Efficacy and safety of simvastatin (alone or in association with cholestyramine). A 1-year study in 66 patients with type II hyperlipoproteinaemia

The effects and safety of simvastatin, an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase, were investigated alone or in association with cholestyramine in 66 patients with hypercholesterolaemia, in a 1-year study. In type IIa hypercholesterolaemia (41 patients), the association was more effective than simvastatin used alone in lowering total cholesterol (37% vs 29%) and LDL-cholesterol (45% vs 37%). In type IIb hypercholesterolaemia (23 patients), the association simvastatin-cholestyramine did not appear more effective than simvastatin used alone. The decrease of apoprotein B was parallel to the LDL-cholesterol decrease. Apoprotein A1 did not change significantly. The long-term safety of simvastatin was good. No lens opacity was noted. The most serious side-effect in our study was myolysis which occurred in two patients with a marked increase in creatine phosphokinase.     

通心络联合辛伐他汀治疗脂肪肝96例临床疗效观察

目的观察通心络联合辛伐他汀在非酒精性脂肪肝治疗中的作用及半年复发率。方法随机将非酒精性脂肪肝门诊患者分为治疗组96例,给通心络胶囊3粒口服,每日3次,辛伐他汀5 mg口服,每日2次;对照组54例,辛伐他汀5 mg口服,每日2次;疗程均2个月。治疗2个月和随访6个月后检查血脂、肝脏超声。结果总有效率及半年血脂复发率治疗组与对照组分别为90.6%、9.2%和72.2%、23.1%,二组比较,有明显差异,P<0.05。结论通心络联合辛伐他汀能有效降低血脂及治疗脂肪肝,无明显副作用。     

辛伐他汀对人牙髓干细胞增殖和分化的影响

目的:研究辛伐他汀对人牙髓干细胞(dental pulpstem cells,DPSCs)增殖和成骨分化的影响。方法:将第3代人DPSCs在矿化培养液中诱导培养,同时加入不同浓度的辛伐他汀(1×10-5mol/L、1×10-6mol/L、1×10-7mol/L、1×10-8mol/L),噻唑蓝(methyl thiazolyl tetrazolium,MTT)法检测细胞增殖情况,碱性磷酸酶试剂盒检测碱性磷酸酶(alkaline phosphatase,ALP)活性,茜素红染色鉴定成骨分化。结果:各浓度辛伐他汀均抑制人DPSCs增值,辛伐他汀浓度为1×10-5mol/L时,抑制作用最明显。适宜浓度辛伐他汀(1×10-6mol/L、1×10-7mol/L、1×10-8mol/L)促进人DPSCs向成骨细胞分化,其中,1×10-7mol/L的辛伐他汀促进ALP活性的作用最明显。结论:辛伐他汀抑制人DPSCs的增值,适宜浓度的辛伐他汀可有效促进人DPSCs的成骨分化。     

辛伐他汀渗透泵型控释片的含量测定

目的建立用高效液相色谱法（HPIC法）测定辛伐他汀渗透泵型控释片含量的方法。方法以十八烷基硅烷键合硅胶为固定相，以乙腈-pH值为4．5的0．0025mol／L磷酸二氢钠溶液（65：35）为流动相，流速为1mL／min，检测波长为238nm。结果辛伐他汀溶液的质量浓度在18．0～60．0μg／mL范围内与峰面积线性关系良好，回收率与精密度均良好。结论HPLC法可准确测定辛伐他汀渗透泵型控释片的含量。     

血脂康与辛伐他汀治疗原发性高脂血症的对比研究

目的比较中药血脂康、辛伐他汀(舒降之)治疗原发性高脂血症的调脂作用和安全性。方法80例原发性高脂血症患者随机分为血脂康组和舒降之组,各服药8周为1个疗程,治疗期间患者保持治疗前的饮食习惯,不用其他干扰血脂代谢的药物。8周后观察两组调脂效果和不良反应。结果血脂康组:TC降低25.15%,TG降低21.22%,DL-C降低38.08%,TC-HDL-C/HDL-C降低44.03%。舒降之组:TC降低26.02%,TG降低22.62%,LDL-C降低38.50%,TC-HDL-C/HDL-C降低44.22%,两组各项指标治疗后的组内相比,均有统计学意义(P<0.001),两组间各项指标治疗后对应比较均无统计学意义(P>0.05),两组间不良反应轻微,不影响继续治疗,不良反应总发生率血脂康组较低(P<0.05)。结论血脂康和辛伐他汀均有强大的降低TC、TG、LDL-C和TC-HDL-C/HDL-C的作用,均为治疗原发性高脂血症有效和安全的药物,血脂康不良反应更低,提示中药血脂康具有更好的耐受性。     

辛伐他汀对老年冠心病患者血脂及血液流变学的影响

目的研究辛伐他汀对老年冠心病患者血脂及血液流变学的影响。方法观察55例老年冠心病患者服用辛伐他汀治疗前后血脂及血液流变学变化。结果冠心病患者服用辛伐他汀血脂下降、血液流变学指标有明显改善,治疗前后比较有显著性差异(p<0.05)。结论辛伐他汀能降低冠心病血脂水平,改善异常的血液流变学指标。     

辛伐他汀对不稳定型心绞痛患者的C反应蛋白、白细胞介素-6和纤维蛋白原水平的影响

目的观察辛伐他汀对不稳定型心绞痛(UAP)患者血清C反应蛋白(CRP)、白细胞介素-6(IL-6)、纤维蛋白原(FIB)等的影响.方法选择UAP患者60例,随机分为辛伐他汀组和对照组,每组30例.对照组常规给药,辛伐他汀组在此基础上加服辛伐他汀20 mg,每晚1次,疗程8周.结果治疗后辛伐他汀组血清中CRP、IL-6、FIB浓度明显降低,和对照组相比P＜0.05,有显著性差异,并且与降脂作用无关.结论辛伐他汀除降脂作用外,具有抗炎、抗血栓形成作用.     

Pharmacokinetics and bioequivalence evaluation of two simvastatin 40 mg tablets (Simvast and Zocor) in healthy human volunteers

The pharmacokinetics of two brands of simvastatin 40 mg tablets were compared in 24 healthy human volunteers after a single oral dose in a randomized cross-over study, conducted at IPRC, Amman, Jordan. Reference (Zocor, MSD, Netherlands) and test (Simvast, Julphar, UAE) products were administered to fasted volunteers; blood samples were collected at specified time intervals, plasma separated and analyzed for simvastatin and its active metabolite (beta-hydoxy acid) using a validated LC-MS/MS method at Cartesius Analytical Unit, Institute of Biomedical Sciences - USP, Sao Paulo, Brazil. The pharmacokinetic parameters AUC(0-t), AUC(0-variant), C(MAX), T(MAX), T(1/2) and elimination rate constant were determined from plasma concentration-time profile for both formulations and were compared statistically to evaluate bioequivalence between the two brands, using the statistical modules recommended by FDA. The analysis of variance (ANOVA) did not show any significant difference between the two formulations and 90% confidence intervals fell within the acceptable range for bioequivalence. Based on these statistical inferences it was concluded that the two brands exhibited comparable pharmacokinetic profiles and that Julphar's Simvast is bioequivalent to Zocor of MSD, Netherlands.     

辛化他汀对原发性高血压心肌纤维化的影响

目的：观察辛化他汀对原发性高血压(EH)心肌纤维化的影响。方法：将60例EH患者随机分为2组：A组28例,单用贝那普利（10mg/d）,B组32例,等量贝那普利加辛化他汀（20mg/d）。应用放射免疫分析技术检测Ⅲ型前胶原末端肽（PⅢP）,Ⅳ型前胶原末端肽（PⅣP）及转化生长因子（ TGFβ1）含量。采用多普勒超声心动图仪测定左室结构及舒缩功能变化。结果：2组患者治疗6个月后,平均动脉压,PⅢP,PⅣP,TGFβ1及室间隔舒张末期厚度,左室后壁厚度指数均较治疗前下降;2组治疗后二尖瓣血流舒张早期流速（VE）和心房收缩期流速（VA）之比均有上升（P<0.01）,而B组上升更明显（P<0.05）,左室收缩功能指标治疗前后无明显变化;2组比较PⅢP,PⅣP,TGFβ1下降和左室舒张功能改善以B组更明显（P<0.05或P<0.01）。结论：EH患者在接受血管紧张素转换酶抑制药同时,再联合使用辛化他汀,能明显减轻心肌纤维化程度,改善左室肥厚和舒张功能。