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Tetrahydroberberine phosphate drug co-crystal and preparation method thereof

A technology of tetrahydroberberine phosphate and tetrahydroberberine, which is applied in organic chemical methods, antibacterial drugs, organic chemistry, etc. The effect of improving solubility and improving inhibitory activity

Inactive Publication Date: 2019-02-22
JIAMUSI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Poor solubility may result in reduced drug bioavailability, especially as a solid dosage form

Method used

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  • Tetrahydroberberine phosphate drug co-crystal and preparation method thereof
  • Tetrahydroberberine phosphate drug co-crystal and preparation method thereof
  • Tetrahydroberberine phosphate drug co-crystal and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] A tetrahydroberberine phosphate pharmaceutical co-crystal, tetrahydroberberine is the active ingredient of the drug, with disodium hydrogen phosphate as the precursor, a protonated tetrahydroberberine molecule, a phosphate radical and two sodium ions Together constitute the basic structural unit of the drug co-crystal, X-ray diffraction structure analysis shows that the formed drug co-crystal is a triclinic system with a space group of P -1 , its axial length a =7.2131(4) Å, b = 10.5184(7) Å, c = 15.2467(9) Å, axis angle α = 72.189(6)°, β = 80.338(5)°, gamma = 87.549(5)°, V = 1085.66(12) Å 3 , Z = 2.

[0034] The characteristic peaks of the XRD spectrum of the drug co-crystal appear at: 6.20°-6.65°, 7.16°-7.56°, 8.28°-8.48°, 9.96°-10.56°, 12.04°-12.44°, 16.68°-17.08°, 23.52°-23.92°, 25.32°-25.72°.

[0035] The infrared absorption spectrum measured by the KBr tablet of the drug cocrystal is at 519, 945, 1058, 1127, 1378, 1459, 1710, 2927, 2858 and 3134 cm ...

Embodiment 2

[0053] A preparation method of tetrahydroberberine phosphate drug cocrystal, adding 0.07 mmol of tetrahydroberberine and 0.45 mmol of disodium hydrogen phosphate to a mixed solution of 5 mL of ethanol and 5 mL of water, adjusting the pH to 4.0 with phosphoric acid, and ultrasonically After dissolving, slowly volatilize at room temperature to obtain tetrahydroberberine phosphate drug co-crystal.

Embodiment 3

[0055] A preparation method of tetrahydroberberine phosphate drug cocrystal, tetrahydroberberine 0.07 mmol and disodium hydrogen phosphate 0.45mmol are added in the mixed solution of isopropanol 5mL and water 5mL, adjust pH=5.0 with phosphoric acid , after ultrasonic dissolution, slowly volatilize at room temperature to obtain tetrahydroberberine phosphate drug co-crystal.

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Abstract

The invention discloses a phosphate tetrahydroberberine drug eutectic and a preparation method thereof. The tetrahydroberberine and phosphate are added and mixed in isopropanol water solution, ethanol water solution or methanol water solution according to the molar ratio; the acquired mixed solution is volatilized under the room temperature. The prepared tetrahydroberberine drug eutectic is a triclinic system, and the space group is P-1, and its axial length (i) is FORMULA; the axial angle is FORMULA. The tetrahydroberberine drug eutectic prepared by the invention inherits the pharmacological activity of tetrahydroberberine, its solubleness, dissolution rate, antibiosis bacillus coli and staphylococcus aureus activities are significantly improved in relative to the tetrahydroberberine, thereby saving drug dosage; the method is good for developing to be drug preparation, and the tetrahydroberberine can be widely applied to the medicine field.

Description

Technical field: [0001] The invention relates to a drug co-crystal of tetrahydroberberine phosphate and a preparation method thereof. Background technique: [0002] Tetrahydroberberine, C 20 h 21 NO 4 , its chemical structure is as follows: [0003] [0004] Tetrahydroberberine (Tetrahydroberberine, THB) belongs to the original berberine alkaloid, mainly derived from Corydalis genus (Papaveraceae), such as snake fruit Viola, Corydalis and other plants. Tetrahydroberberine has a benzylisoquinoline structure and has various pharmacological effects, such as analgesic, sedative and stable effects; cardiovascular and cerebrovascular effects; anti-arrhythmia, anti-hypertension; anti-platelet aggregation, myocardial ischemia protection, Cerebral ischemia protection; anti-tumor; antibacterial; anti-allergic effect; dopamine receptor blocking effect; M-choline receptor affinity effect, etc. However, due to the poor water solubility of tetrahydroberberine, its bioavailability ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D455/03A61P31/04
CPCC07B2200/13C07D455/03
Inventor 张羽男张大俊张宇
Owner JIAMUSI UNIVERSITY
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