厄贝沙坦氢溴酸盐的毒理学和药效学研究

Toxicity and pharmacodynamics of irbesartan hydrobromate

目的比较厄贝沙坦氢溴酸盐与厄贝沙坦的毒性和药效。方法采用无创血压测量比较了厄贝沙坦氢溴酸盐、厄贝沙坦对自发性高血压大鼠血压的影响。分别ip、ig给药,观察两种药物的半数致死量(LD50),对心率、呼吸以及动物自主活动的影响。结果自发性高血压大鼠的血压明显高于非自发性高血压大鼠,给予厄贝沙坦氢溴酸盐、厄贝沙坦后血压均降至正常水平,且两种药物的降压作用差异无显著性,但厄贝沙坦氢溴酸盐的药效持续时间更长。厄贝沙坦氢溴酸盐、厄贝沙坦对动物的呼吸、心率以及自主活动的影响无差异,但厄贝沙坦氢溴酸盐的LD50明显高于厄贝沙坦。结论厄贝沙坦氢溴酸盐具有和厄贝沙坦相同的降压作用,但是作用时间更长,安全性更高。

Objective To compare toxicity and pharmacodynamics between irbesartan and irbesartan hydrobromate.Methods Blood pressures in spontaneously hypertensive rats （SHR） after administered with irbesartan and irbesartan hydrobromate were compared using noninvasive blood pressure. SHR were ip and igadministered with drugs, and effects on heart rate, respiratory rate, and autonomic activities were observed.Results Blood pressure in SHR was higher than that of non spontaneous hypertensive rats. Both irbesartan hydrobromate and irbesartan could lower blood pressure, and there were no differences between two groups, but duration of irbesartan hydrobromate was longer. There was no difference between two groups on heart rate, respiratory rate, and autonomic activities. LD50value of irbesartan hydrobromate was higher than that of irbesartan.Conclusion Irbesartan hydrobromate has anti-hypertensive effect as well as irbesartan, but with longer duration and higher security.