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Twenty-seven cases were treated with BB-K8, a new derivative of kanamycin acylated with L-(-)- γ-amino-α-hydroxybutyric acid at the C-1 amino group of the 2-deoxystreptamine moiety. The majority of them were acute primary pyoderma and acute secondary pyoderma.
BB-K8 was effective in 23 cases (85.2%) out of 27 cases treated and no side effect was encountered. BB-K8 had antibacterial activity against not only Staphylococcus but also Pseudomonas and Klebsiella.
Thus, BB-K8 was considered to be effective in acute pyodermic condition.

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We determined the antibacterial activity of amikacin against 1,277 strains of pathogenic bacteria isolated from clinical materials during 1974, including beta hemolytic streptococci, pneumococci, enterococci, Staphylococcus aureus, Staph. epidermidis, Escherichia coli, Klebsiella, Enterobacter, Citrobacter, Serratia, Proteus morganii and Pseudomonas aeruginosa, and compared the minimum inhibitory concentration (MIC) of this drug with gentamicin, dibekacin, tobramycin and kanamycin.
1) Antibacterial activity of amikacin against beta hemolytic streptococci, pneumococci and enterococci was as weak as the other four aminoglycosides, but against Staph. aureus, Staph. epidermidis, various groups of Enterobacteriaceae and Pseudomonas aeruginosa showed amikacin the good antibacterial activity as gentamicin, dibekacin and tobramycin, and also showed the good activity against kanamycin resistant strains.
2) Amikacin has the similar antibacterial spectrum as gentamicin, dibekacin or tobramycin, but its antibacterial activity is generally weakest among these four drugs.
3) On many strains tested the cross resistance is observed between amikacin and one of gentamicin, dibekacin and tobramycin, but several strains of Proteus morganii and Pseudomonas aeruginosa which have rather large MIC against gentamicin, dibekacin or tobramycin showed rather small MIC against amikacin.

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Seven strains of Y. enterocolitica, of which 2 strains being resistant to SM, TC and SA, 2 to SM and SA 3 to SM, and 3 strains of Y. pseudotuberculosis resistant to SM have been isolated from men and domestic animals.
Tests were carried out with these 10 isolates for transfer of the drug resistance by bacterial conjugation, and evidence was obtained for transfer of resistance from 1 SM-resistant Y. enterocolitica and 2 Y. pseudotuberculosis strains to the sensitive E. coli K-12. Moreover, secondary transfer of this resistance to sensitive strains of the donor species Y. enterocolitica and Y. pseudotuberculosis was also demonstrated.
The findings indicate the spontaneous occurrence of organisms carrying the resistance transfer factor, R(Sm), among the populations of these two species in the natural environment.

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Since the discovery of cephalothin in 1962, many semi-synthetic cephalosporins have appeared. To choose the most suitable drug for the clinical treatment of infections, the characteristics of these antibiotics must be sufficiently understood.
When cephalosporins which are or will be commercially available are divided into two categories, one consists of cephaloridine, cefazolin and cephalexin which are comparatively stable in the living body; and the other cephalothin, cephaloglycin, cephapirin and cephacetrile which are metabolized into desacetyl compounds with low antibacterial activity.1-2)
In this study, the author compared the absorption, excretion and some other properties of cefazolin and cephalothin,(widely used clinically), and cephapirin (still under study in Japan).

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Experimental tuberculosis in mice infected with streptomycin-resistant Mycobacterium tuberculosis SCHACHT strain was treated with streptomycin or rifampicin alone and in combination with schizophyllan. The histopathological tests of various organs of the treated mice were carried out.
1) In the group of mice treated with streptomycin alone, the moderate focal proliferation of RE cells were seen at the beginning of infection. However, durable activation of RE cells and the prolongation of life-span could not be recognized as compared with control animals.
2) The treatment with streptomycin-schizophyllan combination appeared to be somewhat more effective than schizophyllan alone, the phagocytic capacity being more strongly stimulated.
3) In the group treated with rifampicin alone, the therapeutic effect could be exhibited by the direct antibacterial action of rifampicin, but the activation of RE cells was slight. When rifampicin was discontinued, the growth of tubercle bacilli was rapidly resumed, and the durable therapeutic effect seemed not to be expected. Degeneration of hepatic cells tended to develop.
4) In the group treated with rifampicin-schizophyllan combination, the antibacterial effect of rifampicin appeared to be potentiated by the strong activation of RE cells by schizophyllan, showing the durable therapeutic effects.

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Absorption, distribution and excretion of ¹⁴C-josamycin (JM) and ¹⁴C-josamycin propionate (JM-P) were studied in rats by measuring both antibacterial activity and radioactivity.
1. In antibacterial activity, plasma and tissue concentrations of JM-P showed a similar tendency to those of JM. Those concentrations of JM reached a peak at 1 hour after administration with a subsequent rapid decrease, while the peak level of JM-P appeared 2-4 hours after administration and then fell down very slowly.
2. In radioactivity, oral administration of JM-P rapidly produced a very high plasma and tissue concentrations which were in lung, liver, kidney and spleen more than twice those of JM. These results showed that when given orally, JM-P is well absorbed with distributions at high concentrations especially in lung, liver, kidney and spleen.
3. The ratios of bioactivity/radioactivity in JM administration were the highest in lung and the lowest in liver at 1 hour after. But those of JM-P were generally much lower than those of JM because of higher distribution of JM-P radioactivity into tissues.
4. Four days after oral administration of JM and JM-P, 23.1% and 21.8% of the given radioactivity were recovered respectively from urine. However, the antibacterial activities recovered were 0.40% for JM and 0.65% for JM-P.
5. Biliary recoveries of JM and JM-P were 17.2% and 12.1% of administered radioactivity 2 days after oral administration. On the other hand, 0.47% of JM and 0.17% of JM-P were excreted into bile as antibacterial activity.
These results showed that JM and JM-P were excreted into rat urine and bile as some metabolites with less biological activity.
6. The amounts of JM and JM-P recovered from feces were 75.7% and 60.2%, respectively, of the orally given radioactivity. The amount of radioactivity recovered from expiration air was about 1% of either orally given JM or JM-P.

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Purulent meningitis in patients admitted to the pediatric department of Kyoto University Hospital and affiliated institutions from 1951 through 1973 were studied with emphasis on the kinds of the causative organisms and the susceptibility of these organisms to antibiotics. The findings in this study have served to help select antibiotics most likely to be effective against this isease.
The overall incidence of purulent meningitis was 0.68%. This figure decreased little throughout the period.
As for the frequency of causative organisms, Neisseria meningitidis led the list, and Diplococcus pneumoniae ranked just behind. Haemophilus influenzae was rare. The frequency of N. meningitidis, however, decreased sharply in spite of the essentially unchanged overall incidence of this disease.
The probable reason for the poor prognosis of this disease in spite of the remarkable strides in chemotherapy is the decreased frequency of N. meningitidis and the inversely increased organisms that are resistant to usual chemotherapy.
The therapeutic effectiveness of cefazolin against this disease was studied in 15 children including eight newborns and four infants. The daily per kg bodyweight dose was 50 mg or less in four, 50-100 mg in five, and more than 100 mg in the remaining six. The route of administration was either intramuscular or intravenous. No deaths occurred. The rate of effectiveness was as high as 80%. Residual symptoms were recorded in six and, in as many as five of them, the cause was attributable to the delayed detection of the disease.
Neither side effects nor aberrent laboratory findings attributable to large doses of cefazolin were recorded. Diffusibility of cefazolin into the CSF was studied in nine subjects. The CSF concentra-tion of this antibiotic was shown to be somewhat lower than that of ampicillin or cephaloridine and to account on an average for 13% of the mean peak serum level. This relatively low diffusibility will be offset by its high serum concentration and safe large-dose therapy.
These findings have clearly shown that the therapeutic effectiveness of cefazolin is as high as that of ampicillin, and that this excellent effectiveness holds true even when the causative organism happens to be Escherichia coli, Klebsiella, etc. that are resistant to ampicillin. The authors have furthermore scrutinized much literature on the frequency of the causative organisms, emergence of resistant strains, and the diffusibility of antibiotics into the CSF, and arrived at the conclusion that cefazolin is a promising antibiotic of choice for the treatment of purulent meningitis in newborn. The daily dose is preferably 150 mg/kg or more given in three divided intravenous doses. Meanwhile ampicillin proved to be useful as the antibiotic of choice for the treatment of purulent meningitis in infants and children.

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As the results of laboratory and clinical investigation with a new tetracycline derivative, PT-122M (doxycycline) was performed with the results which may lead to the following conclusions.
1) In vitro antibacterial activity: The minimal inhibitory concentration of doxycycline (DOTC) was measured by an agar plate dilution method. The MIC of DOTC against 60 strains of coagulase-positive Staphylococcus aureus isolated from otorrhoea was distributed over a range of 0.2-1.56 mcg/ml and 12.5-50 mcg/ml. Furthermore, Escherichia coli, Proteus mirabilis and Klebsiella pneumoniae was 3.13 to 100 mcg/ml.
2) Concentration in blood: The blood level of DOTC in healthy adults who were given 100 mg of DOTC intravenous reached maximum of 1.97 mcg/ml on the average 15 minutes after injection. Even at 12 hours after intravenous injection clinically effective serum DOTC concentration of 0.47 mcg/ml was still demonstrable.
3) Clinical results: PT-122M (DOTC) was intravenously injected into 30 cases with typical infection in the field of otorhinolaryngology. It was excellent in 15 cases, good in 10 cases, fair in 3 cases, and poor in 2 cases. When the cases in which it was excellent and good were considered together, good results were obtained in 25 cases, a ratio of effectiveness being 83 per cent.
4) Side effect: The comparative examination of hepatic function, electrolyte and auditory acuity before and after injection showed no significant disturbance. No side effect was shown with the intravenous injection.

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[in Japanese]

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[in Japanese]

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[in Japanese]

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When the antibacterial substances of cephalothin and cephapirin in the serum and urine after intramuscular injection were separated and assayed, desacetyl metabolites of both drugs were detected. These tendencies were especially apparent in the tissue concentrations. When both the drugs were given intravenously to healthy volunteers, the amounts of their desacetyl metabolites were not greater in man than in rats.

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It has been found by CAVALLITO (1944) that garlic (Allium sativum L.) has a strong antibacterial activity and the active principle of garlic is named “Allicin” and it has been confirmed by STOLL et al.(1948) that the allicin is derived from the alliin-alliinase system. Nevertheless, one worker in Japan (1951) stands on another view point which the effective component of garlic is some sugarprotein because he could not find alliin in the native garlic. We intend to make sure that the alliin is contained in the native garlic, by using Hitachi Amino acid Analyser with Fraction Collecter and compared with garlic of other countrys' production.
As the result of examinations, we found that the good amounts of alliin is contained in the native garlic also. The contents of alliin in garlic is varied by the species, the cultivation mode, and the district of production.
The form of alliin in the tissue is a free style, and thereupon it is easy to change its chemical conformation by the method of extraction. We compared the relative capacity between 1 allicin unit by KLEIN (1954) and 1 cup unit by SCHMIDT et al.(1947). Furthermore we tested the antibiotic spectrum, using the pure crystallized alliin with the sufficient amount of raw alliinase gained by the isoelectric point precipitation and checked upon wide spectrum for Mycobacterium tuberculosis, Gram-positive and negative bacteria, and some fungi.

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