Bodin N O, Ekström B, Forsgren U, Jalar L P, Magni L, Ramsay C H, Sjöberg B
Antimicrob Agents Chemother. 1975 Nov;8(5):518-25. doi: 10.1128/AAC.8.5.518.
Bacampicillin (proposed international nonproprietary name), 1'-ethoxycarbonyloxyethyl 6-(d-alpha-aminophenylacetamido)penicillanate, is a new orally well-absorbed penicillin, highly active in vivo due to rapid transformation into ampicillin. The compound is stable in vitro at gastric pH and hydrolyzed slowly to ampicillin at neutral pH but very rapidly in the presence of biological fluids, e.g., tissue homogenates or serum. In vivo the transformation into ampicillin is so rapid that no unchanged compound could be detected in the blood after oral administration of bacampicillin to rats, dogs, and humans. On oral administration to mice, rats, and dogs, bacampicillin was found to be better absorbed than ampicillin, giving higher and earlier peak blood levels of ampicillin. The bioavailability of bacampicillin in rats and dogs was three to four times higher than that of an equimolar amount of ampicillin. On oral administration to rats, bacampicillin was found to give higher levels of ampicillin in organs such as the kidney, liver, and spleen than ampicillin itself. In "tissue cages" in rats, higher transudate levels of antibiotic were found after oral administration of bacampicillin than after ampicillin. On oral treatment of experimentally infected mice, bacampicillin was found to be more active than ampicillin.
巴卡西林（建议的国际非专利名称），即1'-乙氧羰基氧乙基6-（d-α-氨基苯乙酰氨基）青霉烷酸，是一种新的口服吸收良好的青霉素，由于能迅速转化为氨苄西林而在体内具有高度活性。该化合物在胃酸pH值下体外稳定，在中性pH值下缓慢水解为氨苄西林，但在生物流体（如组织匀浆或血清）存在下则非常迅速。在体内，转化为氨苄西林的速度非常快，以至于给大鼠、狗和人类口服巴卡西林后，血液中未检测到未变化的化合物。给小鼠、大鼠和狗口服后，发现巴卡西林比氨苄西林吸收更好，氨苄西林的血药峰浓度更高且出现更早。巴卡西林在大鼠和狗体内的生物利用度比等摩尔量的氨苄西林高三到四倍。给大鼠口服后，发现巴卡西林在肾脏、肝脏和脾脏等器官中的氨苄西林水平比氨苄西林本身更高。在大鼠的“组织笼”中，口服巴卡西林后发现渗出液中的抗生素水平比口服氨苄西林后更高。对实验感染的小鼠进行口服治疗时，发现巴卡西林比氨苄西林更具活性。
