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pravastatin(P),罗代他丁(L),mevastatin(M),斯伐他丁(S)为新型3-羟基-3-甲基戊二酰辅酶A(HMG—CoA)还原酶抑制剂,它们可以竞争性抑制微粒体HMG-CoA还原酶,减少肝细胞内胆固醇合成,从而降低循环中脂蛋白胆固醇浓度。临床常用P的活性羟酸型,L,M,S则以前药内酯型给药,用药后部分内酯型可在体内转化为相应的活性羟酸型。本文对比P,L,M,S辛醇-水的分配系数(P_(o/w)),研究了四种药的亲脂性、水溶性及结构和药理作用。P钠盐及内酯型(日本东京Sankyo公司),L,M,S及羟酸型钠盐(美国新泽西州New Brunswick的Squibb医研会),HPLC系列包括WISP 710B自动注射器,Altex
pravastatin (P), lovastatin (L), mevastatin (M), and simvastatin (S) are novel 3-hydroxy-3- methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors, They can competitively inhibit microsomal HMG-CoA reductase, reduce hepatic intracellular cholesterol synthesis, thereby reducing circulating lipoprotein cholesterol levels. The commonly used active hydroxy acid type of P, L, M, S is the prodrug lactone type administration, part of the lactone type can be converted to the corresponding active hydroxy acid type in vivo. In this paper, we compared the partition coefficient (P_ (o / w)) of P, L, M and S octanol-water and studied the lipophilicity, water solubility, structure and pharmacology of the four drugs. P Sodium Salt and Lactone Formulations (Sankyo, Tokyo, Japan), L, M, S and Sodium Hydroxyacid Squibb Research Laboratories, New Brunswick, NJ, USA The HPLC series includes the WISP 710B autoinjector, Altex