Oral Administration Of Bacampicillin Research Articles

Ｂａｃａｍｐｉｃｉｌｌｉｎ経口投与後のヒト血清，歯根嚢胞および膿中へのａｍｐｉｃｉｌｌｉｎの移行に関する研究

Ｂａｃａｍｐｉｃｉｌｌｉｎ経口投与後のヒト血清，歯根嚢胞および膿中へのａｍｐｉｃｉｌｌｉｎの移行に関する研究

Ｂａｃａｍｐｉｃｉｌｌｉｎ経口投与後のヒト血液および歯根肉芽腫中へのＡｍｐｉｃｉｌｌｉｎの移行に関する研究

Ｂａｃａｍｐｉｃｉｌｌｉｎ経口投与後のヒト血液および歯根肉芽腫中へのＡｍｐｉｃｉｌｌｉｎの移行に関する研究

Experimental investigation on intrapulmonary and tracheobronchial distribution of ampicillin after administration of a beta-lactam antibiotic, bacampicillin

Bacampicillin (BAPC) is a esterified derivative of ampicillin (ABPC) developed recently by the Swedish company. In present investigation we measured the concentration of ABPC in plasma, lung and tracheobronchial tissues from normal, pleuritis and pneumonitis male albino rabbits after an oral administration of BAPC. In these 3 groups plasma level of ABPC reached the maximum at 30-50 minutes after oral administration, then showed a gradual decrease. The decaying curves of pleuritis and pneumonitis groups were steeper than that of control group. Plasma level of ABPC in pneumonitis group at the maximum value was about 1/2 comparing with that in control and pleuritis groups. ABPC levels of tracheobronchial tissues in pleuritis and pneumonitis groups were higher than that in control group at 60 minutes after oral administration of BAPC. On the other hand, tissue level of ABPC in control group was higher than that in pleuritis and pneumonitis groups at 120 minutes after oral administration of BAPC. ABPC level of lung tissues (L1 and L5) in control group was higher than that in pleuritis and pneumonitis groups at 60 minutes after oral administration of BAPC, on the other hand ABPC level of L3 in control group was lower than that in pleuritis and pneumonitis groups. ABPC levels of lung tissues (L1 - L5) at 120 minutes after oral administration of BAPC were higher in control group comparing with that in pleuritis and pneumonitis groups.

Ampicillin concentration in normal and pathological lung tissues after oral administration of bacampicillin.

Following oral administration of 800 mg bacampicillin, the concentrations of ampicillin were determined in normal (n = 16) and pathological (n = 12) lung tissue after 3.6 and 9 hours in a total of 28 patients. The serum concentration was determined simultaneously. The mean peak serum concentration (+/- SD) after one hour was 9.7 +/- 7.2 micrograms/ml. The mean concentration (+/- SD) in normal lung tissues were, after 3, 6 and 9 hours, 3.73 +/- 1.10 micrograms/ml, 1.06 +/- 0.99 micrograms/ml, 0.15 +/- 0.30 microgram/ml respectively, and in pathological lung tissues 0.95 +/- 0.31 microliters/ml, 0.86 +/- 1.11 micrograms/ml and 0.40 +/- 0.24 micrograms/ml respectively. Thus bacampicillin produced concentrations well above the MIC of the most important pathogen, Haemophilus influenzae, in both pathological and normal lung tissue.

Penetration of ampicillin into urethral and cervical secretions after oral administration of bacampicillin.

The study comprised 24 male and 24 female patients treated either for uncomplicated gonorrhoea or as a prophylaxis. A single dose of 800 mg of bacampicillin + 1.0 g probenecid was administered orally to each patient. The concentrations of ampicillin in urethra and cervix were assayed by means of alginate swabs that were used as diffusion centres on agar diffusion plates. The inhibition zones were compared with a standard series of swabs containing known amounts of ampicillin. The amounts of secretions absorbed into the swabs were determined by weighing each swab before and after taking the specimen. The median ampicillin concentration in the male urethra one hour after the single dose of bacampicillin plus probenecid was 2.0 micrograms/ml of urethral secretion and increased to 3.2 micrograms/ml two hours after administration of the antibiotic. In the female urethra, the median concentrations of ampicillin were 1.5 micrograms/ml and 2.3 micrograms/ml of urethral secretion one and two hours, respectively, after the same dosage as above. The corresponding ampicillin concentrations in the cervical secretion were 1.6 micrograms/ml and 2.9 micrograms/ml, respectively.

Penetration of ampicillin into human bronchial secretions.

Ampicillin concentrations in serum and bronchial secretions after oral administration of bacampicillin were evaluated. Twenty-eight hospitalized patients with acute bronchopulmonary infections received a single dose of 800 mg of bacampicillin. Samples of bronchial secretions were obtained during diagnostic bronchoscopy and blood samples were drawn simultaneously. Significant concentrations of ampicillin were found in bronchial secretions, the peak level, reached after approximately two hours, being 0.27 micrograms/ml on an average. The penetration of ampicillin into the bronchial secretions after the administration of bacampicillin could be correlated with the degree of bronchial inflammation, as illustrated either by macroscopic purulence or protein concentration in the secretions. The results suggest that bacampicillin is a useful drug in acute bronchopulmonary infections.