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[磺胺多辛与甲氧苄啶联合用于犊牛时的药代动力学、生物利用度及残留]

[Pharmacokinetics, biological availability and residues of sulfadoxine and trimethoprim when used jointly on calves].

作者信息

Pashkov D, Mutafchieva R, Drumev D, Koĭchev K B, Avramova N

出版信息

Vet Med Nauki. 1984;21(4):84-93.

PMID:6740937
Abstract

In calves (cross-breds--Bulgarian Brown Cattle breed and Black Spot Cattle bred) weighing about 189 kg pharmacokinetics of sulphadoxine (SD) and trimethoprim (TMP) was studied. The two substances were administered in combination (5 + 1) as a dosage form Tridoxin (Pharmachim, Bulgaria; 24% injectable solution) (TD) at a dose 15 mg/kg m. The results show that after intramuscular administration TD is absorbed relatively rapidly. SD and TMP have systemic availability 94.1 +/- 18.1% and 52.5 +/- 6.2% and produce blood levels, after a single dose of TD, higher than potentiated minimum inhibitory concentrations for 24-48 h and 5(4-8) h, respectively. Upon intravenous administration the two-compartmental model is applicable for the distribution and elimination of SD and TMP (for TMP in part of the animals one-compartmental model is applicable). The two substances are distributed relatively widely in organs and tissues. The biological half-life of TD--t1/2 beta for SD is 14.36 +/- 1.40 h and for TMP--2.40 +/- 0.31 (for one-compartmental model--1.92 +/- 0.26) h, Vd--429.9 +/- 16.9 ml/kg and for TMP in part of the animals one-compartmental model is applicable). The two substances are distributed relatively widely in organs and tissues. The biological half-life of TD--t1/2 beta for SD is 14.36 +/- 1.40 h and for TMP--2.40 +/- 0.31 (for one-compartmental model--1.92 +/- 0.26) h, Vd--429.9 +/- 16.9 ml/kg and for TMP in part of the animals one-compartmental model is applicable). The two substances are distributed relatively widely in organs and tissues. The biological half-life of TD--t1/2 beta for SD is 14.36 +/- 1.40 h and for TMP--2.40 +/- 0.31 (for one-compartmental model--1.92 +/- 0.26) h, Vd--429.9 +/- 16.9 ml/kg and 655.8 +/- 77.6 (for one-compartmental model--671.7 +/- 40.0) ml/kg, ClB--0.35 +/- 0.02 ml/kg/min and 2.87 +/- 0.35 (for one-compartmental model--4.15 +/- 0.80) ml/kg/min, respectively. After intramuscular injection at the dose used a suitable withdrawal time for meat and internal organs is 5 days and for milk--2 days.

摘要

对体重约189千克的犊牛(杂交品种——保加利亚褐牛和黑斑牛)进行了磺胺多辛(SD)和甲氧苄啶(TMP)的药代动力学研究。两种物质以(5 + 1)组合形式作为制剂Tridoxin(保加利亚Pharmachim公司生产;24%注射溶液)(TD),以15毫克/千克体重的剂量给药。结果表明,肌内注射TD后吸收相对较快。SD和TMP的全身利用率分别为94.1±18.1%和52.5±6.2%,单剂量TD给药后,其血药浓度分别在24 - 48小时和5(4 - 8)小时内高于增效最小抑菌浓度。静脉给药后,二室模型适用于SD和TMP的分布与消除(部分动物的TMP适用一室模型)。这两种物质在器官和组织中的分布相对广泛。TD的生物半衰期——SD的t1/2β为14.36±1.40小时,TMP的为2.40±0.31小时(一室模型为1.92±0.26小时),Vd——SD为429.9±16.9毫升/千克,部分动物的TMP适用一室模型。这两种物质在器官和组织中的分布相对广泛。TD的生物半衰期——SD的t1/2β为14.36±1.40小时,TMP的为2.40±0.31小时(一室模型为1.92±0.26小时),Vd——SD为429.9±16.9毫升/千克,TMP为655.8±77.6(一室模型为671.7±40.0)毫升/千克,ClB——SD为0.35±0.02毫升/千克/分钟,TMP为2.87±0.35(一室模型为4.15±0.80)毫升/千克/分钟。按所用剂量肌内注射后,肉和内脏的适宜休药期为5天,牛奶为2天。

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