高效液相色谱法测定复方坎地沙坦酯片两组分的含量

目的建立以高效液相色谱法同时测定复方坎地沙坦酯片剂中坎地沙坦酯和氢氯噻嗪含量的方法。方法色谱柱为Nucleosil C18柱,流动相为乙腈∶水(40∶60)磷酸调pH至4.0,流速1.0 ml/min,测定波长210 nm,柱温为室温。结果坎地沙坦酯、氢氯噻嗪浓度分别在1~16,1.25~20μg/ml范围内线性关系良好(r=0.9999),平均回收率分别为100.02%,100.12%。结论该法测定简便、快速、重现性好、回收率高,且可同时测定复方坎地沙坦酯片中两组分的含量,并可用于其质量控制。     

2种坎地沙坦酯制剂的人体生物等效性研究

目的:研究2种坎地沙坦酯制剂的人体生物等效性。方法:20名健康男性志愿者随机交叉单剂量口服坎地沙坦酯片(受试制剂)和坎地沙坦酯胶囊(参比制剂),以高效液相色谱法测定血药浓度,3p97软件计算药动学参数与相对生物利用度。结果:受试制剂与参比制剂的Cmax分别为(276.785±28.957)、(269.118±30.116)ng.mL-1,tmax分别为(4.12±0.79)、(3.93±0.87)h,t1/2分别为(8.63±1.04)、(9.06±1.14)h,AUC0～48分别为(2589.248±306.674)、(2438.946±313.259)ng.h.mL-1,AUC0～∞分别为(2613.276±309.460)、(2493.636±324.491)ng.h.mL-1,受试制剂的相对生物利用度为(104.80±16.48)%。结论:2种制剂具有生物等效性。     

坎地沙坦治疗充血性心力衰竭的疗效及对内皮素和心钠素水平的影响

目的研究一种新型血管紧张素II（AngII）受体拈抗剂（ARB）-坎地沙坦治疗充血性心力衰竭（CHF）的疗效以及对血浆内皮素（ET）和心钠素（ANY）水平的影响。方法50例CHF患者随机分为两组，对照组（n=25）用利尿剂和洋地黄治疗，坎地沙坦治疗组（n=25）在前者基础上加用坎地沙坦酯胶囊（4～8mg／d）治疗8周，观察治疗前后NYHA分级、血浆ET和ANP浓度的变化。结果经8周治疗后，坎地沙坦治疗组NYHA分级明显下降（P〈0．01），并使血浆ET和ANP的水平明显降低（P〈0．01），临床有效率优于对照组，但差异无显著性（P〉0．05）。结论在常规治疗的基础上加用坎地沙坦可以更好地改善CHF患者的心功能，坎地沙坦能明显降低血浆ET和ANP的水平，这可能是ARB治疗CHF的机制之一。     

坎地沙坦和卡托普利治疗轻中度高血压临床比较

目的：比较坎地沙坦和卡托普利治疗高血压的临床疗效和不良反应。方法：选取门诊患者88例，随机分为两组，分别口服药物4周后，观察临床疗效和不良反应。结果：治疗前后两组血压均有明显下降（P〈0．01），两组间比较差异不明显（P〉0．05）。坎地沙坦组不良反应发生率较低（2．3％）；卡托普利组不良反应率较高（22．7％），两组差异有明显统计学意义（P〈0．01）。结论：两药均有明显降压效果，但坎地沙坦组不良反应发生率明显低于卡托普利组。     

国产坎地沙坦对高血压病患者内皮功能及胰岛素抵抗的影响

目的:探讨国产坎地沙坦对高血压病患者内皮功能及胰岛素抵抗的影响.方法:42例高血压病患者口服坎地沙坦8周,治疗前、后采静脉血测定空腹血糖、胰岛素计算胰岛素敏感指数,同时测定血浆内皮素-1、一氧化氮水平的变化.结果:坎地沙坦治疗高血压病12周后患者的收缩压和舒张压均降低,空腹胰岛素敏感指数均较前显著升高,血浆一氧化氮显著升高而内皮素-1显著降低.结论:坎地沙坦能有效降压和改善胰岛素抵抗及血管内皮功能.     

坎地沙坦联合胺碘酮转复房颤及预防房颤复发疗效观察

目的:探讨坎地沙坦联合胺碘酮转复房颤及预防房颤复发的疗效。方法:将持续性房颤患者87例随机分为坎地沙坦-胺碘酮联合治疗组(即治疗组)与胺碘酮治疗组(即对照组),进行转复治疗及预防复发治疗,共观察8个月,观察转复率、转复周期及复发率、复发时限并进行对比分析。结果:联合治疗组与胺碘酮治疗组相比,其房颤转复率无显著性差异(72.7%vs 51.2%,P>0.05),而转复周期显著缩短〔(12.6±4.1)d vs(15.3±5.5)d,P<0.05〕,复发率显著降低(34.4%vs63.6%,P<0.05),复发时限显著延长〔(175.3±41.5)d vs(90.9±36.5)d,P<0.05〕。结论:血管紧张素受体拮抗剂坎地沙坦在转复及维持房颤患者窦性节律方面有辅助作用。     

坎地沙坦致血管神经性水肿及骶髂关节疼痛

1例63岁女性患者因高血压给予坎地沙坦酯8mg/d,口服3天后,患者出现口腔咽部水肿,腰腿疼痛.停药7天后骶髂关节疼痛加剧后出现抽搐,半坐位后出现呼吸困难,意识丧失,大动脉波动消失,抢救后心跳恢复,无自主呼吸,支持治疗,肝肾功能进行性减弱,支持治疗5天死亡.     

A comparison of the efficacy and duration of action of candesartan cilexetil and losartan as assessed by clinic and ambulatory blood pressure after a missed dose, in truly hypertensive patients : A placebo-controlled, forced titration study

The purpose of this double-blind, forced titration study was to compare the antihypertensive effect duration of candesartan cilexetil, which has a long-lasting binding to the human AT₁-receptor, to that of losartan on ambulatory BP (ABP) not only during the 24-h dosing interval but also during the day of a missed dose intake. After a 4-week placebo lead-in period, 268 patients with sitting diastolic BP 95 to 110 mm Hg and mean awake ambulatory DBP ≥85 mm Hg were randomized to receive either 8 mg of candesartan, 50 mg of losartan, or placebo for a 4-week period. Thereafter, the doses were doubled in all patients for an additional 4-week period. Ambulatory BP monitoring was performed for 36 h after dosing and clinic BP measured 48 h after dosing.

Candesartan cilexetil (16 mg) reduced ABP to a significantly greater extent than 100 mg of losartan, particularly for systolic ABP during daytime (P < .05), nighttime (P < .05), and 24-h (P < .01) periods, systolic (P < .01) and diastolic (P < .05) ABP between 0 and 36 h, and both systolic (P < .001) and diastolic (P < 0.001) ABP during the day of a missed dose. Clinic BP at 48 h after dosing was significantly reduced exclusively with 16 mg of candesartan. The differences in BP reduction between 8 mg of candesartan and 50 mg of losartan were statistically significant for systolic ABP during daytime (P < .01), nighttime (P < .05), 24-h (P < .01), 0 to 36 h (P < .05) and during the day of missed dose (P < .05). Moreover, although losartan did not significantly reduce ambulatory BP in a dose-related manner, ambulatory systolic and diastolic BP reductions with 16 mg of candesartan were significantly greater (P < .01 and < .001) than those seen with 8 mg of candesartan during every period at the ABP supporting a dose–response relationship.

In conclusion, this forced titration study in ambulatory hypertensive patients demonstrates that candesartan cilexetil provides significant dose-dependent reduction in both clinic and ambulatory BP in doses ranging from 8 to 16 mg once daily. Furthermore, candesartan cilexetil is superior to losartan in reducing systolic ABP and in controlling both systolic and diastolic ABP on the day of a missed dose. The differences observed between both agents are most likely attributable to a tighter binding to, and a slower dissociation from, the receptor binding site with candesartan cilexetil.     

动态血压监测观察坎地沙坦的降压疗效

目的应用动态血压监测（ABPM）的方法评价坎地沙坦治疗原发性高血压的降压疗效、谷／峰比值及不良反应。方法45例研究对象经2周洗脱期，日服一次坎地沙坦8mg，共8周。于洗脱期末及治疗8周末各行一次ABPM。结果ABPM显示8周末24h、日间、夜间收缩压／舒张压（SBP／DBP）较洗脱期末分别下降18．8／12．1mmHg、21．2／15．6mmHg、13．7／9．1mmHg。收缩压、舒张压的谷／峰比值分别为72．6％和63．1％。无严重不良反应。结论坎地沙坦是一种疗效好并能平稳、持续、安全的降压药物，特别适合老年原发性高血压患者。