[Biotransformation and pharmacokinetics of AWD 26-06, 8-chloro- 5,10-dihydro-5-[bis(2-hydroxyethyl)aminoacetyl]-11H-dibenzo[b,c] [1,4]diazepin-11-one hydrochloride, in the rat]. / Pharmakokinetik von AWD 26-06, 8-Chlor-5,10-dihydro-5-[bis(2- hydroxyethyl)aminoacetyl]-11H-dibenzo[b,e][1,4]diazepin-11-on- hydrochlorid an der Ratte.

Following p.o. and i.v. application of the 14C-labelled AWD 26-06 (6 mg/kg b.w.) with anticholinergic activity, blood levels (-24 h) and excretion (urine, feces-72 h; bile-7 h) were studied in Wistar rats. Intestinal absorption amounted to 30% of the dose administered in water solution. Elimination half-lives in blood were 0.6 h and (after Cmax 3-4 h p.a.) 8 h. Excretion was mainly by feces (unchanged drug and biliary excreted metabolites) and to less extent by urine.

[Synthesis of 3-carbethoxyamino-5-dimethylamino-[1-14C]-acetyl- 10,11-dihydro-5h-dibenz[b,f]azepine hydrochloride (Bonnecor, AWD 19-166, GS 015)]. / Radioaktive Markierung von 3-Carbethoxyamino-5-dimethylaminoacetyl- iminodibenzylhydrochlorid (Bonnecor, AWD 19-166, GS 015) mit Kohlenstoff-14.

GS 015-14C was synthetized from [1-14C]-chloracetic acid and 3-carbethoxyamino-10,11-dihydro-5H-dibenz[b,f]azepine. The whole radioactivity yield passing all synthesis stages was 32% at a radiochemical purity of more than 98%.