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巴氨西林和氨苄西林的抗菌活性及药代动力学

Antibacterial activity and pharmacokinetics of bacampicillin and ampicillin.

作者信息

Rozencweig M, Staquet M, Klastersky J

出版信息

Clin Pharmacol Ther. 1976 May;19(5 Pt 1):592-7. doi: 10.1002/cpt1976195part1592.

DOI:10.1002/cpt1976195part1592
PMID:6181
Abstract

Single equimolar oral doses of bacampicillin and ampicillin were given to 9 healthy subjects on a crossover randomized basis. Data were interpreted in terms of a 3-compartment pharmacokinetic open model. Intestinal absorption of bacampicillin was found to be faster and more complete than that of ampicillin, yielding an increase in bioavailability of 30% to 40% as measured by the area under serum levels curve, the urinary excretion and absorption rate constants. After the administration of bacampicillin, much higher and sharper peaks were achieved in the serum and in the "tissue" water than after the administration of ampicillin. The maximum bactericidal dilution (MBD) of the serum samples taken 1 hr after the administration of the antibiotics against 10 strains of Diplococcus pneumoniae was higher following bacampicillin (p less than 0.01), as was the MBD of the 0 to 2 hr urine specimens against 10 strains of Escherichia coli. Further clinical trials are required to accurately assess the possible greater therapeutic effectiveness of bacampicillin than of ampicillin.

摘要

在交叉随机的基础上,给9名健康受试者口服单剂量等摩尔的巴卡西林和氨苄西林。数据根据三室药代动力学开放模型进行解释。发现巴卡西林的肠道吸收比氨苄西林更快且更完全,通过血清水平曲线下面积、尿排泄和吸收速率常数测量,其生物利用度提高了30%至40%。服用巴卡西林后,血清和“组织”水中的峰值比服用氨苄西林后更高且更尖。服用抗生素1小时后采集的血清样本对10株肺炎双球菌的最大杀菌稀释度(MBD),巴卡西林组更高(p小于0.01),0至2小时尿液样本对10株大肠杆菌的MBD也是如此。需要进一步的临床试验来准确评估巴卡西林可能比氨苄西林具有更大的治疗效果。

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1
Antibacterial activity and pharmacokinetics of bacampicillin and ampicillin.巴氨西林和氨苄西林的抗菌活性及药代动力学
Clin Pharmacol Ther. 1976 May;19(5 Pt 1):592-7. doi: 10.1002/cpt1976195part1592.
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Absorption of bacampicillin and ampicillin and penetration into body fluids (skin blister fluid, saliva, tears) in healthy volunteers.健康志愿者体内巴卡西林和氨苄西林的吸收情况以及它们在体液(皮肤疱液、唾液、泪液)中的渗透情况。
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引用本文的文献

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Prodrug and analog approaches to improving the intestinal absorption of a cyclic peptide, GPIIb/IIIa receptor antagonist.前药和类似物方法用于改善环肽(一种糖蛋白IIb/IIIa受体拮抗剂)的肠道吸收
Pharm Res. 1997 Aug;14(8):1026-9. doi: 10.1023/a:1012149227756.
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Bacampicillin HCl in the treatment of acute maxillary sinusitis.盐酸巴氨西林治疗急性上颌窦炎。
Bull N Y Acad Med. 1983 Jun;59(5):477-81.
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A comparison of the pharmacokinetics of bacampicillin, ampicillin, amoxicillin, and cyclacillin: oral administration in infants and children.
巴卡西林、氨苄西林、阿莫西林和环己西林的药代动力学比较:在婴幼儿和儿童中的口服给药
Bull N Y Acad Med. 1983 Jun;59(5):468-76.
4
Pharmacokinetics of bacampicillin tablets in adults.成人服用巴卡西林片的药代动力学
Bull N Y Acad Med. 1983 Jun;59(5):457-67.
5
Comparison of cyclacillin and amoxicillin for therapy for acute maxillary sinusitis.环青霉素与阿莫西林治疗急性上颌窦炎的比较。
Antimicrob Agents Chemother. 1986 Sep;30(3):350-3. doi: 10.1128/AAC.30.3.350.
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Prodrugs.前体药物
Br J Clin Pharmacol. 1989 Nov;28(5):497-507. doi: 10.1111/j.1365-2125.1989.tb03535.x.
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Prodrugs for the improvement of drug absorption via different routes of administration.用于通过不同给药途径改善药物吸收的前体药物。
Eur J Drug Metab Pharmacokinet. 1990 Apr-Jun;15(2):143-53. doi: 10.1007/BF03190197.
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Pharmacokinetics of bacampicillin compared with those of ampicillin, pivampicillin, and amoxycillin.巴卡青霉素与氨苄青霉素、匹氨青霉素和阿莫西林的药代动力学比较。
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Antimicrob Agents Chemother. 1979 Apr;15(4):510-2. doi: 10.1128/AAC.15.4.510.