[Effect of novocaine incorporation into the structure of a water-soluble polymer on its pharmacological activity].
The topically anesthesizing action and acute toxicity of two polymetric derivatives of novocaine-celnovocaine and polynovocaine No 5 (PN-5) were studied. The polymeric derivatives differ in the orientation of the novocaine molecule with respect to the macro-molecule of the water-soluble polymer-the modified cellulose. In celnovocaine novocaine joins the macromolecule through the intermediary of diethylamino-ethanol nitrogen and in PN-5-through the intermediary of paraaminobenzoic acid nitrogen. The ratio of the polymer-carrier (mol. weight 20 000-26 000) to novocaine is 1:1. The chemical bonding between novacaine and modified cellulose potentiates ad prolongs the infiltrative and terminal anesthesia, without changing (PN-5) or lowering  (celnovocaine) the toxicity. The extent to which the action and duration of the effect, as well as changes in the toxicity depend upon the orientation of the novocaine molecule relative to the water-soluble polymer molecule.
D000818:Animals; D002266:Carboxymethylcellulose Sodium / Q000494:pharmacology; D003692:Delayed-Action Preparations; D004338:Drug Combinations; D006168:Guinea Pigs; D007928:Lethal Dose 50; D051379:Mice; D011108:Polymers / Q000494:pharmacology*; D011343:Procaine / Q000031:analogs & derivatives / Q000494:pharmacology* / Q000633:toxicity; D011817:Rabbits; D012995:Solubility; D013329:Structure-Activity Relationship
D003692:Delayed-Action Preparations; D004338:Drug Combinations; D011108:Polymers; D011343:Procaine; D002266:Carboxymethylcellulose Sodium
Vliianie vkliucheniia novokaina v strukturu vodorastvorimogo polimera na ego farmakolgicheskuiu aktivnost.