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Tetrahydropalmatine-sulphosalicylic acid pharmaceutical cocrystal and preparation method thereof

A technology of sulfosalicylic acid and tetrahydropalmatine, applied in the direction of organic chemistry methods, antibacterial drugs, organic chemistry, etc., can solve the problems of changes in toxic and side effects, achieve improved antibacterial ability, enhanced antibacterial ability, and improve clinical The effect of medicinal value

Active Publication Date: 2018-11-06
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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  • Tetrahydropalmatine-sulphosalicylic acid pharmaceutical cocrystal and preparation method thereof
  • Tetrahydropalmatine-sulphosalicylic acid pharmaceutical cocrystal and preparation method thereof
  • Tetrahydropalmatine-sulphosalicylic acid pharmaceutical cocrystal and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] A drug cocrystal of tetrahydropalmatine-sulfosalicylic acid, with tetrahydropalmatine as the active ingredient, sulfosalicylic acid as the cocrystal ligand, protonated tetrahydropalmatine cation and sulfosalicylic acid anion Together constitute the asymmetric unit of the drug co-crystal single crystal structure, single crystal X-ray diffraction structure analysis shows that the single crystal of tetrahydropalmatine-sulfosalicylic acid drug co-crystal 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 infrared absorpti...

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 pharmaceutical cocrystals and particularly relates to a tetrahydropalmatine-sulphosalicylic acid pharmaceutical cocrystal and a preparation method thereof. The method comprises the following steps: dissolving tetrahydropalmatine and sulphosalicylic acid in a solution mixed by one, two or more than two solvents of isopropanol, ethanol, methanol and ethyl acetate according to a certain molar ratio, putting a glass container filled with the mixed solution in a stirrer, stirring the mixed solution for 1-5 hours at room temperature, standing the mixedsolution under room temperature for volatilizing after the mixed solution is fully reacted, and generating a colorless bulk crystal after 1-30 days, wherein the colorless bulk crystal is the tetrahydropalmatine-sulphosalicylic acid pharmaceutical cocrystal. The molecular formula of the prepared tetrahydropalmatine-sulphosalicylic acid pharmaceutical cocrystal is C21H26O4N.C7H5O6S; the monocrystalbelongs to a triclinic crystal system; a space group is P1; the axial length a is 0.85204(8)nm, the axial length b is 1.35001(15)nm, and the axial length c is 1.53733(19)nm; the axial angle alpha is74.399(10) degrees, the axial angle beta is 79.514(9) degrees, the axial angle gamma is 87.075(9) degrees; V is 1.674(3)nm; Z is 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 Applications(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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