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Cyclodextrin inclusion compound of 3,5-dyhydroxyl-4-isopropyl toluylene and preparation method thereof

A technology of isopropyl stilbene and cyclodextrin inclusion complex, applied in the field of chemistry, can solve the problems of low water solubility, low dissolution rate, poor drug stability, etc., and achieves improved stability, bioavailability, solubility and stability. The effect of increased dissolution and high production efficiency

Inactive Publication Date: 2012-01-25
HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the poor molecular stability of 3,5-dihydroxy-4-isopropyl stilbene, it is easily oxidized in the air, resulting in changes in the color and performance of the product, and poor drug stability; in addition, the compound has low water solubility, Low dissolution rate, drug irritating, low bioavailability

Method used

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  • Cyclodextrin inclusion compound of 3,5-dyhydroxyl-4-isopropyl toluylene and preparation method thereof
  • Cyclodextrin inclusion compound of 3,5-dyhydroxyl-4-isopropyl toluylene and preparation method thereof

Examples

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Effect test

Embodiment 1-9

[0026] Example 1-9 Preparation of cyclodextrin inclusion compound of 3,5-dihydroxy-4-isopropylstilbene by grinding method

[0027] The raw material ratio of each embodiment is shown in the table below:

[0028]

[0029] Its preparation method is carried out according to the following step sequence:

[0030] (11) Take clathrate material and deionized water with a weight ratio of 1:1.5-5, mix them in a mortar and grind for 8-12 minutes to obtain solution A1;

[0031] (12) Take the drug 3,5-dihydroxy-4-isopropyl stilbene and alcohol solvent in a weight ratio of 1:2, mix and dissolve to obtain solution B1;

[0032] (13) Solution B1 is gradually added dropwise to solution A1. After continuing to grind, put it in the refrigerator for 24--26 hours, filter it with suction, wash it, dry it and grind it into a uniform powder to obtain 3,5-dihydroxy-4 - Cyclodextrin inclusion complex of isopropylstilbene.

[0033] Below take embodiment 2 as example to illustrate the specific operat...

Embodiment 10-18

[0037] Example 10-18 Preparation of cyclodextrin inclusion compound of 3,5-dihydroxy-4-isopropylstilbene by ultrasonic method

[0038] The raw material ratio of each embodiment is shown in the table below:

[0039]

[0040] Its preparation method is an ultrasonic method, and is carried out according to the following sequence of steps:

[0041] (21) Take clathrate material and deionized water with a weight ratio of 1:12.5--25, heat ultrasonically, mix evenly and dissolve to obtain solution A2;

[0042] (22) Take the drug 3,5-dihydroxy-4-isopropyl stilbene and alcohols inclusion solvent with a weight ratio of 1:2, mix and dissolve to obtain solution B2; gradually drop solution B2 during the ultrasonic process Add it to the solution A2 kept at 10-60°C, continue to sonicate until the total ultrasonic time is 5-35min, put it in the refrigerator for 24-26h, filter with suction, wash and dry to get 3,5-dihydroxy-4-isopropyl Cyclodextrin inclusion complexes of stilbenes.

[0043...

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Abstract

The invention discloses a cyclodextrin inclusion compound of 3,5-dyhydroxyl-4-isopropyl toluylene and a preparation method thereof. In the invention, by adopting cyclodextrin to wrapping a medicine, the solubility and the dissolution of the medicine are increased, the stability and the bioavailability of the medicine are improved, and the aim of slowly-controlled release of the medicine can be simultaneously achieved. The invention also provides the preparation method of the cyclodextrin inclusion compound of the 3,5-dyhydroxyl-4-isopropyl toluylene, which is simple in operation, safe and convenient, and high in production efficiency; and the prepared inclusion compound can be used as a slow-release and targeting preparation and provides a new dosage form for medicine production.

Description

technical field [0001] The invention belongs to the field of chemistry, and in particular relates to a cyclodextrin inclusion compound of 3,5-dihydroxy-4-isopropylstilbene and a preparation method thereof. Background technique [0002] 3,5-dihydroxy-4-isopropyl stilbene has good antifungal properties and can be used to treat intractable psoriasis and other diseases. However, due to the poor molecular stability of 3,5-dihydroxy-4-isopropyl stilbene, it is easily oxidized in the air, resulting in changes in the color and performance of the product, and poor drug stability; in addition, the compound has low water solubility, Dissolution rate is low, drug irritating, bioavailability is low. [0003] Cyclodextrin itself is non-toxic and has a cylindrical structure with both ends and the outside being hydrophilic, while the inside of the cylinder is hydrophobic. Cyclodextrin can contain a variety of drugs. Inclusion is a physical process. Using the particularity of cyclodextrin'...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61K31/047A61P17/06A61P31/10A61K47/61
Inventor 张越韩玉翠赵树春高春辉刘惠娴
Owner HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY
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