Which factors affect Degree of substitution of hydroxypropyl betadex?

Hydroxypropyl betacyclodextrin has good solubilization and solubilization effect, which can increase the bioavailability, control the sustained release and reduce the irritation to human body. Therefore, it has a very broad application prospect in the fields of pharmaceutics and chiral separation.

The influence of reaction conditions on the average degree of substitution was obtained by response surface methodology.

The experimental results as below:

1、 The average degree of substitution and the substitution position of hydroxypropyl group were greatly affected by the concentration of alkali. The average degree of substitution of the product increases with the increase of alkali concentration. When the base concentration is low, it is very easy to form 2-hydroxypropyl- β- When the concentration of cyclodextrin is high, it is easy to form 6-substituted 2-hydroxypropyl- β- Cyclodextrin;

2、 The concentration of propylene oxide in the raw material also has a great influence on the average degree of substitution and the substitution position of hydroxypropyl group. With the increase of propylene oxide in raw materials and β- With the increase of the molar ratio of cyclodextrin, the average degree of substitution of the product will also increase. When propylene oxide: 1 β- When the ratio of cyclodextrin is between 10:1 and 12:1, the average degree of substitution increases slowly.

The reaction time of hydroxypropyl betacyclodextrin is different under different alkali concentration. When the concentration of alkali is relatively low, the reaction will basically end after 24 hours, while when the concentration of alkali is relatively high, it will take at least 72 hours to complete the reaction.

Company name: Shandong Binzhou Zhiyuan Biotechnology Co.,Ltd