Effects of some inhibitors on the nitrosation of drugs in human gastric juice.
The nitrosation of several drugs under simulated stomach conditions was only weakly inhibited by the beverages studied. With easily and rapidly nitrosatable drugs, such as aminophenazone or piperazine, administered orally, the use of an inhibitor of nitrosation is to be recommended. Of all the substances investigated, ascorbic acid should be regarded as the best inhibitor because of its pronounced activity at the pH values occurring in the stomach and its lack of toxic effects. We would like to propose that the drugs under consideration should be made up to contain a sufficient amount of ascorbic acid.
D000632:Aminopyrine / Q000008:administration & dosage / Q000378:metabolism*; D001205:Ascorbic Acid / Q000494:pharmacology; D001515:Beer; D003069:Coffee; D003545:Cysteine / Q000494:pharmacology; D005750:Gastric Juice / Q000378:metabolism*; D006801:Humans; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D009573:Nitrites / Q000037:antagonists & inhibitors*; D009602:Nitrosamines / Q000096:biosynthesis; D009603:Nitroso Compounds / Q000096:biosynthesis*; D010879:Piperazines / Q000008:administration & dosage / Q000378:metabolism*; D013451:Sulfonic Acids / Q000494:pharmacology; D013634:Tannins / Q000494:pharmacology; D013662:Tea; D014920:Wine
D003069:Coffee; D009573:Nitrites; D009602:Nitrosamines; D009603:Nitroso Compounds; D010879:Piperazines; D013451:Sulfonic Acids; D013634:Tannins; D013662:Tea; D000632:Aminopyrine; D003545:Cysteine; D001205:Ascorbic Acid