马来酸托匹司他二水合物共晶及其制备方法

CN114685451BActive Publication Date: 2026-07-17LUNAN PHARMA GROUP CORPORATION
View PDF 7 Cites 0 Cited by

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
LUNAN PHARMA GROUP CORPORATION
Filing Date
2020-12-30
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

Topiprostine crystals have problems such as low solubility, low dissolution rate, low bioavailability, high hygroscopicity, and low stability, and the existing crystal forms are prone to crystal transformation.

Method used

A eutectic of maleic acid topipusta dihydrate is provided, which is formed by combining topipusta, maleic acid and water in a specific molar ratio. Its characteristic peaks are confirmed by Cu-Kα radiation X-ray diffraction and differential scanning calorimetry. The preparation method includes heating and stirring in an organic solvent, filtering and crystallizing and vacuum drying.

Benefits of technology

It improves the chemical stability and solubility of the eutectic, avoids crystal transformation, ensures the stability and safety of the drug formulation, and improves bioavailability.

✦ Generated by Eureka AI based on patent content.

Smart Images

  • Figure BDA0002872480400000011
    Figure BDA0002872480400000011
  • Figure BDA0002872480400000021
    Figure BDA0002872480400000021
  • Figure BDA0002872480400000033
    Figure BDA0002872480400000033
Patent Text Reader

Abstract

本发明属于晶型药物分子技术领域，特别涉及托匹司他晶型技术领域，具体一种马来酸托匹司他二水合物共晶及其制备方法，共晶中托匹司他、马来酸与水的摩尔比为1:1:2，使用Cu‑Kα辐射，以2θ表示的X射线衍射谱图在8.04±0.2°，16.28±0.2°，24.61±0.2°，24.68±0.2°，33.07±0.2°，33.17±0.2°处有特征峰；本发明制备的马来酸托匹司他二水合物共晶具有较好的稳定性，并具有较好的溶解度和稳定性，对于提高托匹司他药物的生物利用度和制剂制备具有重要的意义。
Need to check novelty before this filing date? Find Prior Art