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西咪替丁对大鼠和人体中吡罗昔康药代动力学的影响。

Influence of cimetidine on the pharmacokinetics of piroxicam in rat and man.

作者信息

Said S A, Foda A M

机构信息

Department of Pharmacology and Biochemistry, Faculty of Pharmacy, Mansoura University, Egypt.

出版信息

Arzneimittelforschung. 1989 Jul;39(7):790-2.

PMID:2783182
Abstract

The influence of cimetidine on piroxicam plasma levels and pharmacokinetic parameters was studied in both rats and healthy volunteers. In male rats, intravenous injection of piroxicam (6 mg/kg) in animals pretreated with cimetidine (50 mg/kg intramuscular) resulted in plasma piroxicam concentrations significantly higher than those of animals which received piroxicam alone. The plasma half-life (1/2) of piroxicam in male rats was about 8.3 h and it was increased to 20.74 h by cimetidine pretreatment. The mean area under piroxicam plasma level-time curves was significantly (p less than 0.01) higher in case of rats pretreated with cimetidine compared with those treated with piroxicam alone. Similar results were obtained in male healthy volunteers, where administration of a single dose of piroxicam (20 mg orally) to subjects who received cimetidine (200 mg 3 times a day orally) resulted in plasma piroxicam concentrations significantly higher than those of subjects treated with piroxicam alone. The t1/2 of piroxicam was increased from 37.36 to 52.86 h with cimetidine administration. Also the mean area under piroxicam plasma level-time curves was significantly (p less than 0.05) increased by cimetidine administration.

摘要

在大鼠和健康志愿者中研究了西咪替丁对吡罗昔康血浆水平和药代动力学参数的影响。在雄性大鼠中,给预先用西咪替丁(50mg/kg肌肉注射)预处理的动物静脉注射吡罗昔康(6mg/kg),导致血浆吡罗昔康浓度显著高于单独接受吡罗昔康的动物。雄性大鼠中吡罗昔康的血浆半衰期(t1/2)约为8.3小时,经西咪替丁预处理后增加至20.74小时。与单独用吡罗昔康治疗的大鼠相比,预先用西咪替丁治疗的大鼠的吡罗昔康血浆水平-时间曲线下的平均面积显著更高(p<0.01)。在男性健康志愿者中也得到了类似的结果,给接受西咪替丁(200mg,每日3次口服)的受试者单次口服吡罗昔康(20mg),导致血浆吡罗昔康浓度显著高于单独用吡罗昔康治疗的受试者。服用西咪替丁后,吡罗昔康的t1/2从37.36小时增加到52.86小时。同样,服用西咪替丁后,吡罗昔康血浆水平-时间曲线下的平均面积也显著增加(p<0.05)。

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