Extraction, separation and purification process of rapamycin/sirolimus

Rapamycin (RAPA, trade name Sirolimus) is a new type of macrolide immunosuppressant with highly effective immunosuppressive effect. From the perspective of clinical application, rapamycin has a good anti-rejection effect, and has a good synergistic effect with immunosuppressants such as cyclosporine A (CsA) and tacrolimus (FK506), which is a curative effect A new type of immunosuppressant with good, low toxicity and no renal toxicity. In recent years, the United States Renaming Committee named rapamycin (Rapamycin) as Sirolimus (Sirolimus, SRL), and the marketed product name was Rapamune (RAPA). RAPA is a macrolide compound extracted from the fermentation broth of Streptomyces hygroscopicus. Its relative molecular weight is 914.2. It has a similar structure to another immunosuppressant FK506. It is easily soluble in hexanol and chloroform. , Acetone and other organic solvents, very slightly soluble in water.

Rapamycin derivatives were approved by the U.S. Food and Drug Administration (FDA). For example, temsirolimus was approved by the FDA in May 2007 for the treatment of advanced renal cell carcinoma (RCC). Everolimus ( everolimus) was approved by the FDA in March 2009 for the treatment of advanced RCC that failed sunitinib or sorafenib treatment. There are also several clinical studies on deforolimus in progress.

The structure of rapamycin is similar to tacrolimus, and the extraction and purification method is similar to it. On the basis of learning from foreign separation and purification methods, the process has been greatly improved. Jinan Bona Biological has developed a process that is more suitable for industrial production. :

The fermentation broth is added with filter aid to filter the bacteria-ethanol or acetone extraction-concentrated solution-extraction decolorization-alumina chromatography column (SKS-30-200 acidic alumina)-ethyl acetate n-hexane- Acetone n-hexane-chromatography system-concentration SKP-10-4300 chromatography medium ethanol acetone acetonitrile system gradient-purity greater than 99%, can achieve effective separation of rapamycin and FR901556 impurities.

At the same time, the SKP-10-4300 chromatographic medium developed by the company has also been successfully applied to the separation and purification of temsirolimus isomers and related substances of everolimus products.

If you purchase SKP-10-4300 chromatography packing, SKS-30-200 acid alumina or request samples, please call our company 0531-88804339, our company will provide you with detailed technical support.