S-Space College of Medicine/School of Medicine (의과대학/대학원) Dept. of Medicine (의학과) The Seoul Journal of Medicine The Seoul Journal of Medicine Vol. 25 No.2 (1984)
경구용 Bacampicillin과 Ampicillin의 약력학적 비교
Pharmacokinetic Comparison of Oral Bacampicillin and Ampicillin
- Issue Date
- 서울대학교 의과대학
- Seoul J Med, Vol.25 No.2, pp. 134-138
- 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.