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!

Crystallization of Amorphous Indomethacin during Dissolution: Effect of Processing and Annealing

溶解 无定形固体 结晶 材料科学 化学工程 猝灭(荧光) 溶解度 结晶度 差示扫描量热法 过饱和度 成核 非晶态金属 退火(玻璃) 再结晶(地质) 核化学 化学 结晶学 冶金 复合材料 光学 工程类 物理 荧光
作者
Kristyn Greco,Robin H. Bogner
出处
期刊:Molecular Pharmaceutics [American Chemical Society]
卷期号:7 (5): 1406-1418 被引量:71
标识
DOI:10.1021/mp1000197
摘要

The crystallization of amorphous drugs during dissolution is a type of solution mediated phase transformation that can reduce the bioavailability enhancement one hoped to gain from the amorphous state. The goal of this study was to explore the effects of processing on the dissolution performance of amorphous indomethacin. The amorphous solids were prepared by four techniques, quench cooling the melted solid, cryogrinding γ indomethacin amorphous for 1 or 3 h and quench cooling the solid followed by 1 h of cryogrinding. Dissolution results assessed in a flow-through intrinsic dissolution apparatus reveal decreases in the dissolution rate of amorphous indomethacin during the experimental time frame indicating that a solution mediated phase transformation has occurred. The amorphous solids prepared by melt quenching and melt quenching followed by cryogrinding showed a significant dissolution rate advantage over the γ form of indomethacin. In contrast, indomethacin that was cryoground amorphous for 1 or 3 h did not show any dissolution rate advantage over the crystalline material. Transformation was confirmed by in situ Raman microscopy and polarized light microscopy with differences seen in the nature of the crystals apparent on the surface of the dissolving solid. A portion of the melt quenched amorphous sample was annealed at 25 °C and 0% relative humidity to induce partial crystallization of γ indomethacin. As crystallinity increased, the dissolution rate decreased. The transformation time of partially amorphous indomethacin was not dependent on the level of crystallinity present, indicating only a small fraction of crystalline material needs to be present to affect the kinetics of crystallization. The solution mediated phase transformation of amorphous indomethacin is affected by the processing method even though all solids were confirmed amorphous by polarized light microscopy and X-ray diffraction. Dissolution may distinguish differences in amorphous solids that other methods cannot discern.
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
xiongdi521发布了新的文献求助10
5秒前
美罗培南完成签到 ,获得积分10
10秒前
lige完成签到 ,获得积分10
14秒前
34秒前
38秒前
二十四桥完成签到 ,获得积分10
38秒前
直觉应助背后的鞋垫采纳,获得10
44秒前
桦奕兮完成签到 ,获得积分10
51秒前
Akim应助Borhan采纳,获得10
55秒前
1分钟前
jjjjj发布了新的文献求助10
1分钟前
Liiiiiiiiii发布了新的文献求助10
1分钟前
Eva完成签到 ,获得积分10
1分钟前
上官若男应助Liiiiiiiiii采纳,获得10
1分钟前
Liufgui应助jjjjj采纳,获得10
1分钟前
1分钟前
酷波er应助科研通管家采纳,获得10
1分钟前
科研通AI2S应助科研通管家采纳,获得10
1分钟前
核桃发布了新的文献求助30
2分钟前
田様应助最最最采纳,获得10
2分钟前
2分钟前
2分钟前
不懂白完成签到 ,获得积分10
2分钟前
2分钟前
Borhan发布了新的文献求助10
3分钟前
充电宝应助科研通管家采纳,获得10
3分钟前
天天快乐应助科研通管家采纳,获得10
3分钟前
科研通AI2S应助科研通管家采纳,获得10
3分钟前
爆米花应助科研通管家采纳,获得10
3分钟前
3分钟前
rumengren完成签到 ,获得积分10
4分钟前
4分钟前
嘉嘉完成签到 ,获得积分10
4分钟前
重要元灵完成签到 ,获得积分10
5分钟前
科研通AI2S应助科研通管家采纳,获得10
5分钟前
完美世界应助科研通管家采纳,获得10
5分钟前
俏皮元珊完成签到 ,获得积分10
6分钟前
21完成签到 ,获得积分10
6分钟前
6分钟前
自然芷文发布了新的文献求助10
6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 3990075
求助须知:如何正确求助?哪些是违规求助? 3532108
关于积分的说明 11256369
捐赠科研通 3271016
什么是DOI,文献DOI怎么找? 1805171
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 809228