【作者】 王明霞； 李巍巍； 王敏； 苏喜改； 侯娟； 杜文力； 牛玉凤；

【Author】 Ming-xia WANG1, Wei-wei LEE*, Min WANG*, Xi-gai SU2, Juan HOU1, Wen-li DU1, Yu-feng NIU1 1 The Fourth Affiliated Hospital of Hebei Medical University, Shijiazhuang 050011, Hebei Province, China 2 The First Hospital of Shijiazhuang, Shijiazhuang 050011, Hebei Province, China currently at Shijiazhuang Pharmaceutical Group Co.,Ltd.

【机构】 河北医科大学第四医院药剂科； 石药集团欧意制药公司； 石家庄市第一医院；

【摘要】 目的:替米沙坦是一种新型的口服非肽AngⅡ受体拮抗剂。它选择性、不可逆的拮抗血管紧张素Ⅱ的AT1受体而不影响包括心血管系统的其它受体系统。吲哒帕胺可以通过抑制肾皮质稀释段对钠的重吸收达到利尿效应,从而发挥抗高血压作用。临床上替米沙坦常与利尿剂如吲哒帕胺联合用于高血压的治疗,疗效明显优于单用替米沙坦。本文比较了替米沙坦单用及联用吲哒帕胺后的药代动力学参数,旨在为临床联用两种药物提供理论依据。方法:用9只Wistar大鼠(雌4只,雄5只)进行双周期、交叉试验,两个周期分别为灌胃替米沙坦3.6mg/kg和灌胃替米沙坦3.6mg/kg+吲哒帕胺0.135mg/kg;两周期间的清洗期为14天。灌胃后第0.25、0.75、1.5、2.5、3.5、5、7、9、12、24、48、72、96h取血后用HPLC-FLU法测定大鼠血浆中替米沙坦的浓度。结果:吲哒帕胺对替米沙坦的主要药代动力学参数Cmax、t1/2α、t1/2β有显著影响。结论:替米沙坦可以和吲哒帕胺联合应用用于高血压的治疗,但要调整剂量。更多还原

【Abstract】 This study’s objective is to compare the pharmacokinetics of single- dose telmisartan, an angiotensin II antagonist, with and without coadministered indapamide, a thiazide diuretics. A total of 9 healthy rats received the following oral, single dose of telmisartan 3.6mg/kg and telmisartan 3.6mg/kg plus indapamide 0.135mg/kg (equel to 40mg and 1.5mg of ordernary clinical dose of human). Between medication periods, there was a 14-day washout. Blood was collected at 0.25, 0.75, 1.5, 2.5, 3.5, 5, 7, 9, 12, 24, 48, 72, and 96 hours, respectively. The plasma concentrations of telmisartan was determined by high-performance liquid chromatography. Between indapamide and telmisartan, given alone or in combination, there were significant differences in the maximum average plasma concentrations (Cmax) and elimination half-life (T1/2) of telmisartan, and so, a modification of the dose regimen of telmisartan may be needed, when coadministered indapamide and telmisartan simultaneously.更多还原