阿托伐他汀和匹格列酮对心血管高危人群的影响

目的探讨单独应用阿托伐他汀与联合应用阿托伐他汀和匹格列酮对高危心血管人群颈动脉内膜中层厚度（CIMT）、高敏C反应蛋白（hs-CRP）、基质金属蛋白酶-9（MMP-9）、脂联素及脂质状况的影响。方法90名有心血管危险因素的患者被随机分为两组：单独应用阿托伐他汀治疗组、联合应用阿托伐他汀和匹格列酮治疗组,分别检测两组患者治疗前及治疗六个月后的CIMT、hs-CRP、脂联素、MMP-9的血浆水平及检测血脂水平。结果单独应用阿托伐他汀及联合应用阿托伐他汀和匹格列酮均显示CIMT的显著降低（P〈0.001）,无组间差异（P〉0.05）。两组的MMP-9在治疗后均较治疗前降低,有统计学意义（P〈0.05）,但组间无统计学差异（P〉0.05）。两组对h-CRP、脂联素及血脂水平均有有意义的影响,组间有统计学差异,联合用药组提示影响更显著（P〈0.05）。联合用药组血浆脂联素水平明显升高而单独应用阿托伐他汀组未被观察到。结论阿托伐他汀明显改善CIMT,联合应用阿托伐他汀和匹格列酮对脂质状况和炎症因子有额外的影响。     

阿托伐他汀与辛伐他汀治疗高脂血症的效果

目的分析在高脂血症患者治疗中应用阿托伐他汀和辛伐他汀的降脂效果。方法将2017年1月—2020年1月在我院医治的90例高脂血症患者随机设为两个组别,给予对照组(45例)辛伐他汀治疗,给予试验组(45例)阿托伐他汀治疗。观察两组患者治疗前后血脂水平和生化指标变化情况。结果试验组治疗后总胆固醇、三酰甘油、低密度脂蛋白胆固醇低于对照组,高密度脂蛋白胆固醇高于对照组,两组对比差异具有统计学意义(P<0.05)。两组患者治疗后肌酐、尿素氮指标差异无统计学意义(P>0.05)。结论阿托伐他汀和辛伐他汀应用于高脂血症患者治疗中均能起到不同程度的降脂效果,但阿托伐他汀的效果更好,安全可靠。     

国产与进口阿托伐他汀治疗高脂血症的比较

目的:比较国产与进口阿托代他汀治疗高脂血症的疗效。方法:选择原发性高脂血症患者76例,随机分为国产阿托伐他汀(10mg·d~(-1))组和进口阿托伐他汀(10mg·d~(-1))组各38例,均治疗8周。结果:2组治疗4周时总胆固醇(TC)、三酰甘油(TG)、低密度脂蛋白胆固醇(LDL-C)均开始显著下降(P<0.01),治疗8周高密度脂蛋白胆固醇(HDL-C)开始显著上升(P<0.05),但2组间比较差异无显著意义(P>0.05);不良反应发生率国产组10.5％,进口组7.9％,2组差别无显著意义(P>0.05)。结论:国产阿托伐他汀与进口阿托伐他汀均有明显的调脂效果,两者使用均较安全。     

阿托伐他汀自微乳释药系统的制备和评价

目的制备阿托伐他汀自微乳，为自微乳释药系统的处方设计和体内外评价提供参考。方法采用伪三元相图法研究不同乳化剂、助乳化剂和油相形成微乳的能力和区域，绘制不同处方组成的相图，在此基础上制备阿托伐他汀自微乳，比较温度、介质、稀释等因素对自微乳效率的影响，进行自微乳时间、所成微乳的形态、粒径分布、zeta电位、含量和稳定性等体外评价Beagle犬体内药代动力学研究。结果理想的处方经分散后可得到平均粒径在100 nm以下、呈高斯分布的微乳，稳定性好，自微乳效率高，在Beagle犬体内的吸收明显高于市售片剂。结论本文首次研制阿托伐他汀自微乳，稳定性好，在Beagle犬体内的生物利用度高。     

(S)-3-羟基-γ-丁内酯的合成

(S)-3-羟基-γ-丁内酯(1)是重要的手性源化合物,也是制备降血脂药物阿托伐他汀[1]、神经介质L肉碱[2]、HIV蛋白酶抑制剂氨普那韦(amprenavir)[3]、饱感剂(2S,4S)-2-羟基-4-羟甲基-4-丁内酯[4]、治疗皮肤病药羟基二十碳四烯酸(12-HETE)[5]和抗癌药aplysistatin[6]等的关键中间体.近年来,国外关于1合成的报道较多,国内主要靠进口产品供应.因此,研究工业化合成1的方法具有重要意义.     

Comparative study between atorvastatin and losartan on high fat diet‐induced type 2 diabetes mellitus in rats

Obesity is often associated with chronic inflammatory state which contributes to the development of insulin resistance (IR) and type 2 diabetes mellitus (T2DM). This study investigated the effects of single and combined administration of atorvastatin (ATOR, lipid‐lowering drug) and losartan (LOS, angiotensin receptor antagonist) on metabolic disorders and inflammatory status that are implicated in the development of T2DM with the use of pioglitazone (PIO) as a standard antidiabetic drug. T2DM was induced in male rats by high‐fat diet (HFD) feeding for 16 weeks. Oral administrations of ATOR (10 mg/kg), LOS (20 mg/kg), PIO (3 mg/kg), their binary combinations, or vehicle were started in the last 4 weeks. Fasting serum glucose, oral glucose tolerance, fasting serum insulin, IR, serum lipid profile, serum TNF‐α and body composition index were determined. Results showed that all drugs and their combinations had positive impact effect on all measured parameters, and better results were achieved from binary drug combinations than administration of each drug alone. Combination of PIO with either ATOR or LOS provided better improvements on T2DM‐associated metabolic abnormalities and inflammatory status with respect to each drug alone. However, the most pronounced effects of drugs and their combinations regarding the above parameters were attributed to LOS + PIO combination. In conclusion, this study indicates that combination of ATOR + PIO and, in particular, LOS + PIO can be used as promising effective therapies in the management of HFD‐induced T2DM. This concept may be attributed to the combined effects of the respective monotherapies to improve lipid profile, insulin sensitivity, and TNF‐α level.     

Atorvastatin

Atorvastatin (Lipitor?, Pfizer) is a safe and effective 3-hydroxy-3-methyl-glutaryl-CoA (HMG-CoA) reductase inhibitor (statin). It is the most potent currently available statin in terms of lowering low-density lipoprotein (LDL) and total cholesterol levels. It was the first statin shown to lower triglycerides in patients with isolated hypertriglyceridaemia. It has a good safety profile. In common with other statins, it has non-lipid-lowering effects including improving endothelial function, antiproliferative actions on smooth muscle and reducing platelet aggregation. It also has anti-inflammatory effects and may reduce plasma glucose levels. Clinical trial evidence with this statin is currently limited. It did slightly reduce events in the AVERT trial comparing patients receiving coronary angioplasty with those receiving high-dose atorvastatin therapy and in the MIRACL study reduced ischemia in patients with acute coronary syndromes. Other end point trials are in progress.