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A kind of palmatine-terephthalic acid medicine co-crystal and preparation method thereof

A technology of terephthalic acid and palmatine, applied in the direction of carboxylate preparation, organic chemical methods, antibacterial drugs, etc., can solve the problems of difficulty in ensuring uniformity and stability, deliquescence and mildew, and reduce the production of palmetine hydrochloride Solve problems such as dissolution rate and in vivo absorption, achieve the effect of improving moisture absorption stability and antibacterial ability

Inactive Publication Date: 2020-12-11
JIAMUSI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Palmatine mainly exists in nature in the form of ions, so it is often prepared as palmetine hydrochloride for clinical medicinal use, but palmatine hydrochloride has poor hygroscopic stability, and it is prone to agglomeration and deliquescent after absorbing moisture in the air And mildew and other phenomena, so that it affects its transportation, storage and clinical medicinal effect
Therefore, in the clinical medicinal research and development of palmatine hydrochloride, the poor hygroscopic stability of palmatine hydrochloride is an important factor restricting its industrial production and development
At present, the methods for improving the hygroscopic stability of palmatine hydrochloride mainly include adding pharmaceutical excipients and coating, etc., but after physical mixing of palmetine hydrochloride and pharmaceutical excipients, it is difficult to guarantee its uniformity and stability, and the coating is difficult. May decrease the dissolution rate and in vivo absorption of palmatine hydrochloride

Method used

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  • A kind of palmatine-terephthalic acid medicine co-crystal and preparation method thereof
  • A kind of palmatine-terephthalic acid medicine co-crystal and preparation method thereof
  • A kind of palmatine-terephthalic acid medicine co-crystal and preparation method thereof

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Effect test

Embodiment 1

[0029] A kind of palmatine-terephthalic acid pharmaceutical co-crystal, with palmatine as the active ingredient of the medicine, terephthalic acid as the co-crystal ligand, and the single crystal structure of the palmetine-terephthalic acid pharmaceutical co-crystal The symmetric unit contains a palmatine cation and a terephthalate anion, and the molecular formula is C 21 h 22 NO 4 ·C 8 h 5 o 4 , the relative molecular weight is 517.53, and the single crystal X-ray diffraction structure analysis shows that the single crystal of palmatine-terephthalic acid drug cocrystal is an orthorhombic crystal system, and the space group is P nna , its axial length Shaft angle α=90°, β=90°, γ=90°, Z=4, its structural formula is as follows:

[0030]

[0031] A drug co-crystal of palmetine-terephthalic acid, the characteristic peaks of the XRD spectrum of the drug co-crystal appear at: 6.81-7.22°, 7.93-8.34°, 9.24-9.48°, 13.88-14.26°, 14.48- 14.69°, 16.68-17.08°, 15.70-16.30°...

Embodiment 2

[0037] A kind of preparation method of palmatine-terephthalic acid pharmaceutical co-crystal, 0.07mmol of palmatine hydrochloride and 0.07mmol of terephthalic acid are added to the water of 10mL in molar ratio 1:1, obtain after fully reacting and filtering After the precipitate was dried at 70°C for 3 hours, it was dissolved in a mixed solution of ethanol (5mL) and methanol (5mL). After being dissolved, the resulting mixed solution was slowly volatilized at room temperature to obtain Diformic acid drug cocrystal.

Embodiment 3

[0039] A kind of preparation method of palmatine-terephthalic acid drug co-crystal, 0.07mmol of palmetine hydrochloride and 0.07mmol of terephthalic acid are added into 10mL water in molar ratio of 1:1, fully react and obtain after filtering After the precipitate was dried at 70°C for 4 hours, it was dissolved in a mixed solution of isopropanol (5mL) and ethyl acetate (5mL). After being dissolved, the resulting mixed solution was slowly evaporated at room temperature to obtain a yellow Phalaenol-terephthalic acid drug cocrystal.

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Abstract

The invention provides a fibrauretine-terephthalic acid medicine eutectic crystal and a preparation method thereof, and relates to the technical field of medicine eutectic crystals. Hydrochloric acidfibrauretine and terephthalic acid are jointly dissolved in 10mL of water according to the mole ratio of 1:3-3:1; precipitates obtained after the full reaction and filtering are dried for 3 to 9h in environment of 70 DEG C; the dried precipitates are dissolved into a solution formed by mixing one, two or more than two kinds of solvents from isopropanol, ethanol, methyl alcohol and ethyl acetate; after the dissolution, the obtained mixed solution is volatilized at room temperature; after 1 to 30 days, a reddish brown blocky crystal is generated, i.e., the fibrauretine-terephthalic acid medicineeutectic crystal is obtained. The molecular formula of the prepared fibrauretine-terephthalic acid medicine eutectic crystal is C21H22NO4.C8H5O4; the relative molecular weight is 517.53; the crystalstructure of a monocrystal thereof is an orthorhombic crystal system; the space group is Pnna; the axis lengths are shown in the description; for the axis angles, alpha is 90 degrees, beta is 90 degrees, gamma is 90 degrees; V is shown in the description; and Z is 4.

Description

technical field [0001] The invention relates to the technical field of drug co-crystals, in particular to a padatine-terephthalic acid drug co-crystal and a preparation method thereof. Background technique [0002] Palmatine chloride, C 21 h 22 NO 4 Cl, its chemical structure is as follows: [0003] [0004] Palmatine is an alkaloid extracted from the stem of Phantasia chinensis. It has the effect of clearing away heat and detoxifying. It is mainly used in the treatment of gynecological inflammation, bacillary dysentery, enteritis, respiratory tract and urinary tract infection, surgical infection and conjunctiva in clinical practice. Inflammation and so on. Palmatine mainly exists in nature in the form of ions, so it is often prepared as palmetine hydrochloride for clinical medicinal use, but palmatine hydrochloride has poor hygroscopic stability, and it is prone to agglomeration and deliquescent after absorbing moisture in the air And mildew and other phenomena, so ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D455/03C07C63/26C07C51/41A61P31/04
CPCA61P31/04C07B2200/13C07D455/03
Inventor 张羽男常亮刘立新聂瑞良
Owner JIAMUSI UNIVERSITY
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