Garlicin and garlic oil cyclodextrin derivatives inclusion compound and method for making same

A cyclodextrin and derivative technology, applied in the field of medicine, can solve the problems of unstable chemical properties, low solubility of garlic oil, oxidative deterioration, etc., and achieve the effect of being beneficial to clinical application, improving water solubility and stability, and good dissolution.

Inactive Publication Date: 2003-10-15
GENERAL HOSPITAL OF THE NORTHERN WAR ZONE OF THE CHINESE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, the solubility of garlic oil in water is very low, and the main component allyl sulfide compounds contained in it are chemically unstable, and are easily oxidized and deteriorated by the influence of pH, light, heat and oxygen. The garlicin injection currently on the market, It uses Tween-80 as a solubilizing agent, and the applicant has also used Tween-80 as a solubilizing agent to prepare garlic oil injection, but because Tween-80 can cause more serious toxic and side effects such as hemolysis, it is currently prohibited to use Intravenous injection

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0029] In the above preparation process, the liquid allicin or garlic oil cyclodextrin derivative inclusion compound can be dried at a temperature of 40-80° C. to obtain the solid allicin or garlic oil cyclodextrin derivative inclusion compound.

[0030] The preparation method of the inclusion compound of allicin and garlic oil cyclodextrin derivatives in the present invention can also be that the cyclodextrin derivatives are placed in a colloid mill, a ball mill or a mortar, and an appropriate amount of suitable solvent is added, and ground to make a paste According to the molecular molar ratio of allicin and cyclodextrin derivatives is 1:1-1000, the weight ratio of garlic oil and cyclodextrin derivatives is 1:8.6-8600, add allicin or garlic oil to the paste Grinding for 1-5 hours to obtain a uniform viscous paste, drying at 40-80°C to obtain solid allicin or garlic oil cyclodextrin derivative inclusion compound.

[0031] The preparation method of allicin and garlic oil cyclo...

Embodiment 1

[0038] Example 1: Preparation of liquid allicin or garlic oil hydroxypropyl-β-cyclodextrin derivative inclusion compound

[0039] (1) Weigh 26g of hydroxypropyl-β-cyclodextrin, pour it into 100mL of distilled water, and stir to dissolve;

[0040] (2) Another 1.5 g of allicin or garlic oil was weighed and poured into the above-mentioned hydroxypropyl-β-cyclodextrin solution;

[0041] (3) The mixed solution was stirred by magnetic stirring for 20 minutes. The stirring speed should be such that the liquid does not splash out. Observe the solution until it is clear, and then the liquid allicin or garlic oil hydroxypropyl-β-cyclodextrin inclusion compound is obtained.

Embodiment 2

[0042] Example 2: Preparation of solid allicin or garlic oil hydroxypropyl-β-cyclodextrin derivative inclusion compound

[0043] (1) Weigh 26g of hydroxypropyl-β-cyclodextrin, pour it into 100mL of distilled water, and stir to dissolve;

[0044] (2) Another 1.5 g of allicin or garlic oil was weighed and poured into the above-mentioned hydroxypropyl-β-cyclodextrin solution;

[0045] (3) The mixed solution is stirred for 20 minutes by magnetic stirring method, and the stirring speed is preferably such that the liquid does not splash out, and the solution is observed until it is clear, and the liquid allicin or garlic oil hydroxypropyl-β-cyclodextrin inclusion compound is obtained;

[0046] (4) concentrating the liquid allicin or garlic oil hydroxypropyl-β-cyclodextrin inclusion compound, and drying under reduced pressure to obtain solid allicin or garlic oil hydroxypropyl-β-cyclodextrin inclusion compound.

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PUM

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Abstract

The present invention aims to raise water solubility and stability of allicin and allium sativum oil, develop clinically required solid preparation form and liquid preparation form and make use of the treating effect of allicin and allium sativum oil. Cyclodextrin is used to include allicin and allium sativum oil and the clathrate contains allicin oil and cyclodextrin derivative in the molar ratio of 1 to 1-1000 or allium sativum and cyclodextrin derivative in the molar ratio of 1 to 8.6-8600. The cyclodextrin derivative is preferably propyl-beta- cyclodextrin. The clathrate may be used inpreparing injection, powder for injection, infusion fluid, tablet, capsule, microball, etc. and may be developed into various solid and liquid preparation forms for clinical application.

Description

[0001] 1. Technical field: the present invention belongs to the technical field of medicine, and the present invention relates to a pharmaceutical composition of allicin and garlic oil cyclodextrin derivative inclusion complex and a preparation method thereof. 2. Background technology: [0002] Allicin is a water-insoluble, slightly yellow, clear oily substance with garlic odor. Its chemical name is trithiodipropylene, and its structural formula is as follows: [0003] Molecular formula: C 6 h 10 S 3 , molecular weight: 178.33 [0004] Allicin has inhibitory and bactericidal effects on a variety of cocci, pertussis bacillus, diphtheria bacillus, Shigella, typhoid and paratyphoid bacillus, Escherichia coli, tubercle bacillus, etc. It has inhibitory effect on fungal infection, and also inhibits and kills amoeba, trichomonas vaginalis, pinworm, etc. Allicin injection is clinically applicable to deep fungal and bacterial infections, and is used to prevent and treat acute and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/10A61K47/36A61P31/04A61P31/10
Inventor 郭涛宋洪涛何仲贵
Owner GENERAL HOSPITAL OF THE NORTHERN WAR ZONE OF THE CHINESE PEOPLES LIBERATION ARMY
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