A kind of co-crystal of acetazolamide and proline and preparation method thereof

A technology of acetazolamide and proline, which is applied in the drug co-crystal of acetazolamide and proline and its preparation field, can solve the problems of complex process, high cost, poor solubility of acetazolamide, etc., and achieve a yield and The effect of high purity, low cost and simple process
CN108558791BInactive Publication Date: 2021-05-07OCEAN UNIV OF CHINA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
OCEAN UNIV OF CHINA
Publication Date
2021-05-07
Estimated Expiration
Not applicable · inactive patent

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Abstract

A co-crystal of acetazolamide and proline and a preparation method thereof, the invention relates to the field of drug co-crystals. The molecular formula of the drug co-crystal is [C 4 h 6 N 4 o 3 S 2 ·C 5 h 9 NO 2 ], the basic structural unit is composed of an acetazolamide molecule and a proline molecule. The drug cocrystal belongs to the triclinic crystal system, and the space group is P‑ 1. Using acetazolamide and proline as raw materials, the drug co-crystal is prepared by cooling method and solvent evaporation method respectively. The drug co-crystal of the invention improves the solubility of acetazolamide and is beneficial to improve the bioavailability of acetazolamide. Since there are no solvent molecules in the eutectic structure, it can remain stable for a long time at room temperature. The preparation method and process route of the drug co-crystal of the invention are simple and easy, and are convenient for large-scale production.
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Description

technical field

[0001] The invention relates to the field of drug co-crystals, in particular to a drug co-crystal of acetazolamide and proline and a preparation method thereof. Background technique

[0002] Acetazolamide (Acetazolamide, ACZ) is colorless crystal or white crystalline powder, molecular formula is C 4 h 6 N 4 o 3 S 2 , as a drug for treating various types of glaucoma, it exerts therapeutic effects mainly by inhibiting the activity of carbonic anhydrase in epithelial cells. In addition, acetazolamide also has a certain effect on the treatment of altitude sickness and respiratory diseases. However, the poor solubility of acetazolamide affects the bioavailability of the drug and limits its clinical application to some extent. At present, although various pharmaceutical methods have been used to improve the physical and chemical properties of acetazolamide, these methods have problems such as complicated process and high cost. Therefore, it is of great pract...

Claims

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