경구용 Bacampicillin과 Ampicillin의 약력학적 비교

Abstract

Bacampicillin is a oral prodrug which is rapidly 'Converted to ampicillin during absorption from the gastrointestinal tract. It is much more lipophilic than ampicillin by the substitution at the ampicillin thia' zolidine carboxy group. Bacampicillin orally was compared pharmacokinetically with oral ampicillin. Single usual oral doses of bacampicillin HCl (400mg) and ampicillin trihydrate (500mg) were given to 8 healthy subjects on a cross-over randomized basis Data \vere interpreted in terms of a single compart· mental open model. After administration of bacampicillin, much higher and sharper peaks (4. l6±0. 52 ug!m1) was achieved in serum, compared with ampicillin (2. 90±1. 02 ug! ml). Peak levels were observed at O. 69±0. 18 hr with bacampicillin and at 1. 82±0. 36 hr with ampiciUin. As to differences in pharmacokinetic nature between the two drugs , the main ones were the lag· time before absorption, absorption rate and bioavail· ability. The apparent lag-time before absorption was longer for oral ampicillin (0.47±0.17 hr) than for bacampicillin (0. 24±0.15 hr). Intestinal absorption of bacampicillin was found to be faster(about 6 times in rate) and more complete than that of amp· icillin , yielding an increase in bioavailability 6696 on an equimolar basis as measured by the area under the serum levels of curves.