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Hydroxypropyl cyclodextrin inclusion compound and preparation method thereof

A technology of hydroxypropyl cyclodextrin and inclusion compound is applied in the directions of pharmaceutical formulations, active ingredients of anhydride/acid/halide, and medical preparations of non-active ingredients, which can solve the problem of high production cost and achieve low production cost. Effect

Pending Publication Date: 2022-07-08
湖州嘉亨实业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since this preparation method requires multiple complex processes such as acidification, precipitation, and ultrasonic fusion reaction, the production cost is relatively high

Method used

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  • Hydroxypropyl cyclodextrin inclusion compound and preparation method thereof

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Comparison scheme
Effect test

Embodiment 1

[0034] The preparation method of the hydroxypropyl cyclodextrin inclusion compound provided in this embodiment comprises the following steps:

[0035] S1. Using trimethylpentanediol / adipic acid / glycerin cross-linked polymer as a solvent, at a temperature of 50℃-60℃, dissolve 5% of azelaic acid in 60% of trimethylpentanedioic acid alcohol / adipic acid / glycerin cross-linked polymer, and stirring to a transparent and clear state to obtain azelaic acid mixture as an active phase.

[0036] S2. Completely dissolve 35% of hydroxypropyl cyclodextrin in deionized water, wherein the quality of deionized water is 20 times that of hydroxypropyl cyclodextrin, and stir to a transparent and clear state at the same time to obtain hydroxypropyl cyclodextrin An aqueous solution of cyclodextrin as the cyclodextrin phase.

[0037] S3. Cool the azelaic acid mixture as the active phase to 30°C, and at a temperature of 30°C, add the azelaic acid mixture to the hydroxypropyl cyclodextrin aqueous solu...

Embodiment 2

[0039] The difference between the preparation method of hydroxypropyl cyclodextrin inclusion compound provided in this embodiment and Embodiment 1 is only in that the temperature conditions in step S3 are different. Specifically, step S3 in this embodiment is as follows:

[0040] S3. Cool the azelaic acid mixture as the active phase to 40°C, and at a temperature of 40°C, add the azelaic acid mixture to the hydroxypropyl cyclodextrin aqueous solution uniformly and slowly dropwise, and stir To a transparent and clear state, the addition time is controlled at more than 20 minutes, and the stirring state is maintained during the addition process. The stirring speed used during stirring is 50 rpm; after that, the temperature condition and stirring speed of 40 ° C are maintained, and stirring is continued for more than 60 minutes. Propylcyclodextrin inclusion complex solution.

Embodiment 3

[0042] In the preparation method of the inclusion compound of hydroxypropyl cyclodextrin provided in this example, the difference in Example 1 is only in that the solvent in step S1 is different and the mass percentage of hydroxypropyl cyclodextrin in step S2 is different. In step S1, this embodiment uses 65% trimethylpentanediol / adipic acid / glycerin cross-linked polymer as a solvent, that is, 5% azelaic acid is dissolved in 65% trimethylpentanediol / adipic acid / glycerol cross-linked polymer; in step S2, this example uses 30% hydroxypropyl cyclodextrin, that is, 30% hydroxypropyl cyclodextrin is completely dissolved in deionized in water.

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Abstract

The invention provides a hydroxypropyl cyclodextrin inclusion compound, which is prepared from the following components in percentage by mass: 1 to 8 percent of azelaic acid or ellagic acid, 42 to 89 percent of trimethylpentanediol / adipic acid / glycerol cross-linked polymer, 10 to 50 percent of hydroxypropyl cyclodextrin, 10 to 50 percent of hydroxypropyl cyclodextrin, 10 to 50 percent of sodium carboxymethyl cellulose, 10 to 50 percent of sodium carboxymethyl cellulose and 10 to 50 percent of sodium carboxymethyl cellulose. The mass percentage content of the hydroxypropyl cyclodextrin is greater than or equal to six times of the mass percentage content of the azelaic acid or the ellagic acid. The invention also provides a preparation method of the hydroxypropyl cyclodextrin inclusion compound. According to the hydroxypropyl cyclodextrin inclusion compound and the preparation method thereof provided by the invention, heating and stirring equipment commonly used by production enterprises is adopted, an organic solvent is not needed, inclusion of cyclodextrin molecules with azelaic acid or ellagic acid is realized through synergistic compounding of trimethyl pentanediol / adipic acid / glycerol cross-linked polymers with a moisturizing effect, and the preparation cost is relatively low. According to the preparation method provided by the invention, the active molecules can be stably and efficiently wrapped, and the bioavailability of the active molecules is improved.

Description

technical field [0001] The invention relates to a chemical preparation and a preparation method thereof, in particular to a hydroxypropyl cyclodextrin inclusion compound and a preparation method thereof. Background technique [0002] Azelaic acid (also known as azelaic acid) and ellagic acid are both naturally occurring organic compounds, both of which have relatively low solubility in water and are slightly soluble in water. [0003] Cyclodextrin is a cyclic oligosaccharide substance generated from amylose. It has a variety of homologues and can be divided into α-cyclodextrin, β-cyclodextrin and γ-cyclodextrin according to the structure. Propyl β-cyclodextrin (also known as hydroxypropyl cyclodextrin or hydroxypropyl beta cyclodextrin) has good hydrophilicity at the outer end and hydrophobicity inside, and has properties similar to surfactants. The preparation of the compound provides favorable conditions, so it is widely used in the field of traditional Chinese medicine, ...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K31/20A61K31/366
CPCA61K47/6951A61K31/20A61K31/366Y02P20/54
Inventor 郑中博张浩洋曹平陆徐佳贾兵李晞暘刘陈陈
Owner 湖州嘉亨实业有限公司
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