Berberine cyclodextrin inclusion compound, preparation thereof and preparation method

A cyclodextrin inclusion compound and cyclodextrin technology are applied in the field of pharmaceutical preparations of heterocyclic systems and their preparation, and can solve the problems of inclusion compound encapsulation efficiency, low drug loading and purity, encapsulation efficiency, loading and unloading. Low dosage and purity, low bioavailability of inclusion complexes, etc., to achieve the effect of large effective permeability coefficient, avoid secondary infection, and promote inclusion

Inactive Publication Date: 2009-06-24
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the formation of berberine / β-cyclodextrin inclusion complex can improve the solubility of berberine to a certain extent, but the encapsulation efficiency, drug loading and purity are low, the prepared berberine β-cyclodextrin inclusion complex The bioavailability of the drug is low, especially when it is administered orally, which affects the efficacy of the drug
[0009] Sun Junmei et al. (Sun Junmei, Shen Hui, Luo Wen, He Gang, Study on antibacterial effect of berberine / β-cyclodextrin inclusion compound in Chinese medicine compatibility Journal of Chengdu University (Natural Science Edition) 2007, 26(4): 280 -282) The inclusion complex of berberine hydrochloride / β-cyclodextrin was prepared by ultrasonic method. After the berberine was completely dissolved in water, it was shaken in an ultrasonic oscillator for 2 hours, poured into a plate, and allowed to air-dry to crystallize naturally. The encapsulation efficiency, drug loading and purity of the clathrate prepared by the method are low, and the bioavailability of the clathrate is low, especially when the bioavailability is low during oral administration, which affects the efficacy of the drug

Method used

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  • Berberine cyclodextrin inclusion compound, preparation thereof and preparation method
  • Berberine cyclodextrin inclusion compound, preparation thereof and preparation method
  • Berberine cyclodextrin inclusion compound, preparation thereof and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] 1. Preparation of berberine hydrochloride / hydroxypropyl-β-cyclodextrin inclusion compound

[0044] 1) Put 2g of hydroxypropyl-β-cyclodextrin in a beaker, add 1L of deionized water, and stir to dissolve;

[0045] 2) After heating the hydroxypropyl-β-cyclodextrin solution to 60°C, slowly add 574 mg of berberine hydrochloride solution dissolved in a small amount of absolute ethanol to the hydroxypropyl-β-cyclodextrin while stirring In the solution, the stirring rate is 800rpm. After stirring for 12 hours, the temperature is gradually lowered at a rate of 5°C / h, and the temperature is slowly lowered to 25°C;

[0046] 3) Filter the cooled solution with a 0.22 μm pore size microporous filter (to remove unincluded berberine hydrochloride);

[0047] The filtrate is placed in a spray dryer for spray drying. The inlet temperature of the filtrate spray dryer is 145° C., and the temperature of the sample outlet is 75° C. to obtain a white loose powder, namely berberine hydrochlori...

Embodiment 2

[0057] 1. Preparation of berberine hydrochloride / hydroxypropyl-β-cyclodextrin inclusion compound

[0058] 1) Put 1g of hydroxypropyl-β-cyclodextrin in a beaker, add 1L of deionized water, stir, and heat to 45°C to dissolve it;

[0059] 2) After heating the hydroxypropyl-β-cyclodextrin solution to 45°C, slowly add 574 mg of berberine hydrochloride solution dissolved in a small amount of absolute ethanol to the hydroxypropyl-β-cyclodextrin while stirring In the solution, the stirring rate is 800rpm. After stirring for 24 hours, the temperature is gradually lowered at a rate of 3°C / h, and the temperature is slowly lowered to 20°C;

[0060] 3) Filter the cooled solution with a 0.22 μm pore size microporous filter (to remove unincluded berberine hydrochloride);

[0061] 4) Put the filtrate in a freeze dryer for freeze-drying under reduced pressure. The freeze-drying temperature is -45°C and the relative pressure is -0.06MPa to obtain a white and loose powder, namely berberine hydr...

Embodiment 3

[0066] 1. Preparation of berberine hydrochloride / hydroxypropyl-β-cyclodextrin inclusion compound

[0067] 1) Put 6g of hydroxypropyl-β-cyclodextrin in a beaker, add 2L of deionized water, and stir to dissolve;

[0068] 2) After heating the hydroxypropyl-β-cyclodextrin solution to 50°C, slowly add 574 mg of berberine hydrochloride solution dissolved in a small amount of absolute ethanol to the hydroxypropyl-β-cyclodextrin while stirring In the solution, the stirring rate is 800rpm. After stirring for 12 hours, the temperature is gradually lowered at a rate of 6°C / h, and the temperature is slowly lowered to 25°C;

[0069] 3) Filter the cooled solution with a 0.22 μm pore size microporous filter (to remove unincluded berberine hydrochloride);

[0070] 4) Put the filtrate in a freeze dryer for freeze-drying under reduced pressure. The freeze-drying temperature is -45°C and the relative pressure is -0.06MPa to obtain a white and loose powder, namely berberine hydrochloride / hydroxy...

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Abstract

The invention relates to a hydrochloric acid berberine/hydroxide propyl-beta-cyclodextrin clathrate, a preparation thereof and a method for preparing the same. By a gradient temperature reduction sealing method, the hydrochloric acid berberine and the hydroxide propyl-beta-cyclodextrin between which the mol ratio is 1:0.2-10 are sealed so as to improve the water solubility and biological availability of the hydrochloric acid berberine; the clathrate has the advantages of high sealing rate, large medicine loading capability and high purity; and the clathrate can be prepared into a clinically acceptable formulation with quick curative effect. The invention also clarifies the pharmacological functions of the clathrate.

Description

technical field [0001] The present invention relates to a pharmaceutical preparation containing organic active ingredients and a preparation method thereof, in particular to a medicinal preparation of a six-membered ring heterocyclic system containing nitrogen as a ring heteroatom and a preparation method thereof. Background technique [0002] Berberine hydrochloride (berberine) is an isoquinoline alkaloid extracted from the rhizome of Coptis chinensis Franch. of Ranunculaceae or Phellodendron amurense Rupr. of Rutaceae. Molecular formula: C 20 h 18 ClNO 4 , Molecular weight: 336.37, its molecular structure formula is: [0003] [0004] The clinical application of berberine hydrochloride is mainly used to clear away heat and detoxify, and treat intestinal infection. However, it has been found in recent years that it also has the effects of treating arrhythmia, hypertension, hyperlipidemia, diabetes, depression and anti-tumor. Ehrlich ascites tumor, colon cancer cells, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/4375A61P1/00A61P31/04A61K47/69
Inventor 崔元璐张叶田俊生张艳斌
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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