Braga P C, Fraschini F, Ceccarelli G, Scaglione F, Scarpazza G
Clin Ther. 1981;4(1):32-42.
Bacampicillin is a recently synthesized prodrug of ampicillin. It differs from ampicillin in having an ethoxycarbonyloxyethyl group attached to the carboxyl group in C3 of the penicillin nucleus, thus forming an ester with higher bioavailability than ampicillin. The present study was carried out in 30 patients suffering from acute exacerbations of chronic bronchitis. Bacampicillin was administered orally according to the following outline: Group A--800 mg, group B--1,200 mg, and group C--1,800 mg. The peak mean serum levels were 9.50, 12.07, and 15.83 micrograms/ml, respectively, and were reached in one hour with all doses. The peak mean bronchial mucus levels were 0.49, 0.62, and 0.95 micrograms/ml, respectively, and were achieved in four hours with all doses. During the eight hours after administration of the antibiotic, 71%, 68%, and 73% of the administered doses were excreted in the urine. Blood levels versus time curve were interpreted in terms of a one-compartment open model. Bronchial mucus and serum peaks were in good correlation with progressive doses.
巴卡西林是最近合成的氨苄西林前体药物。它与氨苄西林的不同之处在于，在青霉素核C3的羧基上连接了一个乙氧羰基氧乙基，从而形成了一种生物利用度比氨苄西林更高的酯。本研究对30例慢性支气管炎急性加重患者进行。巴卡西林按以下方案口服给药：A组——800毫克，B组——1200毫克，C组——1800毫克。平均血清峰值水平分别为9.50、12.07和15.83微克/毫升，所有剂量均在1小时内达到峰值。平均支气管黏液峰值水平分别为0.49、0.62和0.95微克/毫升，所有剂量均在4小时内达到峰值。在给予抗生素后的8小时内，71%、68%和73%的给药剂量经尿液排出。血药浓度-时间曲线按照一室开放模型进行解释。支气管黏液和血清峰值与递增剂量具有良好的相关性。
