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磺胺嘧啶(SDZ)在骆驼(单峰驼)体内的药代动力学、生物利用度及给药方案

Pharmacokinetics, bioavailability and dosage regimen of sulphadiazine (SDZ) in camels (Camelus dromedarius).

作者信息

Kumar R, Singh A P, Kapoor M, Rai A K

机构信息

Department of Pharmacology, College of Veterinary and Animal Science, Bikaner, India.

出版信息

J Vet Pharmacol Ther. 1998 Oct;21(5):393-9. doi: 10.1046/j.1365-2885.1998.00164.x.

DOI:10.1046/j.1365-2885.1998.00164.x
PMID:9811441
Abstract

The pharmacokinetics of sulphadiazine (SDZ) (100 mg/kg, body weight) were investigated in six camels (Camelus dromedarius) after intravenous (i.v.) and oral (p.o.) administration. Following i.v. administration, the overall elimination rate constant (beta) was 0.029 +/- 0.001/h and the half-life (t1/2beta) was 23.14 +/- 1.06 h. The apparent volume of distribution (Vd(area)) was 0.790 +/- 0.075 L/kg and the total body clearance (ClB) was 23.29 +/- 2.50 mL/h/kg. After p.o. administration, SDZ reached a peak plasma concentration (Cmax(cal.)) of 62.93 +/- 2.79 microg/mL at a post injection time of (Tmax(cal.)) 22.98 +/- 0.83 h. The elimination half-life was 19.79 +/- 1.22 h, not significantly different from that obtained by the i.v. route. The mean absorption rate constant (Ka) was 0.056 +/- 0.002 h(-1) and the mean absorption half-life (t1/2Ka) was 12.33 +/- 0.37 h. The mean availability (F) of sulphadiazine was 88.2 +/- 6.2%. To achieve and maintain therapeutically satisfactory plasma SDZ levels of > or = 50 microg/mL, the priming and maintenance doses would be 80 mg/kg and 40 mg/kg intravenously and 90 mg/kg and 45 mg/kg orally, respectively, to be repeated at 24 h intervals.

摘要

在六头骆驼(单峰驼)身上静脉注射(i.v.)和口服(p.o.)100毫克/千克体重的磺胺嘧啶(SDZ)后,对其药代动力学进行了研究。静脉注射后,总消除速率常数(β)为0.029±0.001/小时,半衰期(t1/2β)为23.14±1.06小时。表观分布容积(Vd(area))为0.790±0.075升/千克,全身清除率(ClB)为23.29±2.50毫升/小时/千克。口服给药后,磺胺嘧啶在注射后时间(Tmax(cal.))22.98±0.83小时达到血浆峰值浓度(Cmax(cal.))62.93±2.79微克/毫升。消除半衰期为19.79±1.22小时,与静脉注射途径获得的半衰期无显著差异。平均吸收速率常数(Ka)为0.056±0.002小时-1,平均吸收半衰期(t1/2Ka)为12.33±0.37小时。磺胺嘧啶的平均生物利用度(F)为88.2±6.2%。为了达到并维持治疗上满意的血浆磺胺嘧啶水平≥50微克/毫升,静脉注射的初始剂量和维持剂量分别为80毫克/千克和40毫克/千克,口服分别为90毫克/千克和45毫克/千克,每24小时重复一次。

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