Bacteriological examinations of bacampicillin, an esterized derivative of ABPC were performed in comparison with ABPC and AMPC.
Bacampicillin showed an excellent antibacterial effect in vivo because of its high serum level.
The peak serum level with bacampicillin was twice as high as AMPC, and three times as high as ABPC.
This excellent in vivo antibacterial effect was also confirmed by its protecting effect against experimental infection in neutropenic mice.

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In vitro and in vivo antibacterial activities of bacampicillin, a new orally active ester derivative of ampicillin. were compared with those of ampicillin, amoxycillin and talampicillin. The following results were obtained.
1) The antibacterial spectrum of bacampicillin against gram positive and gram negative bacteria was nearly similar to that of ampicillin. In the level of activity, however, ampicillin was slightly more effective than bacampicillin.
2) In sensitivity test on clinical isolates, such as Staphylococcus aureus, Escbericbia coli, Klebsiella pneumoniae, Proteus vulgaris and Proteus mirabilis, ampicillin was slightly more effective than bacampicillin.
3) The antibacterial activity of bacampicillin and ampicillin against S. aureus was decreased as serum concentration became higher and inoculum size larger. The antibacterial activity of bacampicillin was enhanced at alkaline pH.
4) On the antibactericidal activity determined by biophotometer, ampicillin showed more rapid bacteriolytic activity than that of bacampicillin in E. coli.
5) The rate of hydrolysis, measured as the amount of ampicillin, of bacampicillin and talampicillin were compared in heart infusion broth. It was cleared that bacampicillin was more stable than talampicillin.
6) On the protective effect for experimental infection in mice, the effect of bacampicillin was 1.4 to 4.1 times superior to ampicillin for S. aureus, E. coli, K. pneumoniae and P. mirabilis infection. When the challenge dose was increased, the decrease of therapeutic effect of bacampicillin was similar to that of ampicillin and amoxycillin for E. coli infection. When total dosage was fixed, protective effect of bacampicillin, ampicillin and amoxycillin was not influenced with increasing injection times at interval of 1 hr.

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Acute, subacute and chronic toxicities of bacampicillin hydrochloride (BAPC), a new orally active ampicillin derivative, were studied in mice and rats.
In the acute toxicity test, reduced spontaneous locomotor activity and labored respiration were common symptoms in mice and rats treated orally, subcutaneously or intravenously with BAPC. LD₅₀ values (mg/kg) were as follows:(male, female) in mice;(p.o.) 10, 571, 8, 529, (s.c.) 10, 345, 9, 475, (i.v.) 184, 209 in rats;(p.o.) and (s.c.) >10, 000, >10, 000 (i.v.) 176, 176. Death occurred from respiration paralysis, irrespective of the animal species and the route of administration.
In the subacute toxicity test, rats were orally given 100, 250, 500, 1, 000 and 5, 000 mg/kg/day of BAPC for 5 weeks, with 700 mg/kg/day of ampicillin (ABPC) as a reference compound. In the chronic toxicity test, rats were orally given 50, 100, 250, 500 and 1, 000 mg/kg/day of BAPC for 26 weeks. Death occurred from alimentary tympanites in the groups of 5, 000 mg/kg administration of the subacute toxicity test and 1, 000 mg/kg administration of the chronic toxicity test. In both subacute and chronic toxicity tests, the animals in any dose group showed slight decrease in food consumption during the first week of administration without effect on the body weight gain. The animals given BAPC also showed soft feces, diarrhea, enlargement of the cecum and decrease of serum protein. These findings were sirnilar to those of ABPC administration.
No drug related microscopic abnormal finding was observed.
Safe y dose of BAPC in 26-week oral toxicity study in rats was considered to be 500 mg/kg/day.

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Reproductive and teratologic studies were conducted on bacampicillin hydrochloride (BAPC) in rats and rabbits. Doses employed in Sprague-Dawley rats were 50. 250, 1000 and 3000 mg/kg and those in Japanese white rabbits were 50, 100 and 250 mg/kg. They were administered during the appropriate time sequences.
BAPC treatment did not affect either fertility, or the survival and development of the offspring when adult male rats were administered with BAPC orally for 67 days prior to mating and females were given from 14 days prior to mating to day 7 of gestation. Inhibition of maternal weight gain was observed in rats given two top dose levels of 1000 and 3000 mg/kg.
There was no evidence of a teratogenic effect when BAPC was administered daily by gavage to female rats on gestation days 7 through 17 and to female rabbits on gestation days 6 through 18. The rabbit was an unsuitable species for teratology trials in the antibiotics: daily BAPC doses of 250 mg/kg resulted in material death and doses of 100 and 250 mg/kg caused abortion in some rabbits. Exceptionally an interventricular septal defect in rats treated at a dose of 50 mg/kg and a short tail in rabbits treated at a dose of 100 mg/kg were found, but they were considered to be spontaneous in origin.
When rats were given BAPC at a dose of 3000 mg/kg during the perinatal-postnatal period (gestation day 17 through postpartum day 20), maternal death, slight depression in maternal weight gain, a few cases of stillborns and slightly decreased neonatal survival were observed. No adverse effects were confirmed in rats treated at doses of 50, 250 and 1000 mg/kg.

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1.ウサギに皮内注射により感作した場合, BAPC自体の免疫原性はABPCに比べて弱かった。
2.赤血球凝集ハブテン阻止反応で, BAPCとABPCとに強い交叉性がみられた。
3.定量沈降および72時間ラットreagin PCAのハブテン阻止反応で, BAPCはABPCおよびPCGと弱い交叉性を示した。
4.BAPCの蛋白結合能はpH5.0でABPCより弱かった。

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1) At a dose of 1000 mg/kg p.o., bacampicillin exhibited little influences on the central nervous system, somatic and autonomic nervous system.
2) Bacampicillin showed weak spasrnolytic activity in isolated guinea pig ileum and tracheal muscle. At a concentration of 10^-4 M, bacamplicillin also inhibited the spontaneous contraction of the pregnant and non-pregnant uterus of rats.
3) Bacampicillin showed the local anesthetic activity in guinea pigs, and increased gastointestinal propulsion at a dose of 1000 mg/kg p.o., in mice.
4) Bacampicillin, when administered intravenously, induced a slight transient fall in blood pressure, andincrease in heart rate and respiration at a dose of 10 mg/kg in anesthetized dogs.
5) At a dose of 1000 mg/kg p.o., bacampicillin decreased urine volume and excretion of electrolytes in saline-loaded rats.
6) Bacamplicillin had no effects on the bleeding time, blood sugar level and serum lipids in mice, and blood coagulation and fibrinolysis in rats. Anti-inflammatory effect of bacampicillin was not recognized in rats.

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Pharmacokinetics of bacampicillin hydrochloride, an ester derivative of ampicillin, was investigated in rats. Orally administered bacampicillin bydrochloride was well absorbed as ampicillin, hydrolyzed active form in the body, giving more rapid and twice higher peak blood level than amoxycillin in rats.
The two drugs gave the almost comparable tissue concentrations after oral administration at equimolar dose. However, antibiotic was detected in the central nervous system after administration of bacampicillin hydrochloride. but not in the case of amoxycillin. Detectable antibiotic activity in the lung was maintained for more prolonged period with bacampicillin hydrochloride as compared with amoxycillin.
Activity in the urine was also higher during first 6 hours after oral administration of bacampicillin hydrochloride to rats than after amoxycillin. The same phenomenon was observed in the biliary excretion of the first 4 hours after administration.

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1. 血液または血漿中のBacampicillin (BAPC) およびArnpicillin (ABPC)・a-aminobenzy_peniciloic acid (ABPA) のけい光法による分別定重法を確立した。
2. ヒトおよび動物の血漿中エステラーゼによるBAPCの加水分解速度には動物種差がみられ, ラットが最も速く以下ウサギ, ヒト, イヌの順であった。
3. BAPCを経口投与したヒトおよびイヌの末梢血液中には高濃度のABPC・ABPAを認めたが, 未変化のBAPCは全く見出されなかった。
4.バイオオートグラフィーにより, BAPCを経口投与したヒトおよびイヌの血漿中抗菌活性物質は, ABPCのみであることが確認された。

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Pharmacokinetic study was investigated with 6 healthy volumteers administered twice oral doses of bacampicillin (equimolar to 250 mg of ampicillin) in the preprandial and postprandial states using cross-over test. As the mean peak blood concentration of ampicillin by bioassay after each dosing, 3.3 and 4.32 μg/ml was obtained after one hour in preprandial cases, and 4.19 and 1.98 μg/ml after one and two hour in postprandial cases, respectively. On the postprandial cases, the peak blood concentration was lower than the preparandial case, however, it was decreased more slowly. Sixty point six percent of the administered dose was excreted for 10 hours in the preprandial case and 50.1% in the postprandial case.
Twenty five cases, including 10 of respiratory infections and 15 of urinary tract infections were treated with bacampicillin 1g per day for 3 to 8 days orally. Two of those patients were cured excellent and 19 were good. Three patients with urinary tract infections were responsed fair and one patient was failed. Super infection, E. coli altered to Klebsiella, was accured two urinary tract infections.
As to the side effect of the drug, gastric discomfort and anorexia were observed in one patient.

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In 7 cases of respiratory tract infection, and 2 cases of urinary tract infection, bacampicillin was administered. Clinical improvements of symptoms were observed in 5 cases of respiratory tract infection and 2 cases of urinary tract infection.
Disfuction of liver was observed in one case during the administration of this drug.

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Clinical investigations were performed on bacampicillin, a new orally well-absorbed semisynthetic penicillin which is high active in vivo due to rapid transformationinto ampicillin.
Bacampicillin was administered to total 27 cases of respiratory tract infections, at daily dose of 1.0 g for 5-28 days to 8 cases of bronchitis, 18 cases of pneumonia and a daily dose of 1.5 g for 14 days to a case of pneumonia. Clinical response of bacampicillin was excellent in 15 cases, good in 8 cases and fairly effective in 4 cases.
Side effects with bacampicillin were observed in 3 cases consisting of one skin eruption, one eosinophilia and one elevation of serum transaminase. These turned to normal by discontinuing the drug.

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Bacampicillin was used in 14 cases (acute bronchitis 4 cases, acute tonsillitis 3 cases, emphysema 3 cases, bronchiectasis one case, lung abscess one case, chronic bronchitis? one case and fever of a patient with chronic renal failure one case). Results are shown in Table 1 and 2. Effect evaluation was good in 8 cases, fair in one case and poor in 2 cases. Three cases were excluded from the effect evaluation.
No distinct side effects were observed.

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Bacampicillin was tested to the following infectious diseases and the following result was obtained.
It was effective to 2 cases of acute tonsillitis, to 3 cases of acute pyelonephritis, to 2 cases of acute enteritis, to 4 out of 7 cases of acute bronchitis, to 3 out of 6 cases of acute pneumonia including mycoplasma pneumonia. But it was not effective to a case of chronic cystitis, to 2 cases of chronic pyelonephritis, to a case of chronic enteritis, to a case of ovarial abscess. It was effective to 14 out of 25 cases in total and effective rate was 56%.
As side effect, eruption caused by bacampicillin administration was observed in 3 cases and gastric disturbances in 2 cases.

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Basic and clinical studies on a new ABPC derivative, bacampicillin, were carried out and the following results were obtained.
1) In cross over study between bacampicillin and AMPC, the peak blood level was identical each other after the same dose administration. Bacampicillin reached the peak level faster than AMPC, and urinary recovery was equal between both drugs.
2) Successive bacampicillin administrations did not bring out the tendency of accumulation.
3) When ABPC dose administered was doubled in comparison with bacampicillin in cross over method, similar value was found at the peak of blood level.
4) The elevation of Al-p and LAP over the normal range was noticed in certain cases six hours after bacampicillin administration. These cases also showed the same elevation after ABPC administration.
5) Clinically, 15 patients having various infections were treated with bacampicillin. As a result, 8 were good, one was fair, 4 were poor, and 2 were undetermined. In one patient, sore throat and pain at swallowing occurred perhaps because of stimulus by tablet retention at the local site of pharynx.

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The serum concentrations, urinary excretion and clinical efficacy of bacampicillin, an ester form of ampicillin, were investigated and the following results were obtained.
1) Serm levels
The serum concentration in healthy volunteers after a single dose of bacampicillin which was equivalent to 500 mg ampicillin reached a mean peak level of 7.33 μg/ml at one hour, and the concentration declined with half-life value of 0.95 hours.
2) Urinary excretion
Bacampicllin recovered in the urine for 6 hours after an oral dose was 52.5%, which was higher than the amount of ampicillin (32.9%) collected for the same duration.
3) Clinical results
Bacarnpicillin was clinically applied to 9 cases with bacteria infections, including one case of chronic bronchitis, one case of angina lacunaris, and 7 cases of urinary tract infections. Clinical response obtained in these cases was good except for one case from whom the drug was withdrawn because of diarrhoea. No serious side effects were observed other than diarhoea which developed in one case 3 days after administration.

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1) The peak serum level was obtained one hour after administration of bacampicillin and was slightly higher than that of amoxycillin. Bacampicillin seemed to be excreted faster than amoxycillin.
2) We treated with bacampicillin 13 cases of respiratory tract infection. Clinical effect was good in 10.fair in 3 and poor in 3 out of 16 cases.
Bacteriological effect was not obtained in 5 cases.
3) No adverse reaction and no abnormality in laboratory examinations was observed.
Bacampicillin was considered to be a useful drug as oral penicillin.

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Ten cues of pneumonia and eight cases of chronic bronchitis were treated with bacampicillin at one gram (ABPC titer) per day.
In the pneumonia the excellent results were obtained in two cues, good results in seven cues and unchanged result in one case. In the chronic bronchitis good results were obtained five cases and unchanged results in three cues.
The side effects were observed in two cases. One of which was the slight gastrointestinal symptom shown at one day after the administration, and the other observed was the low grade elevation of serum GOT at two weeks after it.
From these clinical results and the antimicrobial spectrum in vitro examinations, bacampicillin may be a useful antibiotics for the respiratory tract infections, above all pneumonia.

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Clinical studies on BAPC were performed with following results:
1) BAPC was administered to 12 patients with acute pyelonephritis, 5 patients with acute bronchitis and one patient with acute enteritis. The daily dose was 1.0 to 2.0 g during 2 to 8 days. The clinical results were as follows: excellen in 6, good in 7, fair in one, poor in 3 and superinfection in one patient.
2) As for the side effect, eruption was observed in 2 patients, diarrhea in one patient and epigastric pain in one patient.
3) No abnormal findings were found in renal and hapatic functions.

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Bacampicillin was administered to patients of respiratory tract infections and favorable results were obtained. The following are the results of the clinical trial.
1) Subjects were 14 out-patients and 5 in-patients (9 males and 10 females). The age ranged from 21 to 74 (41.2 on the average).
2) The diseases are 8 cases of acute bronchitis, 3 cases of pneumonia, 3 cases of bronchiectasis, 2 cases of aggravation of chronic bronchitis. one case of interstitial pneumonia, one case of secondary infection to pulmonary tuberculosis, and one case of secondary infection to pulmonary carcinoma.
3) Regarding the severity of the diseases, there were 8 mild, 8 moderate and 3 severe cases.
4) The daily dosis were 750-1000 mg (ABPC titer), and the total amount of dosis ranged from 1.5g to 15g.
5) There observed 11 effective cases, 5 fairly effective cases, 2 poor cases and one drop-out due to side effects.
6) Two cases showed the gastrointestinal disturbances of nausea, vomiting and anorexia.

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In order to examine the clinical effects of bacampicillin, the drug was administered to 20 patients of relatively mild airway infections at a daily dose of 750 mg (ABPC titer) in postprandial three-divided portions. The results obtained were 2 excellent, 12 good, 4 fair, one poor and one unknown cases. Therefore, bacampicillin is expected to exert favorable effects with less dose than that of amplicillin in the clinical practice. Regarding side effects, caution will be necessary to eruption in the case of the long term administration.

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Clinical investigations have been carried out on bacampicillin (BAPC), a new orally well-absorbed penicillin and following results were obtained.
1) Serum concentration of BAPC after single oral administration was determined to 3 volunteers, comparing with ABPC. The result suggested a different profile for BAPC, with earlier and much higher peak serum levels than that obtained with ABPC.
2) BAPC was applied singly for the mild and moderate respiratory tract infections, urinary tract infections and cholecystitis, then remarkable result was obtained in 17 cases (85.0%) out of 20 respiratory infections, favorable result was obtained in 2 cases (100%) of urinary tract infections, while no effectiveness was observed in a case of cholecystitis.
3) Side effect was observed in only one case, which showed eosinophilia one week after the start of BAPC administration.

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Fundamental and clinical studies of bacampicillin were conducted, and the following results were obtained:
1) Bacampicillin was superior to ampicillin and talampicillin in the absorption from the digestive tracts. When 250 mg of bacampicillin were administered to fasting volunteers, the serum level showed the peak of 6.29 μg/ml, which was more than 3 times and about 1.5 times as high as that of ampicillin and talampicillin, respectively.
2) In accordance with the good and rapid absorption from the digestive tracts, the amount of the urinary excretion was high as compared with ampicillin and talampicillin. In particular, the difference was remarkable within 2 hours after the administration.
3) Bacampicillin was given to 10 cases of respiratory tract infections, 4 cases of urinary tract infections and 2 cases of septicemia, and there observed 2 excellent, 8 good, 5 poor and one unassessable case in the clinical evaluation. As regards the side effects, one case each of eruption, anorexia and diarrhea was found.

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Studies were made on the blood level, the urinary excretion, and on the clinical effectiveness of bacampicillin. The results obtained were as follows:
1) Blood levels and urinary excretion in three adult volunteers: A single oral administration of bacampicillin 500 mg ABPC titer in fasting yielded the average peak blood level as high as 9.9 μg/ml 30 minutes after the dosage, showing rapid absorption of the drug from the intestinal tract. This peak blood level was twice as high as that of ampicillin formerly studied by the authors. The urinary recovery rate of the drug in six hours was found to be 44.5% in average.
2) Clinical trials: Seventeen patients (R.T.1. 11, U.T.I. 4, acute colitis 1, and lymphadenitis 1) were treated with bacampicillion 1.0 g/day. Thirteen of the cases showed good response to the treatment. Neither side effects nor abnormal laboratory findings attributable to the dosage were observed in those patients.

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Pharmacological and clinical investigations were performed on bacampicillin and the results obtained were as follows;
1) Serum levels reached the peak 1 hour after the oral administration of 250 and 500mg of bacampicillin with mean serum concentration of 5.0 and 10.3μg/ml respectively.
2) Four of six parients with respiratory tract infections treated with bacampicillin showed the good clinical effects. No side effect was observed in any patient except one case of eruption. No abnormality in laboratory findings was seen in any case during the medication.

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Bacampicillin was administered on 8 patients: 2 patients with urinary tract infection, 2 patients with acute enterocolitis, one patient with acute tonsillitis, one patient with acute upper respiratory tract infection, one patient with chronic prostatitis, respectively.
The clinical responses were considered to be satisfactory except one patient with chronic prostatitis. No side effects were observed except for one case with skin rash, eosinophiliand an elevation of serum transaminase (S-GPT).

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Laboratory and clinical investigation was performed on bacampicillin (BAPC) and following result was obtained.
1) MIC of BAPC was nearly equal to that of ampicillin (ABPC). To some organisms, MIC of BAPC was a bit bigger than that of ABPC.
2) We compared serum concetration of BAPC and ABPC by cross over method. Peak serum concentration following single oral dosage of BAPC 250mg and 500mg was 9.0μg/ml and 12.5μg/ml, respectively. Peak serum level of 3.0μg/ml and 5.5μg/ml was obtained after administration of 250mg and 500mg ABPC.
3) We treated 13 cases of respiratory infection, 3 cases of urinary infection and one case of another infection by BAPC. Dosage of BAPC was 1g/day, 5-56 days or 1.5g/day, 2 days. Clinical effect was effective in 11, slightly effective in 3, ineffective in one and unknown in 2.
One anorexia and two elevations of GOT and GPT were observed.

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Becampicillin was used in the treatment of pneumonia and exacerbation of chronic bronchitis and bronchiectasis in a series of 20 cases. From nine cases out of 20 cases the infecting bacteria were isolated from sputa; Haemopbilus influenzae 6 cases, Streptococcus penumoniae 2 cases and β-Streptococcus one case. We estimated the effectiveness of the drug from the improvements in subjective symptom and laboratory and radiological findings. The effect was excellent in 8 cases, good in 6 cases, fair in 4 cases and poor in 2 cases. The rate of effectiveness was 70%. No side effects were encountered during this study.
It could be concluded that bacampicillin was useful as the first choice drug against pulmonary infections. But we should always be careful to avoid the superinfection and colonization of pseudomonas aeruginosa and Klebsiella pneumoniae.

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Bacampicillin (BAPC) is a newly developed derivative of ampicillin which is well absorbed when given orally and is hydrolyzed to ampicillin in the body to give peak levels of ampicillin higher than those obtained with ampicillin itself. Fundamental and clinical studies on this drug were carried out and the results were as follows:
1) Absorption and excretion in man
Three healthy male adults volunteers were given orally 250 mg of BAPC after fasting and peak levels of BAPC in the blood of two volunteers were 3.5μg/ml and 4.8μg/ml one hour after administration of BAPC. Residual one has 2.1μg/ml of peak level two hours afterwards.
Urinary recovery rate during the initial two hours after administration of BAPC was 40-50 percent and 59-67 percent, 62 on the average were excreted by the end of the study for 6 hours.
2) Clinical study
Thirty one patients with pulmonary infection including one case with lung cancer and one with pulmonary tuberculosis respectively, were treated with one gram of BAPC daily for 3-21 days and good results were obtained in 21 cases with efficacy rate being 75 percent. In five cases out of six patients with chronic bronchitis due to Haemophilus influenzae, this organism was eliminated completely with BAPC.
3) Adverse reaction
Two patients complained of mild diarrhea and one heart burn. Eosinophilia was seen in one case.

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Laboratory and clinical studies were made on bacampicillin, a new orally well-absorbed derivative of amplicillin belonging to ampicillin esters.
In the determination of tissue levels in rats, the absorption of bacampicillin as rapid as compared with ampicillin, and the peak value of the blood level was twice higher than that of ampicillin.
Bacampicillin was orally administered to 24 patients with respiratory tract infections and 5 patients with urinary tract infections at the daily dose of 750 mg or 1000 mg in 3-or 4-divided portions. As the results, it was confirmed that bacampicillin was effective to respiratory tract infections caused by H. influenzae and Str. pneumoniae and Str. pyogenes and urinary tract infections caused by E. coll. No side effects were observed in all the 29 subjects. it was concluded that bacampicillin is more useful than ampicillin.

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Bacampicillin shows 2-3 times higher serum level than ampicillin by oral administration.
We investigated bacampicillin in the field of pediatrics and following results were obtained.
1) Bacampicillin was administered orally about 7-15mg/kg to children. The serum level peak (average 6.08-7.75μg/ml) was obtained at 30min.-1h. after administration and high serum level (average 3.75-5.12μg/ml) was kept till 2h.
2) Urinary excretion rate within 6h. was about 60-70% of dose administered.
3) Twenty one cases of acute tonsillitis, scarlet fever, lacunar tonsillitis and acute bronchitis were administered at a dose of 30mg/kg/day (t. i. d. or q. i. d) continuously and good clinical effect was obtained in all patients treated.
4) No abnormal laboratory finding was observed in liver, kidney and blood after continuous oral administration.(about 30mg/kg daily)
5) In no case, rash was observed.

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Clinical studies were done on bacampicillin, an ester of ampicillin, and the following results were obtained.
1) Blood concentrations of the drug were determined after a single oral dose of 250 mg ABPC titer was given to two children after meal (5.1 mg/kg and 7.4 mg/kg, respectively). Peak values of 11.2 μg/ml and 11.6μg/ml were obtained 2 hours and 1 hour after administration, respectively, and were much higher than those of ampicillin. Difference of the peaks, i.e., 2 hours and 1 hour, between the two patients appeared to result from postprandial administration of the drug. A urinary recovery rate up to 6 hours was 36.1% in one case.
2) Bacampicillin was given to 18 cases of acute bacterial infections in children and its dosage was mostly 25-34mg/kg/day in 4 divided doses. The overall efficacy rate was 77.8%(excellent in 10, good in 4 and failure in 4); tonsillitis (13 cases), excellent in 8, good in 3 and failure in 2, an efficacy rate being 84.6%; failure in 2 cases of urinary tract infection, both of which were caused by resistant organisms; enteritis (3), excellent in 2 and good in one.
3) Adverse reactions included each one case of eosinophilia and a slight elevation of BUN. Skin eruption or diarrhea was not noted.
4) Based on the above results, it is concluded that an efficient absorption rate of bacampicillin makes it a potent new antibiotic in the treatment of infections caused by ampicillin-sensitive organisms.

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Bacampicillin hydrochloride (BAPC) for oral administration was given to 51 patients with acute or subacute infectious diseases, 23 cases were outpatients and 28 patients were hospitalized. They were 10 acute mastitis, 10 acute peritonitis after perforative appendicitis, 12 cholecystitis with cholelithiasis, 5 pyelonephritis and others.
The clinical evaluation of results was classified into excellent in 13 cases, good 32, fair 6, poor none, the effectiveness rate was 88.2 percent.
With BAPC, the following side effect developed: the increase of GOT was observed in one case of cholecystitis, but other cases were none.

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Bacampicillin hydrochloride for oral administration were tested in 31 patients who were hospitalized with acute or subacute abdominal infectious diseases. They were 16 appendicitis, 13 cholelithiasis and 2 choledochal fistula with cholagltis who undergone an operation of choledocho-lithiasis.
Tissue specimens were taken from removed organs. The plasma samples were taken when the removed organ was clamped to stop blood flow. Weight of specimens was at least 3 grams.
Determination of Bacampicillin concentration was performed according to the bioassay method (bioassay with Bacillus subtills ATCC 6633 strain).
In the appendicitis, Bacampicillin concentrations in the appendixes were almost directly proportional to the degree of pathological inflammatory changes.
The Bacampicillin concentrations of bile in bile duct were higher than those in gall bladder.
In the patients of choledochal fistula, Bacampicillin concentration in the bile and the plasma were higher than Ampicillin concentration when a same dose administered orally.

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Bacampicillin (BAPC) was administered to 31 patients with surgical infection, and its effect and adverse reaction were assessed clinically. Daily dose given was 1g in 27 cases, 2g in 2 cases and 0.5g in 2 cases which include a 9 year old child and a case of chronic renal failure.
The clinical effect was good in 18 cases, fair in 8 cases, poor in 4 cases, and not evaluated in a case. Adverse reaction was minimal; only a case of epigastrial discomfort was noted. There was no side effect indicated by CRC and blood chemistry.

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Fundamental and clinical studies were conducted on bacampicillin, and following results were obtained.
1) Absorption and excretion
Concentrations in blood and urinary excretion were measured with bacampicillin 500mg at fasting. Drug was given in 3 healthy adults. The peak ABPC concentration in the blood was observed 1-2 hours after an oral administration of BAPC, showing an average value of 10.7 μ/ml.
The urinary recovery of bacampicillin as ABPC was 81.1% of the dose in 6 hours.
2) Clinical result
Bacampicillin was used in 15 cases with surgical infections, and the clinical results were excellent in onecase, good in 11, fair in 2 and unknown in one. No side effects were observed in any case.

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Bacampicillin, a new synthetic penicillin, was tried on 43 patients with infections in the field of surgery by means of oral administration.
The results obtained are summarized as follows: excellent and/or good responses were seen in 30 cases, fair in 6 cases, poor in 7 cases without any serious side effect. Conclusively, BAPC was thought to be a new antibiotic effective for acute infections of the soft tissues in the field of surgery.

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After single oral administration of 250mg bacampicillin, serum level, biliary level and urinary excretion of ampicillin was determined in two surgical patients.
The maximum serum level, 2.4μg/ml was obtained at 3 or 4 hours after administration.
The maximum biliary level was 5.2μg/ml at 4-5 hours.
Urinary excretion rate within 24 hours was about 30% and most of dose was excreted within 6 hours.
We treated 8 patients with post-operative infection with bacampicillin 1, 000mg/day, given in four divided doses for 4-21 days.
Clinical result was excellent in 3 patients, good in 3, poor in 2.(effective rate 75.0%)
No side effect or no abnormal rise of GOT, GPT, BUN and Creatinine was observed.

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1.000 mg of bacampicillin/day was administered to 14 aged patients with difficult urinary tract infection and 2 patients with pneumonia.
In the urinary tract infection group, the therapy with this drug resulted in “excellent” and “good” in 3 patients (25%) and unchanged in 9 patients (75%) following the criteria for clinical evaluation of antimicrobial agents on chronic complicated urinary tract infection. On the other hand, regarding to bacteriological response to this drug, the rate of eradicated pathogens was 44.4% and thinking only of the strains which were indicated as objects in the protocol of this clinical evaluation, the rate of eradicated pathogen was 71%.
Two patients with pneumonia were treated. One responded satisfactorily.
Whether small doses of bacampicillin has as equal effiect as large doses of ampicillin on pathogens should be determined following many clinical evaluation of this drugs.

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1) Bacampicillin was administered to 28 outpatients and clinical efficacy was judged in 22 patients.
Daily dose was mainly 250 mg four times and duration was mainly 3 days but one case was treated for 21 days.
Effective rate was 90.9%.
No side effect or no abnormality in laboratory examination was observed.
2) MIC and disc susceptibility of isolated organisms did not always correlate to clinical effect.

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The absorption and excretion of bacampicillin, ampicillin and amoxycillin were studied in two healthy volunteers in a cross over fashion. The peak blood level of bacampicillin achieved 5.3 times as high as that of ampicillin and 2.9 times as that of amoxycillin. These three drugs were hardly detected in blood 6 hour after the administration. The urinary recovery rate of bacampicillin during 0-6 hours was approximately twice that of ampicillin and 1.3 times that of amoxycillin.
Ninety-two patients (96 diseases) of genitourinary tract infections were treated with bacampicillin.
The results showed as follows:
1) In the small dose therapy on uncomplicated acute cystitis, the efficacy rate of 50% was obtained at a dose of 20-25mg/day.
2) In another cases of simple acute cystitis, the efficacy rate was 82.4% at a dose of 375mg/day and 76.4% at 500-1000mg/day.
3) In 4 cases of acute pyelonephritis, all were gained satisfactory results at a dose of 1000-2000mg/day.
4) In complicated chronic urinary tract infections, the efficacy rate was 60% in chronic cystitis and 42.9% in chronic pyelonephritis respectively at a dose of 375-2000mg/day.
5) As a whole, the efficacy rate of 74.1% and 52.9% was obtained in the acute and the chronic diseases respectively.
6) In acute urethritis, bacampicillin was very effective against gonorrheal infections, but insufficient against the non-gonorrheal. In the treatment of acute epididymitis, the drug was considered to be effective in some cases.
7) With respect to the disc sensitivity of ampicillin against E. coli isolated from infected urines, 47.8% of isolates in acute and 44.4% in chronic infection showed resistant.
Side effects.
Of the individual symptoms, gastrointestinal complaints were observed in 12 (13.0%) of 92 patients. These were, however, mild and transient except one case. The cases of the discontinuance of the drug administration were 5 (5.4%). In the investigations of laboratory tests, mild elevation of GOT and GPT yieled in one case, and in another case, eosinophilia. These abnormal values returned to normal level within 10-14 days after the discontinuance of the drug.

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1) Bacampicillin (750 mg/day) was administrated to 27 patients with urinary tract infections.
2) In acute simple cystitis, excellent results were observed in 10 cases, good in 3 and poor in 2. Oerall effectiveness rate in acute cases was 87%.
3) In chronic complicated infections, excellent results were in one case, good in 2 and poor in 5. Overall effectiveness rate in chronic cases was 38%.
4) Drop out cases were 4.
5) As to side effects, two cases with stomach pain were noticed. No abnormal values in GOT, GPT, Al-pase etc. after bacampicillin administration were observed.

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1) We treated following 48 cases of urinary tract infection by Bacampicillin (BAPC).
11 cases of male and 37 cases of female, from 16 years till 68 years old. 27 cues of simple cystitis, 2 cues of simple pyelonephritis, 11 cases of complicated cystitis and 8 cases of complicated pyelonephritis.
2) Clinical efficacy judged by the Evaluation Criteria for Urinary Tract Infection was 82.3% in simple UTI cases, 57.9% in complicated UTI cases and 72.9% in total cases.
3) E. coil, Staph. epidermidis and Staph. aureus were sensitive to BAPC. This fact was also proved by the clinical evidence.
4) Good clinical response was obtained in complicated UTI by BAPC. This was probably due to its high absorption rate and high urinary excretion rate.
5) No abnormal findings in hematology and blood chemistry.
6) One vomiting and one anorexia were observed during BAPC therapy.
7) BAPC was considered an excellent drug for treating urinary tract infection.

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1) Blood concentration
Bacampicillin in blood, after the oral administration of 500mg, reached an average peak 12.0μg/ml after one hour, and the concentration was still 0.4μg/ml after 6 hours.
2) Urinary excretion
In the same cases in which the blood concentraiton was measured, 78.0% of the dose was recovered on the average from 8 hour urine.
3) Clinical results
In 17 cases of acute simple cystitis, and 34 cases of chronic complicated urinary tract infection, totaling 51 cases, excellent effect was obtained in 26, good effect in 11, and no effect in 14, giving the effectiveness of 72.6%.
4) Among 54 cases including 3 cases with measurement of blood concentration, no noteworthy side effects were observed.

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1) Serum and urinary levels of bacampicillin (BAPC) and ampicillin (ABPC) administered orally before lunchat dose of 500 mg in a cross-over experiment, were determined in a healthy volunteer.
The maximum serum level of BAPC was 5.1μg/ml in 2 hours and that of ABPC, 2.0μg/ml in 4 hours after administration.
The maximum urinary level of BAPC was 1400μg/ml in 0-2 hours and that of ABPC, 750μg/ml in 2-4 hours. The urinary recovery rate of BAPC was 25.0% and that of ABPC, 22.4% during 6 hours administration.
2) Thirty-nine cases with urogenital tract infections were treated with BAPC 750-1000 mg per day orally. The criteria recomended by UTI Drug Evaluation Committee in Japan was applied for clinical evaluation of BAPC. Excellent or good effects were obtained in 13 cases of 25 cases. Fourteen cases were dropped out.
3) Side effects were observed in 4 cases of 39 cases: one was epigastric discomfort, two, skin eruption and the other one, paresthesia of right arm, precordial oppression and slight face edema. BAPC administration was discontinued in 3 cases of them.
Laboratory examinations were done in 27 cases of this series, and a slight elevation of Al-p was observed in only one case.

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Bacampicillin was administered to 9 cases of acute simple pyelonephritis and 25 cases of chronic complicated pyelonephritis. and the effects were examined. The results were as follows:
1) Regarding the therapeutic effect, the effective result was obtained in 6 cases (67%) of 9 of acute simple pyelonephrits and in 11 cases (46%) of 23 of chronic complicated pyelonephritis.
2) Side effects observed were eruption (one case) and gastrointestinal disturbances (2 cases). The administration was discountinued in the latter two cases.

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Twenty-eight out-patients suffering from simple and complicated cystitis were treated with bacampicillin. Bacampicillin was administered orally at the dosage of 750mg or 1500mg for 7 days.
Of 18 patients with acute and chronic simple cystitis, clinical responses were excellent in 9, good in 4, fair in one, poor in 4. Of 10 patients with complicated chronic cystitis, excellent in 3, good in 3, fair in one, poor in 3.
Efficacy rates were 67.9% on all patients, 72.2% of 18 patients with simple cystitis and 60.0% of 10 patients with complicated cystitis.
Out of 28 strains, 16 strains (57.1%) were eradicated, 3 strains (10.7%) were decreased, 4 strains (14.3%) were unchanged and 5 strains (17, 9%) were colonizated.
As for side effect, anorexia was observed in 3 patients and drug eruption in one patient.

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1) Bacampicillin was administered to 20 out-patients who visited Department of Urology of Kyushu University Hospital and Fukuoka University Hospital from october 1976 to september 1977 and diagnosed as urinary tract infections.
2) Bacampicillin was orally administered at a dose of 250 mg (1g daily) 4 times, namely before meals and at bedtime. The duration of treatment was 3 to 7 days for acute simple urinary tract infections and 5 to 14 days for chronic complicated urinary tract infections.
3) In 15 cases of acute simple urinary tract infactions, 2 cases were excluded because there were no bacteria in the urinary tract, 12 cases of excellent result and one case of poor result were obtained, showing 92% of the rate of excellent result. In 5 cases of chronic complicated urinary tract infections, one case of excellent result and 4 cases of poor result were obtained, showing 25% of the rate of excellent result. As a whole, there observed 13 excellent cases and 5 poor cases, the rate of excellent result being 72%.
4) Bacteriologically, 13 strains of 18 disappeared and 5 strains remained. This finding well accorded with the results of ampicillin sensitivity and clinical effects.
5) Clinical laboratory tests of peripheral blood revealed no remarkable changes by the administration of the drug.

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1) Clinical efficacy of bacampicillin was evaluated among 14 patients with urinary tract infections. Simple urinary tract infections were 6 cases (Three cases of acute cystitis, 2 cases of chronic cystitis and one case of chronic pyelonephritis). Complicated urinary tract infections were 8 cases (Seven cases of chronic pyelonephritis and one case of chronic cystitis).
One gram of bacampicillin was given per os every day for 7 days.
2) Of 6 cases with simple urinary tract infections, clinical responses to therapy were excellent in 3 cases, good in 2 and poor in one.
Of 8 cases with complicated urinary tract infections, clinical responses to therapy were excellent in one case, good in 3 and poor in 4.
3) No serious side effect of bacampicillin was observed in this series.

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MIC of bacampicillin against 100 strains of E. coli isolated from patients with urinary tract infections were measured. Sensitivity distribution demonstrated two peaks at 25 μg/ml (27%) and higher than 100 μg/ml (39%) with inoculum size of 10⁸/ml. Sensitivity of 41 strains (41%) ranged lower than 0.2μg/ml but 19 trains were found to be resistant with inoculum size of 10⁶ /ml. Bacampicillin was thought to be two to three times resistant than ABPC to E. coli isolated from urinary tract infections. Serum level of bacampicillin after oral administration of 500 mg reached at peak of 4.6μg/ml after 30 minutes in fasting group and 4.2 μg/ml after two hours in non-fasting group.
Urinary recovery rate of the drug up to 6 hours was estimated at 14.5%, while 11.4% in non-fasting group.
Bacampicillin was given to 26 cases of urinary tract infections; 16 cases of acute simple cystitis, 9 cases of chronic complicated cystitis and a case of chronic pyelonephritis. Chemotherapeutic efficacies were evaluated according to the criteria made by UTI committee in Japan in 1977. Overall clinical efficacies were proved in 88.9% of patients with acute simple cystitis, while 60% in patients with chronic urinary tract infections.
No adverse side effect by administration of the drug was noticed.

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To study the efficacy and tolerance of bacampicillin in the treatment of urinary tract infections, a comparative study of bacampicillin (BAPC) and arnpicillin (ABPC) was carried out with patients suffering from acute simple cystitis.
BAPC was administered at a daily dose of 1g or 0.5g and ABPC at a daily dose of 1g.
The results are summarized as follows.
1) The back ground characteristics of three group populations were statistically analyzed in terms of age, body weight, duration of illness, frequency of each symptom, distribution of causative organisms and M. I. C. distribution.
No significant difference was found, indicating that three groups were nearly homogeneous
2) Clinical improvement was judged after three days administration. Patients included in assessment were 98 patients in the BAPC 1g group, 93 in the BAPC 0.5g group and 99 in the ABPC 1g group.
3) The overall clinical effectiveness was judged by the Evaluation Criteria for Urinary Tract Infections.
Excellent resuslts were obtained in 70.4% of patients in the BAPC 1g group, 52.7% in the BAPC 0.5g group and 54.4% in the BAPC 1g group.
The rate of patients who showed excellent response in the BAPC 1g group was significantly higher than those in other groups.
The rate of excellent or good response was 90.8% in the BAPC 1g group, 89.2% in the BAPC 0.5g group and 90.2% in the ABPC 1g group.
No significant difference was found between three groups.
4) Efficacy rating was judged by physicians also. There was no significant difference between three groups.
5) The rate of patients for whom the treatment was judged to be sufficiently satisfactory or satisfactory was 88.8% in the BAPC 1g group, 75.3% in the BAPC 0.5g group and 82.8% in the ABPC 1g group.
Usefulness of the BAPC lg group was significantly higher than that of the BAPC 0.5g group.
6) Ratio of pyuria cleared in the BAPC 1g group was significantly higher than the ratio in the BAPC 0.5g group. There was no significant difference found between three groups as to other clinical parameters such as ratio of pyuria cleared or decreased, ratio of pain on urination resolved or improved and ratio of bacteriuria eliminated or suppressed.
7) Five (3.8%) of 131 patients treated with BAPC 1g and one (0.8%) of 129 patients given BAPC 0.5g complained of side effects, while no patient of the ABPC 1g group had side effect in 131 patinets.
There was a significant difference in the incidence ratio of side effect between the BAPC 1g group and the ABPC 1g group.
Side effects observed during BAPC 1g therapy were four gastro intestinal disorders and one rash.
The formers passed off as treatment continued, whereas the drug was withdrawn for the latter.
One case of numbness of limbs observed during the BAPC 0.5g therapy was discontinued administration.
8) Clinical effectiveness of BAPC against acute simple cystitis may well be ascribed to its good absorption and BAPC may be considered to be a useful drug for treatment of the infection.

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