It was already reported by KUWAHARA and his coworkers (1963) that the multiple drug-resistance of Shigella fiexneri can be transmitted to sensitive strains of V. cholerae and El Tor vibrio through conjugation, and that the recipients generally lost the transmitted resistance after repeated transfers on drug-free nutrient media. Later, ABE et al. (1966) confirmed that such transmission process also tak e place between Shigella or E. coil and NAG vibrio or Aeromonas. In Japan, there are many cases of food-poisoning due to V. parahaemolyticus, which are detected frequently in the near-sea water of Japan and South East Asia. Although none of the isolates of V. parahaemolyticus are resistant to chloramphenicol and tetracycline, there may give rise to the possibility of the emergence of multiple-resistant strains. This report deals chiefly with the experimental results of the transmission of R factor from resistant E. coil to sensitive strains of V. parahaemolyticus and V. alginolyticus. Two strains of multiple-resistant E. coli (SA. SM. CM. TC) were chosen as the donors of R factor, and 20 strains of V. parahaemolyticus and 5 strains of V. alginolyticus were tested for their competence to serve as recipients of R factor. Using TCBS agar containing 5 mcg/ml of CM as selective plate. A few strains out of the test strains of V. parahaemolyticus were found competent recipient of R factor according to the donor used, and among 5 strains of V. alginolyticus only one strain received R factor, when the strain 60-R₄, was used as the donor. Many of the recipient colonies of V. p arahaemolyticus were resistant to CM and TC at the level of 5-10 mcg/ml, considerably lower than the resistances of the donors; whereas recipient colonies of V. alginolyticus were highly resistant to CM, although TC resistance was generally low. Retransmission from resistantized vibrio to sensitive strains of E. coli, Shigella flexneri or Sal. typhi were also accomplished, and the recipients were highly resistant to SM, CM and TC, quite same level as the original donor. As in the case s of other species of Vibrio, resistantized V. parahaemotyticus and V. alginolyticus lost their resistances after 3 successive transfers on drug-free nutrient agar.

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Thirteen patients with postoperative wound in urological field were treated with local administration of polymyxin B. Among 13 cases, including 2 cases of partial cystectomy, 1 total cystectomy, 1 bilateral ureterocutaneostomy, 3 pyelolithotomy, 2 ureterolithotomy, 1 fisterectomy of urethral fistula, 1 radical operation of urinary incontinence and 1 prostatectomy, good effect and no effect were seen in 9 and 4 cases, making 69. 2% effectiveness showing a distinguished result. No noticeable side effect was observed in all.

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The indwelling urethral catheter has been subjected to much criticism during recent years. Previous studies have shown that almost patients treated in this method acquire significant bacteriuria with the potential risks of cystitis, pyelonephritis, and life-threatening gram negative rod bacteremia. However the catheterization is indispensable for urological management, and some methods to minimize these complications should be undertaken. The present study was done for 34 catheterized patients, using a closed irrigation system and saline solution containing polymyxin B in concentration of 100 mcg/ ml.
Patients irrigated with saline were the controls. In the course of 10 days irrigation, 75% of the patients irrigated with drug solution, on the other hand 38% of the cases with saline showed sterile urine after removal of the catheters. In longer term managemen t, positive urine culture was in increasing frequency, i. e. 71% in drug irrigation cases and 83% in saline irrigations.

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This study was undertaken to evaluate clinically thiophenicol (methylsulphenidol) in several urinary tract infections because of its high renal excretion. Absorption and urinary excretion of thiophenicol (TP) was examined on 3 male volunteers in comparison with chloramphenicol (CP), when 500 mg of TP or CP was orally administered as a single dosis. Urinary concentration of TP reached a peak at 3 hours after administration in three times of CP and recovery in urine was 35. 4% in average. In addition, excretion of this drug more prolonged than that of CP. Determination of minimal inhibitory concentrations to multiresistant gram-negative isolates from our cases of urinary tract infections revealed all the strains being more resistant than 62. 5 mcg/ml using plate dilution method, and showed this drug was not so effective as CP in vitro.
While clinical data given from 32 cases of several urinary tract infections showed its effectiveness in 78. 1% during 3 to 7 days treatment in 2 g daily dosis. This dyscrepancy between the clinical and laboratory results may be explained by high urinary concentration of this drug, and suggest that drug level in urine is not insignificant in management of urinary tract infection.
Subjective untoward effects were rather mild but reversible bone marrow suppression was noticed in 2 cases after 7 days administration.

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1) Ampicillin was administered to 9 cases with upper urinary infections, 11 with urinary infections complicated with uterine cancer and 25 with lower urinary infections resistant to other antibiotics in a daily dose of 2 g for 1 to 2 weeks and effective in 6 and 17 cases respectively. Ampicillin was inefective bacause of alternation of causative organisms in upper urinary infections, disordered local factors on host in urinary infections complicated with uterine cancer, and also resistance of organisms in lower urinary infections resistant to other antibiotics.
Treatment with ampicillin was effective whe n the MIC of causative organisms was 12. 5 mcg/ml or less.
2) Sensitivity distribution curve of E. coli isolated from focuses has been almost constant since 1963 when ampicillin began to be used.
3) Disappearance of organis ms does not always reflect clinical effect in chemotherapy of infections of urinary tracts.
An intima te interrelation was found between clinical effect and changes of number of leucocytes in urinary sediment.

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In our clinic, ampicillin was administered to patients with various urinary infections and observations were performed on clinical effects as well as basic experiments. The results of this study are summarized as follows.
1) Blood leve l and urinary exeretion rate. After oral administration of 0. 5 g of the drug, the blood level reached the maximum level at 3 rd hour and the effective level retained for almost 8 hours. The urinary excretion rate after oral administration of O. 5 g of the drug was 36. 7%.
2) Of 26 cases given ampicillin, remarkable effect, good effect and no effect were observed in 7, 11 and 4 cases respectively, making 81. 54% of effectiveness rate which shows a distinguished effect of ampicillin.
3) No noticeable side effects were observed.

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A clinical study on ampicillin was made in surgical field. The results were obtained as follows. Ampicillin attained the maximum blood level at 1 to 2 hours after oral administration, and was highly excreted in urine and exudate exhibiting a potent antibacterial activity against E. coil and a part of Proteus, the causative organisms. Below the levels of 1. 6 mcg/ml, ampicillin suppressed only 22. 2% of the strains of pathogenic Staphylococci. Ampicillin was effective against infections mainly induced by gram-negative bacilli in surgical field, the efficacy 62%. As regards the side effects, transient chill and fever were observed in 2 patients who received intramuscular injection.

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A clinical and experimental evaluation was made on penbritin (ampicillin). The results obtained were as followings.
1) In rat, ampicillin is well absorbed and achieves high tissue level after both oral and intramuscular administration.
2) Bile level of ampicillin in rabbit is higher than that of PC-G, and exceeds blood level of ampicillin.
3) In man, ampicillin levels in bile, gallbladder wall and blood are excellent.
4) Ampicillin was administered to 13 patients with cholecystitis, chol elithiasis or pyelonephritis and showed excellent therapeutic effect.

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This report relates to some fundamental evaluation of aminobenzyl penicillin (AB-PC) in particular reference to the urinary tract infection.
(1) Absorption and excretion:
The urinary concentration of the drug is relatively high. When administered orally in 500 mg or intramuscularly in a single dosage of 250 mg the urinary recovery at 6 hours was approximately 68%.
The organ concentration of the drug was determined in rats and was found to be highest in the kidneys followed by the liver, blood, lungs and spleen in order, indicative of its specific affinity to the kidneys.
(2) Sensitivity of AB-PC to E. coli:
The sensitivity of the drug to E. coli isolated from the patients with urinary tract infection lies in the range of 1. 6 to 100 mcg/ml with its peak sensitivity at 3. 2 to 6. 3 mcg/ml.
(3) Clinical data:
(a) The effect in urinary tract infections;
The effect of AB-PC was studied in 11 patie n ts with acute or chronic pyelonephritis in whom 6 improved remarkably, 2 mild to moderately and the rest little or none.
(b) The effect of AB-PC to E. coli pyelonephritis:
When administered to E. coli pyelonephritis, the req u ired period for the disappearance of bacteriuria was not significantly different from that of NA, CER, and KM, however the period for impra ving the urinary sediments was difinitely shorter in AB-PC as compared to NA but slower than that by KM and CER.

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1) The minimum inhibitory concentrations (MIC) were determined against those strains isolated lately from patients. The MIC of ampicillin against Staphylococci, E. coil, Klebsiella and Shigella was 6. 2 5 m cg/ml or less for 15 and 12. 5 for 4 out of 21 strains, 12. 5 m cg/ml for 10 out of 12, 6. 2 5 for 1 out of 10, 1. 6 to 6. 25 for all 10 strains respectively, the remaining showing the MIC of 25 mcg/ml or more. Ampicillin was not active against Pseudomonas.
2) With oral 250 mg or 500 mg, blood leve l reached the maximum of 1. 26 mcg/ml or 2. 87 respectively at 2 hours. With 6 hourly oral 250 mg, the B-bile level of 3. 3 mcg/ml was 6 times as high as blood level determined simultaneously. Urinary excretion rate after oral 250 mg or 500 mg was 59. 9% or 50. 9% for 6 hours respectively.
3) Among 11 cases given ampicillin, including 8 of biliary, 2 urinary and 1 respiratory infections, the drug was effective in 3 both clinically and bacteriologically, in 6 only clinically and non-effective in 2.

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Anti-tumor activities of novel compounds, N, N′-diethylene-N″- (5-methyl-1, 3, 4-thiadiazole-2-y1) phosphoramide (5 261) and Bis-(β-ethylenimino propionyl) piperazine (S 509) were investigated.
These compounds having ethyl enimino radicals as functional groups showed poten t anti-tumor activities against Ehrlich carcima, Sarcoma 180 in mice and Yoshida sarcoma, AH 130 hepatoma in rats, and their therapeutic indices against mouse tumors were greater than that of TESPA. Remarkable activities on mouse ascitic tumor of S 261 were found to be associated with direct marked cytotoxic activities on the tumor cells.

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Serum level, tissue distribution and urinary excretion of N, N′-diethylene-N″- (5-methyl 1, 3, 4thiadiazole-2-y1) phosphoramide (S 261) were investigated. When S 261 was administered intraperitoneally in doses of 100 mg/kg on rats, peak serum levels one hour after administration were 60 μg. / ml, and in the first three hours about 60% of the total amounts of S 261 administered were excreted in urine with unchanged form, indicating the rapid absorption and the subsequent excretion. In rabbits bearing Brown-Pearce carcinoma received 50 mg/kg of S261 intrave nously, the drug concentrations in both the kidney and tumor after one hour exceeded serum levels. These drug levels in blood and tissues of rabbits disappeared completely without any positive reaction with NBP test five hours after drug administration. It was suggested that S 261 had a remarkable tumor affinity.

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Three kinds of new compounds, decamethylenebis- (4-amino-5, 6, 7, 8-tetrahydroquinaldinium) salts were investigated on their antimicrobial activities in vitro and in vivo, and the results were obtained as follows
1. THQ acetate and chloride possessed a powerful antimicrobial activity against Gram-positive and Gram-negative bacteria and fungi.
2. The bactericidal activity of THQ acetate against Staphylococcus aureus was more powerful than that of dequadin and THQ chloride.
3. The antimicrobial acti vities of THQ salts increased in proportion to the tendency of alkalinity of pH.
4. The decrease of antimicrobial activities of THQ salts was almost none by addition of serum.
5. The antimicrobial activities of THQ salts in vivo were further discussed.

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Thirty cases were treated with aminobenzyl penicillin (Pentrex) in our clinic and the hospitals related with our department.
The effect of th e drug was confirmed in various infections such as dysentery, diphtheria, respiratory infections and urinary infections due to gram-positive or gram-negative organisms.
Favourable results were obtained in most cases excellent effect was ob tained in 2 cases, good effect 19 cases, moderate effect 4 cases, no effect 4 cases and other one case out of 30 cases.
In this clinical experiments, several advantages of aminobenzyl penicillin were observed and especially less side effect is considered as the excellent one.

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The Japan Society of Chemotherapy has carried out controlled trials on reproducibility of bacterial drug-sensitivity values by both the plate dilution method andthe disk method, which were repeated twice during a period from summer of 1966 to summer of 1967.
In the first examinations, the laboratories belonging to Th e Japan Society of Chemotherapy were each supplied with 4 test strains, and requested to investigate their sensitivities to antibiotics by the plate dilution method and the disk method (with mono- or three-concentration disks). Six antibiotics (penicillinG, dihydrostreptomycin, kanamycin, erythromycin, chloramphenicol and tetracycline) were used in these investigations. In the plate dilution method, sensitivities to streptomycin and kanamycin showed a trend of greater fluctuation of the results than those to the other 4 drugs. When the reading of the results was made by 4 grades with the disk method (_??_, _??_, + and -), no difference was observed in the reproducibility of the results between the two disk methods. However, the sensitivity values in terms of MIC obtained by the standard method with the mono-concentration disk, which were computed, with reference to the standard curve, from the length of diameter of the inhibitory zone around the used disk, showed still greater fluctuation than those obtained by the plate dilution method.
In the second examinations, the laboratories were each supplied with 5 test strains, and requested to investigate only the plate dilution method. In this trial, the experimental conditions such as the media used, the inoculum size and incubation time were indicated in greater detail than in the first trial. The fluctuation in the sensitivity values was smaller as compared with the results of the first trial.
Through these two examinations, it was confirmed that the reproducibility was greater in the case of the highly resistant and the highly sensitive area. The moderately sensitive zone, on the other hand, showed wider fluctuation of the results.
From these results, it was considered of vital necessity for elevating the reproducibility of the sensitivity values that the standard method, which indicates in detail the kinds of used media, inocula sizes and procedures of inoculation, should be established and that all the investigators should use some well-known strains as controls.

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The result of clinicolaboratory and clinical study on acetyl-spiramycin, which is a new derivative of spiramycin, is presented in this paper.
The highest serum concentration o f acetyl-spiramycin was 2. 20 mcg/ml on average one hour after single administration of 250 mg orally in healthy adults, while that of spiramycin was 1. 82 mcgiml on average 4 hours after oral administration of 250 mg.
Minimal inhibitory concentration of acetyl-spiramycin to 238 strains of staphylococcus aureus in surgical fields was tested. 151 Strains out of 238 (63. 4%) were distributed at concentration of 12. 5 mcg/ ml, and 205 strains (86. 1%) were inhibited to growth in concentration less than 12. 5 mcg/ml. On anti-staphylococcal activity of acetyl-spiramycin, it seems to have a cross resistance to spiramycin, leucomycin and oleandomycin.
Oral use of 80 0-1, 600 mg of acetyl-spiramycin daily were tried on 14 cases of surgical infections including 9 cases of staphylococcus aureus infection and 1 case of mixed infection of staphylococcus aureus and a-streptococcus. Good clinical response were observed in 11 cases and 1 of them was excellent.

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We discussed on sensibility, absorption and excretion, concentration in the organs and clinical results of acetylspiramycin.
(1) Sensibility of acetylspiramycin to staphylococci was distributed between 3. 2 and 25 mcg/ml, which does not show significant difference from that of spiramycin.
(2) Blood concentration of acetylspiramycin was kept much higher and longer than that of spiramycin, and its urinary recovery rate was low as compared to that of spiramycin.
(3) Concentration in the organs of rats was' high as compared to that o f spiramycin. Acetylspiramycin showed large amount of transition especially into the kidney, liver and lung.
(4) As to clinical results, acetylspiramycin was effective in 4 out of 5 cases and as to side effects, gastro-intestinal disorder was observed in 1 case.

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Sensitivity of coagulase-positive Staphylococcus isolated from patients to acetyl-spiramycin was examined and compared with that to spiramycin and erythromycin.
Further, absorption and excretion of acetyl-spiramyc in in children were determined by the crossover method, As a result, the peak of the blood concentration of acetyl-spiramycin appeared a little later, but it showed a tendency to present higher value.
Seeing from the clinical result, acetylspiramycin is a substance which is available for infections of adaptation provided that in future, consideration on forms for children will be necessary.

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On a new spiramycin (SPM) derivative, acetyl-spiramycin (AC-SPM), several basic studies were performed in comparison with the parent substance SPM and the following results were obtained.
1. The sensitivity test of Staphylococcus aureus using two-fold dilution plates showed that AC-SPM has lower sensitivity by one plate than SPM in general and there was complete cross resistance between both SPMs.
2. The a bility of adsorption of AC-SPM to red blood corpuscle was as low as SPM. The inactivation of AC-SPM by mouse liver homogenate was less than SPM, while the protein binding rate measured by cellophane bag dialysis was higher in AC-SPM.
3. The organ level following oral administratio n reached to the somewhat higher value in case of SPM in general.

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