Fatty-acid monoesters of estrogens for the treatment of obesity and/or overweight
申请人:LABORATORIOS S.A.L.V.A.T., S.A.
公开号:EP0771817A2
公开(公告)日:1997-05-07
The estrogen is selected from the group consisting of estrone, diethylstilbestrol, estriol, estradiol and ethinyl estradiol; the fatty acid is selected from the group consisting of oleic, linoleic, linolenic, stearic, palmitic, palmitoleic and arachidonic acids. They mimic the function of estrone monooleate, as a signal that informs the brain of the size of fat tissue mass. Preferred compositions for intravenous injection comprise the monoester incorporated in a lipidic suspension, prepared from lipoproteins or from liposome components such a soy oil and egg phospolipids. When administered to rats with a 15% of total adipose tissue, they produce weight reduction of about 10%, by a new and unexpected mechanism. They are useful for the treatment of obesity and/or overweight in mammals, with the advantages of high efficacy and low toxicity.
雌激素选自雌酮、己烯雌酚、雌三醇、雌二醇和炔雌醇组成的组;脂肪酸选自油酸、亚油酸、亚麻酸、硬脂酸、棕榈酸、棕榈油酸和花生四烯酸组成的组。它们模仿单油酸雌酮的功能,作为一种信号,告知大脑脂肪组织的大小。用于静脉注射的优选组合物包括掺入脂质悬浮液中的单酯,该悬浮液由脂蛋白或脂质体成分(如大豆油和鸡蛋磷脂)制备而成。当给总脂肪组织含量为 15%的大鼠用药时,它们通过一种意想不到的新机制使体重减轻约 10%。它们具有高效、低毒的优点,可用于治疗哺乳动物的肥胖和/或超重。