Jian-Rong; Lin, Kai-Lei; Mei, Xuefeng
刊名	PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
	2017-02
卷号	22 期号:1 页码:69-76
关键词	Amino acid co-amorphous intrinsic dissolution rate small molecular excipients solubility valsartan
ISSN号	1083-7450
DOI	10.3109/10837450.2016.1163390
文献子类	Article
英文摘要	Co-amorphization has recently been shown to be a promising approach for stabilizing amorphous drugs and improving the dissolution rate of poorly water-soluble drugs. In this study, three basic amino acids were chosen as small molecular weight excipients to interact with the drug to form co-amorphous combinations. The co-amorphous combinations of valsartan (VAL) with l-histidine, l-arginine, and l-lysine were prepared by vibrational ball milling. Solid-state characterization with X-ray powder diffraction and differential scanning calorimetry (DSC) revealed that all of the co-amorphous mixtures were homogeneous. The molecular interactions of the co-amorphous mixtures were investigated through the glass transition temperature (T-g) in the DSC measurements and Fourier transform infrared spectroscopy. The drug remained chemically stable during the milling process, and the co-amorphous formulations were generally physically stable over at least 3 months at 40 degrees C under dry conditions. The dissolution rate of all of the co-amorphous mixtures was significantly increased over that of the amorphous VAL alone. The results of this study demonstrated the potential of amino acids as small molecular weight excipients in co-amorphous formulations to improve the drug solubility and dissolution rate.
资助项目	National Natural Science Foundation of China[81273479] ; National Natural Science Foundation of China[81402898] ; CAS Key Technology Talent Program[00000000] ; Youth Innovation Promotion Association CAS[00000000]
WOS关键词	WATER-SOLUBLE DRUGS ; SOLID DISPERSIONS ; PHYSICAL STABILITY ; MOLECULAR MOBILITY ; DISSOLUTION RATE ; SYSTEMS ; BIOAVAILABILITY ; FORMS ; GLIBENCLAMIDE ; ENHANCEMENT
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	TAYLOR & FRANCIS LTD
WOS记录号	WOS:000394644600009
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/275642]
专题	药物质量控制与固体化学研究中心
通讯作者	Mei, Xuefeng
作者单位	Chinese Acad Sci, Pharmaceut Analyt & Solid State Chem Res Ctr, Shanghai Inst Mat Med, Shanghai, Peoples R China
推荐引用方式 GB/T 7714	Huang, Ying,Zhang, Qi,Wang, Jian-Rong,et al. Amino acids as co-amorphous excipients for tackling the poor aqueous solubility of valsartan[J]. PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY,2017,22(1):69-76.
APA	Huang, Ying,Zhang, Qi,Wang, Jian-Rong,Lin, Kai-Lei,&Mei, Xuefeng.(2017).Amino acids as co-amorphous excipients for tackling the poor aqueous solubility of valsartan.PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY,22(1),69-76.
MLA	Huang, Ying,et al."Amino acids as co-amorphous excipients for tackling the poor aqueous solubility of valsartan".PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY 22.1(2017):69-76.