Amino acids as co-amorphous excipients for tackling the poor aqueous solubility of valsartan
文献类型：期刊论文
| 作者 | Huang, Ying; Zhang, Qi; Wang, Jian-Rong ; Lin, Kai-Lei; Mei, Xuefeng
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| 刊名 | PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
 |
| 出版日期 | 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. |
| WOS关键词 | WATER-SOLUBLE DRUGS ; SOLID DISPERSIONS ; PHYSICAL STABILITY ; MOLECULAR MOBILITY ; DISSOLUTION RATE ; SYSTEMS ; BIOAVAILABILITY ; FORMS ; GLIBENCLAMIDE ; ENHANCEMENT |
| 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研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000394644600009 |
| 出版者 | TAYLOR & FRANCIS LTD |
| 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. |
入库方式： OAI收割
来源：上海药物研究所
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