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[Citrate as an inhibitor of stone formation--with reference to intestinal citrate absorption and the influence of citrate on intestinal calcium absorption].

The response of serum citrate to the oral citrate load was studied in seven healthy subjects. Serum citrate was significantly elevated from 15 to 60 min post-load with some individual variations. In 27 stone-formers serum citrate and the response to the oral citrate administration was studied and compared with the results obtained on healthy subjects. The serum citrate concentration of stone-formers was 1.99 +/- 0.49 mg/dl as compared to 1.61 +/- 0.35 mg/dl in healthy subjects. After citrate administration serum citrate increased significantly in both groups, but no significant difference was shown in response to the oral citrate load between these two groups (3.44 +/- 0.94 mg/dl in stone-formers, 3.16 +/- 0.38 mg/dl in healthy subjects). In Sprague-Dawley rats each weighing about 200 g urinary citrate and calcium excretion were studied after administration of sodium citrate or calcium chloride or both. The concomitant equimolar administration of sodium citrate and calcium chloride did not have significant influence on urinary citrate or calcium excretion as compared when citrate or calcium was given alone. However, the calcium excretion was significantly decreased with the administration of citrate and calcium ata molar ratio of 1:2.

Animals↗

Absorption of horseradish peroxidase by neonatal pig intestinal epithelium: effect of Escherichia coli (055B5) on absorption.

The pathway of macromolecular transport through the neonatal pig small intestinal epithelium was examined, utilizing the cytochemical marker horseradish peroxidase (HRP). The marker was found adsorbed to the apical microvillous of the enterocytes, within apical tubules, and cytoplasmic vacuoles. Extracellular absorbed marker assumed a spherical appearance within the subepithelial spaces but was dispersed within the capillary lumens. Uptake of HRP into the enterocyte occurred in 48-hour old neonatal pigs, but transport into the circulation was not observed. Adherence of Escherichia coli to the surface of the ileal enterocyte did not totally inhibit HRP uptake. The E coli adhered to the surface of the enterocyte or within intercellular vacuoles appeared to be static in as much as they were not involved in the transepithelial migration of envacuolated HRP.

Animals↗

[Comparison between FT-207 and 5-FU on intravesical absorption--experimental study on intravesical absorption in the dog].

FT-207 and 5-FU (1,200 mg) were administered intravesically to 5 mongrel dogs, and their concentration in the serum and bladder wall was measured. The serum concentration was high in both groups because their molecular weights are less than 200. The serum concentration of FT-207 was approximately 40 times higher than that of 5-FU. This difference may be due to the fact that non-ionized molecules in FT-207 account for more than 80% but those in 5-FU account for less than 10%.

Absorption↗

[Absorption, distribution, metabolism and excretion of bacmecillinam. III. Absorption, metabolism and excretion of 14C-bacmecillinam following oral administration to dogs].

The pharmacokinetics (i.e., blood level, biological half-lives and excretion) of bacmecillinam (KW-1100) was investigated. KW-1100 was orally administered to dogs at the dose of 20 mg/kg (as mecillinam). Biological half-lives (radioactivity) of 14C-KW-1100 in plasma were 1.2 hours (T1/2 alpha) and 52 hours (T1/2 beta). The Cmax and Tmax were 8.4 micrograms/ml and 2 hours. The biological half-life (microbiological activity) of KW-1100 in plasma was 0.9 hour. The Cmax and Tmax were 5.6 micrograms/ml and 1 hour. The urinary and fecal excretion of 14C-KW-1100 were approximately 46% and 49% (0 approximately 72 hours), respectively. The major metabolites in the urine (0 approximately 8 hours) were mecillinam, 5,5-dimethyl-2-(1'-formamidomethyl)-thiazolidine-1',4-dicarboxy lat e (M-1) and 6-beta-[(hexahydro-1 H-azepin-1-yl)-methyleneamino]penicilloic acid (M-6), each distribution ratio of which was 57.2, 24.2 and 12.0% of the total radioactivity in the sample, respectively. The major metabolite in the plasma at peak time (2 hours) was mecillinam (56.2%).

Administration, Oral↗