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Cocrystal of berberine hydrochloride and malic acid, preparation method, composition and use thereof

A technology of berberine hydrochloride and malic acid, which is applied in the directions of drug combination, organic chemistry method, pharmaceutical formula, etc., to achieve the effect of increasing antibacterial biological activity, good safety, and improving clinical treatment effect.

Active Publication Date: 2021-12-07
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no report about berberine hydrochloride co-crystal

Method used

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  • Cocrystal of berberine hydrochloride and malic acid, preparation method, composition and use thereof
  • Cocrystal of berberine hydrochloride and malic acid, preparation method, composition and use thereof
  • Cocrystal of berberine hydrochloride and malic acid, preparation method, composition and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Preparation method of berberine with berberine hydrochloric acid 1:

[0054] According to the following table, the amount of hydrochloride and the right amount of malic acid and the amount of malic acid were placed in a mortar, and the appropriate amount of organic solvent was added and artificially grinded. Powder X-ray diffraction analysis, the diffraction pattern and figure 1 The resulting sample is a copray of hydrochloride with berberine hydrochloride.

[0055]

[0056]

[0057] Preparation method of berberine with berberine hydrochloric acid 2:

[0058] According to the following table, the amount of siberraine with hydrochloride and the amount of malic acid is placed in a ball mill according to the molar ratio, and the appropriate amount of organic solvent is added, and the appropriate spherical ratio is selected, and the appropriate rotational speed is set, and the polishing is appropriate. Powder X-ray diffraction analysis, the diffraction pattern and figure 1 ...

Embodiment 2

[0064] Berberine and malic acid eutectic in rats absorb characteristics and blood concentration characteristics:

[0065] 6 SD rats were randomly divided into 2 groups, 3 per group, and 12h before administration, no water is not allowed. Weigh the weight, according to 100mg · kg -1 Case of hydrochloride, calculated, berberine and berberine hydrochloride and berberine with malic acid co-crystalline samples into solid administration, and directly into the stomach in the stomach through the oral cavity. 5 min, 15 min, 30 min, 45min, 1H, 1.5H, 2H, 45Min, 1H, 12h were given in the eyes of 5 min, 12 hours, respectively, 4 ° C, 4000 rpm centrifugation 10min, frozen to -40 ° C The refrigerator is tested. Precision quantitative plasma 100 μl, set 1.5 ml of EP tube, add 10 μl of the internal standard kamas flat working fluid, then add 290 μL of acetonitrile (protein precipitant), sufficiently oscillating 5 min, centrifuge (13400 rpm, 10min), and take 100 μl of the upper layer solution at an...

Embodiment 3

[0074] Method for combining pharmaceutical preparations 1 (tablet):

[0075] A method for combining a pharmaceutical tablet, characterized in that the use of berberine hydrochloride with a common crystal of hydrochloride, using several excipients as an excipient ingredient to prepare a combination pharmaceutical tablet, which is made of each piece according to a certain ratio ratio. Tablet sample containing 5 ~ 500 mg, Table 5 gives a tablet formulation ratio:

[0076] Preparation formulation of berberine and malic acid copies of hydrochloric acid

[0077]

[0078] The method for preparing a tablet formulation using berberine and malic acid co-transistor as a raw material is to mix several excipients and raw materials, direct tablets; or excipient mixed dry method, mix with the raw material mixture A uniform tablet is obtained.

[0079] Method for combining pharmaceutical preparations 2 (tablet):

[0080] A method for producing a pharmaceutical tablet, characterized in that the ...

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PUM

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Abstract

The invention discloses a berberine hydrochloride and malic acid co-crystal, a preparation method, a composition and an application thereof. Specifically, the present invention discloses a new co-crystal of berberine hydrochloride and malic acid, which uses berberine hydrochloride as the active ingredient of the drug and malic acid as the co-crystal precursor; the co-crystal of berberine hydrochloride and malic acid The preparation method; the application of berberine hydrochloride and malic acid co-crystals as active ingredients in the preparation of anti-cardiovascular disease, anti-virus, anti-cancer, hypolipidemic, hypoglycemic, anti-inflammatory, antibacterial and anti-infective drugs.

Description

Technical field [0001] The present invention discloses berberine hydrochloride and a co-transistor and preparation method thereof and a composition thereof. Specifically, the present invention discloses a polymer formed of berberine hydrochloride and malic acid; a method for preparing berberine with berberine hydrochloride and a common crystal of malic acid; berberine with berberine hydrochloride and malic acid co-transistor as a pharmaceutical activity The composition is prepared to prevent cardiovascular disease, antiviral, anti-cancer, lowering blood fat, hypophache, anti-inflammatory, antibacterial and anti-infective drugs. Background technique [0002] Drug eutectic refers to a crystal formed by a polycrystal ligand in a certain proportion of the active drug molecules and the eutectic ligand. The drug can improve its physical and chemical properties and improve clinical therapeutics, on the one hand, and the other hand can enrich its crystalline form. For chemical imitation ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D455/03A61K31/4375A61P9/00A61P31/12A61P35/00A61P3/06A61P3/10A61P29/00A61P31/00A61P31/04A61P31/10
CPCC07B2200/13C07D455/03
Inventor 吕扬杜冠华曹俊姿赵晓悦杨世颖
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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