Alfred Hunger

Synthese basisch substituierter, analgetisch wirksamer Benzimidazol-Derivate

The syntheses of 1-(β-dialkylamino-ethyl)-2-benzyl-5-nitro-benzimidazoles, a new series of powerful analgesics, are described.

A note on the diffusion of drugs through artificial phospholipid membranes

A relatively simple method for the assessment of the passive diffusion of drugs through artificial phospholipid membranes composed of lecithin and collodion yields data on the permeability of some pharmaceutical substances through lipid barriers. Although there are inherent limitations in using artificial phospholipid membranes as substitutes for more complex biological membranes, this model system can furnish information on permeability kinetics and on the effect of structural groups on biological activity.

The passage of drugs across the rat intestine in vitro

The in vitro methods of Smyth & Taylor (1957) and everted sac technique of Crane & Wilson (1958) have been evaluated for studying the passage of ferrioxamine‐B hydrochloride and its derivatives, glutethimide, thalidomide, a polypeptide, salicylic acid, aniline and phenol red from the mucosal to serosal side of the rat intestinal barrier in vitro. The ferrioxamines were not significantly absorbed, glutethimide was more rapidly absorbed than thalidomide, the polypeptide was broken down rapidly and appeared as amino‐acids in the serosal fluid, salicylic acid and aniline were found in the serosal fluid but phenol red was little absorbed. Although allowance must be made for differences in the transit pathways of in vivo and in vitro systems because of the non‐functional nature of the capillary network in in vitro studies, our results suggest that these methods can supply useful information on the permeability characteristics of newly developed drugs through the intestinal barrier.