高效液相色谱法测定替米沙坦胶囊中替米沙坦含量

目的建立测定替米沙坦胶囊中替米沙坦含量的高效液相色谱法。方法采用依利特C18柱(200 mm×4.6 mm,5μm),以乙腈-水-冰醋酸(45∶55∶0.1)为流动相,检测波长为242 nm。结果替米沙坦质量浓度在20～160μg/mL范围内与峰面积线性关系良好(r=0.999 8),替米沙坦的平均回收率为96.90%,RSD=0.39%(n=5)。结论所用方法准确、简便、可靠,可作为替米沙坦胶囊的质量控制方法。     

替米沙坦联合氢氯噻嗪治疗高血压的临床疗效观察

目的:观察并评价替米沙坦联合氢氯噻嗪治疗高血压的临床疗效及安全性。方法:2009年3月~2009年7月我院收治高血压患者208例,随机分为两组,其中对照组102例,单纯采用替米沙坦治疗;实验组106例,在对照组治疗基础之上,加用氢氯噻嗪;疗程均为20周,疗程结束后评价治疗效果和安全性。结果:临床治疗20周后,实验组总有效例数为98例,总有效率为92.5%,对照组总有效例数为69例,总有效率为67.6%,两者组间比较差异有统计学意义(P<0.05),实验组与对照组不良反应发生率分别为5.7%和6.9%。结论:替米沙坦联合氢氯噻嗪治疗高血压临床疗效显著,安全性理想,值得在临床加以推广应用。     

替米沙坦联合非洛地平治疗高血压病合并肾功能不全的临床观察

目的观察替米沙坦联合非洛地平治疗高血压合并肾功能不全时对胱抑素（CYS-C）、尿素氮、血肌酐、内生肌酐清除率（Ccr）的影响。方法选择近期在我院接受治疗的原发性高血压2、3级患者60例,按随机、双盲、对照的原则分成治疗组和对照组各30例。治疗组给予替米沙坦、非洛地平口服,对照组给予非洛地平、倍他乐克口服。疗程8周。比较两组胱抑素（CYS-C）、尿素氮、血肌酐、Ccr的变化。结果治疗组胱抑素（CYS-C）、尿素氮、血肌酐、Ccr治疗前后差别明显,有统计学意义。对照组治疗前后胱抑素（CYS-C）、尿素氮、血肌酐、Ccr差别不明显,无统计学意义。结论替米沙坦在降压的同时,具有保护肾功能、延缓肾功能衰竭的作用。     

替米沙坦对老年高血压病患者血压蛋白排泄率及β2微球蛋白的影响

目的 观察替米沙坦(telmisartan)对高血压患者血压水平、尿蛋白排泄率(UAER)和尿β2微球蛋白(β2-MG)的影响.方法 将84例高血压病伴MAU患者随机分为治疗组和对照组,各42例.治疗组给予替米沙坦,对照组给予硝苯吡啶缓释片,治疗8周后评定疗效.结果 治疗后两组血压水平、UAER及β2-MG较治疗前均明显下降(P＜0.05),治疗组下降幅度大于对照组.结论 替米沙坦更有效地降低高血压病患者的血压,对肾脏亦具有保护作用.     

替米沙坦改善血液透析患者心功能的疗效观察

目的探讨口服替米沙坦对尿毒症维持性血液透析患者心功能保护作用以及应用安全性。方法选择蚌埠市第三人民医院86例慢性肾功能不全(尿毒症期)合并慢性心力衰竭,心功能Ⅲ～Ⅳ级患者,随机分为对照组(硝苯地平组)与观察组(替米沙坦治疗组),经3个月规律血液透析治疗后,重新评定心功能分级,并使用彩色多普勒心脏超声检查左室结构和功能。结果经3个月降血压及血液透析治疗后,两组收缩压、舒张压、心功能分级与治疗前比较差异具有统计学意义(P<0.01),但组间比较,差异无统计学意义(P>0.05)。与透析前比较,两组左心室舒张末期内径透析治疗3个月后均有明显减少(P<0.05);但对照组室间隔厚度(IVST)、左室后壁舒张末期厚度(LVPwT)和最大血流速度比(E/A)透析前后比较差异无统计学意义(P>0.05),观察组透析3个月后IVST、LVPwT明显降低,E/A值显著升高,与透析前及对照组透析后比较差异均有统计学意义(P<0.05)。结论口服替米沙坦对维持性血液透析患者心功能具有保护作用,且服用安全。     

替米沙坦氨氯地平双层片的制备及体外释放度研究

目的制备复方替米沙坦氨氯地平片并考查其体外释放度。方法采用直压法制备替米沙坦氨氯地平片;建立同时测定替米沙坦、氨氯地平含量的高效液相色谱法;以水、pH2.0盐酸溶液、pH6.8、pH7.4磷酸盐缓冲液为溶出介质,桨法测定本品释放度,并与参比制剂Twynst进行比较。结果释放曲线经相似因子判断,与参比制剂相似。结论本品处方工艺稳定,重现性好,体外累积释放度符合要求。     

Angiotensin-converting enzyme inhibition and angiotensin AT1-receptor antagonism equally improve doxorubicin-induced cardiotoxicity and nephrotoxicity

Doxorubicin (Dox) is a potent anticancer agent; its clinical use is limited for its marked cardiotoxicity and nephrotoxicity. The present study investigated the possible protective effect of telmisartan, an angiotensin AT₁-receptor blocker versus captopril, an angiotensin-converting enzyme inhibitor, on Dox-induced cardiotoxicity and nephrotoxicity in rats. Rats were allocated into four groups. Control group, Dox group, Dox + telmisartan group, and Dox + captopril group. Cardiotoxicity and nephrotoxicity were assessed biochemically and histopathologically. Frozen heart and kidney specimens were used for estimation of lipid peroxides product (MDA), reduced glutathione (GSH), glutathione peroxidase (GPx), superoxide dismutase (SOD) and nitric oxide (NO). Expression of induced nitric oxide synthase (iNOS) was detected by immunohistochemistry. Coadministration of either telmisartan or captopril with Dox equally decreased the biochemical markers of both cardiotoxicity (LDH and CK–MP) and nephrotoxicity (urea and creatinine). Both telmisartan and captopril attenuated the effects of Dox on oxidative stress parameters and NO. Histopathologically, coadministration of either drug with Dox was able to attenuate Dox-induced myocardial fibrosis and renal tubular damage. Immunohistochemistry, expression of iNOS was increased in both cardiac and renal tissues. Both telmisartan and captopril significantly and equally attenuated the effect of Dox on all measured parameters. These results suggested that telmisartan has protective effects equal to that of captopril against Dox-induced cardiotoxicity and nephrotoxicity; implying that angiotensin II pathway plays a role in Dox-induced cardiac and renal damage. The protective effect of either drug relies, at least in part, on their antioxidant effects and decreased the expression of iNOS.     

替米沙坦联合单硝酸异山梨酯治疗肺心病心力衰竭疗效观察

目的观察替米沙坦、单硝酸异山梨酯（ISMN）联合治疗重症肺心病心力衰竭的疗效。方法印例肺心病心力衰竭患者随机分为甲乙两组,每组30例。甲组（治疗组）在乙组常规治疗基础上加用替米沙坦、单硝酸异山梨酯,5d为1个疗程。结果治疗组显效率74．3％,总有效率为92．7％;对照组显效率为46．6％,总有效率为68．3％,两组显效率、总有效率差异均有统计学意义（均P〈0．01．）。结论替米沙坦、单硝酸异山梨酯（ISMN）合用治疗老年慢性肺源性心脏病心力衰竭疗效显著,不良反应少,使用安全。     

Effect of telmisartan-amlodipine combination at different doses on urinary albumin excretion in hypertensive diabetic patients with microalbuminuria

BACKGROUND: Aim of this study was to evaluate the effect of the telmisartan-amlodipine combination at different doses on urinary albumin excretion rate (UAER) in hypertensive diabetic patients with microalbuminuria. METHODS: After a 2-week placebo period, 300 hypertensive patients with type 2 diabetes and microalbuminuria were treated with the 40 mg of telmisartan and 2.5 mg of amlodipine combination. After 4 weeks 210 patients whose blood pressure (BP) was not controlled (BP >130/80 mm Hg) were randomized to two-dose titration regimens, one based on increasing doses of telmisartan (up to 160 mg daily) and fixed 2.5-mg dose of amlodipine, the other based on increasing doses of amlodipine (up to 10 mg daily) and fixed 40-mg dose of telmisartan. After 12 weeks the nonresponder patients were given transdermic clonidine (0.1mg/d). After 16 weeks the patients yet not controlled were discontinued, the others were followed for 48 weeks. Office BP, UAER, creatinine clearance, plasma potassium, fasting glycemia, and glycosylated hemoglobin were assessed at the end of the telmisartan (40 mg)/amlodipine (2.5 mg) treatment period and after 48 weeks of treatment. RESULTS: Similar decrease in systolic/diastolic BP values were obtained with both regimens (-24/-21, -23/-21, and -24/-21 mm Hg, all P < .001 v baseline, with increasing telmisartan; -25/-22, -25/-21, and -25/-22 mm Hg, all P < .001 v baseline with increasing amlodipine). Reductions of UAER were 47.5% (P < .01), 65.3% (P < .001), and 77% (P < .0001) for telmisartan 80, 120, and 160 mg/amlodipine 2.5 mg daily, respectively, whereas reductions of UAER were 34% (P < .03), 37% (P < .03), and 33% (P < .03) for amlodipine 5, 7.5, and 10 mg/telmisartan 40 mg daily, respectively, The difference between the two regimens was statistically significant (P < .05, P < .01, and P < .001, respectively). CONCLUSIONS: These findings indicate that, at comparable levels of BP reduction, UAE decreased more in subjects treated with escalating doses of telmisartan.     

Angiotensin II receptor blockers downsize adipocytes in spontaneously type 2 diabetic rats with visceral fat obesity

OBJECTIVE: To investigate the influence of blockade of the renin-angiotensin system (RAS) on adipocytes, we compared the effect of telmisartan versus valsartan and amlodipine on adipocyte cellularity in the spontaneously type 2 diabetic, obese rat model. METHODS: Male Otsuka Long Evans Tokushima Fatty rats, 8-week-old, were divided into four groups as follows: valsartan (V) group (10 mg/kg, n = 12), telmisartan (T) group (5 mg/kg, n = 12), amlodipine (A) group (2 mg/kg, n = 12), and control (C) group (n = 12). Each drug was mixed with chow and given for 16 weeks. RESULTS: Although no significant differences were observed in the fasting plasma glucose level between the groups, the fasting plasma insulin level for group T was significantly lower than that for group C. Histopathologic examination showed that the ratio of small adipocytes in groups V and T was significantly higher than that in group C, with the ratio of large adipocytes and the mean adipocyte size shown to be significantly lower in groups V and T than in group C. Furthermore, group T was shown to have a significantly higher ratio of small adipocytes, a significantly lower ratio of large adipocytes, as well as a significantly lower mean adipocyte size, compared to group V. CONCLUSIONS: Although both valsartan and telmisartan downsized adipocytes, adipocyte downsizing was significantly greater with telmisartan compared to valsartan. The likely mechanism for this difference was thought to be the PPAR-gamma-mediated action of telmisartan.