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Baicalein caffeine co-crystal, its preparation method, pharmaceutical composition and application thereof

A technology of caffeine and baicalein, which is applied in the direction of drug combinations, active ingredients of heterocyclic compounds, antipyretics, etc., can solve the problems of limited clinical application, poor water solubility of baicalein, poor oral absorption, etc., and achieve improved dissolution rate and crystallization The process is easy to control and the effect of high bioavailability

Active Publication Date: 2018-06-15
ZHUCHENG HAOTIAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the poor water solubility of baicalein and poor oral absorption, its clinical application is greatly limited.

Method used

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  • Baicalein caffeine co-crystal, its preparation method, pharmaceutical composition and application thereof
  • Baicalein caffeine co-crystal, its preparation method, pharmaceutical composition and application thereof
  • Baicalein caffeine co-crystal, its preparation method, pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Add 0.1mmol of baicalein and 0.05mmol of caffeine into a mixed solution of acetone (3 milliliters) and water (1 milliliter) according to the stoichiometric ratio of 2:1, after completely dissolving, slowly volatilize at room temperature to obtain baicalein Caffeine eutectic.

Embodiment 2

[0046] Add 0.1mmol of baicalein and 0.05mmol of caffeine into a mixed solution of methyl ethyl ketone (3 milliliters) and water (1 milliliter) according to the stoichiometric ratio of 2:1, after completely dissolving, slowly volatilize at room temperature to obtain baicalein Caffeine eutectic.

Embodiment 3

[0048] Add 0.1mmol of baicalein and 0.05mmol of caffeine into a mixed solution of tetrahydrofuran (2 milliliters) and acetonitrile (2 milliliters) according to the stoichiometric ratio of 2:1, after completely dissolving, slowly volatilize at room temperature to obtain baicalein Caffeine eutectic.

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Abstract

The present invention provides a baicalein caffeine eutectic crystal, a preparation method therefor, a pharmaceutical composition, and application thereof. The baicalein caffeine eutectic crystal of the present invention has an excellent dissolution rate and bioavailability. The preparation method for the baicalein caffeine eutectic crystal provided in the present invention is simple, easy to control, and high in reproducibility, and can obtain a target eutectic crystal stably.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry and crystallization technology, in particular to baicalein-caffeine co-crystal, its preparation method, pharmaceutical composition and application thereof. Background technique [0002] The chemical name of baicalein is: 5,6,7-trihydroxyflavone, and its chemical structure is as follows: [0003] [0004] As a flavonoid compound, baicalein has various pharmacological effects such as antibacterial, antiviral, hepatoprotective, choleretic, diuretic, and anticancer. At present, it is mainly used for antibacterial, anti-inflammatory and anti-infection clinically. However, due to the poor water solubility and poor oral absorption of baicalein, its clinical application is greatly limited. [0005] Drug co-crystallization refers to the formation of active pharmaceutical ingredient (API, active pharmaceutical ingredient) molecules and other physiologically acceptable acids, bases, salts and...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D311/30C07D473/12A61K31/522A61K31/352A61P25/00A61P9/00A61P29/00A61P37/02A61P3/00A61P31/04A61P31/12
CPCA61K31/352A61K31/522C07D311/30C07D473/12
Inventor 朱理平梅雪锋朱冰清王建荣
Owner ZHUCHENG HAOTIAN PHARMA
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