Micro-capsules of berberine hydrochloride and their preparations

A technology of berberine hydrochloride and stearate, applied in microcapsules, capsule delivery, pharmaceutical formulations, etc., can solve the problem of low oral bioavailability, berberine hydrochloride preparations are not suitable for children and patients with dysphagia, hydrochloric acid Problems such as poor water solubility of berberine

Inactive Publication Date: 2005-02-23
HUBEI LIYI PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its taste is extremely bitter, and methods such as coating its tablets or putting medicines into capsules are generally used to cover the bitter taste, but the berberine hydrochloride preparations prepared by these methods are not suitable for children and patients with dysphagia.
Moreover, berberine hydrochloride has poor water solubility and low oral bioavailability, which affects the further development of its curative effect.

Method used

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  • Micro-capsules of berberine hydrochloride and their preparations

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Example 1: Dissolve 1.2 grams of acrylic resin E100 in 20 milliliters of acetone, add 3.8 grams of berberine hydrochloride with a particle size of ≤75 microns, stir to form a uniformly dispersed suspension and control the liquid temperature at 5 to 15°C; under stirring, Add the above suspension into 160 ml of liquid paraffin at 5-15°C, heat up to 30-40°C, remove acetone by evaporation, wash the separated microcapsules with n-hexane several times, and dry to obtain the desired berberis hydrochloride Alkaline microcapsules. Taste-masking effect: No taste of berberine hydrochloride was detected.

Embodiment 2

[0016] Example 2: Dissolve 2.0 grams of acrylic resin E100 in 20 milliliters of acetone, add 3.0 grams of berberine hydrochloride with a particle size of ≤25 microns and 0.15 grams of silica gel, stir to form a uniformly dispersed suspension, and then control the liquid temperature at 5-15°C ; under stirring, add the above suspension into 180 ml of liquid paraffin at 5-15 ° C, after the addition is completed, heat up to 30-40 ° C, evaporate and remove acetone, wash the separated microcapsules with n-hexane in stages, and dry to obtain the obtained product Need berberine hydrochloride microcapsules. Taste-masking effect: No taste of berberine hydrochloride was detected.

Embodiment 3

[0017] Embodiment 3: No. 2.5 grams of acrylic resin IV are dissolved in 20 milliliters of acetone, add 2.5 grams of berberine hydrochloride and 0.20 grams of magnesium stearate with a particle diameter≤25 microns, stir to form a uniformly dispersed suspension and control the liquid temperature at 5-15°C; under stirring, add the above suspension into 200 ml of liquid paraffin at 5-15°C, after the addition is complete, heat up to 30-40°C, evaporate the acetone, and wash the separated microcapsules with n-hexane several times. Dry to obtain the desired berberine hydrochloride microcapsules. Taste-masking effect: No taste of berberine hydrochloride was detected.

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Abstract

A microsoftgel of berberine hydrochloride is prepared from the berberine hydrochloride and acrylic resin through dissolving acrylic resin in acetone, adding berberine hydrochloride and antisticking agent, dispersing, stirring, adding it to atoleine, heating for removing acetone, washing by hexane and drying.

Description

technical field [0001] The invention relates to berberine hydrochloride microcapsules and a preparation method thereof. Background technique [0002] Berberine hydrochloride is an alkaloid extracted from Phellodendron Phellodendri, Coptidis Rhizoma, Sankepin and other plants, and can also be synthesized artificially. It is a broad-spectrum antibiotic, but it has only a weak inhibitory effect on common bacteria, and has a significant effect on Shigella and Escherichia coli. It also has a certain inhibitory effect on Helicobacter pylori and Campylobacter. lighten. Berberine hydrochloride can reduce the number of pili on the surface of the bacteria, so that bacteria cannot attach to human cells to cause infection, thus playing a therapeutic role. Oral administration of berberine hydrochloride has few adverse reactions and is widely used clinically. However, its taste is extremely bitter, and methods such as coating its tablets or putting medicines into capsules are generally...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/4375A61P1/04A61P31/04
Inventor 吴海燕刘洁王阿强周利娟谷亦平
Owner HUBEI LIYI PHARM TECH CO LTD
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