Preparation and application of astragaloside IV hydroxypropyl beta cyclodextrin inclusion complex

Astragaloside IV is a high purity drug extracted from Astragalus membranaceus. It can improve cardiopulmonary function, strengthen cardiac contractility, dilate blood vessels, reduce blood pressure, improve skin blood circulation and nutritional status; it can also protect liver, prevent the decrease of liver glycogen, enhance immunity, increase energy, resist fatigue, make mutation, protect liver and inhibit osteoclasts.

However, the solubility of astragaloside IV in water is very poor, and the bioavailability of oral administration is very low, which can not meet the clinical needs. If it is prepared into various injection types, the efficacy of intravenous administration will be significantly improved. It is proved that the inclusion of HPLCD and p-astragaloside IV can be used as the route of injection, and it is the best way to enhance the solubility of astragaloside IV in water.

The preparation method of astragaloside IV hydroxypropyl betacyclodextrin inclusion complex is as follows:

In water or aqueous ethanol medium, the astragaloside IV was reacted with hydroxypropyl beta cyclodextrin at a certain ratio of 1: 1-150. The solution was filtered to clarify by microporous filter membrane, and the inclusion compound was separated from the mixture. The inclusion compound could be separated from the mixture by filtration, centrifugation, freeze drying, spray drying or real air drying, and the desired pharmaceutical preparations were prepared.

Hydroxypropyl betacyclodextrin, with barrel molecular structure, molecular weight of 1540, easily soluble in water, large inclusion amount, no hemolytic reaction, low toxicity, can be used in injection. The results show that astragaloside IV and hydroxypropyl betacyclodextrin can be easily dissolved in water and the stability is improved.

Astragaloside IV hydroxypropyl beta cyclodextrin inclusion complex is currently used in the preparation of injection. For example, it can be used in small needle, infusion, injection or powder injection and other pharmaceutical preparations. It can significantly improve the solubility of astragaloside IV in water, thus providing the inclusion compound of astragaloside IV cyclodextrin derivatives for injection, meeting the clinical needs.