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Using inversion of SV receiver functions, defined for various directions at each of the three broad-band stations located in the Baikal rift zone, detailed S velocity models of the crust and upper mantle down to 260 km have been obtained. These models reflect peculiarities of the velocity structure beneath Baikal depressions and mountains.

第33回極域気水圏シンポジウム11月30日（火） 国立極地研究所 ２階大会議室

Accepted: 2005-12-21, 資料番号: SA1000459000

We introduced an on-line system of biochemical, hematological, serological, urinary, bacteriological, and emergency examinations and associated office work using a client server system NEC PC-LACS based on a system consisting of concentration of outpatient blood collection, concentration of outpatient reception, and outpatient examination by reservation. Using this on-line system, results of 71 items in chemical serological, hematological, and urinary examinations are rapidly reported within 1 hour. Since the ordering system at our hospital has not been completed yet, we constructed a rapid time series reporting system in which time series data obtained on 5 serial occasions are printed on 2 sheets of A4 paper at the time of the final report. In each consultation room of the medical outpatient clinic, at the neuromedical outpatient clinic, and at the kidney center where examinations are frequently performed, terminal equipment and a printer for inquiry were established for real-time output of time series reports. Results are reported by FAX to the other outpatient clinics and wards, and subsequently, time series reports are output at the clinical laboratory department. This system allowed rapid examination, especially preconsultation examination. This system was also useful for reducing office work and effectively utilize examination data.

The parent compound and one metabolite have been isolated from urine of five healthy male volunteers who received a single 200 mg oral dose of DP-1904. These compounds were extracted by using a Sep-Pak C18 cartridge and purified by the preparative HPLC method. On the basis of proton magnetic resonance and mass spectral data, unchanged drug and its ester glucuronide have been identified in human urine. DP-1904 has one asymmetric carbon and is used as a racemate in the current clinical trial. The enantiomeric compositions of unchanged DP-1904 and aglycon of DP-1904 glucuronide were determined by HPLC with optical activity and ultraviolet detection. The (R)-(+)-enantiomer percentages in unchanged DP-1904 and aglycon of its ester glucuronide in human urine collected at 0-4 hr after oral dosing were 60 +/- 1.3% and 38 +/- 1.4% (mean +/- SE, n = 5), respectively. The 0-4 hr urine collection represented approximately 80% of the given dose. These studies demonstrate that DP-1904 undergoes stereoselective disposition in humans. However, the difference in urinary excretion between DP-1904 enantiomers was rather small.

Fatigue crack propagation rates and threshold stress intensity factors were measured for welded joints and base metal by using 200 mm wide centre-cracked specimens. The fatigue crack propagation properties of welded joints were similar in spite of the different zones in which the cracks propagated (ie, in the heat-affected zone and in the weld metal) and the different welding process used (submerged arc welding and gas metal arc welding). They were, however, inferior to those of the base metal. It was revealed by observation of the crack closure that the fatigue cracks were fully open during the whole range of loading, due to the tensile residual stress distribution in the middle part of the welded joints. This observation also explains the lack of a stress ratio effect on the fatigue crack propagation properties of welded joints, and their inferiority to those of the base metal.

N-[(Benzoyloxy)alkyl]-1,2,3,4-tetrahydro-2-naphthylamine derivatives were synthesized from 1,2,3,4-tetrahydro-2-naphthylamines and evaluated for their spasmolytic. Some of these compounds showed a nerve-selective effect on colon rather than stomach in anesthetized dogs and were found to be equal to or more active than the reference drug (mebeverine). The biological data have indicated some structure-activity relationships. Among these compounds, N-ethyl-N-[6-(3,4-dimethoxybenzoyl)oxy]hexyl]-1,2,3,4-tetrahydro-6-methoxy-2- napththylamine hydrochloride (63) was found to be the most active spasmolytic agent.

Fundamental and clinical studies on gynecological use of cefotetan (CTT), a new cephamycin antibiotic, were performed with following results. Following the intravenous administration of 2.0 g of CTT, T 1/2 beta in serum was 3.1 hours and longer than the previous cephamycin antibiotics. The yields of CTT from serum to various uterine tissues and discharge from retroperitoneum were about 30 approximately 50%. In clinical use, 14 patients with gynecological infections were administrated CTT, and it showed excellent or good efficacy in all patients. No side effects were noted except 1 transient disturbance in liver function.

Pharmacokinetic and clinical studies on cefotiam (CTM) in the perinatal period were performed and results obtained are summarized below. Concentrations of CTM in maternal serum, umbilical cord serum and amniotic fluid were examined after a bolus intravenous administration at a dose of 1 g. Data were analyzed using simulation curves drawn by the two- or three-compartment open model. The peak level of CTM in maternal serum was 86.6 micrograms/ml and the half-life of the beta-phase was 0.91 hour. Peak levels of CTM in umbilical cord serum and amniotic fluid were 20.8 micrograms/ml at 0.1 hour and 9.2 micrograms/ml at 3.2 hours after the administration, respectively. The concentration of CTM in amniotic fluid decreased after reaching the peak, but it was still as high as 1.6 micrograms/ml even at 12.0 hours after the administration. These results clearly demonstrated that the transfer of CTM to umbilical cord serum and to amniotic fluid was efficient in protection of perinatal infections. In a clinical trial, CTM was given to 11 patients with perinatal infections. Clinical efficacies were evaluated as excellent in 2 patients, good in 8 patients and poor in 1 patient. No adverse effects were observed in any of the patients studied. In conclusion, CTM was useful and safe antibiotic for the treatment of infections in the perinatal period.

Pharmacokinetic and clinical studies were carried out on the use of ceftizoxime (CZX) in the perinatal period. The results obtained are summarized below. 1. Mean maternal serum concentrations of CZX reached 57.3 micrograms/ml at about 15 minutes after a single intravenous injection of CZX 1 g and then gradually decreased to 13.1 micrograms/ml in 1 hour and 55 minutes, 3.59 micrograms/ml in 4 hours and 20 minutes and 0.11 microgram/ml in 17 hours and 51 minutes. CZX in umbilical cord serum was at detectable concentrations soon after administration and peaked to 23.5 micrograms/ml in 32 minutes. Although the concentrations in umbilical cord serum gradually decreased thereafter, they were higher than those in maternal serum at 3 hours and more after an injection and was 0.41 microgram/ml at 17 hours and 51 minutes. The CZX in amniotic fluid became detectable a little later than CZX in umbilical cord serum. The concentration of CZX in amniotic fluid was below 1.00 microgram/ml at 30 minutes after administration. Concentrations then gradually increased to 21.3 micrograms/ml in 1 hour and 55 minutes and, even in 17 hours and 51 minutes, they were as high as 9.44 micrograms/ml. 2. In the clinical evaluation, CZX was given to a total of 7 cases, i.e., 1 of amnionitis, 2 of puerperal endometritis, 1 of puerperal fever, and 3 of pyelonephritis. The treatment showed satisfactory results, i.e. excellent result was obtained in 1 case, good in 5 and poor in 1 with an clinical efficacy rate of 85.7%. Microbiological examinations resulted in the isolation of 5 bacterial strains of 4 species and 1 fungal strain from 5 cases.(ABSTRACT TRUNCATED AT 250 WORDS)

Fundamental and clinical studies were carried out on T-1982 (cefbuperazone) a new cephamycin antibiotic, with the following result. Following a single intravenous administration of 1.0 g of T-1982, the transfer of T-1982 to the internal genital organs was found to be good. The transfer of T-1982 to retroperitoneal fluid was also good. In clinical trial, T-1982 was administered to 10 patients with obstetrical and gynecological infection. Efficacy was excellent in 4 cases and good in 6 cases. No side effects were observed. In laboratory findings, a transient elevation of alkaline phosphatase was noted in 1 case.

The study group was organized to evaluate the usefulness of cefmenoxime (CMX) injection, a new synthetic cephalosporin, for the treatment of infections in the field of obstetrics and gynecology. Fundamental and clinical studies were made by the society and the following results were obtained. 1. The peak distribution of CMX's MIC for E. coli, Klebsiella sp., Enterobacter sp., Bacteroides sp. and Peptococcus sp. isolated from obstetrical and gynecological infections with relatively high frequencies area 0.1, less than or equal to 0.05, 0.2, 3.13, 1.56 micrograms/ml, respectively, with an inoculation of 10(6) cells/ml. 2. When 1 g of CMX is administered by intravenous drip infusion for 1 hour, the maximum concentrations in various tissues of female genital organs were as follows: 14.2 and 13.2 micrograms/g in ovary and oviduct, respectively, at 1.20 hours after the start of administration, and 16.9 and 26.3 micrograms/g in corpus uteri and cervix uteri, respectively, after 1 hour. As for the transfer to the exudate in the pelvic dead cavity, the peak concentration was 15.6 micrograms/ml after 2.13 hours. 3. In the clinical studies, CMX was given to 258 cases with female genital organ infections and others. As for the clinical effects, with exclusion of 3 cases in which other antibiotics are concomitantly used, responses were excellent in 76 cases, good in 162 cases and poor in 17 cases, among 255 cases in total. The efficacy rate was 93.3%. The efficacy rates by diseases were 97.1% (68/70) for intrauterine infections, 88.8% (79/89) for intrapelvic infections, 98.4% (62/63) for adnexitis, and 100% (23/23) for infections of external genital organs. As for the clinical effects on causative bacteria, the efficacy rates were 100% (19/19) for single infections due to Gram-positive bacteria, 94.8% (55/58) for single infections due to Gram-negative bacteria, and 88.2% (15/17) for single infections due to anaerobic bacteria. And its efficacy rates were 89.6% (69/77) for mixed infection cases. Side effects were observed in 2 cases (0.8%); 1 case with eruption, and 1 case with diarrhea and vomiting. As for abnormal laboratory findings, lower white blood cell count was observed in 2 cases and elevation of the values regarding hepatic functions in 9 cases. All cases were returned to the normal after the completion of the administration. Cefmenoxime showed a satisfactory clinical efficacy and a potent bacteriological effect in treatment of the infections in the field of obstetrics and gynecology, and it has been concluded that cefmenoxime will be useful addition to the antibiotics for the therapy of these infections.

Fundamental and clinical studies on sulbactam/cefoperazone (SBT/CPZ), a newly developed combined beta-lactam antibiotics, were carried out and the following results were obtained. Each concentration of SBT and CPZ was examined in serum and internal genital organs after single intravenous administration of 2.0 g dose of SBT/CPZ. Each venous serum level of SBT and CPZ was 41.5 micrograms/ml, 122.3 micrograms/ml at 30 minutes after administration respectively. The transfer of SBT and CPZ to internal genital organs was similarly good. Each concentration of SBT and CPZ was examined in serum and retroperitoneal fluid after 1 hour drip infusion of 2.0 g dose of SBT/CPZ. The transfer of SBT and CPZ to retroperitoneal fluid was similarly excellent and the transfer ratio vs. serum level of the former was about 76.2 approximately 321.7%, and the latter was about 27.2 approximately 93.2% respectively. In clinical trial, SBT/CPZ was given to 10 patients with obstetrical and gynecological infections. The efficacy was evaluated as good in 9 patients and poor in 1 patient. As the side effects, diarrhea was appeared in 1 case. In laboratory findings, a transient elevation of serum transaminase was noticed in another one case. From the above results, it was concluded that SBT/CPZ was useful drug for infections in the field of obstetrics and gynecology.

Fundamental and clinical studies were performed on ceftazidime ( CAZ ), a new cephem antibiotic. Following a single intravenous administration of 1 g dose of CAZ , the transfer of CAZ to the internal genital organs was good. The transfer of CAZ to retroperitoneal fluid was excellent. In a clinical trial, CAZ was given to 6 patients with obstetrical and gynecological infections. The efficacy was evaluated as excellent in 3 cases and good in the other 3 cases. No adverse effects were observed in any of the patients treated with CAZ .

It was confirmed that esterolytic activity was significantly elevated in plasma of patients with acute pancreatitis, which correlated better with the stage of the disease than serum amylase level. Using the several column chromatography procedures, pancreatic kallikrein, trypsin and pancreatic elastase were separated and purified from alpha 2-macroglobulin (alpha 2-M) fractions of patients plasma with acute pancreatitis. From this this result, it was confirmed that kallikrein was liberated into the blood stream from the pancreas during attacks of acute pancreatitis and the liberated kallikrein combined with alpha 2-M. Furthermore, the coexistence of trypsin is required for the complex formation of alpha 2-M and pancreatic kallikrein. It was speculated that alpha 2-M might be decomposed by the excessive amount of elastase, and consequently, might release all of its combining enzymes into the blood stream. In the present study, the activation mechanism of fibrinolytic enzyme system in plasma by human pancreatic elastase was investigated. Elastase not only converted the co-existing plasminogen to low molecular weight plasminogen which could be easily activated by the activators, but also inhibited alpha 2-M and alpha 2-plasmin inhibitor, and consequently, induced the activation of the fibrinolytic enzyme system in plasma. Furthermore, it was also confirmed that elastase could activate plasma kallikreinogen to kallikrein.

This study was to investigate the transfer of cefmenoxime (CMX) to the retroperitoneal fluid after extensive panhysterectomy. Twenty-two cases were examined and they were divided into 2 groups, 10 with 1.0 g and 12 with 2.0 g bolus intravenous administration of CMX. In 1.0 g group, CMX concentration in the retroperitoneal fluid was observed 42.0 +/- 9.59 micrograms/ml (Mean +/- S.D.) at 1 hour and thereafter decreased gradually, but it still remained 7.91 +/- 5.18 micrograms/ml at 6 hours after the administration. In 2.0 g group, its concentration was 33.4 +/- 34.5 micrograms/ml at 30 minutes and reached to the peak level of 45.1 +/- 24.6 micrograms/ml at 1 hour and then declined slowly, but it remained 13.3 +/- 8.28 micrograms/ml at 6 hours after the injection. The results demonstrated sufficient transfer of CMX to the retroperitoneal fluid.

Fundamental and clinical studies on imipenem/cilastatin sodium (MK-0787/MK-0791), a new carbapenem antibiotic, were performed and the following results were obtained. Concentrations of MK-0787 and MK-0791 in serum, internal genital organs and retroperitoneal fluid were determined after a 30 minutes drip infusion of 500 mg/500 mg dose. Venous serum levels of MK-0787 and MK-0791 were 47.3 to 67.5 micrograms/ml and 44.2 to 61.4 micrograms/ml, respectively, at the end of the administration. Sufficient transfer of MK-0787 and MK-0791 to internal genital organs and retroperitoneal fluid was demonstrated. In clinical trials, MK-0787/MK-0791 was given to 18 cases with obstetrical and gynecological infections, such as endometritis, puerperal fever, pelvic peritonitis, parametritis and lymphocystitis. The clinical efficacy was evaluated as excellent in 1 case, good in 14 and poor in 3. The efficacy rate was 83.3%. In a bacteriological study, 43 strains were isolated from 16 cases and the eradication rate was 61.1%. No side effects were observed in any of the cases. In laboratory findings, a transient elevation of GOT, GPT was noted in 1 case. From the above results, it was concluded that MK-0787/MK-0791 was useful drug for infections in the field of obstetrics and gynecology.

Fundamental and clinical studies on cefminox (CMNX, MT-141), a new cephamycin antibiotic, were performed and the following results were obtained. Concentration of CMNX was examined in serum, internal genital organs and retroperitoneal fluid after a single intravenous administration of 1.0 g dose. The venous serum level of CMNX was 62.8 +/- 7.02 microgram/ml (Mean +/- S.D.) at 30 minutes after the administration. The sufficient transfer of CMNX to internal genital organs and retroperitoneal fluid was demonstrated. In clinical trial, CMNX was given to 10 cases with obstetrical and gynecological infections. The efficacy was evaluated as excellent in 1 case, good in 8 cases and poor in 1 case. No side effects were observed in any of the cases treated with CMNX.

Fundamental and clinical studies were made on cefotaxime (HR-756, CTX), a new cephalosporin antibiotic, with the following results. 1. Cefotaxime was given to 22 patients. Efficacy was excellent in 3 cases, good in 17 cases and poor in 2 cases. No side effects were observed in any cases. 2. Following a single intravenous injection of 1.0 or 2.0 g, the transfer of CTX to the internal genital organs was found to be good. The transfer of CTX to exudate of the dead space of pelvis was also good. 3. The above data demonstrated that CTX is a safe and effective drug.

N-[(Benzoyloxy)alkyl]-1,2,3,4-tetrahydro-2-naphthylamine derivatives were synthesized from 1,2,3,4-tetrahydro-2-naphthylamines and evaluated for their spasmolytic. Some of these compounds showed a nerve-selective effect on colon rather than stomach in anesthetized dogs and were found to be equal to or more active than the reference drug (mebeverine). The biological data have indicated some structure-activity relationships. Among these compounds, N-ethyl-N-[6-(3,4-dimethoxybenzoyl)oxy]hexyl]-1,2,3,4-tetrahydro-6-methoxy-2- napththylamine hydrochloride (63) was found to be the most active spasmolytic agent.

Fourteen patients suffering from female genital organ infections including mastitis and urinary tract infections were treated with cefoperazone (CPZ). CPZ was administered intravenously or by drip infusion at a dose of 2.0-4.0 g/day for 3-7 days. Clinical results obtained were as follows: Of 8 patients with genital organ infections, excellent responses were seen in 2 patients, good responses in 5 patients. Of 3 patients with mastitis, good responses were seen in all the patients. Of 3 patients with pyelonephritis, excellent and good responses were seen in all the patients. No adverse effects and abnormal laboratory findings were observed. From the above results, we concluded that CPZ was an effective and safe antibiotic against infections in the field of obstetrics and gynecology.

Clinical studies on cefodizime (THR-221, CDZM), a new injectable cephem antibiotic, were performed and the following results were obtained. Ten patients with obstetrical and gynecological infections such as intrauterine infections, pyometra, adnexitis, parametritis and lymphocystitis. The clinical results were evaluated as excellent in 1 case, good in 4 cases and poor in 5 cases. The efficacy rate was 50.0%. Bacteriologically, 10 organisms were isolated from 8 patients and the eradication rate was 44.4%. No side effects were observed in any of the cases treated with CDZM. In laboratory examinations, transient elevations of serum GOT, GPT and Al-P were noted in 1 case.

Fundamental and clinical studies on the perinatal use of cefotaxime (CTX, HR-756), a new cephalosporin antibiotic, were done, with the following results. 1. Following intravenous administration of 2 g of CTX, transport of CTX from maternal serum to umbilical cord serum and to amniotic fluid was found to be good. CTX was not transferred into mother's milk. 2. In clinical use, CTX was given to 16 pregnant patients with premature rupture of the membrane. It showed excellent efficacy in preventing perinatal infection. Five patients with perinatal infections were administered CTX, and in 4 patients CTX had good efficacy. No side effects were noted in any cases.

Fundamental and clinical studies on cefpimizole (AC-1370), a new cephem antibiotic, were performed and the following results were obtained: Concentration of AC-1370 was examined in serum, internal genital organs and retroperitoneal fluid after single intravenous administration of 2.0 g dose. The venous serum level of AC-1370 was 243 micrograms/ml at 30 minutes after the administration. The sufficient transfer of AC-1370 to internal genital organs and retroperitoneal fluid was recognized. In clinical trial, AC-1370 was given to 10 cases with obstetrical and gynecological infections. The efficacy was evaluated as good in 8 cases and poor in 2 cases. No side effects were observed in any of the cases treated with AC-1370.

Fosfomycin sodium was administered to 36 cases with obstetrical and gynecological infection. Efficacy was excellent in 6 cases, good in 27 cases and poor in 3 cases and so effective ratio obtained was 91.7% in all. No side effects were observed in all patients except transient increase of serum transaminase in 2 cases.

Fundamental and clinical studies on cefuzonam (CZON, L-105), a new oxime type cephalosporin, were performed and the results obtained are summarized below: 1. Concentrations of CZON were determined in serum, internal genital organs and retroperitoneal fluid after a single intravenous administration of 1 g dose. The peripheral serum level of CZON was 74.0 micrograms/ml at 15 minutes after the administration. A sufficient transfer of CZON into internal genital organs and retroperitoneal fluid was demonstrated. 2. In clinical trial, CZON was given to 11 cases with obstetrical and gynecological infections. Efficacies were evaluated as good in 9 cases and poor in 2 cases. No side effects were observed in any of the cases treated with CZON. In laboratory examinations, transient elevation of serum GOT, GPT and alkaline phosphatase was noted in 1 case.

Fundamental and clinical studies on aztreonam (AZT), a new synthetic monobactam antibiotic, were performed and following results were obtained. Concentration of AZT was examined in serum, internal genital tissues and retroperitoneal fluid after a single intravenous administration of 1 g dose. The venous serum level of AZT was 114.0 micrograms/ml at 10 minutes after the administration, then decreased to 7.0 micrograms/ml at 3 hours. Since concentration of AZT in examined tissues showed wide variation, it was irrelevant to calculate transfer ratio. Concentration in retroperitoneal fluid made the peak of 40.0 +/- 22.6 micrograms/ml at 1 hour after the administration, then slowly decreased to 13.4 +/- 3.2 micrograms/ml at 6 hours. Judging from above data, the transfer of AZT to retroperitoneal fluid was favorable. In clinical trial, AZT was given to 17 cases with obstetrical and gynecological infections such as endometritis, uterine adnexitis, pelvic peritonitis, parametritis and lymphocystitis. The efficacy was evaluated as excellent in 2 cases, good in 12 and poor in 3, and efficacy rate was 82.4%. No side effects were observed in any of the cases. In laboratory findings, transient elevation of liver function in 2 cases and eosinophilia in 1 case were noticed.

A clinical study was carried out on imipenem/cilastatin sodium (IPM/CS) in the perinatal period, and the results obtained are summarized as follows. IPM/CS was given to 5 cases with puerperal intrauterine infection and 2 with puerperal fever. The clinical efficacies were evaluated as good in 6 cases and poor in 1. The clinical efficacy rate was 85.7%. In a bacteriological examination, 9 strains were isolated from 6 cases, and 7 strains were eradicated with an eradication rate of 77.8%. No side effects were observed in any of the cases treated with IPM/CS.

Fundamental and clinical studies on the perinatal use of latamoxef (LMOX) were performed, with the following results. Concentration of LMOX was examined in maternal serum, umbilical cord serum and amniotic fluid after intravenous administration of 2 g dose. Data were analyzed by the simulation curves using the two-compartment model. The peak level of LMOX in maternal serum was 218.4 micrograms/ml and half-life of the beta-phase was 1.9 hours. The peak levels of LMOX in umbilical cord serum and amniotic fluid were 37.4 micrograms/ml (1.4 hours) and 27.5 micrograms/ml (8.9 hours) after administration. The concentration of LMOX in amniotic fluid decreased in amount after the peak, but it still remained 21.9 micrograms/ml (16 hours) after administration. Above these results, it was concluded that the transfer of LMOX to umbilical cord serum and to amniotic fluid was sufficient. In clinical use, LMOX was administered to 30 pregnant patients with premature rupture of membrane. It showed excellent efficacy in preventing perinatal infection. Seven patients with perinatal infections were treated with LMOX and all of them had excellent efficacy. No side effects were observed in any of the cases studied.

We conducted a study on the utility in the obstetric and gynecological field of piperacillin (PIPC) which is a broad spectrum penicillin developed here in Japan. After administration of PIPC by intravenous one shot injection or intravenous dripping infusion the yield of PIPC to the various uterine tissues was a favorable 30 approximately 40% in comparison with the serum concentration and the discharge from retroperitoneum was about 100% to 300% in 4 hours. Thus it is thought to be useful in the treatment of infections of the retroperitoneum. During a clinical trial PIPC was administered to 16 patients with obstetrical and gynecological infections and it proved to be excellent in 4 patients, good in 10 patients and ineffective in 2 patients. Thus an overall efficacy rate of 87.5% was obtained. The only side effects observed was a slight transitory abnormality of liver function in 2 patients. Thus in the overall evaluation, this drug was considered to be useful in the treatment of infections in the obstetric and gynecological field.

Fundamental and clinical studies were carried out on ceftazidime (CAZ) in the perinatal period, and the results obtained were summarized below. Following bolus intravenous injection of CAZ 2 g, maternal serum concentrations of CAZ were as high as 145.3 +/- 17.2 micrograms/ml (mean +/- S.D.) at about 10 minutes, and then gradually decreased to 46.7 micrograms/ml at 2 hours, 5.31 micrograms/ml at 5 hours and 4 minutes, and 1.54 micrograms/ml at 11 hours and 10 minutes. The CAZ was detected in umbilical cord serum immediately after the administration, and concentrations were 31.0 +/- 1.54 micrograms/ml at about 10 minutes. Although the concentrations gradually decreased thereafter, they were higher than those in maternal serum at 3 hours and later and was 3.00 micrograms/ml at 11 hours and 10 minutes. The CAZ was detected in amniotic fluid a little later than in umbilical cord serum, and concentrations of CAZ in amniotic fluid were as low as 1.50 +/- 0.67 micrograms/ml at about 10 minutes after the administration. Concentrations then gradually increased to 12.8 micrograms/ml at 2 hours and 26.5 micrograms/ml at 5 hours and 4 minutes, and even at 11 hours and 10 minutes, they were as high as 14.2 micrograms/ml. The above results demonstrated that the transfer of CAZ through placental barrier was very rapid and satisfactory. Also, CAZ showed good transfer into amniotic fluid, as well as sufficient retention, and was considered to be an effective antibiotic for prophylaxis of both fetal infections and amniotic fluid infections.(ABSTRACT TRUNCATED AT 250 WORDS)