Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Capsules
Patent
1992-03-10
1995-05-30
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Capsules
424435, 424489, 424464, A61K 948
Patent
active
054199158
ABSTRACT:
The present invention relates to a medicament with an analgesic, antipyretic and/or antiphlogistic action based on a salicylic acid derivative. The prior art has constantly sought alternatives for active components such as acetyl salicylic acid (ASS) and ethenzamide in order to prevent incompatibility, or provide simpler and better, rapidly acting substances in the most varied administration forms. The invention has surprisingly proved that ethenzamide is very rapidly and completely metabolized in the human body to 2-ethoxybenzoic acid. Ethenzamide is only a pro-drug. A metabolization to salicylamide was exluded. It was also possible to prove the analgesic action of 2-ethoxybenzoic acid. It is correlated with the serum levels and is maintained for longer than 8 hours. 2-ethoxybenzoic acid is very rapidly resorbed. The serum maxima were reached after only 30 minutes and 2-ethoxybenzoic acid can still be detected in the serum after 24 hours. These characteristics make 2-ethoxybenzoic acid an ideal analgesic with a rapid action, which has no influence on blood clotting. The single doses can be reduced due to the higher bioavailability. Due to the physicochemical characteristics of 2-ethoxybenzoic acid the use in the form of a solution is possible, so that besides solid medicament forms for oral and rectal administration, it is also possible to prepare and use liquid formulations, such as dropping or injection solutions.
REFERENCES:
patent: 3681445 (1922-08-01), Ruyle
patent: 3859338 (1975-01-01), Engel
patent: 3953496 (1976-04-01), Mori et al.
patent: 4055574 (1977-10-01), Ackrell
patent: 4672066 (1987-06-01), Carson et al.
Bertholdt Heinz
Hartl Rudolf
Lieb Herbert
Michalczyk Dieter
Benston, Jr. William E.
Page Thurman K.
R. Pfleger Chemische Fabrik GmbH
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