On a new macrolide antibiotic, SF-837, produced in Japan, several laboratory and clinical investigations were performed, and the following results were obtained.
1. The sensitivities of Staphylococci against SF-837 distributed around 1.6 mcg per ml in MIC value, which were comparable to that of kitasamycin. SF-837 showed excellent antimicrobial activity against Mycoplasma pneumoniae which was equal to that of acetyl-spiramycin.
2. The mode of action of SF-837 was mainly considered to be bacteriostatic.
3. The effect of SF-837 against staphylococcal subcutaneous infection to mice was comparable to that of kitasamycin.
4. Serum protein binding rate of SF-837 using cellophane bag dialysis was relatively low.
5. Adsorption rate of SF-837 to sheep red cells was found to be low.
6. Both of bile and urine level after oral administration of SF-837 to rabbit raised up to about 50 folds of serum in the peak value.
7. The peak value of organ levels of SF-837 administered orally to mice ranked in order of lung, spleen, kidney, serum and liver, while from bowel contents considerable high value of SF-837 was detected.
8. The reduction of activity of SF-837 by mixing with homogenate of each mice organ was in high grade, especially remained only 7% in the liver.
9. SF-837 was administered to 10 patients with various infectious diseases. In a case of scarlet fever, no good response was obtained, but SF-837 was judged as effective in 6 of other 9 cases.

抄録全体を表示

We studied on the antimicrobial activities of SF-837, a new macrolide antibiotic, comparing with leucomycin, josamycin, erythromycin and lincomycin.
Newly isolated 412 strains of beta-streptococci, pneumococci, enterococci, staphylococci, haemophilus bacilli and anaerobes of several genera were tested.
SF-837 showed very strong antimicrobial activity to beta-streptococci, pneumococci and staphylococci, and also relatively strong activity to anaerobes, however 16 percent of staphylococci was highly resistant to this drug. Sixty-four percent of enterococci was resistant and haemophilus bacilli including H. influenzae, H. parainfluenzae and H. parahaemolyticus were relatively resistant.
SF-837 has rather similar antimicrobial activity as leucomycin and josamycin.

抄録全体を表示

The bacteriological evaluation was made on SF-837, a new macrolide antibiotic developed by Research Laboratories of Meiji Seika Company, and it was proved that this substance shows almost the same antibacterial spectrum, sensitivity distribution of clinically isolated strains, cross resistance between macrolide resistant strains, effects of pH, human serum, and inoculum size on antibacterial activity as control drugs leucomycin and josamycin, as well as bactericidal effect, in vitro resistantization and cross resistance between artificial resistant strains.
As to the treatment effect for mice experimental infections due to Staphylococcus and Pneumococcus, however, SF-837 was a little inferior to usual macrolide antibiotics. The difference between in vitro effect and in vivo effect of SF-837, should be investigated further pursueing the examinations on absorption, distribution, excretion and drug metabolism in mice.

抄録全体を表示

Some pharmacological actions of SF-837, a new macrolide antibiotic, were investigated.
The spontaneous contractile force of the isolated heart of the frog and atrium of the guinea-pig was stimulated with SF-837 at concentrations of 10^-3g/ml and 2×10^-4g/ml, respectively, however, the action of SF-837 at a concentration of 5×10-4 g/ml on the isolated atrium of guinea-pig was almost antagonized by propranolol at a concentration of 5×10^-6 g/ml.
Tachycardia took place when given intravenously at the dose of 10 mg/kg on the rabbit, however, the positive chronotropic action which appeared at the dose of 20 mg/kg was almost antagonized by the pretreatment with 0.2 mg/kg of propranolol.
The spontaneous movement of the isolated intestine of the rabbit was slightly inhibited at a concentration of 10^-3 g/ml, while no effect was found on the isolated guinea-pig intestine at a concentration of 5x10^-4 g/ml. SF-837 did not influence the action of adrenaline and acetylcholine on the isolated intestine of the rabbit and guinea-pig. However, the actions of histamine and barium chloride on the isolated intestine of the guinea-pig were slightly antagonized by SF-837 at the concentration of 10^-4 g/ml.
The perfusion experiment with SF-837 using the isolated rabbit ear caused an increase in the perfusion flow at a concentration of 10^-3 g/ml. An increase in capillary permeability was observed with 0.1 ml of SF-837 injected intracutaneously to the rabbit at the dose of 1, 000 mcg.
SF-837 given intravenously at a dose of 10 mg/kg caused the fall of blood pressure in the pentobarbital anesthetized rabbit, and the acceleration of respiration was also observed at a dose of 5 mg/kg. However, the fall in blood pressure and acceleration of respiration were moderately antagonized by pretreatment with 2 mg/kg of atropine or vagotomy.

抄録全体を表示

The comparison was made on the antibacterial activity of SF-837 and other macrolide antibiotics against 96 strains of Staphylococcus aureus isolated clinically, as well as the cross resistance was investigated.
The MIC of SF-837 was distributed among 0.8-3.1 mcg/ml, and the peak was recognized at 1.5 mcg/ml. Fourteen strains showed an MIC even at >100 mcg/ml. The MIC of SF-837 was almost the same as that of JM (josamycin) or LM (leucomycin).
The cross resistance was investigated between SF-837 and LM, EM (erythromycin), MJ and Acetyl-SPM (acetyl-spiramycin) respectively. The results obtained demonstrated that a correlation exists between SF-837 and each other drug. The resistant strains of >100 mcg/ml were noticed at the ratio of 14-15% with each antibiotic.

抄録全体を表示

The antimicrobial activities of SF-837, newly developed at the Meiji Seika Kaisha, Ltd., were studied in vitro and in vivo. The results obtained are summarized as follows.
1. The antimicrobial activities of SF-837 against 15 strains of stock culture were equal to those of leucomycin.
2. The minimum inhibitory concentrations of SF-837 were ranged from 0.39 to 3.12 mcg/ml against Staphylococci isolated from patients, and more than 50 mcg/ml against all strains of Shigella.
3. The numbers of survived bacilli were counted in nutrient agar containing different concentrations of the drugs. As the results, the antimicrobial effects of SF-837 were equal to those of leucomycin against Staphylococcus, Streptococcus and Diplococcus.
4. The effects of treatment with SF-837 on experimentally infected mice were examined. The treatments with SF-837 were effective against Staphylococcus, Streptococcus and Diplococcus infections.

抄録全体を表示

The laboratory investigation on a new macrolide antibiotic - mydecamycin was carried out as follows :
1) The result of sensitivity test with 59 strains of Staphylococcus aureus using plate dilution method was similar to those with kitasamycin and maridomycin.
2) In tissue distribution study of the rats and those with fatty liver pretreated by carbon tetrachloride, similar results were obtained and high tissue level was shown in the lung but not in the liver.
3) Further investigation on tissue level in the liver was carried out, and the results seem to indicate essentially lower liver level of the substance than oleandomycin.
4) In in vitro investigation of metabolism using thin layer chromatography depropionated metabolite of the original substance (Ml) was found following incubation with liver homogenate of rat but not with acetone pretreatment.
Similar results has been obtained from the liver of rat pretreated with carbon tetrachloride.
5) In analysis of human urine using thin layer chromatography, Ml, original substance and other unknown metabolites were detected following oral medication.
Clinical investigation study of 22 cases with infectious disease including 6 cases with pneumonia was carried out.
Sixteen cases responded well to the treatment, 3 failed and 3 were unknown. No serious side effect has been observed.

抄録全体を表示

Medemycin is a new macrolide antibiotic developed in Japan. Clinical effect, antibacterial activity, blood concentration, and concentrations in various organs were studied with this drug. The conclusions are summarized as following :
1. Antibacterial activity
Twenty-five strains out of 50 strains of coagulase-positive Staphylococci derived from lesions, were inhibited the growth by 1.6 mcg/ml or less of medemycin. This result is equivalent to that of leucomycin or josamycin, though it is slightly inferior to that orf erythromycin.
2. Blood concentration
The blood concentration of medemycin attained a peak of 2.18 mcg/ml 1 hour after 1 g was administered once orally, and decreased gradually thereafter. It was undetectable after 6 hours.
The blood levels exhibited some scattering, though the drug was given to all the patients with empty stomach ealry in the morning. This may suggest that there is an individual difference among the drug absorption from the intestine and its metabolism in the body.
3. Concentrations in various organs
The concentrations in various organs attained the highest peak in liver, followed by spleen, lung, serum and kidney in order, when 200 mg/kg of medemycin were administered once orally in rats. This transference in organs demonstrated a similar tendency to that with other macrolide antibiotics.
4. Clinical results
Medemycin was given in 6 cases of acute respiratory tract infection, and an excellent result was obtained except 1 case with tonsillitis.
As to the side effect of the drug, a disorder of digestive tract was observed in 1 case, and no undesirable influence was noticed on peripheral blood, liver and kidney function.

抄録全体を表示

1) Forty-five strains of Staphylococcus aureus cultured from clinical specimens were tested for susceptibility to SF-837 and erythromycin. Most of the strains were inhibited in 0.78 mcg/ml of SF-837 and in 0.20 mcg/ml of erythromycin. However, 4 strains showed more than 100 mcg/ml of MIC to both SF-837 and erythromycin.
2) Blood levels of SF-837 after a single oral administration of 1, 000 mg in healthy volunteers were very low (trace to 0.2 mcg/ml at 2 hours after administration). Urinary excretion rate was 1.22% in mean value of 6 cases during 8 hours after a single oral administration of 1, 000 mg SF-837.
3) Clinical results of SF-837 in 9 cases of respiratory infectious diseases were remarkable (excellent 1, good 8). No side effects were seen in all patients.

抄録全体を表示

The antibacterial activity of SF-837 and its therapeutic evaluation in the infections of each field were investigated, and the following results were obtained.
1. The antibacterial activity of SF-837 was measured on 19 strains of Staphylococcus aureus, 9 strains of Diplococcus and 3 strains of Enterococcus isolated clinically. The MIC was 3.12 mcg/ml in 16 strains out of 19 strains of Staphylococcus, and less than 6.25 mcg/ml in 8 strains out of 9 strains of Diplococcus, while it was more than 100 mcg/ml in 3 strains of Enterococcus.
In comparison with the usual macrolide antibiotics of which the tests were made simultaneously, the MIC of SF-837 showed to be almost the same as that of LM.
2. SF-837 was administered at a daily dose of 6 capsules (containing 200 mg per capsule, a daily dose being 1, 200 mg) to the adults suffering mostly from the infections due to Gram-positive bacteria in each field, and the therapeutic results were obtained as follows.
The antibiotic was effective in 36 cases out of 58 cases in the field of internal medicine, 13 cases out of21 cases in the field of surgery, 13 cases out of 14 cases in the field of orthopedics, and 27 cases out of 33 cases in the field of otorhinolaryngology, effective ratio being thus 60-90%. In contrast to this, the effective ratio was low as 30-50% for the urinary tract infections in the fields of urology and obstetrics and gynecology, that is, effective in 8 cases out of 23 cases and 1 case out of 2 cases respectively. In particular, the antibiotic was ineffective in all 5 cases of gonorrheal urethritis.
3. The side effects of SF-837 were observed in 12 cases among all 151 cases. They consisted of digestive disorders such as anorexia, precordial pain, diarrhea, nausea and vomitting in 9 cases, stomatitis in 1 case, and skin eczema in 2 cases.
The blood picture (erythrocyte-, leukocyte-and hemoglobin-counts) was examined before and after the antibiotic administration, and no abnormality was observed. The hepatic function (GOT, GPT, and alkaline phosphatase) was investigated in 21 cases, and the creatinine in 2 cases as well, and no abnormality was noticed.

抄録全体を表示

SF-837 is a new antibiotic which is primarily active against gram-positive bacteria.
Clinical application was performed to 8 cases with respiratory disease, 1 case with rheumatic fever and 1 case with pyelonephritis. The results were excellent in 8 and ineffective in 2.
No significant side effects were seen at all.

抄録全体を表示

The laboratory and clinical investigations were performed on SF-837, a macrolide antibiotic produced by Streptomyces mycarofaciens nov. sp., to evaluate the usefulness of the antibiotic for the treatment of infection, and the results were obtained as follows :
1) The SF-837 sensitivity was measured on Staphylococci isolated clinically, and it was confirmed that the peak exists at 1.56 mcg/ml, and the resistant strains of more than MIC 100 mcg/ml are quite a few. The antibacterial acitvity of SF-837 against Staphylococci is fairly inferior to that of EM (erythromycin).
2) One g of SF-837 was administered orally once. The blood concentration reached the peak of 1.0-12 mcg/ml after 1-2 hours, exhibiting a considerable individual difference. The recovery ratio of SF-837 in urine was around 3%.
3) SF-837 was administered to 7 cases of respiratory apparatus infection and 1 case of bile duct infection. The results obtained were remarkably effective in 3 cases, effective in 1 case and ineffective in 3 cases for respiratory apparatus infection, while remarkably effective in 1 case of bile duct infection.
No noticeable side effect was observed with SF-837.

抄録全体を表示

Studies were made on SF-837, a new macrolide antibiotic developed in Japan. The results obtained were as follow :
1) The M. I. C. of SF-837 against 58 strains of Staphylococcus aureus isolated from human infectious foci were between 0.2 and 3.1 mcg/ml, except for 9 resistant strains. Although the M. I. C. of erythromycin against the sensitive strains were a little lower than those of SF-837, some of the EM resistant strains (10/19) were found to be sensitive (M. I. C. < 3.1) to SF-837. The M. I. C. distribution of the drug was similar to those of lincomycin, josamycin and leucomycin.
2) The average serum peak level of SF-837 in normal human adults was 0.59 mcg/ml 30 min. after 1, 000 mg single oral daministration of the “coated” sample, and 0.48 mcg/ml for “non-coated” one. The average urinary recovery of the drug in 8 hours was 1.8% for coated sample and 1.6% for non-coated one.
3) Ten patients with various infections (bronchitis 2, bronchopneumonia 3, upper respiratory tract infections 4, and furuncle 1) were treated with SF-837, and satisfactory effects were obtained in eight of them.

抄録全体を表示

1) Assays with a series of 291 gram-positive coccic isolates from various clinical specimens revealed that erythromycin (EM) was the most active against organisms susceptible to macrolides among the isolates and the antibacterial activity of SF-837 against these strains was virtually comparable to that of josamycin (JM) or lincomycin (LcM). Of particular note was the finding obtained with 84 Staphylococcus aureus strains, of which 35 proved resistant to EM; 10 strains among the 35 exhibited significant sensitivity to SF-837 and were demonstrated invariably to have inducible drug resistance, one strain being of Mac. B a nd all the rest of Mac. C, respectively. These strains, furthermore, proved to be notably sensitive to JM and LCM as well.
2) Tissue assays for SF-837 were performed by the cup-plate technique, using Sarcina lutea as reference organism, with various organ and tissue homogenates from rats that had received 200 mg of the drug per kg of body weight by intragastric administration. Peak concentrations in these tissues were produced at 2 hours after administration. The liver displayed the highest concentrations consistently and the lungs showed comparable or slightly lower SF-837 levels, followed, in order, by the kidneys and serum; hence the oral administration yielding high tissue concentrations predominantly in the first two organs.
3) Blood levels and excretions in the urine of SF-837 were determined in a series of healthy adults receiving 600 mg or 1, 000 mg of the drug by oral route. Peak plasma levels were accomplished one hour after administration, and the drug dissipated completely from the circulating plasma within 6 hours post administration. Rate of absorption of the drug from the gastrointestinal tract varied considerably among the individuals, and the average urinary recovery rate was as low as a few per cent in all instanecs.
4) Seven cases of respiratory tract infections were treated with SF-837 and the treatment produced satisfactory therapeutic results in 5 cases. Nausea and vomiting occurred after oral administration of the drug in a case, whereas in the remaining 6 cases, no significant adverse findings were noted in the liver function tests and hematologic and blood chemical as well as physical examinations.
The findings altogether indicate that SF-837 is fairly comparable in pharmacodynamic and clinical characteristics to the previously introduced non-resistance-inducible macrolides.

抄録全体を表示

To ascertain therapeutic effect of SF-837 as compared with erythrocin in Mycoplasma pneumoniae (M. pneumoniae) infection, a study was carried out among children with mycoplasma pneumonia. Serum antibody response to M. pneumoniae in these patients was determined by complement fixation test. One group of the patients was treated with SF-837 and another group with erythrocin. There were no significant differences in the clinical course between these two groups.
Response of M. pneumoniae to various antibiotics was tested in vitro using a standard strain and two isolated strains. At the dilutions tested, erythrocin was the most inhibitory on the growth of these organisms and SF-837 showed nearly the same efficacy.
It has been concluded in the past reports that erythrocin and tetracycline were the drugs of choice for M. pneumoniae infection and it was suggested in the present study that SF-837 should be included among these drugs.

抄録全体を表示

SF-837, a new Japanese macrolide antibiotic, has been used in the field of pediatrics, and some findings obtained will be described in the present report. 1) The MICs were compared among SF-837, JM (Josamycin), CER (Cephaloridine) and CEZ (Cephazoline) on 41 strains of Streptococcus haemolyticus A group isolated clinically. The results revealed that MIC of SF-837 centered at ≤0.19 mcg/ml at the ratio of 73.2%, showing thus almost the same range as that of JM.
2) The absorption and excretion of SF-837 were measured on 6 cases of children. As for the blood. concentration, 600 mg or 1, 000 mg of the antibiotic were administered orally once, and the concent-ration reached the peak (0.58-2.5 mcg/ml) after 3 hours, then it was detectable even after 6 hours. As to the excretion ratio in urine, it was 0.8-4.2% in the cases administered 600 mg, while 2.7-4.5% in the cases administered 1, 000 mg.
The above tendency was almost the same as the absorption and excretion of JM.
3) SF-837 was administered orally at the dose of 600-1, 200 mg per day for 3-25 days to 43 cases of infantile respiratory tract infection, 2 cases of lymphadenitis, 2 cases of abscess and 10 cases of scarlet fever, totalling 57 cases. The treatment results were obtained as remarkably effective in 28 cases, ef-fective in 15 cases and undecided in 14 cases, effective ratio being 75%. The comparison of the effect was made with that of JM on scarlet fever, and yet no difference was observed there between two drugs. The bacteria detected from lesion were Staphylococcus in 5 cases, Streptococcus in 17 cases, Haemophylus in 1 case and mixed in 22 cases. The EM sensitivity tests were performed on these bacteria, and results obtained were mostly +∼+++.
4) No side effect was observed with SF-837 throughout all the cases. The hepato-renal function tests were made before and after the drug administration in 1 case of long period treatment, and no abnormal finding was noticed.

抄録全体を表示

From the laboratory and clinical studies on SF-837 in the pediatric field, the following results were obtained.
1) The minimal growth inhibiting concentration of SF-837 against 25 strains of coagulase positive staphylococci was measured by two fold dilution plate method. 32% of all strains were inhibited in the concentration of less than 0.39 mcg/ml.
2) SF-837 was given a single oral dose of 200-400 mg to 2 children. After administration of 200 mg the detectable blood level was not demonstrated. But the peak blood level (0.9 mcg/ml) was observed at 1 hour after administration of 400 mg. The excretion of SF-837 in the urine after a single oral dosing was not demonstrated.
3) SF-837 was effective in 5 of 7 cases of pediatric bacterial infections. No particular side effects were observed.

抄録全体を表示

The antibacterial tests and the clinical experiments have been carried out with SF-837, a new macrolide antibiotic, and the results were obtained as follows :
1) The MIC of SF-837 was determined against 30 stranis of Coagulase positive Staphylococci isolated clinically, and there observed the distribution of two peaks type, showing 1.56-3.12 mcg/mlin 23 strains and >100 mcg/ ml in 7 strains. The MIC of SF-837 was slightly inferior to that of EM (erythromycin), and yet there encountered a strain which was sensitive to SF-837 though resistant to EM at <100 mcg/ml.
2) The acute infantile infections treated consisted of 8 cases of suppurative tonsillitis, 8 cases, of angina and pharyngitis, 5 cases of neck lymphadenitis, 4 cases of pyodermia, 4 cases of primary atypical pneumonia and 2 cases of bronchitis, totalling 31 cases. They were administered orally SF-837 at the dose of 400, -900 mg/ day (30-40 mg/ kg) for 3-15 days, and the excellent results were obtained as remarkably effective in 7 cases, effective in 20 cases, and ineffective in 4 cases, effective ratio being 87.1%.
3) As for the side effect of SF-837, any abnormality was noticed on hepato-renal functions and blood pictures in 15 cases of which the tests were performed of a certainty before and after SF-837 administration, except that 1 case complained of anorexia.

抄録全体を表示

1. Antibacterial spectrum of SF-837 is quite the same as that of usual macrolide antibiotics. Its antibacterial activity is inferior to that of EM, almost equal to that of LM, JM and LCM, and stronger than that of SPM and A-SPM.
2. SF-837 belongs, as LM and others, to non-inducible type. A few SF-837 sensitive strains are observed among EM resistant Staphylococcus aureus, while all SF-837 resistant Staphylococcus aureus demonstrate EM resistance.
3. Blood concentration, excretion in urine and concentration in organs in rats are low with SF-837 as they are with usual macrolide antibiotics.
4. SF-837 is metabolized and inactivated in living body as it is with usual macrolide antibiotics.. This inactivation is remarkable in serum and liver emulsion in rats, while it is weak in human serum.
5. It is said that SF-837 exists mainly as M₁ in serum and urine, and as M₂ in bile. This was confirmed by a bioautography of rat serum after SF-837 was administered orally, that is, a large antibacterial activity was observed at the part corresponding to M₁.
6. SF-837 was tried clinically on 22 cases of surgical infections, and the results obtained were effective in 15 cases and ineffective in 7 cases, effective ratio being 68.2%. No side effect was noticed with the drug throughout all cases treated.

抄録全体を表示

SF-837, a new macrolide antibiotic, was applied to the surgical infections to investigate the effect of the drug.
1) SF-837 was administered orally for 2-13 days at the dose of 600-1, 800 mg per day to 37 cases consisting of 34 cases to treat the surgical infection and 3 cases to prevent the postoperative wound. infection. The results obtained were remarkably effective in 12 cases, effective in 11 cases and ineffective in 11 cases for the treatment group, while effective in all 3 cases for the prophylaxis group.
The surgical treatment was performed in 22 cases out of 34 cases with the progressive lesions, and it seemed that the treatment would have shortened the recovery days.
2) The MIC of SF-837 was measured on 18 strains derived from lesions consisting of 13 strains of Staphylococcus aureus and 5 strains of Staphylococcus epidermidis. It was confirmed that the MIC was<3.12 mcg/ml in 8 strains out of 13 strains and> 100 mcg/ml in 5 strains for S. aureus, while it was <3.12 mcg/ ml in all 5 strains for S. epidermidis.
The cross resistance was observed between SF-837 and other macrolide antibiotics including EM on SF-837 resistant strains of a grade as>100 mcg/ml.
3) As to the side effect of SF-837, 1 case complained the malaise of gastric region, and another 1 case the persistent vomitting and stomachache.

抄録全体を表示

The results of bacterial and clinical experiments concerning surgical use of SF-837 were summarized as follows :
1) Antibacterial activity
The sensitivity of 23 staphylococcal strains isolated recently from infectious lesions ranged from 6.25 to 0.78 mcg/ml with SF-837.
The resistant Staphylococcus aureus was found in 13% of all strains. The MIC to these strains was more than 10 mcg/ml, and was also more than 100 mcg/ml of EM, LM, OM, and JM.
2) Serum concentration
With a single oral administration in a dose of 400 mg, the serum concentration reached to the maximum level of 0.2 mcg/m1-0.8 mcg/ml at the first 2 hours.
3) Bile concentration
With a single oral administration in a dose of 400 mg, the bile concentration reached to the maximum level of 30 times as serum at the first 2 hours.
4) Clinical evaluation
Of 20 cases of acute soft tissue infection treated with SF-837, 4 cases responded excellently, 11 well, 1 slightly well, 0 poorly and in one the effectiveness remained undecided.
5) Side effect
Tachycardia and vomitting was experienced in 1 of 20 cases, and no change in liver functional test was noticed.

抄録全体を表示

The laboratory and clinical investigations in the field of surgery have been carried out with SF-837, a new macrolide antibiotic.
1) Four hundreds mg of SF-837 were orally administered in one dosis to 3 healthy adults in the fasting states, and the blood level reached the peak (0.76-1.30 mcg/ml) after 1 hour, and it was undetectable 4 hours after the administration. In 1 case, however, the same dosis of the drug was administered orally after meal, and the peak attained after 2 hours, and the level continued even after 4 hours. The urinary excretion of the drug was low as 1.1-2.9% of the administered dosis within 12 hours.
2) The MIC of SF-837 was measured on 27 strains of Staphylococcus aureus isolated from various surgical lesions and it centered around 0.8-1.6 mcg/ml, antibacterial activity being thus almost the same as that of JM. No cross resistance was observed between SF-837 and EM.
3) The clinical results with SF-837 in superficial surgical infections were remarkably effective in 1 case, effective in 8 cases, fairly effective in 1 case, and undeterminable in 2 cases. The comparison was made with leucomycin by means of the double blind test, and the result obtained was almost the same between these two antibiotics.

抄録全体を表示

1) SF-837 was administered orally at the dose of 800-1, 600 mg per day for 3-27 days to 75 cases of surgical infections. The results obtained were remarkably effective in 24 cases, effective in 41 cases, ineffective in 9 cases and undecided in 1 case, effective ratio being thus 87.8%.
2) The causative bacteria were collected from the lesions of 21 cases out of 75 cases, and their sensitivities were measured for various macrolide antibiotics (erythromycin (EM), oleandomycin (OL) and leucomycin (LM)). SF-837 was judged to be clinically effective in all the cases in which high grade or middle grade sensitivities were demonstrated for EM, OL and LM.
3) As to the side effects with SF-837, 5 cases out of 75 cases (6.6%) complained of gastro-intestinal symptoms such as nausea, vomitting and malaise in gastric region.
The hepato-renal functions were examined before and after SF-837 administration in 12 cases, and any abnormal finding was noticed there.

抄録全体を表示

1) The MIC of SF-837 was examined on 23 strains of Staphylococcus aureus derived from lesions. The peak showed 3.13 mcg/ml, and there were 2 resistant strains as >100 mcg/ml. In comparsion with the MIC of other drugs of the same family, that of SF-837 was nearly equal to those of LM and JM, though it was slightly inferior to that of EM. The cross resistance was observed among macrolide drugs, and there encountered SF-837 sensitive strains in a part of EM resistant bacteria.
2) SF-837 was administered orally once at a dose of 400 mg to 2 healthy adults, and the blood concentration showed the peak of 1.9-0.85 mcg/ml after 2 hours, and higher blood levels were maintained even after 6 hours. As for the rate of excretion in urine, 3.15-2.73% was recovered within 12 hours.
3) SF-837 was administered orally for 3-8 days ata dose of 1, 200 mg per day to 18 cases of superficial infection, and the results obtained were remarkably effective in 3cases, effective in 6 cases, slightly effective in 7 cases, and ineffective in 2 cases.,
4) As for the side-effect of SF-837, no digestive disorder was experienced as well as eruption, and no abnormal finding was observed throughout the cases of which were performed the tests on hepatic functions, renal functions and hepatologic items.

抄録全体を表示

SF-837 (Mydecamycin), a new antibiotic developed in Japan, has been studied experimentally and clinically in the field of orthopedic infections.
Sixty strains of Staphylococcus aureus isolated from the patients of osteomyelitis, were measured the sensitivities to SF-837, in comparison with those to LM (leucomycin) and EM (erythromycin), by the plate dilution method. Eighty-three percent of the strains tested, was found to have the sensitivities in the range of 0.1 to 50 mcg/ml, and 30 percent to have the M.I.C. (minimum inhibitory concentration) of 1.56 mcg/ml.
Seven cases of chronic osteomyelitis and 2 cases of subcutaneous infection were treated with SF-837. The results obtained were good in 7 cases, fair in 1 case and no effective in 1 case. No side effect was. noticed with SF-837 throughout the cases treated.
It may be expected therefore that the application of a new antibiotic SF-837 to the infections in the field of orthopedic surgery, will bring on the good results similar to those with macrolide antibiotics in common use.

抄録全体を表示

SF-837, a new macrolide antibiotic, was applied to bone and joint infections in the field of orthopaedic surgery, and some findings were obtained as follows :
1) SF-837 was administered orally at the dose of 800-2, 400 mg per day for 4-44 days to 31 foci of 27 cases of bone and joint infections (postoperative infection 25, suppurative arthritis 3, suppurative burstitis 1, hematogenous and suppurative osteomyelitis 2). The results obtained were remarkably effective in 11 foci, effective in 9, fairly effective in 7, and ineffective in 4.
2) Seven strains of Staphylococcus aureus were detected from foci, and all of them exhibited an EM sensitivity (+).
3) No side effect as digestive disturbance was demonstrated with SF-837 throughout all the cases. The hepato-renal function and the hematocyte were examined before and after SF-837 administration, and no abnormal finding was observed except that a positivization of urobilinogen was noticed in 1 case.

抄録全体を表示

SF-837, a new macrolide antibiotic, has been applied clinically to the infections in the orthopedic field, and the findings obtained will be described as follows :
1. The patients treated consisted of 1 case of suppurative osteomyelitis, 6 cases of postoperative septic wound, 1 case of infectious fistula due to suppurative spondylitis, 6 cases of infectious decubitus, each 1 case of BRODIE'S bone abscess and knee joint pain (origin unknown), totalling 16 cases. SF-837 was administered consecutively to the above cases at a daily dose of 1, 200 mg for 14 days, and the result obtained was remarkably effective in 1 case, effective in 7 cases, ineffective in 4 cases, and undecided in 4 cases, effective ratio being thus 75%.
Classifying the clinical results into causative bacteria, a high effective ratio was observed in the infections due to Staphylococcus aureus, this result being almost the same as that with the usual macrolide antibiotics.
2. As for the side effect with SF-837, no remarkable complaint was observed except a nausea in 1 case. The tests were carried out on the hepato-renal functions and the hematologic and biochemical examinations before and after the antibiotic administration, and no remarkable abnormal finding was noticed.

抄録全体を表示

Laboratory and clinical investigations on SF-837, one of the new macrolide agent, were as follows.
The sensitivity distribution of SF-837 against coagulase positive Staphylococci (37 strains) showed from 0.39 mcg/ml to 100 mcg/ml and mainly from 0.78 mcg/ml to 1.56 mcg/ml.
Serum levels after single oral administration of 400 mg were determined using Staph. aureus 209P as the test organism. Peak serum level with this test organism was 1.1 mcg/ml at 2 hours after administration.
Excretion into milk was hardly recognized. Urinary recovery rate was 2.7% for 6 hours. The usefullness of SF-837 in the treatment of vulval abscess, adnexitis, perveoperitonitis, postoperative infection, mastitis and urinary infection was confirmed isolated bacteria from these infectious diseases were Staphylococcus, Streptococcus nonhaemolyticus, Enterococcus, Corynebacterium and anaerobic bacteriae.
Significant side effect was not observed.

抄録全体を表示

We tested the clinical studies on a new macrolide antibiotic SF-837, and obtained following results.
1. SF-837 was administered in the daily dose of 800 mg to 45 cases consisting of cystitis, mastitis and intrapelvic infections.
2. Of 45 cases, 28 cases (62.2%) showed good effect.
3. No side effects including hepatic and renal dysfunction were observed.
4. No abnormality was observed except a momentary slight palpitation and distension of the stomach in 2 cases.

抄録全体を表示

SF-837, a new macrolide antibiotic, was applied clinically, and the results obtained are described as follows :
1) The SF-837 sensitivity was measured on 78 strains of Gram-positive bacteria isolated recently from clinical materials. The peak attained at 1.56 mcg/ml, showing almost the same tendency as that of leucomycin.
2) SF-837 was administered orally once on an empty stomach at the dose of 400 mg to 6 healthy adults, and the blood concentrations reached the peak (0.7-0.8 mcg/ml) after 2-3 hours, being detected until 4-6 hours later. The excretion ratio of SF-837 in urine was 0.8-1.5% within 6 hours, and this ratio is as low as that with other macrolide drugs.
The transfer into fetus was examined with SF-837. Although the transfer into amniotic fluid was not clear, there observed the transfer into umbilical cord blood and milk.
3) SF-837 was adminstered at the dose of 1, 600 mg per day for 4-12 days to 17 cases of the infections in the field of obstetrics and gynecology. The results obtained were remarkably effective in 2 cases, effective in 7 cases, fairly effective in 2 cases, ineffective in 4 cases and undecided in 2 cases, effective ratio being thus 64.7%.
4) No noticeable side effect was observed with SF-837.

抄録全体を表示

SF-837, a new macrolide antibiotic, was administered orally at the dose of 600-1, 200 mg per day to 27 cases of suppurative dermal infection. The results were obtained as follows : remarkably effective in 4 cases, effective in 17 cases, and ineffective in 6 cases.
The antibiotic was effective in all 12 cases of impetigo, while it was mostly ineffective in multiple folliculitis.
The MIC of SF-837 was measured on 52 strains of Staphylococcus isolated from lesion and 2 strains of 209P strain and it centered mostly to 1.56 mcg / ml, whereas 6 strains demontsrated>100 mcg / ml.

抄録全体を表示

The blood concentration and the excretion ratio in urine were measured with SF-837, a new macrolide antibiotic, and the antibiotic was applied to the cases of urinary tract infections due to Grampositive bacteria and some Gram-negative bacteria to investigate the effects.
1) One g of SF-837 was administered orally to 3 healthy adults, and the blood concentration reached the peak (0.5-2.5 mcg/ml) after 1 hour, and it was unmeasured after 6 hours.
One g of SF-837 was administered orally to 2 healthy adults, and the drug was recovered at the cumulative excretion ratio in urine of 1.6-2.1% within 8 hours.
2) SF-837 was administered orally at the dose of 400-1, 200 mg/day for 3-19 days to 22 cases of simple urinary tract infection and 8 cases of complicated urinary tract infection, totalling 30 cases. The results obtained were remarkably effective in 12 cases, effective in 8 cases, and ineffective in 10 cases, effective ratio being thus 76.6%.
The clinical effects of the antibiotic were investigated by classifying by causative bacteria. The effective ratio was 86.7% in 15 cases of Staphylococcal infection, 50% in 5 cases of the infection due to Streptococcus faecalis, and 44.4% in 9 cases of Gonococcal urethritis. The effect of SF-837 may be expected thus especially for the urinary tract infection due to Staphylococcus.
No remarkable side effect was observed with the antibiotic throughout all the cases.

抄録全体を表示

Fundamental and clinical evaluations of the new macrolide family antibiotic SF-837 were performed with the results which may lead to the following conclusions :
1) In vitro antibacterial activity : The minimum inhibitory concentration of SF-837 was measured by an agar plate dilution method. SF-837 inhibited the growth of 80 strains of coagulase positive Staphylococcus aureus at≤ 0.19-≥100 mcg/ml. SF-837 also demonstrated antibacterial effect against Streptococcus hemolyticus and Diplococcus pneumoniae isolated from clinical specimens.
2) Concentration in blood : The maximal level reached 1.63 mcg/ml on the average one hour after administration of 1, 000 mg in healthy adults, and the level was still 0.47 mcg/ml in four hour after the administration.
3) Concentration in tissues : SF-837 activity was demonstrable in concentration of 0.3 mcg/ml in a human platine tonsilla specimen respectively at one hour after administration of 1, 000 mg. Corresponding plasma levels of SF-837 were 1.9 mcg/ml respectively.
4) Clinical evaluation : In the clinical tests of SF-837 in otorhinolaryngological infection, it was found that the results were good to excellent response in as many as 33 of 37 cases (89 per cent) by administration.
5) Side effect : The comparative examination of liver, electrocyte and audiogram before and after administration showed no significant disturbances, and SF-837 showed no side effect at all in administration.

抄録全体を表示

SF-837, a new macrolide antibiotic, was administered orally at the dose of 400-1, 200 mg/day for 3-35 days to 28 cases of the infections in the field of otorhinolaryngology, and a satisfactory result was obtained as effective in 20 cases, fairly effective in 2 cases and unknown in 2 cases. The bacteria isolated from lesions consisted of 6 Gram-positive bacteria, 2 Gram-negative bacteria, and 8 mixed of Gram-positive and -negative bacteria. The sensitivity measurement of SF-837 revealed that the above bacteria were highly sensitive in 14 strains out of 16 strains.
As for the side effect of SF-837, 1 case complained of a malaise in gastric region during the administration of the antibiotic.

抄録全体を表示

Ophthalmic use of SF-837, a new antibiotic was studied to evaluate their merits. The results obtained were as follows.
1. The sensitivity was measured by the plate dilution method with 30 strains of St. aureus isolated from patients. The MIC of this agent was less than 1.56 mcg/ml in 66.6%.
2. SF-837 was given by a single oral administration dose of 200 mg/kg in rabbits. The maximum blood levels were 1.3 mcg/ml in 30 minutes after oral administration and the maximum aqueous levels were 0.7 mcg/ml after 2 hours of administration.
3. Maximum blood levels in adults in 400 mg total doses were 0.6 mcg/ml 3 hours after oral administration and remained at a measurable level as long as 4 hours.
4. The therapeutic effects in 21 patients with external ocular infection were as follows, very effective in 10 patients and effective in 5 patients, the total effectiveness rate being 71.4%. One patient complained of epigastric pain.

抄録全体を表示

The bacteriological and clinical experiments for ophthalmic use of SF-837 were performed. These results were summarized as follows.
1) Minimum inhibitory concentrations of SF-837 for various organisms concerning in ocular infection were 0.19 mcg/ml for Koch-Weeks bacillus, 0.78 mcg/ml for Morax-Axenfeld diplobacillus, 0.19-3.13 mcg/ml for Pneumococcus, 0.39-1.56 mcg/ml for C. diphtheriae, 1.56 mcg/ml for Gonococcus, 0.39-6.25 mcg/ml for Streptococcus, 0.78-3.13 mcg/ml for Staphylococcus and> 100 mcg/ml for Ps. aeruginosa.
2) The sensitivity for 100 strains of Staphylococcus aureus was in the range of 0.78-≥100 mcg/ml of SF-837 and 51 strains were in 1.56 mcg/ml.
Cross resistance was recognized between SF-837 and the other macrolide drugs : EM, OL, SPM and JM.
3) The peak of blood level (0.3-0.5 mcg/ml) was attained at 2 hours after oral administration of 400 mg SF-837 in a single dose.
4) The ocular penetration of SF-837 into the rabbit eye was investigated.
After oral administration of 200 mg/kg, the concentrations into the tissue of outer parts of the eye were observed relatively higher while in the inner parts of the eye almost not recognized. After instillation of 1% SF-837 solution, the tissue level was proved merely in the outer parts of the eye. After subconjunctival injection of 5 mg/0.5 ml, the remarkable penetration was shown in the outer parts of the eye and also good penetration in the inner parts of the eye.
5) Various ocular suppurative diseases, such as external hordeolum, internal hordeolum, acute and chronic dacryocystitis, episcleritis purulenta, corneal ulcer and foreign body of the cornea, were well cured by SF-837 treatment, oral administration of 1 or 2 capsules in a dose 4 times a day.
6) Side effects : A patient complained of gastrointestinal disorder, but any other serious one was not noticed.

抄録全体を表示

The authors studied experimental and clinical use of SF-837, and obtained followings :
1) In experimental osteitis of jaw in rats affected with Staphylococcus aureus 209P, SF-837 was remarkably effective.
2) In clinical use, good results were obtained in the treatment of cases such as osteitis of jaw. Side effects were obtained in 2 cases out of 24 cases.

抄録全体を表示

1. The MIC of SF-837 was measured on 36 strains of pathogenic Staphylococcus derived from oral cavity, and it was confirmed that the majority centered around 0.78-1.56 mcg/ml, besides 4 strains were resistant as ≥100 mcg/ml.
In comparison with leucomycin of which the same measurement was made simultaneously, SF-837 showed almost the same MIC as that of leucomycin, and the cross resistance was observed between two antibiotics.
2. SF-837 was administered orally at the dose of 600-1, 600 mg/day for 3-10 days to 26 cases of the infections of maxillary region, and the results obtained were remarkably effective in 13 cases, effective in 7 cases, fairly effective in 5 cases and ineffective in 1 case, effective ratio being thus 76.9%.
3. As to the side effect due to the administration of SF-837, 5 cases out of 26 cases exhibited the slight digestive disorders such as anorexia and stomachache.

抄録全体を表示