Berberine hydrochloride and ibuprofen eutectic substance as well as preparation method, composition and application thereof

A kind of technology of berberine hydrochloride and co-crystal, applied in the field of co-crystal formed by berberine hydrochloride and ibuprofen

Active Publication Date: 2019-07-23
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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  • Berberine hydrochloride and ibuprofen eutectic substance as well as preparation method, composition and application thereof
  • Berberine hydrochloride and ibuprofen eutectic substance as well as preparation method, composition and application thereof
  • Berberine hydrochloride and ibuprofen eutectic substance as well as preparation method, composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Preparation method 1 of berberine hydrochloride and ibuprofen cocrystal:

[0059] As shown in the table below, take an appropriate amount of berberine hydrochloride and ibuprofen and put them into a mortar with a molar ratio of 1:1, 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 cocrystal of berberine hydrochloride and ibuprofen.

[0060]

[0061] Preparation method 2 of berberine hydrochloride and ibuprofen cocrystal:

[0062] According to the table below, take appropriate amount of berberine hydrochloride and ibuprofen and put them into the ball mill tank according to the molar ratio of 1:1, 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 diffraction analys...

Embodiment 2

[0068] The solubility characteristics of berberine hydrochloride and ibuprofen co-crystal and berberine hydrochloride bulk drug in 0.1N hydrochloric acid solution and aqueous solution with pH value of 1.0 were investigated. Measured with reference to the "Technical Guidelines for Dissolution Test of Ordinary Oral Solid Preparations", the dissolution curve comparison adopts the model-independent similarity factor (f2) method, and the calculation of f2 value compares berberine hydrochloride and berberine hydrochloride with ibuprofen. The similarity of the dissolution curves of crystal samples in the two solvent systems, when the f2 value is higher than 50, the two curves are considered to be similar, and when the f2 value is lower than 50, the two curves are considered to be different. In the experiment, the berberine hydrochloride sample was used as a reference, and the model-independent similarity factor f2 was calculated. The dissolution percentage adopts the high performance...

Embodiment 3

[0073] Absorption characteristics and plasma concentration characteristics of berberine hydrochloride and ibuprofen co-crystal in rats:

[0074] 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 calculation, the berberine hydrochloride and the berberine hydrochloride and ibuprofen co-crystal samples were loaded into the solid dispenser, and the drug powder was directly inserted 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 carbamazepine...

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PUM

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Abstract

The invention discloses a berberine hydrochloride and ibuprofen eutectic substance as well as a preparation method, composition and an application thereof, specifically discloses a novel berberine hydrochloride and ibuprofen eutectic with berberine hydrochloride as an active pharmaceutical ingredient and ibuprofen as a eutectic precursor, a preparation method of the berberine hydrochloride and ibuprofen eutectic as well as an application of the berberine hydrochloride and ibuprofen eutectic as the active pharmaceutical ingredient in preparation of drugs for preventing and treating cardiovascular diseases, resisting viruses and cancer, reducing blood fat and blood sugar and resisting inflammation, bacteria and infection.

Description

technical field [0001] The invention discloses a berberine hydrochloride and ibuprofen co-crystal, a preparation method, a composition and an application thereof. Specifically, the invention discloses a co-crystal formed by berberine hydrochloride and ibuprofen; a preparation method of the co-crystal of berberine hydrochloride and ibuprofen; a co-crystal of berberine hydrochloride and ibuprofen It is used as a drug active ingredient in the preparation of drugs for preventing and treating cardiovascular diseases, anti-virus, anti-cancer, lowering blood fat, lowering blood sugar, anti-inflammation, anti-bacteria and anti-infection. 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 ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D455/03C07C57/30C07C51/43A61K31/4375A61K31/192A61P9/00A61P31/12A61P35/00A61P3/06A61P3/10A61P29/00A61P31/00A61P31/04
CPCC07D455/03C07C57/30A61K31/4375A61K31/192C07B2200/13A61K2300/00
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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