The Purification And Identification Of Impurities In Lovastatin

This article reviewed the pharmacological effects and clinical applications of statins (a kind of medicines inhibiting hydroxymethyl coenzyme A reductase), as well as the update progress in the studies on pharmacology and production of lovastatin-one important member of statins, and made a conclusion that the prospect of lovastatin will still be good or even better.The development of technology put a higher standard on the pharmaceutical products. USP requires that the total impurities in lovastatin should be less than 1.0% and a single impurity should be less than 0.2%, unless sufficient data are provided to prove that the impurity has the same pharmacological activities as the principal component, and that the impurity has no other toxicological effects. China is the major supplier of raw materials of lovastatin to the whole world. In order to meet the new national pharmacopoeia requirements of lovastatin, it is necessary to carry out basic study on impurities in lovastatin. First, compounds should be obtained to identify their structures and study their properties. Then those should make clear in which steps these impurities are generated, how to reduce the production of the impurities, and how to remove them. Meanwhile, enough amount of monomer impurities should be accumulated to conduct various pharmacological and toxicological studies.This paper is aimed at purifying the impurities of lovastatin and identifying their structures. In this study, the crystal liquor of lovastatin from the final step of extraction and purification was separated by repeatedly silica gel column chromatography, silica gel preparative TLC, RP-silica gel column chromatography, semi-preparative HPLC and other methods and 6 pure compounds were obtained. The structures of the 6 compounds were elucidated on the basis of analying the spectral data of FT-IR, 'H-NMR,13C-NMR,'H-'H COSY, HSQC, HMBC and MS and they were identified as: 1, anhydromonacolin L; 2, anhydrodihydromonacolin K; 3, acid form of Monacolin L; 4, methyl ester of hydroxy acid form of monacolin L; 5, dihydromonacolin K; 6, acid form of dihydromonacolin K.