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[in Japanese]

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[in Japanese]

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[in Japanese]

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[in Japanese]

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[in Japanese]

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[in Japanese]

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The blood concentration and urinary excretion of OE-7 (erythromycin stearate capsules) and control drug were investigated in 6 volunteers having gastroptosis.
OE-7, newly arranged capsules containing erythromycin stearate, was investigated and obtained the results of high blood concentration by oral administration.
To confirm the above, we measured blood concentration and urinary excretion of OE-7 comparing with ordinary erythromycin stearate capsules in 6 volunteers having gastroptosis.
The peaks of blood concentration were noted at 3 hours after administration in 6 volunteers uniformly. The mean maximum blood concentration of OE-7 was 1.17 mcg/ml which was significantly higher than ordinary erythromycin stearate capsules.
In time course of mean blood concentration, the blood concentration levels of OE-7 were higher than those of control erythromycin stearate capsules at any measurement. Effective blood levels were continuously high in OE-7.
Urinary excretion of OE-7 reached to the maximum from 4 to 6 hours after administration which was also higher than control erythromycin stearate.
Clinical efficacy of OE-7 was investigated in 28 cases in acute respiratory infection. The results noted were excellent in 5 cases (17.9%), good in 16 cases (57.1%), no change in 6 cases (21.4%), and undetermined in 1 case (3.6%).
There were 5 cases of slight gastro-intestinal discomfort as the side effects.
As the conclusion, OE-7 revealed good bioavailability and seemed to be useful antibiotic for acute respiratory infections.

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Growth inhibitory effect of combined treatment of tetracycline (TC) and oleandomycin (OM), at a ratio of 2:1, on certain species of pathoge nic bacteria including drug-resistant ones was examined. By the crossed paper strip method, synergistic effects were demonstrated against 9 of the 16 strains of Staphylococcus aureus, and all of the 5 strains of Escherichia coli studied. Antagonism was observed with none of these strains and with 2 strains of Streptococcus pyogenes and 2 strains of Streptococcus pneumoniae tested in the present experiments. The MICs determined by the agar dilution method, also gave similar results, although synergism was not conclusively demonstrated by this method. With representative strains of S. aureus, synergism was evidenced by quantitative measurement of growth inhibition. In some strains, 1.0μg of one drug perml of medium inhibited the induction of resistance to the second drug. Such a small dose of one drug also inhibited the development of a mutant resistant to the second drug. These inhibitory actions were thought to be one of the important factors causing the synergistic effect of TC and OM on drug resistant bacteria.

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The combination effect of tetracycline (TC) and oleandomycin (OM) on acute infection of mice with four strains of Staphylococcus aureus including TC or OM resistant ones was examined by the quantitative determination of protective potencies of single and combined drugs. The grade of synergism was expressed by the synergistic ratio (SR), a ratio of experimentally determined potency of the combined drug over a hypothetical potency in which additive effect of the both drugs is assumed. With 3 out of the 4 strains of S. aureus synergism between TC and OM or triacetyloleandomycin (TAO) was demonstrated by the determination of the 50% effective dose and by statistical examination of the SR. The grade of synergistic protection by these drugs varied with the strains infected and it did not depend upon the sensitivity to antibiotics or grade of synergism in vitro. There was no synergistic enhancement of acute toxic action in the combined administration of TC and OM to mice.

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Bonnamycin which is a new tetracycline group antibiotic isolated from a variant strain of Streptomyces rimosus and is identified chemically as doxycycline was investigated, comparing with tetracycline. The results are as follows:
(1) In in vitro studies of anti-bacterial spectrum, doxycycline is widely effective against standard strains kept in our department.
(2) The distribution of susceptibility of 75 Staphylococci, 62 Salmonella and 64 Shigella strains isolated from clinical materials was similar to that of tetracycline.
(3) As to the therapeutic experiment in acute infection of Klebsiella pneumoniae in mice, the drugs were equally effective and the ED₅₀ was both 70.8 mcg.
(4) Doxycycline administrated orally or subcutaneously in rats was distributed in kidneys, livers, lungs and spleens at relatively high concentration among organs.

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