Vitamin D2 and vitamin D3 eutectic crystal as well as preparation method and application thereof

A vitamin and co-crystal technology, applied in the co-crystal of vitamin D2 and D3 and its preparation field, can solve the problems of limited solvent types, unstable amorphous, poor solubility, etc., achieve good stability, good reproducibility, prolong The effect of shelf life

Active Publication Date: 2015-02-18
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

First of all, for solvates, because the types of solvents acceptable in pharmacy are limited, and solvates often undergo desolvation (water) phenomenon during the preparation process, transforming into unstable amorphous or less soluble crystals. type

Method used

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  • Vitamin D2 and vitamin D3 eutectic crystal as well as preparation method and application thereof
  • Vitamin D2 and vitamin D3 eutectic crystal as well as preparation method and application thereof
  • Vitamin D2 and vitamin D3 eutectic crystal as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Vitamin D 2 and D 3 Add it into ethyl acetate according to the stoichiometric ratio of 1:1, after completely dissolving, volatilize slowly to obtain vitamin D 2 with D 3 eutectic.

[0041] Figure 1-3 Example 1 vitamin D is shown respectively 2 with D 3 X-ray powder diffraction (XRPD) pattern, thermogravimetric analysis (TG) pattern and differential scanning calorimetry (DSC) pattern of the eutectic.

Embodiment 2

[0043] Vitamin D 2 and D 3 Add it into acetone according to the stoichiometric ratio of 1:1, after completely dissolving, volatilize slowly to obtain vitamin D 2 with D 3 eutectic.

Embodiment 3

[0045] Vitamin D 2 and D 3 Add it into methanol according to the stoichiometric ratio of 1:1, after completely dissolving, volatilize slowly to obtain vitamin D 2 with D 3 eutectic.

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Abstract

The invention relates to a vitamin D2 and vitamin D3 eutectic crystal, a preparation method and application thereof as well as pharmaceutical composition comprising the eutectic crystal. The vitamin D2 and vitamin D3 eutectic crystal has the advantages of high degree of crystallinity and low hygroscopicity and forms neat crystal shape, and the stability is improved remarkably, so that fabrication processing of medicine and improvement of physicochemical properties are facilitated and performance of patent medicine is improved.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry and crystallization technology, and specifically relates to vitamin D 2 with D 3 The eutectic and its preparation method and use. Background technique [0002] Drug co-crystallization (co-crystal) refers to the interaction between active pharmaceutical ingredient (API) molecules and other physiologically acceptable acids, bases, salts, non-ionic compound molecules through hydrogen bonding, π-π stacking, van der Waals forces and other non-covalent interactions. bonded together in the same crystal lattice. The greatest application value of co-crystals in drugs is that they can introduce new components without changing the covalent structure of drugs, greatly improving the physical and chemical properties of drugs, such as stability, melting point, dissolution rate, dissolution rate, bioavailability, etc. And because there are many types of ligands (CCF), the properties of the drug can...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C401/00A61K31/593A61P19/08
CPCA61K31/593C07C401/00
Inventor 梅雪锋王建荣朱冰清李莎
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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