Poly[sulfadiazineacrylamide] (5), labeled with 14C in the main chain, was synthesized and its molecular weight viscosimetrically determined by comparison with unlabeled samples of poly[sulfadiazineacrylamide] with similar molecular weights which were determined by membrane osmometry. The material showed a polymer-specific prolongation of its systemic behaviour in mice. Rates of excretion of the polymer were negligibly low, whereas the toxicity was considerable. It was concentrated in the liver during the course of the experiment, but no affinity toward the PC6 plasmacytoma in mice could be detected. Poly[sulfadiazinacrylamid] (5) mit 14C-Hauptkettenmarkierung wurde synthetisiert und sein Mo…

Pharmakologisch aktive polymere, 8.Poly[2-(methylsulfinyl)äthylacrylat]e und ihre vermittelnde wirkung auf die transkutane resorption von pharmaka

Poly[2-(methylsulfinyl)athylacrylat] (2a) und Poly[2-(methylsulfinyl)athylmethacrylat] (2b) wurden synthetisiert und auf ihre vermittelnde Wirkung bei transkutaner Resorption einiger Pharmaka untersucht. 2b verbesserte die Resorption der Phosphorsaureester Dimethoat® und Paraoxon® und der p-Aminohippursaure und war etwa mit der Wirksamkeit von DMSO vergleichbar. Ein geringer penetrationsfordernder Effekt ergab sich fur Dinitrochlorbenzol. Nicht beeinflust wurde die dermale Resorption von Isoprenalinsulfat. Die beiden Polymeren zeigten eine gute Lokalvertraglichkeit und 2b auch keine akute Allgemeintoxizitat bei systematischer Anwendung. Der fur DMSO charakteristische knoblauchartige Geruch …

Pharmakologisch aktive polymere, 4. Monomere und polymere alkylsulfinyl-alkylacrylate und -methacrylate als mögliche resorptionsvermittler

Pharmakologisch-aktive polymere, 21. Orientierende Untersuchungen zur körperverteilung und Ausscheidung von poly[2-(methylsulfinyl)ethylacrylat]en bei der Ratte

Poly[2-(methylsulfinyl)ethyl acrylate] (1) was synthesized as well as derivatives 14C-labelled in side groups (6) or 14C-labelled in the main chain (11). Polymer 11 with the 14C-labelled main chain was fractionated by precipitation. The η-M-relation determined by measurements of unlabelled polymers in the ultracentrifuge for comparison was used to establish the viscosimetrically determined molecular weights of the labelled fractions. After intravenous application of aqueous solutions of the polymer in rats the excretion rate up to 72 h after treatment was ascertained to ca. 50%; the concentration in the blood serum was found to be strikingly high. A tendency to reinforced storage in organs …

Pharmakologisch-aktive polymere, 19. Polymere mit kovalent gebundenem streptomycinsulfat

A number of acryl and methacryl derivatives of different sulfanilamides (1a—I) were prepared and polymerized. The fixation of the sulfonamide to the polymerizable group was carried out directly, using the acryl- and methacrylamides, and by means of spacer groups, to favour the enzymatic or hydrolytic release of the drug moiety. Selected sulfonamide types of different pKA values were used, and the pH-dependant solubility of the corresponding polymers was studied. The monomeric acryloyl and methacryloyl sulfonamides were homopolymerized radically by AIBN. For distribution studies polysulfadiazineacrylamide, 14C-labelled in the main chain (2e'), was synthesized. Copolymerization with 2-methyls…

Pharmakologisch-aktive polymere, 18. Körperverteilung und ausscheidungsverhalten von monomerem und polymerem sulfadiazinacrylamid

Sulfadiazinacrylamid was absorbed after oral and intraperitoneal application in rats to a high extent; the absorption from the intraperitoneum was retarded. Glucose treatment delayed the absorption after both application forms. At comparatively high renal and enteral excretion rates the biological half life time of the monomer was estimated to 8 h. A tumouraffinity was not found but there were indications for a preferred storage in the RES. Poly[sulfadiazinacrylamide] was absorbed after intraperitoneal injection to a clear extent, where at the beginning of the treatment under simultaneous glucose load the absorption was delayed. 24 h after injection higher concentrations in metabolic organs…