Cholestanol co crystal of vitamin D3 and its preparation method and application

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The invention belongs to the technical field of medicinal chemistry and crystallization process, and discloses cholestanol co crystal of vitamin D3 and its preparation method. By means of X-ray powder diffraction analysis, thermogravimetric analysis, differential scanning calorimetry and other means, the co crystal is comprehensively characterized to find that the co crystal has more excellent physical chemical and pharmaceutical properties. The preparation method of the co crystal of the vitamin D3 is simple, easy to control and good in reproducibility, and the target co crystal can be stably obtained.

Vitamin D3 bile stay alcohol co-crystallization and preparation method and application invention belongs to the field of pharmaceutical chemistry and crystallization process technology, in particular to the present.

The pharmaceutical co-crystal (eutectic) is the active pharmaceutical ingredient (API) molecule and other physiologically acceptable acids, bases, salts, non-ionic compound molecular hydrogen bonding, stacking interactions, van der Waals and other non-covalent bond linked and combined in the same lattice. Eutectic in medicine biggest value is that you can introduce new components without changing the structure of the drug covalently, while greatly improving the physicochemical properties of the drug, such as stability, melting, dissolution rate, dissolution rate, bioavailability, and since the type of the ligand (CCF) There are many properties of the drug may also be a corresponding adjustment to varying degrees. Different every new active pharmaceutical ingredient in solid form demonstrated by the physical properties will affect the storage stability, compressibility and density, as well as the solubility and dissolution rate.

Compared with other solid form salts, solvates and other eutectic has a greater advantage in drug development. First, the solvate is, because in pharmaceutically acceptable solvent species is limited, and solvates occur to solvent (water) in the formulation process often phenomenon, into an unstable amorphous or crystalline solubility worse type. Secondly, with respect to the salt, the salt-forming raw material requirements because drug at least one ionized centers, and pharmaceutical co-crystal of the individual components may be neutral molecules, thus pharmaceutical co-crystal can cover all the API, including acids, base and non-ionic compounds; and potential for eutectic formation and API are also many molecules, these substances may include food additives, preservatives, medicinal chemistry materials, minerals, vitamins, amino acids and other active molecules, or even Other API. Overall, the eutectic is a broad prospect in solid form, having a profound impact on research and design forms before prescribing the drug.

A eutectic because of its specific crystal morphology and specific chemical ingredients that may have unique properties. For example, compared with the API, eutectic having more excellent pharmacological and pharmaceutical properties, easier processing; co-crystal has advantages of dissolution and solubility, the body can more efficiently use the pharmaceutically active ingredient, and therefore have better Bioavailability; eutectic have better storage stability. In short, the eutectic may have a therapeutic effect in addition to other advantageous properties.