| 摘要 |
NEW MATERIAL:Basic amino acid salt of 2-(2,6-dichloroanilino)phenylacetic acid (general name: Diclofenac). EXAMPLE:Diclofenac 1-lysine salt. USE:Antiphlogistic, analgesic and antipyretic agent for rectal administration. It can be absorbed rapidly through rectum, gives high concentration in blood, and also gives extremely low stimulation to mucous membranes. The distinctive character of this compound is that the side effects such as gastroenteric disorder of the Diclofenac Na salt for oral administation are improved by converting to a suppository preparation. PROCESS:The reaction of Diclofenac with a basis amino acid, e.g. lysine, arginine, histidine etc., in water-containing methanol gives a salt of formula I (Y is a group of formula II and n is 4 when lysine is used; Y is a group of formula III and n is 3 when arginine is used; Y is a group of formula IV and n is 1 when histidine is used). |
