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Palmatine hydrochloride-naringenin pharmaceutical eutectic crystal with slow-release effect

A technology of palmatine hydrochloride and naringenin, which is applied in the field of drug crystallization, can solve the problems that there are no public reports of palmatine hydrochloride and naringenin drugs, and achieve the effect of simple and easy preparation method and clear crystal structure

Active Publication Date: 2019-07-16
MINJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] There is no public report on the drug-drug co-crystal of palmatine hydrochloride and naringenin

Method used

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  • Palmatine hydrochloride-naringenin pharmaceutical eutectic crystal with slow-release effect
  • Palmatine hydrochloride-naringenin pharmaceutical eutectic crystal with slow-release effect
  • Palmatine hydrochloride-naringenin pharmaceutical eutectic crystal with slow-release effect

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] 0.3 mmol of palmatine hydrochloride and 0.3 mmol of naringenin were completely dissolved in 200 mL of absolute ethanol to prepare a mixed solution; the above mixed solution was placed at room temperature and dried naturally to obtain Parmesan hydrochloride with sustained release Tin-naringenin drug co-crystal.

[0039] figure 1 It is the XRD figure of the palmatine hydrochloride-naringenin drug cocrystal prepared in the present embodiment. Depend on figure 1 It is known that the prepared drug co-crystal has a diffraction angle of 2 θ ° ± 0.2 for: 6.1, 7.7, 10.0, 12.4, 12.9, 13.6, 14.7, 15.3, 15.8, 16.7, 17.2, 17.9, 18.2, 19.0, 19.7, 19.8, 20.2, 20.6, 21.2, 21.3, 22.3, 22.8, 23.1 , 23.4, 23.9, 24.2, 24.7, 25.5, 26.2, 27.6, 29.9, 30.6, 31.2, 31.6, 32.0, 34.0, 36.0, 36.9 have characteristic diffraction peaks.

[0040] figure 2 It is the crystal structure unit of the palmatine hydrochloride-naringenin drug cocrystal prepared in this embodiment. Depend on figure 2...

Embodiment 2

[0050] Put 0.3 mmol of palmatine hydrochloride and 0.3 mmol of naringenin into 5 mL of absolute ethanol and mix, seal the beaker containing the mixture and stir at room temperature for 48 hours. The resulting precipitate is filtered, washed with a small amount of ethanol, and dried in the air A palmatine hydrochloride-naringenin co-crystal with sustained release is obtained.

[0051] Figure 11 It is the XRD figure of the palmatine hydrochloride-naringenin drug cocrystal prepared in the present embodiment. Depend on Figure 11 It is known that the palmatine hydrochloride-naringenin drug co-crystal prepared in this example and Example 1 have peaks at the same 2θ angle, indicating that the crystal structures of the two are the same.

Embodiment 3

[0053] Put 0.3 mmol of palmatine hydrochloride and 0.3 mmol of naringenin into 5 mL of methanol and mix, seal the beaker holding the mixture and stir at room temperature for 48 hours. The resulting precipitate is filtered, washed with a small amount of methanol, and dried to obtain A drug co-crystal of palmatine hydrochloride-naringenin with sustained release.

[0054] Figure 12 It is the XRD figure of the palmatine hydrochloride-naringenin drug cocrystal prepared in the present embodiment. Depend on Figure 12 It is known that the palmatine hydrochloride-naringenin drug co-crystal prepared in this example and Example 1 have peaks at the same 2θ angle, indicating that the crystal structures of the two are the same.

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Abstract

The invention discloses a palmatine hydrochloride-naringenin pharmaceutical eutectic crystal with a slow-release effect, and belongs to the technical field of pharmaceutical crystallization. The structure unit of the pharmaceutical eutectic crystal contains palmatine hydrochloride molecules and naringenin molecules, and the molar ratio of the palmatine hydrochloride molecules to the naringenin molecules is 1:1, wherein the molecular formula is [C21H22ClNO4].[C15H12O5]. According to the invention, the palmatine hydrochloride is mixed with the naringenin according to a ratio, and solvent evaporation, and stirring or grinding processing are carried out to obtain the palmatine hydrochloride pharmaceutical eutectic crystal. The preparation method disclosed by the invention is simple and feasible, and the yield of the eutectic crystal is high. In addition, a prepared palmatine hydrochloride-naringenin medicine has no hygroscopicity, is high in thermal stability and light stability, has a slow release effect on the palmatine hydrochloride, and can be applied to develop a palmatine hydrochloride slow-release preparation.

Description

technical field [0001] The invention belongs to the technical field of drug crystallization, and in particular relates to a palmatine hydrochloride-naringenin drug co-crystal with sustained release effect. Background technique [0002] Palmatine hydrochloride (palmatine hydrochloride) is an important isocarine alkaloid, which is an active ingredient in the traditional Chinese medicine Huangteng. It has anti-inflammatory and broad-spectrum antibacterial effects, and is known as "natural plant antibiotics". Clinically, palmatine hydrochloride is mainly used to treat enteritis, bacillary dysentery, respiratory tract and urinary tract infection, gynecological inflammation, surgical infection and conjunctivitis. Studies in recent years have shown that palmatine hydrochloride also has significant pharmacological activities such as anti-tumor, anti-depression and anti-Alzheimer's disease (BBA-Gen. Subjects, 2018, 1862, 1565-1575.). Although palmatine hydrochloride has high medicin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D455/03C07D311/32A61K47/22
CPCA61K47/22C07D311/32C07D455/03
Inventor 娄本勇张燕杰张梅黄雅丽郭璐倩
Owner MINJIANG UNIV
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