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Berberine hydrochloride and malic acid eutectic substance and preparation method, composition and application thereof

A technology of berberine hydrochloride and malic acid, which is applied in the directions of drug combination, organic chemistry method, pharmaceutical formula, etc.

Active Publication Date: 2019-07-09
INST OF MATERIA MEDICA AN INST OF THE 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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  • Berberine hydrochloride and malic acid eutectic substance and preparation method, composition and application thereof
  • Berberine hydrochloride and malic acid eutectic substance and preparation method, composition and application thereof
  • Berberine hydrochloride and malic acid eutectic substance and preparation method, composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Preparation method 1 of berberine hydrochloride and malic acid cocrystal:

[0054] According to the table below, take an appropriate amount of berberine hydrochloride and malic acid and put them into a mortar according to the molar ratio of 2:1, add an appropriate amount of organic solvent, and manually grind for an appropriate time. Carry out powder X-ray diffraction analysis to it, its diffraction pattern and figure 1 Consistent, indicating that the obtained sample is a co-crystal of berberine hydrochloride and malic acid.

[0055]

[0056]

[0057] Preparation method 2 of berberine hydrochloride and malic acid cocrystal:

[0058] As shown in the table below, take appropriate amount of berberine hydrochloride and malic acid and put them into a ball mill tank with a molar ratio of 2:1, add an appropriate amount of organic solvent, select an appropriate ball-to-material ratio, set an appropriate speed, and grind for an appropriate time. Carry out powder X-ray di...

Embodiment 2

[0064] Absorption characteristics and plasma concentration characteristics of berberine hydrochloride and malic acid co-crystal in rats:

[0065] Six SD rats were randomly divided into 2 groups, 3 rats in each group, and they were fasted without water for 12 hours before administration. Weigh the body weight of the rat, according to 100mg·kg -1 The berberine hydrochloride dosage was calculated, the berberine hydrochloride and the berberine hydrochloride and malic acid eutectic samples were loaded into the solid dispenser, and the drug powder was directly placed into the stomach of the rat through the oral cavity. 5min, 15min, 30min, 45min, 1h, 1.5h, 2h, 4h, 8h, and 12h after administration, blood was collected from the inner canthus of the eye, placed in a heparinized tube, centrifuged at 4000rpm for 10min at 4°C, and frozen at -40°C In the refrigerator to be tested. Accurately measure 100 μL of plasma, put it into a 1.5ml EP tube, add 10 μL of internal standard carbamazepin...

Embodiment 3

[0074] The preparation method 1 (tablet) of combination pharmaceutical preparation:

[0075] A method for preparing a combination drug tablet, which is characterized in that berberine hydrochloride and malic acid co-crystals are used, and several excipients are used as auxiliary material components for preparing the combination drug tablet, and each tablet is prepared according to a certain ratio For tablet samples containing eutectics in the range of 5-500 mg, Table 5 gives the tablet formula ratio:

[0076] The preparation formula of table 5 berberine hydrochloride and malic acid eutectic combination medicine tablet

[0077]

[0078] The method of preparing berberine hydrochloride and malic acid co-crystals as raw materials into tablet preparations is: mixing several excipients and raw materials uniformly, and directly compressing tablets; or mixing excipients with dry granulation and then mixing with raw materials Press evenly and press into tablets.

[0079] The prepa...

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Abstract

The invention discloses a berberine hydrochloride and malic acid eutectic compound as well as a preparation method, a composition and application thereof. Specifically, the invention discloses a novelberberine hydrochloride and malic acid eutectic substance which takes berberine hydrochloride as a medicinal active component and malic acid as a eutectic precursor, a preparation method of the berberine hydrochloride and malic acid eutectic substance, and application of the berberine hydrochloride and malic acid eutectic substance as a medicinal active ingredient in preparation of medicines forpreventing and treating cardiovascular diseases, resisting viruses and cancers, reducing blood fat, reducing blood sugar, resisting inflammation, resisting bacteria and resisting infection.

Description

technical field [0001] 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 co-crystal formed by berberine hydrochloride and malic acid; a method for preparing the co-crystal of berberine hydrochloride and malic acid; The application of the components in the preparation of anti-cardiovascular disease, anti-virus, anti-cancer, hypolipidemic, hypoglycemic, anti-inflammatory, antibacterial and anti-infective drugs. Background technique [0002] Drug co-crystal refers to the crystal formed by the intermolecular non-covalent interaction force between the active drug molecule and the co-crystal ligand in a certain ratio. By forming co-crystals, drugs can improve their physical and chemical properties and improve clinical therapeutic effects on the one hand, and on the other hand, co-crystals can enrich their crystalline forms. For chemical gener...

Claims

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Application Information

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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 AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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