[Correlations between the pharmacological effects of menilon and its concentrations in the plasma and brain of experimental animals]. / Korelatsii mezhdu niakoi farmakologichni efekti na preparata menilon i kontsentratsiite mu v plazma i mozuk na opitni zhivotni.

The authors carried out studies on the preparation menilon in order to establish eventual correlations between some pharmacological and pharmakokinetic indices. For this purpose they examined the activity of menilon in rats and mice during electric shock and hypothermia and determined the concentrations of the preparation in plasma and brain in rats. The obtained results from the pharmacological investigation revealed manifested action against the seizures after electric shock in both groups of animals. It was established as early as 30 minutes after oral administration of the preparation reached maximal activity after 1-2 hours and disappeared after 6 hours. The authors found strong and continuous hypothermic activity. The hypothermic effect of the doses used was preserved up to the end the 24 th hour. The lowering of temperature in rats was comparatively weaker and shorter. The pharmacokinetic studies showed quick oral resportion of menilon. It was found in plasma and brain of the experimental animals on the 30 th minite after its administration, reached maximal concentration between the first and second hour and still was established on the 24 th hour after administration. The maximal level of the preparation in plasma and brain after oral administration correlated well with the time of maximal activity of its antiseizure and hypothermic effects. The preparation menilon was comparatively slightly toxic.

[Resorption, distribution and excretion of the Bulgarian preparation, adepren, in experimental animals]. / Prouchvane vurkhu rezorbtiiata, razpredelenieto i ekskretsiiata na bulgarskiia preparat adepren v opitni zhivotni.

The authors carried out studies of the original Bulgarian preparation Adepren on male rats Wistar with a weight of 170-200 gm. Single groups of animals were treated singly with venous doses respectively 2,5 and 10 mg/kg of body weight, but other three groups with oral administration of 10, 100 and 200 mg/kg of body weight. The content of the preparation was determined after decapitation of the rats at various intervals of time in plasma, brain, liver and kidneys. Excretion was examined in urine and feces for a period of four days and nights (in metabolic cages). There was a slow resorption of Adepren in the gastro-intestinal tract. The preparation underwent biotransformation in the organism of the rats after oral usage and the basic metabolite was 4-aminocholine, excreted in urine. Adepren and its metabolites were excreted in rats mainly through urine.

[Pharmcokinetics of an echinopsin preparation]. / Farmakokinetika na preparata ekhinopsin.

The purpose of the present work is to describe the pharmacokynetic characteristics of the preparation Ehinopsine, which represents N-methyl-gamma-chinoline and is synthetised in NIHFI during 1965. The experiments were carried out on male rats of the strain Wistar with weight of 170 to 190. The authors examine in dynamics plasma and tissues after single intraperitonenal administration of a dose of 30 mg/kg of body weight, plasma after venous administration of 25 mg/kg of body weight and 100 mg/kg of body weight and plasma and tissues-after oral administration of 100 mg/kg of body weight. The excretion of the preparation was examined also in bile, urine and feces after oral administration and there were metabolites in urine. On the basis of the experimental data after oral and venous treatment the respective mathematical models of distribution were determined as well as the basic pharmacokynetic parameters, characterizing the behaviour of Ehinopsine in the organism of rats. The obtained results gave a picture for good resorption of the preparation, quick distribution, weak excretion and wide biotransformation in the organism of the experimental animals.