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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

Inactive Publication Date: 2021-05-07
OCEAN UNIV OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the poor solubility of acetazolamide affects the bioavailability of the drug, which limits the clinical application to a certain extent.
At present, although a variety of pharmaceutical methods have been used to improve the physical and chemical properties of acetazolamide, these methods have problems such as complex processes and high costs.

Method used

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

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specific Embodiment approach 1

[0020] Specific embodiment one: the molecular formula of the present embodiment acetazolamide-proline cocrystal 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 acetazolamide-proline cocrystal belongs to the triclinic crystal system, and the space group is P- 1. The unit cell parameters are: a = 5.2350 Å, b = 10.4510 Å, c = 13.2627 Å, α = 80.451°, β = 85.302°, γ = 83.095°. Its PXRD characteristic diffraction peaks appear at 8.711°, 9.998°, 11.804°, 16.472°, 17.631°, 19.630°, 20.329°, 21.816°, 24.917°, 29.585°.

[0021] The acetazolamide-proline co-crystal described in this embodiment consists of one acetazolamide molecule and one proline molecule bonded together through hydrogen bonds. Such as figure 1 As shown, the H atom on the amino group of the acetazolamide molecule in the co-crystal acts as a hydrogen bond donor and the O atom on the carboxyl group of the proline molecule act...

specific Embodiment approach 2

[0022] Specific embodiment two: the preparation method of acetazolamide-proline co-crystal of this embodiment is implemented according to the following steps:

[0023] Put the acetazolamide raw material and proline in a round-bottomed flask at a molar ratio of 1:1, add a mixed solution of methanol, acetone and ethyl acetate to the mixed powder, heat and stir in a water bath at 30 °C for 3-5 h, and then filter , the filtrate was allowed to stand for volatilization for 3 to 5 days, and then the solid phase was collected to obtain the acetazolamide-proline co-crystal.

[0024] This embodiment prepares an acetazolamide-proline co-crystal with good chemical stability, high purity and high yield.

specific Embodiment approach 3

[0025] Embodiment 3: The difference between this embodiment and Embodiment 2 is that the volume ratio of methanol, acetone and ethyl acetate in the system is 1:1:1. Other steps and parameters are the same as in the second embodiment.

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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.

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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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D285/135C07D207/16A61K31/401A61K31/433A61P27/06C08G83/00
CPCA61K31/401A61K31/433A61P27/06C07B2200/13C07D207/16C07D285/135C08G83/008A61K2300/00
Inventor 李延团宋昱刘方焉翠蔚管华诗
Owner OCEAN UNIV OF CHINA
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