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Use of 2-ethoxy benzoic acid for the manufacture of a medicament as analgesic, antipyretic, and/or antiphlogistic

机译:2-乙氧基苯甲酸在制造止痛,解热和/或消炎药中的用途

摘要

The present invention relates to a medicament with an analgesic, antipyretic and/or antiinflammatory effect based on a salicylic acid derivative. The state of the art is always searching for alternatives to active ingredients such as acetylsalicylic acid (ASA) and ethenzamide in order to eliminate intolerance or to be able to offer simpler and better ingredients, which act as rapidly as possible, for a wide variety of possible administrations. Surprisingly, the invention has now succeeded in demonstrating that ethenzamide is very rapidly and completely metabolised in the human body to 2-Ethoxybenzoic acid. Ethenzamide is only a prodrug. It was possible to rule out metabolism to salicylamide. It was likewise possible to demonstrate the analgesic effect of 2-ethoxybenzoic acid. It correlates with the serum levels and persists for more than 8 hours. 2-Ethoxybenzoic acid is very rapidly absorbed. The serum maxima are reached after only 30 minutes; 2-ethoxybenzoic acid is still detectable in the serum even after 24 hours. These properties make 2-ethoxybenzoic acid an ideal analgesic which has a rapid onset of action and which has no effect on blood coagulation. Since the bioavailability is higher, it is also possible to reduce the single doses. By virtue of the physicochemical properties of 2-ethoxybenzoic acid, use in the form of a solution is possible so that, besides solid drug forms for oral and rectal use, it is also possible to prepare and use liquid formulations such as solutions for administration as drops or by injection. IMAGE
机译:基于水杨酸衍生物的具有止痛,解热和/或抗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/或抗炎作用的药物。现有技术一直在寻找诸如乙酰水杨酸(ASA)和乙酰胺的活性成分的替代品,以消除不耐症或能够提供更简单,更好的成分,这些成分对于各种类型的人尽可能快地起作用。可能的主管部门。出人意料的是,本发明现在已经成功地证明了乙酰胺在人体中非常迅速且完全代谢为2-乙氧基苯甲酸。乙酰胺只是前药。有可能排除新陈代谢为水杨酰胺。同样有可能证明2-乙氧基苯甲酸的镇痛作用。它与血清水平相关并且持续超过8小时。 2-乙氧基苯甲酸非常迅速地被吸收。仅30分钟后即可达到血清最大值。即使在24小时后,血清中仍可检测到2-乙氧基苯甲酸。这些特性使2-乙氧基苯甲酸成为一种理想的镇痛药,它起效快并且对凝血没有影响。由于生物利用度较高,因此也有可能减少单剂量。由于2-乙氧基苯甲酸的物理化学性质,可以以溶液形式使用,因此,除了用于口服和直肠使用的固体药物形式外,还可以制备和使用液体制剂,例如溶液,用于给药。滴剂或注射剂。 <图像>

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