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A kind of cocrystal of hydrochlorothiazide and proline and preparation method thereof

A hydrochlorothiazide, proline technology, applied in the direction of organic chemistry, organic chemistry, etc., can solve the problems of low bioavailability, poor permeability and low solubility of hydrochlorothiazide

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, according to the biopharmaceutics classification system (Biopharmaceutics Classification System, BCS), hydrochlorothiazide belongs to BCS-IV drugs, which has the problems of low solubility and poor permeability, resulting in low bioavailability of hydrochlorothiazide, which limits its clinical application to a certain extent

Method used

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  • A kind of cocrystal of hydrochlorothiazide and proline and preparation method thereof
  • A kind of cocrystal of hydrochlorothiazide and proline and preparation method thereof
  • A kind of cocrystal of hydrochlorothiazide 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 hydrochlorothiazide-proline cocrystal is [C 7 h 8 N 3 o 4 S 2 Cl·C 5 h 9 NO 2 ], the basic structural unit is composed of a hydrochlorothiazide molecule and a proline molecule. The hydrochlorothiazide-proline cocrystal belongs to the orthorhombic crystal system, and the space group is P ca2 1 , the unit cell parameters are: a = 20.5038 Å, b = 9.7066 Å, c = 8.2625 Å, α = β = γ = 90°. Its PXRD characteristic diffraction peaks appear at 8.619°, 14.718°, 15.842°, 18.262°, 19.159°, 21.497°, 22.938°, 23.782°, 30.501°.

[0021] The hydrochlorothiazide-proline co-crystal described in this embodiment consists of one hydrochlorothiazide molecule and one proline molecule bonded together through hydrogen bonds. like figure 1 As shown, the two molecules are connected by two N-H...O hydrogen bonds, in which the H atom on the hydrochlorothiazide molecule N1 acts as a hydrogen bond donor and O5 in the p...

specific Embodiment approach 2

[0022] Specific embodiment two: the preparation method of hydrochlorothiazide-proline cocrystal of the present embodiment is implemented according to the following steps:

[0023] Put the hydrochlorothiazide raw material and proline in a round-bottomed flask at a molar ratio of 1:1, add ethanol into the round-bottomed flask, heat and stir in a water bath at 30°C for 3-5 h, then filter, and let the filtrate stand for 3-5 h to evaporate. The solid phase was collected in 5 days to obtain hydrochlorothiazide-proline co-crystal.

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

specific Embodiment approach 3

[0025] Embodiment 3: This embodiment differs from Embodiment 2 in that the solid-to-liquid ratio of the mixed powder to ethanol is (0.080-0.085) g: (8-10) mL, and other steps and parameters are the same as Embodiment 2.

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Abstract

A drug co-crystal of hydrochlorothiazide drug and proline and a preparation method thereof, the invention relates to the field of drug co-crystal. The composition of this hydrochlorothiazide-proline cocrystal is [C 7 h 8 N 3 o 4 S 2 Cl·C 5 h 9 NO 2 ], the basic structural unit is constituted by a hydrochlorothiazide molecule and a proline molecule. The eutectic belongs to the orthorhombic crystal system, and the space group is P ca2 1 . Using hydrochlorothiazide and proline as raw materials, the drug eutectic is prepared by solvent evaporation and temperature reduction. The drug eutectic of the invention improves the solubility of hydrochlorothiazide, and lays a foundation for improving its bioavailability and drug efficacy. The preparation method of the drug co-crystal is simple and easy, has low cost and is 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 hydrochlorothiazide and proline and a preparation method thereof. Background technique [0002] Pharmaceutical co-crystals are new co-crystals formed by combining pharmaceutical active ingredients and physiologically acceptable co-crystal formers in the same crystal lattice in the form of non-covalent bonds such as hydrogen bonds. As a new type of drug entity, drug co-crystals do not change the covalent structure of drug molecules, and realize drug innovation by regulating its crystal structure, which greatly shortens the drug development cycle and prolongs the drug property rights period. Due to its unique development advantages and potential commercial value, pharmaceutical co-crystals have attracted great attention from academia and industry in recent years. [0003] Hydrochlorothiazide (HCT) is a colorless crystal or white crystalline powder with the mole...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D285/28C07D207/16
CPCC07B2200/13C07D207/16C07D285/28
Inventor 李延团刘方张美娇焉翠蔚管华诗
Owner OCEAN UNIV OF CHINA
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