Oridonin clathrate compound, and medicinal prepn. thereof

Abstract

An inclusion compound of rebescensine A is prepared from the rebescensine A as active component and cyclodextrin as including material in the weight ratio of 1: (0.5-50). A medicine containing said inclusion compound is also disclosed.

Description

technical field [0001] The invention relates to a pharmaceutical preparation of oridonin A as a therapeutic active ingredient, in particular to an inclusion compound of oridonin obtained by adopting cyclodextrin inclusion technology and related pharmaceutical preparations prepared by using the inclusion compound. Background technique [0002] Oridonin A is an alkene diterpene extracted from Oridonin grass. Rabdosiarubescens (Hemsl) Hara, also known as broken mia, snowflake grass, is a plant of the genus Coriander in the Lamiaceae family. It is a traditional Chinese herbal medicine that has the effects of clearing heat, detoxifying, reducing inflammation and relieving pain. In 1991, the Ministry of Health of my country approved its dried leaves and aerial parts as Chinese herbal medicines, which were included in the Ministry of Health's standards for Chinese herbal medicines. Since the 1970s in my country, a lot of research has been done on the chemical constituents, pharmac...

AI Technical Summary

Problems solved by technology

Chinese patent application 200510046253.3 provides a kind of oridonin liposome for the defects of low drug loading and encapsulation efficiency of the above-mentioned oridonin emulsion, indicating that it can increase the drug loading of the medicament

[0007] From the records of the above-mentioned prior patents, it can be seen that in order to stabilize the preparation, a relatively large amount of oil, emulsifier and isotonic agent must be added to the preparation of Rubescensin A emulsion, which is easy to introduce some allergenic ingredients

The earliest developed Rubescensin A emulsion is because it contains a lot of alcohol and oil, which is obviously sensitized in clinical use and cannot be applied.

The preparation of Rubescensin A liposome then requires a relatively large amount of packaging material (phospholipid), stabilizer, water-soluble carrier, etc.; from the perspective of industrial production, the preparation of pharmaceutical preparations in the form of microemulsions and liposomes requires production equipment High, especially after encapsulating the main drug, high-power emulsification equipment is required to make the encapsulation highly dispersed, such as high-pressure homogenization equipment, which makes the process more complicated; in addition, the main ones currently used in liposome preparation The raw material is still lecithin, and its quality has a great influence on the final liposome, so the lecithin used in the pharmaceutical industry is mainly imported

[0008] Therefore, processing oridonin into appropriate preparations at this stage, its complex process, high input equipment and high cost of raw materials constitute constraints for some small-scale pharmaceutical companies

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