Recover Lovastatin From Mother Liquor Of Crude Crystalline By Large Porous Resin

As one of hypocholesterol-lowering drugs, Lovastatin has a clear mechanism of action and outstanding curative effects. So it is generously recognized in both medical field and industry field. At the same time, being precursor of worldwide popular medicine--Simvastatin, Lovastatin is very important to development and application of statins. Improving quality of Lovastatin is an effective mean to decrease manufacture costs, improve quality and increase profits.At present, two basic methods were widely used in purification and extraction of Lovastatin. The first method was developed by Merck Co.. After one or two steps of silica chromatography combined with gel filtration, pure Lovastatin was obtained. Although the quality of final product was excellent, the yield was not high, for its long purification route and complex chromatography process. The other method is quite simple. Lovastatin was converted into different solvents. Then, crude Lovastatin was crystallized directly from organic solvent. The biggest problem of this process is that the yield of crystallization is only 50%.This study is based on the structure analysis of Lovastatin lactone ring. Firstly, the mother liquor of Lovastatin was treated with sodium hydroxide to cleave the lactone ring. Thus, soluble (in water) Lovastatin salt was formed. Then big porous absorbent was introduced to wipe off most impurities. And followed with crystallization in organic reagents. In this way, the total recovery increased 10%. This study also established the favorable conditions to this reaction by orthogonal experiments.: Base concentration: 0.2mol/L, Reaction temperature: 50℃, Reaction time: 2hours.Under this condition, the percentage of cleaved Lovastatin was more than 90. Moreover, the content of open-ring Lovastatin in water phase was 92% detected by HPLC.In this article, one big porous absorbent C001 was screened out from 14 absorbents by dynamic-state and static-state method. On this basis, optimizations about adsorption and desorption parameters was performed and the proper operating parameters were obtained.: Loading sample pH <5.0,Loading flow rate: 0.6 times column volume/hour, PH of eluant: 8.0-8.5, Ethanol content in eluant :>80%. When this process was applied in pilot-scale production, the total recovery improved about 10%.At last, this article discussed dynamic behavior of Lovastatin on absorbent C001 with Freundilich empirical equation. This absorption behavior can be described as: m = 7.79c0.1756...