1.
Agents Actions
; 10(3): 240-5, 1980 Jun.
Article
in English
| MEDLINE
| ID: mdl-6967685
ABSTRACT
A triglyceride of aspirin, A-45474: [2-(1,3-didecanoyloxy)-propyl]2-acetyloxybenzoate, was developed to reduce the direct gastric irritant properties of aspirin. Studies in the rat show that oral administration of A-45474 produces anti-inflammatory activity comparable to aspirin with negligible gastric irritation. Compared with aspirin, plasma salicylate levels of A-45474 appeared less rapidly and were more sustained. It is concluded that incorporation of aspirin in the 2-position of a triglyceride bearing n-decanoyl groups in the 1- and 3-positions markedly reduces the gastric irritating properties of aspirin while maintaining its pharmacological effects.
Subject(s)
Anti-Inflammatory Agents/pharmacology , Aspirin/analogs & derivatives , Stomach/drug effects , Administration, Oral , Animals , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Aspirin/adverse effects , Aspirin/metabolism , Aspirin/pharmacology , Biological Availability , Carrageenan/antagonists & inhibitors , Delayed-Action Preparations , Edema/drug therapy , Injections, Intravenous , Intestinal Absorption , Male , Rats , Salicylates/blood , Time Factors , Triglycerides/metabolism
2.
Arch Int Pharmacodyn Ther
; 202(1): 119-34, 1973 Mar.
Article
in English
| MEDLINE
| ID: mdl-4694349
Subject(s)
Benzazepines/pharmacology , Pyrazoles/pharmacology , Analgesia , Animals , Benzazepines/toxicity , Benzazepines/urine , Blood Glucose/metabolism , Blood Pressure/drug effects , Body Temperature/drug effects , Carbon Isotopes , Cats , Edema/prevention & control , Electroencephalography , Female , Granuloma/prevention & control , Heart Rate/drug effects , Ileum/drug effects , Lethal Dose 50 , Male , Mice , Motor Activity/drug effects , Muscle, Smooth/drug effects , Pyrazoles/toxicity , Pyrazoles/urine , Rats , Respiration/drug effects , Stomach/drug effects
3.
J Med Chem
; 15(1): 42-5, 1972 Jan.
Article
in English
| MEDLINE
| ID: mdl-5007094
Subject(s)
Anti-Inflammatory Agents/chemical synthesis , Benzazepines/chemical synthesis , Administration, Oral , Analgesics/administration & dosage , Analgesics/chemical synthesis , Analgesics/pharmacology , Analgesics/toxicity , Animals , Anti-Inflammatory Agents/administration & dosage , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/toxicity , Benzazepines/administration & dosage , Benzazepines/pharmacology , Benzazepines/toxicity , Edema/drug therapy , Lethal Dose 50 , Male , Pyrazoles/administration & dosage , Pyrazoles/chemical synthesis , Pyrazoles/pharmacology , Pyrazoles/toxicity , Rats , Rats, Inbred Strains , Structure-Activity Relationship
4.
J Med Chem
; 13(5): 968-70, 1970 Sep.
Article
in English
| MEDLINE
| ID: mdl-5458392