CN Patent

CN117088809A — 一种索拉非尼-丙二酸共晶及其制备方法

Assigned to Zhejiang University of Technology ZJUT · Expires 2023-11-21 · 2y expired

What this patent protects

本发明公开了一种索拉非尼‑丙二酸共晶及其制备方法,该共晶中索拉非尼与丙二酸的化学计量比为1:1,粉末X射线衍射图在2θ值为7.27°、8.40°、9.23°、11.11°、13.12°、13.71°、14.53°、15.05°、16.71°处具有特征峰。本发明提供的索拉非尼‑丙二酸共晶在0.1 M盐酸溶液和0.1 M磷酸二氢钠缓冲液(pH=6.8)中表现出较高的表观溶解度,是索拉非尼游离碱稳定晶型Form I的6.3倍和4.5倍,并且其制备工艺简单,结晶过程易于控制。另外本发明所述的索拉非尼‑丙二酸共晶在40℃、相对湿度为75±5%和60℃、相对湿度为0…

USPTO Abstract

本发明公开了一种索拉非尼‑丙二酸共晶及其制备方法,该共晶中索拉非尼与丙二酸的化学计量比为1:1,粉末X射线衍射图在2θ值为7.27°、8.40°、9.23°、11.11°、13.12°、13.71°、14.53°、15.05°、16.71°处具有特征峰。本发明提供的索拉非尼‑丙二酸共晶在0.1 M盐酸溶液和0.1 M磷酸二氢钠缓冲液(pH=6.8)中表现出较高的表观溶解度,是索拉非尼游离碱稳定晶型Form I的6.3倍和4.5倍,并且其制备工艺简单,结晶过程易于控制。另外本发明所述的索拉非尼‑丙二酸共晶在40℃、相对湿度为75±5%和60℃、相对湿度为0%的条件分别放置180天和60天,未发生任何转晶,说明其稳定性良好,适合药物的生产和贮存。这种索拉非尼新固体形式具有较大开发成制剂的潜力。

Drugs covered by this patent

Patent Metadata

Patent number
CN117088809A
Jurisdiction
CN
Classification
Expires
2023-11-21
Drug substance claim
No
Drug product claim
No
Assignee
Zhejiang University of Technology ZJUT
Source
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