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Preparation method of inclusion compound of salicylate hydroxypropyl beta-cyclodextrin

A technology of hydroxypropyl salicylic acid and beta cyclodextrin, applied in the directions of active ingredients of salicylic acid, medical preparations of non-active ingredients, pharmaceutical formulations, etc., can solve the problems of limited application, difficult storage and transportation, and stable aqueous solution. It can overcome the problems of poor stability, low cost and simple production process.

Inactive Publication Date: 2018-07-20
SHANDONG BINZHOU ZHIYUAN BIO TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In summary, using different cyclodextrins or cyclodextrin derivatives to clathrate salicylic acid will obtain different effects; meanwhile, the clathrate aqueous solution obtained by the above-mentioned patent method has poor stability, is not easy to store and transport, and limits Its application in medicine, health care and cosmetics

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1 A preparation method for inclusion compound of hydroxypropyl beta-cyclodextrin salicylate, comprising the following steps: adding 70kg of purified water and 30kg of hydroxypropyl-beta-cyclodextrin to a 100L glass kettle successively, and slowly passing through Enter nitrogen, heat up to 60°C, stir to dissolve; add 3kg of salicylic acid, keep stirring at 60°C for 3 hours, then cool down to below 40°C, filter out impurities through multi-layer filter cloth; use LPG-20 dryer at 60°C Spray drying to obtain the inclusion compound of hydroxypropyl beta-cyclodextrin salicylate.

Embodiment 2

[0021] Example 2 A preparation method for inclusion compound of hydroxypropyl beta-cyclodextrin salicylate, comprising the following steps: adding 70kg of purified water and 30kg of hydroxypropyl-beta-cyclodextrin to a 100L glass kettle in sequence, and slowly passing through Enter nitrogen, heat up to 60°C, stir and dissolve; add 4.5kg salicylic acid, keep stirring at 60°C for 3 hours, then cool down to below 40°C, filter out impurities through multi-layer filter cloth; use LPG-20 dryer at 80°C °C spray-dry to obtain the inclusion compound of hydroxypropyl beta-cyclodextrin salicylate.

Embodiment 3

[0022] Example 3 A preparation method for inclusion compound of hydroxypropyl beta-cyclodextrin salicylate, comprising the following steps: sequentially add 70kg of purified water and 30kg of hydroxypropyl-beta-cyclodextrin into a 100L glass kettle, and slowly pass through Enter nitrogen, heat up to 60°C, stir and dissolve; add 3.6kg salicylic acid, keep stirring at 60°C for 3 hours, then cool down to below 40°C, filter out impurities through multi-layer filter cloth; use LPG-20 dryer at 70°C °C spray-dry to obtain the inclusion compound of hydroxypropyl beta-cyclodextrin salicylate.

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Abstract

The invention discloses a preparation method of an inclusion compound of salicylate hydroxypropyl beta-cyclodextrin. The method comprises the following steps: sequentially adding purified water and hydroxypropyl beta-cyclodextrin into a glass kettle, slowly introducing nitrogen gas, heating up to 60 DEG C, and stirring for dissolving; adding salicylic acid, stirring for 3 hours at 60 DEG C, then cooling to 40 DEG C or below, and filtering out impurities by means of multi-layer filter cloth; carrying out spray drying at 60-80 DEG C to obtain the inclusion compound of the salicylate hydroxypropyl beta-cyclodextrin. The solid inclusion compound prepared by the method can be completely dissolved in water, and overcomes the defects that salicylic acid is poor in stability and the high in irritation. Furthermore, the inclusion compound of the salicylate hydroxypropyl beta-cyclodextrin overcomes the defects that the original natural cyclodextrin is low in inclusion rate, poor in aqueous solution stability, and difficult in preservation, transportation and use; the preparation method is beneficial to the application of salicylic acid in medicine, health care and cosmetics.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a preparation method of a hydroxypropyl beta cyclodextrin inclusion compound of salicylate. Background technique [0002] Salicylic acid (also known as salicylic acid and o-hydroxybenzoic acid) is easily soluble in ethanol, ether, chloroform, benzene, acetone, and turpentine, but not easily soluble in water (solubility at 20°C is 0.2g / 100ml). Salicylic acid can be used in medicine to relieve pain and fever, as well as anti-inflammatory effects. Salicylic acid is also a key ingredient in many skin care products, used to treat seborrheic dermatitis, acne, psoriasis, corns, keratosis pilaris, etc. Topical application has antimicrobial properties against microorganisms. Salicylic acid is a phenolic hormone in agriculture that regulates plant growth and development. However, its application is greatly limited due to its side effects such as strong irritation and poor peel...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/60A61K47/69A61K8/365A61K8/73A61K8/02
CPCA61K31/60A61K8/0225A61K8/365A61K8/738
Inventor 赵大波安伟李媛媛梁宁宁盛玉春
Owner SHANDONG BINZHOU ZHIYUAN BIO TECH CO LTD