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Eutectic crystal of acetazolamide and proline and preparation method of eutectic crystal

A technology of acetazolamide and proline, which is applied to the pharmaceutical co-crystal of acetazolamide and proline and the preparation field thereof, can solve the problems of complicated process, high cost, poor solubility of acetazolamide and the like, and achieves simple process, Low cost, high yield and high purity

Inactive Publication Date: 2018-09-21
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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  • Eutectic crystal of acetazolamide and proline and preparation method of eutectic crystal
  • Eutectic crystal of acetazolamide and proline and preparation method of eutectic crystal
  • Eutectic crystal of acetazolamide and proline and preparation method of eutectic crystal

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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

The invention provides a eutectic crystal of acetazolamide and proline and a preparation method of the eutectic crystal and relates to the field of medicine eutectic crystals. A molecular formula of the medicine eutectic crystal is [C4H6N4O3S2.C5H9NO2] and a basic structural unit is composed of an acetazolamide molecule and a proline molecule. The medicine eutectic crystal belongs to a triclinic crystal system and a space group is P-1. Acetazolamide and the proline are used as raw materials and the medicine eutectic crystal is prepared by adopting a cooling method and a solvent volatilizationmethod respectively. According to the medicine eutectic crystal provided by the invention, the solubility of acetazolamide is improved and the bioavailability of acetazolamide is easy to improve. A eutectic crystal structure does not contain any solvent molecule so that the eutectic crystal structure still can keep stable after being placed for a long time under a room-temperature condition. The preparation method and a technological route of the medicine eutectic crystal are simple and feasible and large-scale production is convenient to realize.

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 Applications(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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