亲爱的研友该休息了!由于当前在线用户较少,发布求助请尽量完整地填写文献信息,科研通机器人24小时在线,伴您度过漫漫科研夜!身体可是革命的本钱,早点休息,好梦!

Cocrystals of Favipiravir: Improved Physicochemical Properties and Solution Stability Study

共晶 溶解度 差示扫描量热法 热重分析 化学 粉末衍射 化学工程 材料科学 结晶学 有机化学 氢键 分子 工程类 热力学 物理
作者
Huimin Li,Lei Wang,Guanying Xie,Changlin Yao,Shuhong Song,Yaqian Qu,Peizhuo Han,Hongshuai Wang,Yanyan Sun,Huachang Wu,Xutang Tao
出处
期刊:Crystal Growth & Design [American Chemical Society]
卷期号:23 (12): 8656-8669 被引量:4
标识
DOI:10.1021/acs.cgd.3c00805
摘要

Favipiravir (FPV) is used in the treatment of viral influenza, but it faces challenges due to its moderate solubility and poor tabletability. As an oral drug, it is necessary to develop a drug candidate that can improve its solubility and bioavailability. In addition, solution instability is one of the challenging issues of FPV cocrystals that should be noticed. On the premise of maintaining the solution stability, we aim to improve the solubility and tabletability through the preparation of FPV cocrystals to provide good alternative drugs. Herein, besides FPV-PHBA, we report the preparation and characterization of three new cocrystals of FPV with 3-hydroxybenzoic acid (FPV-3HBA, 1:1), 3,5-dihydroxybenzoic acid (FPV-3,5DHBA, 1:1), and also a cocrystal-hydrate with 3,4-dihydroxybenzoic acid (FPV-3,4DHBA-H2O, 1:1:1). All the cocrystals were characterized by single crystal X-ray diffraction (SCXRD), powder X-ray diffraction (PXRD), infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), Hirshfeld surface (HS) analysis, and molecular electrostatic potential surface (MEPS) analysis. Furthermore, we evaluated the solubility, tabletability, hygroscopicity, and accelerated stability of the cocrystals and explored the relationship between their structure and properties. The cocrystals exhibited a 6-fold increase in solubility and improved tabletability while maintaining good stability under certain temperature and humidity conditions. The hygroscopicity of the FPV cocrystals slightly increased to 2%, which still meets the storage requirements. However, during the dissolution of FPV-3HBA or FPV-3,5DHBA cocrystals, high supersaturation levels led to the dissociation of these cocrystals, indicating poor solution stability, which may hinder the achievement of the desired bioavailability for FPV. To address this issue, we introduced polyvinylpyrrolidone (PVP), which significantly inhibited the dissociation of the cocrystals by interacting with their surfaces. Our research has presented promising FPV candidate drugs and thoroughly investigated the solution stability of the highly soluble FPV cocrystals.
最长约 10秒,即可获得该文献文件

科研通智能强力驱动
Strongly Powered by AbleSci AI
更新
PDF的下载单位、IP信息已删除 (2025-6-4)

科研通是完全免费的文献互助平台,具备全网最快的应助速度,最高的求助完成率。 对每一个文献求助,科研通都将尽心尽力,给求助人一个满意的交代。
实时播报
Akim应助拼搏的二哈采纳,获得10
7秒前
10秒前
hob完成签到,获得积分10
10秒前
凉的白开完成签到,获得积分10
11秒前
weixiaosi完成签到 ,获得积分10
14秒前
WATeam发布了新的文献求助10
15秒前
17秒前
leave完成签到 ,获得积分10
17秒前
明理晓霜发布了新的文献求助10
22秒前
25秒前
可爱的函函应助酷酷白萱采纳,获得10
26秒前
酷酷白萱完成签到,获得积分20
36秒前
39秒前
无花果应助ceeray23采纳,获得20
40秒前
棣棣完成签到,获得积分10
43秒前
00完成签到,获得积分10
45秒前
c2发布了新的文献求助10
45秒前
小汤完成签到,获得积分20
48秒前
舟舟完成签到 ,获得积分10
58秒前
linkman发布了新的文献求助10
1分钟前
linkman发布了新的文献求助30
1分钟前
linkman发布了新的文献求助10
1分钟前
1分钟前
1分钟前
1分钟前
1分钟前
003完成签到,获得积分10
1分钟前
Splaink完成签到 ,获得积分10
1分钟前
经年发布了新的文献求助10
1分钟前
1分钟前
1分钟前
短短急个球完成签到,获得积分10
1分钟前
1分钟前
ceeray23发布了新的文献求助20
1分钟前
科研通AI2S应助科研通管家采纳,获得10
1分钟前
1分钟前
linkman完成签到,获得积分10
1分钟前
Cain发布了新的文献求助10
1分钟前
123123完成签到 ,获得积分10
1分钟前
经年完成签到,获得积分20
1分钟前
高分求助中
The Mother of All Tableaux: Order, Equivalence, and Geometry in the Large-scale Structure of Optimality Theory 3000
A new approach to the extrapolation of accelerated life test data 1000
ACSM’s Guidelines for Exercise Testing and Prescription, 12th edition 500
Indomethacinのヒトにおける経皮吸収 400
Phylogenetic study of the order Polydesmida (Myriapoda: Diplopoda) 370
基于可调谐半导体激光吸收光谱技术泄漏气体检测系统的研究 350
Robot-supported joining of reinforcement textiles with one-sided sewing heads 320
热门求助领域 (近24小时)
化学 材料科学 医学 生物 工程类 有机化学 生物化学 物理 内科学 纳米技术 计算机科学 化学工程 复合材料 遗传学 基因 物理化学 催化作用 冶金 细胞生物学 免疫学
热门帖子
关注 科研通微信公众号,转发送积分 3990012
求助须知:如何正确求助?哪些是违规求助? 3532068
关于积分的说明 11256227
捐赠科研通 3270933
什么是DOI,文献DOI怎么找? 1805123
邀请新用户注册赠送积分活动 882270
科研通“疑难数据库(出版商)”最低求助积分说明 809216