Distribution (Autoradiography) of a New Synthetic Antibacterial Agent OPB-2045 in Rats.

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Abstract

For the purpose of clarifying in vivo pharmacokinetics of OPB-2045 (1-(3, 4-dichlorobenzyl)-5-octyl-biguanide hydrochloride) in rats, a single subcutaneous administration of 14C-OPB-2045 was given to male, female and pregnant rats to study the distribution of the compound by whole body autoradiography. Also, a single percutaneous administration of 14C-OPB-2045 and 14C-Chlorhexidine was given to rats to study and compare the distribution at the site of administration by microautoradiography.<BR> 1. In male and female rats, very high radioactivity was distributed at the site of administration and in the contents of the intestine, and high radioactivity in the adrenals and in the contents of the bladder. Disappearance of the radioactivity at the injection site was slow. Distribution of radioactivity in the brain, blood, testis, seminal vesicle, ovaries and uterus was slight.<BR> 2. Distribution in pregnant rats was characterized by slight radioactivity distribution in the ovaries and placenta and almost no present in the fetus and amniotic fluid.<BR> 3. When 14C-OPB-2045 was administered percutaneously, radioactivity was distributed mainly in the corneal layer of epidermis and was slightly distibuted in the hair and hair follicles. When Hibiten solution containing 14C-Chlorhexidine was administered percutaneously, radioactivity was distributed in the epidermis from the corneal to the basal layers, sebaceous gland and hair, and were slightly distributed in the hair follicles.

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