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A kind of tetrahydropalmatine-sulfosalicylic acid drug co-crystal and preparation method thereof

A technology of sulfosalicylic acid and ethyl fumarate, applied in organic chemistry methods, antibacterial drugs, organic chemistry, etc., can solve problems such as changes in toxic and side effects, improve bacteriostatic ability, avoid deterioration and mildew, and improve dissolution sexual effect

Active Publication Date: 2021-02-09
JIAMUSI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Studies have shown that improving the solubility of tetrahydropalmatine in water can enhance its clinical pharmacological effects. Therefore, the current research on tetrahydropalmatine mainly focuses on improving its solubility by modifying the structure of the original medicinally active molecules. However, the change of the original medicinally active molecular structure will make it into a new compound, and its toxic and side effects will also undergo unpredictable changes

Method used

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  • A kind of tetrahydropalmatine-sulfosalicylic acid drug co-crystal and preparation method thereof
  • A kind of tetrahydropalmatine-sulfosalicylic acid drug co-crystal and preparation method thereof
  • A kind of tetrahydropalmatine-sulfosalicylic acid drug co-crystal and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0029] A drug cocrystal of tetrahydropalmatine-sulfosalicylic acid, with tetrahydropalmatine as the drug active ingredient, sulfosalicylic acid as the ligand of the cocrystal, protonated tetrahydropalmatine cation and sulfosalicylic acid anion Together constitute the asymmetric unit of the drug cocrystal single crystal structure, single crystal X-ray diffraction structure analysis shows that the single crystal of tetrahydropalmatine-sulfosalicylic acid drug cocrystal is a triclinic system, and the space group is P 1 , its axial length Shaft angle α=74.399(10)°, β=79.514(9)°, γ=87.075(9)°, Z=1. Its chemical structural formula is as follows:

[0030]

[0031] A drug cocrystal of tetrahydropalmatine-sulfosalicylic acid, the characteristic peaks of the XRD spectrum of the drug cocrystal appear at: 5.75-6.20°, 6.62-6.93°, 7.58-8.05°, 10.01-10.75°, 11.94° -12.72°, 17.14-17.78°, 23.34-23.80°.

[0032] A drug cocrystal of tetrahydropalmatine-sulfosalicylic acid. The infrare...

Embodiment 2

[0037] A kind of preparation method of described tetrahydropalmatine-sulfosalicylic acid drug co-crystal, put tetrahydropalmatine 0.07mmol and sulfosalicylic acid 0.35mmol in a glass container together with a molar ratio of 1:5, and then jointly Dissolve in a mixed solution of ethanol (5mL) and ethyl acetate (5mL), place the glass container containing the mixed solution on a stirrer, stir at room temperature for 3 hours, and after fully reacting, slowly volatilize at room temperature, 1 - After 30 days, a colorless massive crystal is generated, which is the cocrystal of tetrahydropalmatine-sulfosalicylic acid drug.

Embodiment 3

[0039] A kind of preparation method of described tetrahydropalmatine-sulfosalicylic acid drug cocrystal, put tetrahydropalmatine 0.07mmol and sulfosalicylic acid 0.14mmol together in a glass container with a molar ratio of 1:2, and then jointly Dissolve in a mixed solution of ethyl acetate (5mL) and isopropanol (5mL), place the glass container containing the mixed solution on a stirrer, stir at room temperature for 2 hours, and slowly volatilize at room temperature after fully reacting , After 1-30 days, a colorless massive crystal is formed, which is the cocrystal of tetrahydropalmatine-sulfosalicylic acid drug.

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Abstract

The invention relates to the technical field of drug co-crystals, in particular to fumaric acid-sulfosalicylic acid drug co-crystals and a preparation method thereof. Dissolve fumaric acid and sulfosalicylic acid in a solution of one, two or more solvents in isopropanol, ethanol, methanol and ethyl acetate according to a certain molar ratio. The glass container of the solution is placed on a stirrer and stirred at room temperature for 1-5 hours. After fully reacting, the mixed solution is volatilized at room temperature. After 1-30 days, a colorless block crystal is formed, which is Tetrahydroe-Sulfonate based salicylic acid drug co-crystal. The prepared fumaric acid sulfosalicylic acid drug co-crystal molecular formula is C 21 H 26 O 4 N·C 7 H 5 O 6 S, its single crystal belongs to the triclinic system, the space group is P 1 , its long axis angle α=74.399(10)°, β=79.514(9)°, γ=87.075(9)°, Z=1.

Description

technical field [0001] The invention relates to the technical field of drug co-crystals, in particular to tetrahydropalmatine-sulfosalicylic acid drug co-crystals and a preparation method thereof. Background technique [0002] Tetrahydropalmatine (THP), C 21 h 25 o 4 N, its chemical structure is as follows: [0003] [0004] Tetrahydropalmatine (THP) belongs to the original berberine alkaloids, derived from the dry tubers of Corydalis Corydalis in the family Papaveraceae, has sedative, stable, analgesic and central muscle relaxation effects, and is mainly used clinically for Treatment of dull pain, dysmenorrhea and childbirth pain caused by medical diseases. Studies have shown that improving the solubility of tetrahydropalmatine in water can enhance its clinical pharmacological effects. Therefore, the current research on tetrahydropalmatine mainly focuses on improving its solubility by modifying the structure of the original medicinally active molecules. However, the...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D455/03A61P31/04
CPCA61P31/04C07B2200/13C07D455/03
Inventor 张羽男苏鑫刘立新彭碧辉
Owner JIAMUSI UNIVERSITY
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