The concentrations of sulbenicillin in maternal and fetal blood and in the amniotic fluid compartment were measured in 27 women at parturition. With an intramuscular injection of 2,000 mg of sulbenicillin, the highest concentration of sulbenicillin in maternal blood (109.0 ,ug/ml) was attained at 55 min. The highest concentrations in umbilical cord blood (-25 pLg/ml) were attained between 1 and 3 h after dosage. The peak concentration in amniotic fluid (27.1 vtg/ml) was attained approximately 7.5 h after sulbenicillin administration.This report is concerned with the distribution into the fetus and amniotic fluid of disodium sulbenicillin (SBPC, Lilacillin, Takeda Chemical Industries, Ltd., Osaka, Japan), a derivative of 6-aminopenicillanic acid. The subjects studied were 27 pregnant Japanese women with gestation periods between 38 and 41 weeks, who were admitted to the Department of Obstetrics and Gynecology, Miyazaki Medical College. The subjects were between the ages of 23 years, 6 months, and 36 years, 4 months. Of the 27 subjects, 11 were pregnant for the first time. The women weighed between 51.4 and 72.0 kg. All had normal deliveries.SBPC in a dose of 2,000 mg was administered intramuscularly in the deltoid region. Samples of maternal and umbilical cord blood and amniotic fluid were obtained at parturition. The latter samples were collected at the time of induced rupture of the membranes in patients in active labor without the contamination of maternal blood or vaginal microbial organisms. All specimens were centrifuged promptly after collection. Serum and supernatant from the amniotic fluid were frozen at -20°C until assayed.The concentrations of SBPC in clinical specimens were measured by the cylinder-plate diffusion method with Pseudomonas aeruginosa NCTC 10490 as the test organism and DST-agar medium (Oxoid Ltd., London, England) supplemented with 0.1% sodium acetate. Concentrations in serum were calculated from the standard curve of penicillin dissolved in serum. Concentrations in amniotic fluids were calculated from the standard curve of penicillin dissolved in 0.1 M phosphate buffer, pH 7.0 (3, 7).The concentrations of SBPC in maternal blood increased immediately, reaching a maximum of 109.0 p.g/ml at 55 min after administration (
The concentrations of cefotiam dihydrochloride (CTM) in maternal and fetal blood and in amniotic fluid were determined by bioassay in 38 women at parturition. With an intravenous infusion of 1 g of CTM, the decline in concentration of CTM in maternal blood was biphasic; CTM was not detectable at 6 h after administration. Peak levels of CTM in umbilical cord blood (13.0 to 23.9 pug/ml) were attained between 15 and 28 min after intravenous infusion; those in amniotic fluid (19.6 to 23.5 ,ug/ml) were attained at ca. 2.5 h.When one considers using antibiotics for pregnant women, placental drug transfer must be taken into account. Substantial transfer to the fetus and amniotic fluid is not necessarily a disadvantage if the drug exerts minimal side effects. In fact, this may make the drug a reasonable choice for treatment of amnionitis and fetal infection. Accordingly, we studied the placental transfer of cefotiam dihydrochloride (CTM) (Pansporin; Takeda Chemical Industries, Ltd., Osaka, Japan), a cefem with a broad spectrum (6, 9), to the fetus and amniotic fluid.Seven normal pregnant women (four primiparas and three multiparas, aged 24 to 37 years) who agreed to participate in this study were each given 1 g of CTM dissolved in 10 ml of distilled water by intravenous infusion during weeks 37 to 41 of pregnancy. Blood samples were collected at 5, 15, 30, 60, 120, 180, and 300 min after infusion.Also, 38 normal pregnant women in labor (17 primiparas and 21 multiparas, aged 21 to 37 years) who agreed to participate in this study were each given 1 g of CTM by intravenous infusion. Maternal and fetal (umbilical cord) blood were collected at parturition. Amniotic fluid was obtained by induced rupture of membranes immediately before parturition to minimize contamination of the fluid by maternal blood. Each of the mothers delivered a normal term baby via easy labor.The concentrations of CTM in serum and in amniotic fluid were determined by bioassay, using the cylinder-plate diffusion method (5, 9) and Proteus mirabilis ATCC 21100 as the assay organism. Sensitivity of the procedure applied to blood and amniotic fluid was 0.2 p.g/ml.
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