Tachibana A, Ohtani K, Komiya M, Naito S, Shimizu C, Yano K
Jpn J Antibiot. 1978 Mar;31(3):166-76.
The antibacterial activities, absorption and excretion of talampicillin hydrochloride were compared with those of amoxicillin and ampicillin. Talampicillin hydrochloride showed a broad-spectrum antibacterial activity against Gram-positive and Gram-negative bacteria as seen in amoxicillin and ampicillin. The antibacterial activities of talampicillin hydrochloride, amoxicillin and ampicillin were quite similar. In experimental murine infection with Staphylococcus aureus, protective effect of talampicillin hydrochloride was superior to ampicillin. For Escherichia coli infection, protective effect of talampicillin hydrochloride was similar to that of amoxicillin, while ampicillin was less active than both talampicillin hydrochloride and amoxicillin. The absorption and excretion of 250 mg equivalent doses of talampicillin hydrochloride, amoxicillin and ampicillin were compared in nine fasting healthy volunteers after oral administration of these antibiotics in randomized triple crossover study. In order to calculate the pharmacokinetic parameters, plasma levels were analyzed using an one-compartment open model, as well as area under the plasma concentration curve (AUC) and urinary excretion. Maximum plasma levels calculated were 2.8 times higher for talampicillin hydrochloride and 1.45 times higher for amoxicillin than for ampicillin. AUC was greater for talampicillin hydrochloride than for amoxicillin and lowest for ampicillin. Urinary excretion of talampicillin hydrochloride as penicillin determined in biological assay was comparable to that of amoxicillin and 1.55 times higher than that of ampicillin. Penicillins can be metabolized to penicilloic acids in the body. After taking into account the penicilloic acid contents in urine, total excretion in urine was 61% for talampicillin hydrochloride, 67% for amoxicillin and 42% for ampicillin during 6 hours after dosing. The absorption of the drugs was evaluated according to the plasma levels, the area under plasma concentration curve and the percentage of excretion in urine. The results obtained showed that talampicillin hydrochloride was well absorbed from the gastro-intestinal tract.
对盐酸替卡西林的抗菌活性、吸收及排泄情况与阿莫西林和氨苄西林进行了比较。盐酸替卡西林对革兰氏阳性菌和革兰氏阴性菌均显示出广谱抗菌活性，这与阿莫西林和氨苄西林类似。盐酸替卡西林、阿莫西林和氨苄西林的抗菌活性相当相似。在实验性小鼠金黄色葡萄球菌感染中，盐酸替卡西林的保护作用优于氨苄西林。对于大肠杆菌感染，盐酸替卡西林的保护作用与阿莫西林相似，而氨苄西林的活性低于盐酸替卡西林和阿莫西林两者。在9名空腹健康志愿者中进行了随机三交叉研究，口服250mg等效剂量的盐酸替卡西林、阿莫西林和氨苄西林后，比较了它们的吸收和排泄情况。为了计算药代动力学参数，采用单室开放模型分析血浆水平，以及血浆浓度曲线下面积（AUC）和尿排泄量。计算得出的最大血浆水平，盐酸替卡西林比氨苄西林高2.8倍，阿莫西林比氨苄西林高1.45倍。盐酸替卡西林的AUC大于阿莫西林，氨苄西林的最低。生物测定中测定的盐酸替卡西林以青霉素计的尿排泄量与阿莫西林相当，比氨苄西林高1.55倍。青霉素在体内可代谢为青霉素酸。考虑到尿中青霉素酸含量后，给药后6小时内，盐酸替卡西林的尿总排泄量为61%，阿莫西林为67%，氨苄西林为42%。根据血浆水平、血浆浓度曲线下面积和尿排泄百分比评估药物的吸收情况。所得结果表明，盐酸替卡西林从胃肠道吸收良好。
