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Medicament with an analgesic, antipyretic and/or antiphlogistic action and use of 2-ethoxybenzoic acid

机译:具有止痛,解热和/或消炎作用的药物,并使用2-乙氧基苯甲酸

摘要

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.
机译:基于水杨酸衍生物的具有止痛,解热和/或消炎作用的药物技术领域本发明涉及基于水杨酸衍生物的具有止痛,解热和/或消炎作用的药物。现有技术一直在寻求活性成分例如乙酰水杨酸(ASS)和乙酰胺的替代物,以防止不相容性,或者以最多样化的给药形式提供更简单,更好,快速作用的物质。令人惊讶地,本发明证明了乙酰胺在人体内非常迅速且完全代谢为2-乙氧基苯甲酸。乙酰胺只是一种前药。排除代谢为水杨酰胺。也可以证明2-乙氧基苯甲酸的镇痛作用。它与血清水平相关,并维持超过8小时。 2-乙氧基苯甲酸非常迅速地被吸收。仅在30分钟后即可达到血清最大值,而24小时后仍可在血清中检测到2-乙氧基苯甲酸。这些特性使2-乙氧基苯甲酸具有快速作用的理想镇痛药,而不会影响血液凝结。由于较高的生物利用度,可以降低单剂量。由于2-乙氧基苯甲酸的物理化学特性,可以以溶液形式使用,因此除了用于口服和直肠给药的固体药物形式外,还可以制备和使用液体制剂,例如滴剂或注射剂。

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