78 results about "Paricalcitol" patented technology

The invention relates to a preparation method of paricalcitol, which is characterized in that after hydroxyl in the vitamin D2 is protected by p-toluenesulfonates, in the presence of alkali, intramolecular cyclization reaction happens in methanol to generate a compound 5; the compound 5 undergoes allylic oxidation and hydroxyl is protected to obtain a key intermediate 7; in the presence of ozone,the side chains and exocyclic terminal double bonds of the key intermediate 7 are cut off to obtain a compound 8; the primary hydroxyl in the compound 8 is selectively protected, a three-membered ring is opened in the presence of acid and then hydroxyl is protected to obtain a key intermediate 11; after the secondary hydroxyl in the key intermediate 11 is protected by sulphonate, a compound 12 isobtained through reduction by LiAlH4; a compound 13 is obtained after the compound 12 is subjected to Swern oxidation and carries out Wittig reaction with the compound 12 to obtain a compound 14; andthe target compound can be obtained by removing the protective group in the compound 14. The reagents used in the method are simple and are convenient to operate, the reactions concerning regioselectivity and stereoselectivity are few, the route is shorter and 12 steps of reactions are carried out.

The invention discloses a high-stability paricalcitol pharmaceutical composition and a preparation method thereof. The medicinal composition comprises a cyclodextrin inclusion compound containing an active component paricalcitol and other pharmaceutically acceptable carriers, and is prepared by adopting a freeze-drying dry granulation process and strictly controlling temperature and humidity in the preparation process. The paricalcitol is included by cyclodextrin, and the freeze-drying and dry granulating preparation process is adopted, so that the defects that the main drug paricalcitol is extremely easily hygroscopic and extremely poor in stability and cannot be prepared into oral preparations can be greatly overcome, and the disintegration or main drug component dissolution cannot be influenced; and the paricalcitol pharmaceutical composition is not a coated tablet, so that the defect of slow dissolution of a conventional coated tablet can be avoided.