PHARMACOKINETICS OF SULFAMETHOXAZOLE AND TRIMETHOPRIM ASSOCIATION IN HENS
PHARMACOKINETICS OF SULFAMETHOXAZOLE AND TRIMETHOPRIM ASSOCIATION IN HENS
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DOI：
10.3382/ps.0642362
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发表时间：
1985-12-01
期刊：
影响因子：
4.4
通讯作者：
CASTELLS, I
中科院分区：
文献类型：
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作者：
QUERALT, J;CASTELLS, I
研究了磺胺甲恶唑(SMZ)和甲氧苄氨嘧啶(TMP)静脉注射给药(4：1)和口服给药(5：1和2.5：1)在华伦母鸡体内的药代动力学。SMZ和TMP的半衰期分别为8.2和2.4小时。静脉注射4：1剂量后，SMZ与TMP血药浓度的比值(S/T比值)约为20，仅维持1小时不变；口服5：1和2.5：1剂量后，S/T比值分别为40和20，12小时内保持不变。SMZ和TMP的口服生物利用度分别为0.46和0.36。口服给药后TMP从血清中的清除速度明显较慢，当采用这种给药途径时，应该会延长协同抗菌效果的持续时间。2.5：1的组合口服给药后，血清中的药物有一个合适的增效比(S/T=20：1)。
A pharmacokinetic study of sulfamethoxazole (SMZ) and trimethoprim (TMP) was carried out on Warren hens after intravenous (iv) dosage of 4:1, and oral administration of dosages of 5;1, and 2.5:1. The SMZ and TMP half-lives were 8.2 and 2.4 hr, respectively. The ratio between SMZ and TMP serum levels (S/T ratio), after iv administration of the 4:1 dosage, was approximately 20 and remained constant for only 1 hr, while after 5:1 and 2.5:1 oral dosages, the S/T ratio was 40 and 20, respectively, and remained invariable for 12 hr. The oral bioavailability of SMZ and TMP was .46 and .36 respectively. The apparently slower elimination of TMP from serum following oral administration should provide an extended duration of the synergistic antibacterial effect when this route of administration is employed. Finally, the 2.5:1 combination, after oral administration, resulted in an appropriate synergistic ratio (S/T ratio = 20:1) of the drugs in the serum.