The current references written in English concerning effect of prophylactic antibiotics in vaginal and abdominal simple hysterectomy have been reviewed.
Febrile morbidity was evaluated for antibiotic treated and untreated groups.In most studies, the definition of febrile morbidity was a temperature of 38°Cor greater on 2 separate occations excluding the first 24hours after the operation.Fever index in degree hours was also compared between 2 groups in some studies.
Of 30 studies in vaginal hysterectomy reported between 1969 and 1981, 29 showed that antibiotic prophylaxis successfully decreased postoperative febrile morbidity.Of 15 studies in abdominal hysterectomy reported between 1972 and 1982, 12 showed the significant decrease of febrile morbidity in the treated group.However, pelvic infection in only 2 and wound infection in 5 were reduced.The length of hospital stay was found to be shorter for the treated group in vaginal and abdominal hysterectomy. The beneficial effect of prophylactic antibiotics in abdominal hysterectomy were less compelling than those for vaginal hysterectomy.
Although recent studies indicated that a short perioperative use of antibiotics or even a single dose was effective as long-term prophylaxis, the most effective method and duration awaits further evaluation.

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To confirm efficacy and safety of fosfomysin sodium (FOM-Na) in the field of obstetrics and gynecology, hemodynamics and pelvic transferrence were analyzed using so-called three-compartment model in adult women treated with the drug at a dose of 2g either as an one shot injection or an intravenous infusion over 1 hour. Following results were obtained.
1.Hemodynamics in these patients were similar to those obtained in healthy adult males, although there was a tendency that levels reached were lower and elimination was more rapid in cases of genital cancer.
2.As to drug concentration of dead cavity fluid, T_max appeared at 1.75 hours after completion of administration irrespective of administration methods, with C_maxbeing 67.8μg/ml and 50.5μg/ml of intravenous injection and intravenous infusion, respectively.Thereafter, there was no difference between two administration methods.
3.Uterine tissue concentration reached to its T_max.at 15 to 30 minutes after intravenous injection and within 10 minutes after completion of intravenous infusion, C_max being higher than 90μg/g.Even at 5 hours, 15 to 25μg/g of the drug was detected.
From these results and from susceptibilities of clinical isolates to the drug, it was considered that FOM-Na at a dose level of 2g is highly effective in the treatment of various infections in the field of obstetrics and gynecology including intrapelvic infections, uterine infections and adnexitis.

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Micronornicin (MCR, Sagamicin®), a new derivative of aminoglycoside, was used in 9 patients with postoperative infection mainly caused by Gram-negative bacilli.
A dose of 60-120mg was intramuscularly administered continuously twice a day for 3-21 days.
The therapeutic results were excellent in 2, good in 3, fair in 1 and poor in 2 cases.
The assesment was impossible in 1 patient.
The effective rate was 62.5%.
No side effects were encountered in any cases.

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In vitro synergistic activities of new aminoglycoside antibiotic micronomicin (MCR, Sagamicin®) combined with oxacephem antibiotic latamoxef (LMOX, Siomarin®) were investigated.These antibiotics exhibited synergistic activities at FIC index lower than 0.5 against 20.8%, 32.7% and 1.9% of clinical isolates of Pseudomonas aeruginosa (48 strains), Serratia marcescens (52 strains) and Escherichia coli (54 strains), respectively.Partial synergism (0.5<FIC index<1) was observed in 79.2%, 55.8% and 31.5% of the same microorganisms, too.Each bacteriostatic concentrations of MCR and LMOX showed synergistically bactericidal effects when the drugs were administered at the same time against P.aeruginosa BMH No.1, S.marcescens F-3283 and E.coliGN2411-5.

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A new antibiotic drug of cephalosporin, with marked resistance to β-lactarnase, cefmenoxime (CMX) for parenteral use was used in 14 patients with acute or subacute cholecystitis and cholangitis.CMX was given byintramuscular or intravenous drip infusion at a daily dose of 500mg to 2g.Clinical responce was excellentin 3 cases, good in 10 cases, fair in 1 case and poor in none.Any clinical adverse effect was not recognized.
CMX in a dose of 500mg was given by intramuscular administration before the operation to 8 patients, and in 7 cases CMX in a dose of 1g was given by intravenous administration before or during the operation.Tissue specimens of different sites were taken from the removed organs.The materials of A-bile and B-bile were subsequently taken at intervals.
CMX concentrations in the A-bile increased after intramuscular injection and reached to peak 2 hours, then declined very slowly.CMX concentrations in the A-bile after intravenous administration reached topeak at 1 hour, then declined very slowly, too.CMX concentration in the B-bile reached to high level of the concentration comparative quickly after intramuscular and intravenous administration, and it was thought to be excreted through the gallbladder wall.CMX concentration in the gallbladder wall was directly proportional to the degree of pathological changes of the inflammation.
On the CMX concentration in patients with cholecystitis and cholangitis, the concentration in A-bile, Bbile and gallbladder wall were observed higher than the MIC of CMX for pathogenic Gram-negative bacilli.
CMX therefore will be a very useful drug when used for chemotherapy of the infectious diseases of the biliary tract.

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Three kinds of H-ThrAcyl-Lys-Lys-Giu-OH were synthesized to investigate the relationship between the chemical structure and the antibacterial activities by acylation of the corresponding tetrapeptides.Acyl chlorides of (+)-6-Methyloctanoic acid (a component of colistin) and two kinds of other organic acid were employed as acylating agents.It was proved that one of three, H-Thr (+)-6-Methyloctanoyl-Lys-Lys-Glu-OH shows antibacterial activity against four kinds of Gram-negative bacteria and against Gram-positive bacteria, but that the other only have weak antibacterial activity.

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In vitro susceptibilities of 1478 strains of various pathogens isolated from clinical materials in 1981 to 23 antibiotics were studied using Showa disk diffusion test. Prevalence of bacterial resistance to antibiotics was evaluated. New cephem antibiotics such as cefmetazole (CMZ), cefoxitin (CFX) and cefotiam (CTM) had no increased activity over old cephalosporins such as cephalothin (CET) and cefazolin (CEZ) against Grampositive cocci. However, ll the new ones showed greater activities, broadened spectra, and/or both against Gram-negative bacilli, each offering unique advantages.
S.aureus: Susceptible strains (MICs less than 15μg/ml) to CET, CEZ, CTM, CFX and CMZ were 95%, 69%, 92%, 88% and 99%, respectively. Prevalence of resistance to CEZ was greater than to other cephalosporins, showing bimodal distribution of MICs.This may be due to more use of this drug in the past. Sensitive strains to benzylpenicillin (PCG), ampicillin (ABPC), sulbenicillin (SBPC) and piperacillin (PIPC) were 22 to 63%. A striking bimodal distribution of MICs of these penicillins was characteristic. Sensitive strains to various aminoglycosides and tetracyclines were 52-93% and 97-100%, respectively.
S.pyogenes: 83-100% of strains were susceptible to various penicillins, CET and CEZ, whereas susceptible strains to CTM, CFX and CMZ were 66-90%.
S.pneumoniae: Almost all strains (99%) were susceptible to PCG at the level less than 0.2 units/ml (0.12tug/ml).All strains were susceptible to various penicillins, cephalosporins, and cephamycins studied atthe level less than 3μg/ml.
E.coli, K.pneumoniae and Proteus spp.: CTM, CFX and CMZ showed greater activity than CET and CEZ. Susceptible strains to the former antibiotics at the level less than 15μg/ml were 93-94%, 82-95%, and 63-90%, respectively.Those to CET and CEZ were 61-83%, 85-92% and 53-58%, respectively.Among these cephalosporins, CMZ and CTM were the most effective, showing the least prevalence of resistance to these pathogens.
H.influenzae: Susceptible strains (MICs less than 15μg/ml) to ABPC, PIPC, CTM, CFX and CMZ were 80%, 81%, 84%, 55% and 71%, respectively.The majority of resistant strains to these β-lactam antibiotics were sensitive to chloramphenicol, minocycline, doxycycline and erythromycin.
P.aeruginosa, S.marcescens, E.aerogenes, Citrobacter and Achromobacter: CTM, CMZ and CFX werenot effective against these pathogens.

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This experiment was carried out, in order to investigate the effect of antibiotics and natural mycotoxin on the hematopoietic stem cells at the normal and inflammatory condition.Adjuvant-treated rats (Aj-rats) are considered as a model of human rheumatoid arthritis.We measured the CFU-C and CFU-E of bone marrow of normal and Aj-rats which were injected with large (1.0g/kg×3) and small doses (0.5g/kg×3) of ampicillin (ABPC), cefazolin (CEZ), chloramphenicol (CP) and fusarenon-X (F-X).
In Aj-rats the number of CFU-C was 1.5 times higher and CFU-E 60% less than normal.Injection of large doses of ABPC enhanced markedly the numbers of CFU-C in Aj-rats and suppressed slightly CFU-E in normal rats.Large doses of CEZ inclined to increase CFU-C and decreased CFU-E in normal and Aj-rats. Injection of small doses of CP tended to increase CFU-C and to decrease CFU-E, and large doses of CP to suppress both CFU-C and CFU-E levels in normal or Aj-rats.F-X, natural mycotoxin suppressed markedly both CFU-C and CFU-E levels of normal rats, and slightly the CFU-E in Aj-rats.
These results suggest that one should pay attention to the fact that some doses of antibiotics or natural mycotoxin might be harmful on the bone marrow hematopoietic stem cells.

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Ceftizoxime (CZX) and latamoxef (LMOX), new synthetic cephems, are stable against various types ofbeta-lactamase and highly active against Gram-negative rods, such as H.influenzae, Serratia, Enterobacter and indole (+) Proteus. In this study, we evaluated clinical effects of CZX and LMOX in the clinical management of infections in acute leukemia. Sixteen episodes of infections were treated with CZX or LMOX. Four causative organisms, P. aeruginosa, S. faecalis, K. pneumoniae and A. faecalis, were identified in 2 episodes of infections.
Clinical effects were recognized at 75% in 8 episodes treated with CZX and at 71% in 7 episodes treated with LMOX, respectively. The transient elevation of GOT, GPT and Al-P, recognized in several cases.
In conclusion, the clinical effects of CZX and LMOX are promised in clinical management of infections in acute leukemia.

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Cefotaxime (CTX) was used for 129 cases in respiratory tract and other infections;57 cases of pneumonia, 20 cases of bronchopneumonia, 20 cases of acute bronchitis, 14 cases of chronic bronchitis, 7 cases of acute exacerbation of bronchiectasia or pulmonary emphysema, 4 cases of suppurative diseases of the lung, 1 case of pyothorax, 1 case of retropharyngeal abscess, 3 cases of pleurisy and 1 case of urinary tract infection.(A case was excepted on clinical evaluation.)
CTX was administered by intravenous injection or drip infusion at a daily dose ranging from 0.5 to 8g, for a term of 2 to 61 days.The total dose patients received ranged from 3 to 226g. The results obtained were as follows.
1. Clinical effects;excellent in 45 cases, good in 63 cases, fair in 9 cases, poor in 7 cases and unevaluable in 4 cases.The efficacy rate was 87.1% (108/124).
2. Bacteriological effects; eliminated in 30 cases, decreased in 8 cases, unchanged in 2 cases and replaced in 1 case.The elimination rate was 75.6% (31/41).
3. Side effects and abnormal laboratory findings;general itching, fatigue in lower extremities and albuminuria in 1 case each, and anemia in 2 cases.Increased number of eosinophiles and elevated GOT in 1 case each, elevated GOT and GPT in 3 cases and elevated GOT, GPT and Al-P in 2 cases.
These symptoms or abnormal laboratory findings disappeared after the discontinuation or termination of CTX therapy.
In view of the above, CTX may be considered to be a clinically useful antibiotic against respiratory tract infections.

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Susceptibility of 124 strains of 28 bacterial species or subspecies to cefuroxime were determined by the 2-fold agar dilution method in parallel with the diameter of inhibition zone by the single-disc method.
The experiments demonstrated significant correlation between MIC by the dilution method and diameter of inhibition zone in each of conventional assay of the over-night (about 16 hours) incubation, delayed assay (about 24 hours incubation), and rapid assay (after 3-4 or 5 6 hours incubation), thus confirming applicability of the single-disc assay for cefuroxime.
Analysis of the data obtained by using cefuroxime disc containing 30μg revealed the primary regression equation to be: D (diameter, mm) =28.2-0.1log MIC (μg/ml) in conventional assay, D=33.1-3.2log MIC (μg/ml) in delayed assay, D=23.9-8.2log MIC (μg/ml) in 5-6 hours rapid assay, and D=20.0-6.5log MIC (μg/ml) in 3-4 hours rapid assay, respectively.
The range of variations in MICs estimated from the diameter of inhibition zone by the disc test was then calculated in comparison with that in MIC determined by the 2-fold dilution assay, as reference for the experimental errors which may be involved in the estimation of MIC of cefuroxime by the single-disc assay.

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KS-R1, a new suppository of ampicillin (ABPC) sodium, was rectally administered to study its absorption, excretion and distribution in mice, rats and rabbits.
1. Concentrations of ABPC in plasma when 12.5 and 25.0mg/kg of KS-R1 were rectally administered to experimental animals reached the peak levels rapidly.The values were 7.3 and 13.9μg/ml in mice, 7.7 and 15.9μg/ml in rats, and 14.1 and 35.3μg/ml in rabbits, respectively.All of these values were about 3.5 times as high as those attained by oral administration of the same doses.
2. Concentrations of ABPC in tissues when 25.0mg/kg of KS-R1 was rectally administered to rats reached the peak level rapidly, as in the concentration in plasma.The concentrations distributed into various tissues were found as follows;liver=kakidney>spleen>heart>lung.
3. Urinary recoveries of ABPC after rectal administration of 12.5 and 25.0mg/kg were 23.4 and 28.4% (0-12 hours) in rats while 79.4 and 75.4% (0-6 hours) in rabbits, respectively.When 25.0mg/kg of KS-R1 was administered to rats, 10.7% of the dose was excreted into bile during 6 hours after administration.
4. The relative bioavailabilities of KS-R1, calculated on the basis of AUC and urinary recovery after parenteral administration of ABPC sodium, were 81.0 to 87.5% in mice, 37.6 to 45.9% in rats and 75.6 to 101% in rabbits, which were 1.5 to 2.8 times higher than those of ABPC orally administered.

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KS-R1, a new suppository of ampicillin (ABPC) sodium, was compared with the widely used oral ABPC and parenteral ABPC sodium in terms of absorption and excretion in mature and infant Beagle dogs.
1. Plasma levels of ABPC in mature dogs when administered rectally with 12.5 and 25.0mg/kg of KS-R1 reached the respective peaks of 8.0 and 13.5μg/ml in 10 to 20 minutes.Thereafter, the plasma levels declined with biological half-lives of 0.72 and 0.93 hours, respectively.During the first 6 hours after administration of 12.5mg/kg, 14.3% of the dose was excreted in urine.The relative bioavailability of KS-R1, calculated on the basis of AUC and urinary recovery after intramuscular administration of ABPC sodium, was 23.1% to 28.9%, compared with 31.1% to 50.2% in the case of oral ABPC.
2. Plasma levels of ABPC in infant dogs rectally administered with 12.5mg/kg of KS-R1 reached 11.9μg/ml in 10 minutes, and then declined with biological half-life of 1.24 hours.During the first 6 hours after rectal administration, 31.9% of the dose was recovered in the urine.The relative bioavailability of KS-R1 in infant dogs was 53.8% to 58.0%, which was better than that of mature dogs and was equal to that of oral ABPC.
3. In the case of multiple doses of KS-R1 to mature dogs, no remarkable difference was found in concentration in plasma, and no accumulation of ABPC was demonstrated.Macroscopically, no remarkable abnormality was found at all around the sites of continuous administration.

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KS-R1 is a new rectal preparation of ampicillin (ABPC) sodium.Changes of cecal microflora, changes of cecal weight and ABPC concentrations in the cecum after rectal administration of KS-R1 to mice were compared with those after oral and subcutaneous administration of ABPC.
1. When KS-RI was administered to mice by 25.0 mg/kg 3 times a day for 10 days continuously, a little changes were observed in the number of Enterobacteriaceae, Staphylococcus and Lactobacillus in the cecum.However, at the fifth day after completing the rectal administrations, normal level of microflora was gained.This change ofmicroflora closely resemble those in case when ABPC sodium was administered subcutaneously.On the other hand, when ABPC was administered orally, changes of microflora were large, i.e.the number of Enterobacteriaceae and Streptococcus increased remarkably, the number of Fusobacterium increased and the number of Staphylococcus and Bacteroides decreased. Recovery of normal level of microflora was late.
2. The cecal weight did not show changes but the increase observed in the case when ABPC was orally administered. This increase was due to the increase of moisture in the cecum.
3. The concentrations of ABPC in the cecum when administered by 25.0 mg/kg were in the order of oral administration>rectal administration (KS-R1) >subcutaneous administration.The highest concentrations were respectively 219.6, 54.1 and 5.1μg/g.Changes of microflora in the cecum was great in proportion to theconcentrations of ABPC.
From the foregoing results, it was suggested that the effect of rectally administered KS-R1 on the microflora in the cecum was considerably lower as compared with the case when administered orally, like in thecase when ABPC was administered subcutaneously.

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In experimental infections induced with S.aureus, S.pneumoniae, E.coli, K.pneumoniae, P.mirabilis and H.influenzae in mice, the therapeutic efficacies of ampicillin (ABPC) after its rectal administration werecompared with those obtained after its oral and subcutaneous administration, and the following results were obtained.
Generally, in experimental intraperitoneal infections of mice, the effects of ABPC after rectal administration were inferior to those after subcutaneous administration and superior to those after oral administration.In experimentally induced intraperitoneal and urinary tract infection of E.coli KC-14, similar results were obtained. The plasma levels were reflected as the difference between various administration in the therapeutic efficacies observed with ABPC.

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KS-R1, a new rectal suppository of ampicillin (ABPC) sodium, was compared with oral and parenteral ABPC in terms of absorption and excretion in childish patients and healthy adult male volunteers.In addition, the irritation of KS-R1 to the rectum was studied.
1. sight healthy adult male volunteers received 250mg (potency) of KS-R1 rectally and 125mg of ABPC intravenously in a cross-over study.Then, 4 of them were given intramuscularly 250mg of ABPC, and 3 of the remaining 4 volunteers were given 250mg of ABPC orally.
The rectal administration of 250mg of KS-R1 resulted in a mean peak ABPC plasma level (C_max) of 2.6 mcg/ml at 30 minutes, and then ABPC levels declined with biological half-life (T2/1) of 0.55 hour.The peak time (T_max) of occurence after rectal dose of KS-R1 was earlier than that after oral dose of AMC, and was equal to that after intramuscular dose of ABPC.C_max after rectal dose of KS-R1 was equal to that after the oral dose, and was about 40% of the value attained with the intramuscular dose.
Urinary recovery of ABPC during 6 hours after rectal dose of KS-R1 was 24.0%, compared with 34.0% for the oral dose, 59.6% for the intramuscular dose and 61.4% for the intravenous dose.The relative bioavailability of KS-R1, calculated on the basis of urinary recovery after intravenous administration of ABPC, was about 40%.
2. When KS-R1 (250mg) was given to 2 adult volunteers 3 times daily for 5days, no remarkable difference was found in plasma concentration and urinary recovery of ABPC.The pharmacokinetic parameters following the last administration were similar to those following a single administration of KS-R1.
3. KS-R1, oral ABPC and intravenous ABPC were administered at the dose of 125 mg (potency) to 5, 4 and 3 children and at the dose of 250mg (potency) to 5, 3 and 3 children, respectively.Peak plasma level (C_max) of ABPC after rectal administration of 125mg and 250mg of KS-R1 was reached in 15 minutes, indicating 4.8 and 7.1 mcg/ml, respectively.Peak time (T_max) of ABPC after the rectal doses of KS-R1 was about 2 hours earlier than that after oral doses of ABPC.C_max after KS-R1 was 3-4 times as high as that after the oral doses.Area under the curve (AUC) with KS-R1 was 1.380-1.55 times greater than that of oral ABPC, and about 24% of the values obtained with intravenous doses of ABPC.Urinary recoveries of ABPC rectal doses of KS-R1 were 30.4 to 45.6%, compared with 29.2 to 30.8% for the oral doses and 61.1 to 76.1% for the intravenous doses. The relative bioavailability of KS-R1, calculated on the basis of urinary recovery after intravenous administration of ABPC, was 40 to 75%.
4. When erythromycin (EM) suppository was administered to 3 children, the peak EM concentration in serum was 0.404mcg/ml at 1 hour, and the urinary recovery up to 6 hours was 0.4%.These values were remarkably lower than those obtained with the administration of KS-R1.
5. As to the irritation to the rectum after rectal administration of 125mg and 250mg KS-R1, no complaint of defecation feeling or pain was made in children.Eight adults administered KS-R1 rectally had slight feeling of foreign immediately after insertion and very slight feeling of defecation.Among the adults, 2 had slight feeling of burn, 1 had very slight feeling of burn, and each one adult had severe, moderate, and slight pain respectively.
From these facts, KS-R1 was considered to be a useful rectal suppository for the pediatric patients with bacterial infections.

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A comparative well-controlled study was performed to evaluate the efficacy and tolerability of ampicillin rectal suppository (KS-R1) compared with those of oral form of ampicillin (ABPC) against acute respiratory tract Infections in pediatric field.
KS-R1 at the dose of 125mg×4/day of ABPC in potency, or the oral form at the same dosage, was given to 166 cases of patients with acute respiratory tract infection due to Streptococcus pyogenes, Streptococcus pneumoniaeor Haemophilus influenzae for 7 days, as a rule.
The clinical efficacy rates evaluated in 151 cases (KS-R1 group in 77 cases, oral group in 74 cases) on standard criteria of committee members were 88.3% for the KS-R1 group and 86.5% for the oral group, respectively.There was no significant difference between 2 groups
Evaluation by stratification according to the diagnosis showed that the efficacy rates for the KS-R1 group and for the oral group were 87.5% and 85.0% against pharyngitis, 90.5% and 90.0% against tonsillitis and 84.2% and 78.6% against bronchitis, respectively.None of them showed significant difference between 2 groups.
The bacteriological effect was evaluated in 55 cases (KS-R1 group in 33 cases, oral group in 22 cases), and disappearance rate was 93.9% for the KS-R1 group and 95.5% for the oral group, showing no significant difference.
Side effect including subjective and objective symptoms were strictly evaluated in 163 cases (KS-R1 group in 83 cases, oral group in 80 cases), but the incidence rate which was 22.9% for the KS-R1 group and 23.8% for the oral group showed no significant difference.
The above results indicate that against acute respiratory tract infections in pediatric field, KS-R1 possesses clinical efficacy and safety similar to the oral form of ABPC, and that it is a useful suppository.

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A comparative well-controlled study was performed to evaluate the efficacy and tolerability of KS-R1 (ampicillin (ABPC) rectal suppository) compared with those of intravenous injection of ABPC against acute bacterial pneumonia caused by ABPC-sensitive bacteria, such as Streptococcus pyogenes, Streptococcus pneumoniaeand Haemophilus influenzae in pediatric field.
KS-R1 at the dose of 250mg×4/day of ABPC in potency, or the intravenous injection at the dose of 125mg×4/day of ABPC in potency, was given to 68 cases of patients with bacterial pneumonia, aged between 10 months and 8 years and 2 months, for 7 days, as a rule.
The clinical efficacy rates evaluated in 61 cases (KS-R1 group in 31 cases, intravenous group in 30 cases) on standard criteria of committee members were 93.5% for the KS-R1 group and 83.3% for the intravenous group, respectively.There was no significant difference between 2 groups.
Evaluation by stratification according to the age showed that KS-R1 was significantly superior, the rate being 90.5% among the children from 1 year to 3 years in the KS-R1 group and 61.5% in the intravenous group.
The bacteriological effect was evaluated in 16 cases (KS-R1 group in 7 cases, intravenous group in 9 cases), the disappearance rate was 100% for the KS-R1 group and 88.9% for the intravenous group, without significant difference.
With regard to side effects, 66 cases (KS-R1 group in 35 cases, intravenous group in 31 cases) were strictly evaluated in relation to subjective and objective symptoms.As a result, no significant difference was noted between 2 groups in the incidence rate which was 17.1% for the KS-R1 group and 9.7% for the intravenous group.
The above results indicate that against acute bacterial pneumonia in pediatric field, the KS-R1 at the dose of 250mg×4/day of ABPC in potency possesses clinical efficacy and safety similar to the intravenous injection at the dose of 125mg×4/day of ABPC in potency, and that it is a useful suppository.

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1.Blood levels of ampicillin (ABPC) were measured in 10 childrish patients with heart disease after the rectal administration of KS-R1 at doses of 125mg and 250mg.
Average blood levels of ABPC at 15, 30 minutes, 1, 2 hours and 4 hours after the administration of KS-R 1 were 6.8, 6.9, 3.1, 1.1 mcg/ml and 0.1mcg/ml with half-life of 0.64 hours in patients of age from 1 year to 4 years 7months old (dose level 8.9 13.9mg/kg, average 10.5mg/kg), and 5.2, 6.1, 3.4, 1.0mcg/ml and 0.1mcg/ml with half-life of 0.65 hours in patients of age from 7 years 10 months to 10 years 7 months old (dose level 8.3-13.9mg/kg, average 9.8mg/kg), respectively.
2.Clinical effective rate (excellent and good) was 87% in 55 childish patients with infections.
3.Bacteriologically, 13 strains (74%) out of 18 strains which were isolated from the patients were eradicated.
4.No severe side effects were observed.Diarrhea was observed in 3 cases.

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1. Absorption of ampicillin (ABPC) suppository (KS-R 1) was good with the peak level of ABPC at 15 minutes and the continuous high level for 1 hour by the administration of about 10-18mg/kg.About 40% of active form of administered ABPC was excreted into urine within 6 hours.
2. KS-R1 at the dose of about 20-40mg/kg/day divided into 3-4 times was very effective against acute respiratory tract infection by the treatment for 3 5 days.The effective rate was 94% in 35 cases.
3. By the administration of KS-R1, group A Streptococcus, S.pneumoniae and H.influenzae were eradicated.
4. After the insertion of KS-R1, weak diarrhea and the discharge of KS-R1 were observed in 2 cases and 3 cases, respectively.
5. It was concluded that KS-R1 is very useful drug for the treatment of infections by ABPC sensitive organisms in place of the oral form of ABPC.

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Ampicillin suppository (KS-R1) was given to 67 childish patients with acute febrile upper respiratory infection and 1 patient with urinary tract infection at dose level of 29-63mg/kg/day divided into 3-4.
Twenty-five strains of pathogens were isolated in 23 patients out of 68 before the administration of KS-R1, and 19 strains (76.0%) among them were eradicated by KS-R1. Clinically, all cases were effective.
The clinical efficacy alone was determined in other 44 patients with acute febrile upper respiratory infection and 1 patient with urinary tract infection, and only 3 cases among them showed poor effect with KS-R1 treatment. No side effects were observed.

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Clinical trials of KS-R1 have been carried out on 28 infections in children, including 8 pharyngitises, 11 tonsillitises, a pharyngolaryngobronchitis, 3 lymphadenitises and 5 urinary tract infections.
The following results were obtained.
1. KS-R1 30-50 mg/kg/day, was clinically effective in 27 out of 28 infections.
2. Bacteriologically, the following routine clinical isolates were identified;Enterococci in 1 case, S.viridans 1 case, S.pneumoniae 1 case, S.pyogenes 2 cases, H. parainfluenzae 1 case, E.coli 5 cases and S.aureus+H.influenzae 1 case.
Every isolated organism showed +++ sensitivity to the ABPC sensitivity disc in vitro without only 1 case of E.coli.The organisms were eradicated in 11 patients after the administration of KS-R1.
3. Adverse effects did not occur in any patient without case 25, who complained of pollakiuria.

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Pharmacokinetic and clinical studies of ampicillin suppository (KS-R1) was performed in children.The results were as follows.
1. Peak serum level of ampicillin (ABPC) after single administration of KS-R1 contains 125 mg or 250 mg of ABPC in potency was 6.03μg/ml after 15 minutes and 5.78 μ/ml after 30 minutes, respectively.The half-life was 30.4 minutes and 30.9 minutes, respectively.Urinary excretion rate was 34.2-70.1% within 6hours.
2. A clinical study of KS-R1 was performed in 40 patients including purulent tonsillitis (10 cases), pharyngitis (9 cases), bronchitis (6 cases), bronchopneumonia (2 cases), scarlet fever (8 cases), otitis media (1case) and urinary tract infection (4 cases).
The clinical effects, excellent and good responses, were showed in 37 cases (efficacy rate;92.5%).
3. No side effects and abnormal laboratory findings were observed.

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The following results were obtained in clinical trials of new ampicillin suppository (KS-R1) in the pediatric infection.
1. Twenty-four patients comprising 15 with respiratory tract infection, 9 with urinary tract infection were received KS-R1 at the dose ranging from 31 mg/kg to 75 mg/kg divided 3 or 4 times a day.
The results in the respiratory tract infection were “excellent” in 8 and “good” in 6, and the efficacy rate was 93.3%. The results in the urinary tract infection were “excellent” in 4 and “good” in 3, and the efficacy rate was 77.8%.
2. Diarrhea were observed in 4 patients, and anal pain was observed in 1. But the symptoms were transient. No abnormal laboratory findings were observed.

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Fundamental and clinical studies of ampicillin (ABPC) suppository (KS-R1) were performed in children with respiratory tract infections.
1. Serum levels of ABPC after rectal administration of KS-R1 at a dose of 250mg (11.4-17.7mg/kg) in 3 children (3-5 years old) were 4.0-10.2μg/ml (average 6.4μg/ml) at 1/4 hour, 3.8-9.4μg/ml (average 6.2 μg/ml) at 1/2 hour, 1.2-4.5μg/ml (average 2.8μg/ml) at 1 hour, 0.3-4.4 etigival (average 0.7μg/ml) at 2 hours, and 0.3μg/ml in 1 case and unmeasurable amount in 2 cases at 4 hours. Urine concentrations of ABPC were 230-445μg/ml (average 312μg/ml) in 0-2 hours, 5.3-156μg/ml (average 66.7μg/ml) in 2-4 hours, and 1.3-13.4μg/ml (average 6.1μg/ml) in 4-6 hours, and the recovery rate into urine was 6.6-27.7% (average 15.6%) up to 6 hours.
2. Clinical effects of KS-R1 on 16 childish patients with respiratory tract infections (acute purulent tonsillitis in 9 cases, acute bronchitis in 5 cases, acute bronchopneumonia in 1 case and acute purulent otitis media in 1 case) were excellent in 13 cases, good in 2 cases and poor in 1 case, and the effective rate was 93.8%. Bacteriologically, 5 strains of S. pyogenes, 4 strains of S. pneumoniae and 3 strains of H. influenzae were all eradicated with eradication rate of 100%.
3. Side effect was weak diarrhea in 1 case, but this diarrhea immediately disappeared with discontinuation of treatment. There was no abnormality of clinical laboratory findings.
It was concluded that KS-R1 is a useful drug for the treatment of respiratory tract infections in children.

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The basic and clinical studies of ampicillin suppository (KS-R1) in pediatric infections were carried out, and the following results were obtained:
For study of absorption and excretion of KS-R1, a single dose of 250mg of KS-R1 was administered to 3 cases.
The mean serum levels were obtained 4.10±1.55μg/ml at 30 minutes, and 1.52±0.25μg/ml, 0.38±0.04μg/ml at 1 and 2 hours after rectal administration, respectively.
The serum levels were not detectable after 4 hours in all cases.
The half lives were 0.39, 0.54 hour and 0.44 hour, respectively.
The mean urinary excretion rate to 6 hours was 14.8%.
Clinical efficacy was evaluated in 17 cases with tonsillitis (15 cases), bronchitis (1 case) and scarlet fever (1 case).
Good responses were obtained in 15 of 17 cases (88.2%).
Bacteriological response in the form of eradication was noted in 4 of 5 cases.
Side effects were examined with all of the 19 cases, and eosinophllia, was observed in 1 case.

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Clinical evaluations of ampicillin (ABPC) suppository (KS-R 1) were preformed in 9 cases with infectious diseases in the pediatric field and the following results were obtained;
1. When 2.7 mg/kg of KS-R1 was rectally administered to 1 case, the plasma levels of ABPC were 3.9μg/ml at 15 minutes, 2.2μg/ml at 30 minutes and 1.2μg/ml at 60 minutes after administration.
The urinary excretion rate within 6hours was 5.0%.
2. Clinical effects of KS-R1 were examined in 6 cases (4 cases of tonsillitis and 2 cases of urinary tract infection) at the dose of 20-50mg/kg/day for 3-7days. Clinical responses were excellent in 4 cases, good in 1 case and poor in 1 case (tonsillitis).
3. As to the side effects, slight increase of eosinophil was observed in 1 case, but no diarrhea, perianal redness and eruption were observed.
4. Since discharge ratio of KS-R1 within 5 minutes was 11.0%, the tolerance of KS-R1 was considered to be good.
5. From the above results, KS-R1 is useful for treating the pediatric patients with various infections, who refuse to oral administration or are impossible to give oral administration because of vomitting and are multiple handicapped ones.

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Ampicillin suppository (KS-R1) was given to 16 patients with various infections in pediatric field. Clinical effects were excellent in 13 cases and good in 3 cases, and the effective rate was 100%. Side effects and the rejection of treatment were not observed.

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1. Blood level of ampicillin (ABPC) after the administration of ABPC suppository (KS-R1) reached a peak in 15-60 minutes with the level of 300ng/ml at a dose of 1mg/kg/day.This level was almost the same as that after the intramuscular injection of ABPC, and higher than that after the oral administration of ABPC which were reported.
2. The clinical effective rate (excellent and good) of KS-R1 was more the 95%, and the overall effective rate including bacteriological effect was more than 95%.
3. It is concluded that KS-R1 is a useful drug for the treatment of bacterial infections in pediatric field.

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Ampicillin suppository (KS-R1) was given to 16 children with the following acute bacterial infection;4 cases of acute pharyngitis, 2 cases of acute tonsillitis, 5 cases of acute bronchitis, 4 cases of bronchopnetunonia, 1 case of group A β-streptococcal infection.Out of 16 patients, good clinical responses were obtained in 16 patients, and bacteriological effectiveness was seen in all 3 cases.Side effects with KS-R1 were observed in 4 cases: 3 cases were perianal redness, and 4 cases were soft stool.
From the above clinical results, KS-R1 is useful antibiotic suppository for treating the pediatric patients with various kinds of bacterial infections.

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In order to evaluate effectiveness of ABPC suppository (KS-R1) in the treatment of bacterial infections of children, the clinical studies were carried out.
KS-R1 was given in rectum to 14 patients in doses of 24.2-65.8mg/kg (average 38.5mg/kg) in 3-4 divided doses for 3-8days (average 4.0days);6 with acute tonsillitis, 3 with pneumonia, 1 with otitis media, 4 with UTI.
The overall efficacy rate was 100%.Bacterial efficacy was good, i.e.8 of the 8 strains disappeared.
Any clinical side effects and laboratory abnormalities were not observed during treatment.
The above results suggested that KS-R1 is a useful antibiotics for pediatric bacterial infections.

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1. Plasma levels of ampicillin (ABPC) after the single rectal insertion of KS-R1 at doses of 125 and 250mg in 154 children reached a peak at 11-15 minutes in children of age less than 1 year old, at 16-20 minutes in children of 1-3 years, 4-6 years and more than 7 years old with the highest levels of 11.50, 8.69, 10.33 and 8.30μg/ml, respectively.
2. Highest plasma levels of ABPC were 6.48, 8.00, 12.32 and 17.83μ by the administration of KS-R1 at doses of less than 10.9mg/kg, 11.0-15.9, 16.0-20.9mg/kg and more than 21.0mg/kg, respectively, with dosedependent response which were observed at 11-15 minutes or 16-20 minutes.There was no difference of plasma levels between the administration of 125 and 250mg of KS-R1.
3. The pain of insertion was observed in 0.6% of total 167 cases, the feeling of defection in 2.4% and the discharge of suppository or its dissolved material or defecation within 30 minutes after insertion in 12.6%, without the influence of patients ages and dosage level.These figures were almost the same as those after the insertion of other suppositories such as erythromycin suppository or antipyretic suppository.
4. Clinical effectiveness of KS-R1 was examined in 51 childish patients with various infections.KS-R1 was rectally given to them at doses of average 41.6mg/kg/day divided into 3 to 4 times for 7 days.All cases showed excellent and good effects.
5. Bacteriologically, all pathogens which were isolated from 12 patients were eradicated.

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Clinical and bacteriological effects of ampicillin suppository (KS-R1) were determined in 9 cases with urinary tract infection and 13 cases with upper respiratory tract infection in children.
Clinical effects were excellent in 1 case, good in 18 cases, fair in 2 cases and poor in 1 case.Bacteriological effects were eradication in 6 cases, decrease in 1 case, persistance in 3 cases and replacement in 1 case among 11 cases which were measured the pathogens before and after treatment.
As to the side effects, one patient showed watery diarrhea, and another one showed the elevation of GOT.
KS-R1 is considered to be a useful drug for the treatment of infection in children both clinically and bacteriologically.

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1. Clinical effects of ampicillin suppository (KS-R1) were examined in 24 children (11 male and 13 female) aged fkrom 5 months to 7 years 5 months with urinary tract infection. KS-R1 was rectally given to the patients at doses of average 45.6mg/kg/day divided into 3 to 4 times for average 8 days.
2. Clinical effectiveness was 95.8%.
3. Bacteriologically, the eradication of isolated organisms was observed in 10 (71.4%) out of 14 cases, the decrease in 3 (21.4%) and the persistence in 1 (7.1%).
4. The discharge of suppository within 5 minutes after insertion was observed in 8.7% of patients without diarrhea and in 6.9% of patients with diarrhea.
5. The evacuation rate of the bowels within 10 minutes after insertion was observed in 5.9% of patients without diarrhea and in 41.9% of patients with diarrhea. It was suggested that the administration of KS-R1 to childish patients with diarrhea should be careful.
6. As to the side effects, diarrhea was observed in 2 cases (7.1%) and the elevation of GPT and GOT in 1 case (3.6%).

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A comparative well-controlled study was performed to evaluate the efficacy and tolerability of KS-R1 (ampicillin rectal suppository, 125 mg%times;4/day) administered to the rectum as compared with those of orally administered ampicillin (ABPC) with same dosage.The results obtained were as follows.
The clinical effect of the drug was judged in 100 cases (suppository group in 45 cases, oral group in 55cases) out of 111 cases The overall efficacy rates evaluated on standard criteria were 93.3% for the suppository group and 89.1% for the oral group.There was no statistically significant difference between 2 groups.
Evaluation by stratification according to the dose, disease type and age also revealed a slightly higher efficacy rate oneach parameter in the suppository group, but no significant difference between 2 groups.
The bacteriological effects evaluated in 84 cases (suppository group in 38 cases, oral group in 46 cases) were 94.7% and 93.5%, respectively.There was no statistically significant difference between 2 groups.
Side effects were evaluated in 101 cases (suppository group in 46 cases, oral group in 55 cases), but the incidence rate showed no significant difference between the 2 groups;3 cases (each 1 of abdominal pain, periproctal redness and periproctal erosion) were observed in suppository group and 2 cases (each 1 ofstomach pain+soft stool and diarrhea) in oral group.
The results indicate that KS-R1 is equally effective and tolerable against acute suppurative otitis media compared to oral administration of ABPC, and considered to be useful.

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