Colchicines microcapsule and preparation method

A technology of colchicine and microcapsules, which is applied in the field of colchicine microcapsules, can solve the problems of harming the health of patients, increasing patients, harm, etc., and achieve the effects of reducing clinical doses, stable and reliable products, and improving patient compliance

Inactive Publication Date: 2005-11-16
云南一尧科技开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, doing so will increase the risk of drug harm to patients and damage the health of patients, especially the damage to kidney function, which is more likely to cause permanent damage.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Colchicine microcapsules were prepared by single coacervation method, formula:

[0019] Colchicine 0.5g

[0020] Gelatin 5g

[0021] Preparation process: under the condition of 100,000 grades, dissolve gelatin into 150ml gelatin solution, keep it warm at 37°C, add colchicine and stir to dissolve, add 10% acetic acid solution dropwise to pH 3.5-3.8, put the reactor in Insulate and stir in a water bath at 50°C for 45 minutes, add sodium sulfate solution (diluted solution) dropwise, observe under a microscope until it gathers into capsules, immediately pour it into the diluted solution that is being stirred, and pour the supernatant after gelling and settling solution, washed 2 to 3 times with diluent to remove uncoagulated capsule material, and finally suspended the microcapsules in an appropriate amount of diluent, added 2 to 3ml of 37% formaldehyde solution, stirred, and added dropwise sodium hydroxide to adjust the pH to 8-9, place overnight at low temperature, filte...

Embodiment 2

[0023] Production of colchicine microcapsules by complex coacervation method, formula:

[0024] Colchicine 0.5g

[0025] Gelatin 10g

[0026] Gum Arabic 5g

[0027] Preparation process: under the condition of 100,000 grades, first dissolve colchicine in 6ml of ethyl acetate, and pay attention to make it completely dissolved, and set aside; take an appropriate amount of the above solution of gum arabic and colchicine to make colostrum , dilute the colostrum with 300ml of 3% acacia gum solution to become an O / W emulsion; in addition, dissolve the gelatin into a 300ml gelatin solution, adjust the pH to 8 with 10% sodium hydroxide, and place the two-liquid reactor in a 50°C water bath Stir at medium temperature for 45 minutes. Use 10% acetic acid solution to adjust the mixture to pH 4.05, continue to stir for 5 minutes, dilute with twice the volume of water, let cool to about 28°C, then transfer to an ice-water bath to quickly cool to below 10°C, add 37% formaldehyde 4-8ml of ...

Embodiment 3

[0029] Prepare colchicine microcapsules by solvent-non-solvent method, formula:

[0030] Colchicine 0.5g

[0031] Butyl cellulose acetate 12g

[0032] Butanone 300g

[0033] Preparation process: Under the condition of 100,000 grades, first dissolve colchicine in 300ml of methyl ethyl ketone, and pay attention to make it completely dissolved before use. Then dissolve it into butyl cellulose acetate, place the reactor containing the reaction solution in a water bath at 55° C. and heat and stir for 45 minutes. Slowly add the non-solvent isopropyl ether under the condition of stirring, and wrap the suspended core material into microcapsules when the condensed phase separation occurs. Slowly cool down to room temperature, separate the microcapsules by centrifugation, wash with isopropyl ether, and vacuum-dry to obtain microcapsules each containing 0.003 mg of colchicine.

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Abstract

A microsoftgel of colcin and its preparing process are disclosed. It can be used to prepare any taget medicine by proportionally mixing it with medicinal auxiliary for higher stability and bioactivity and low irritation to stomach and intestine.

Description

technical field [0001] The invention relates to a colchicine microcapsule with significant analgesic and anti-inflammatory effects on gout and a production method thereof. Background technique [0002] When metabolic enzymes in the body are deficient and purines are synthesized too much, excessive uric acid will appear in the blood. Due to the low solubility of uric acid, it is easy to crystallize and precipitate in the joint cavity, connective tissue and kidneys, etc., causing cell phagocytosis and degranulation, lysozyme The body releases various decomposing enzymes, and produces inflammatory mediators such as histamine and slow-release peptides locally in the human body, causing gouty arthritis and kidney stones and other diseases. Colchicine is produced from the bulbs of Liliaceae plants, Colchicum autumnale L., Lilium brownii F.E. Brownvar. cokchesteri Wils, bulbs, stems, leaves, seeds, etc. Extract the isolated alkaloids. The colchicine included in the Chinese Pharma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/165
Inventor 任杨帆
Owner 云南一尧科技开发有限公司
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