申请人:——
公开号:US06696419B1
公开(公告)日:2004-02-24
Inflammation is affected by topical application of a boron containing compound/complex in which a central tetrahedral boron atom is covalently bound to four ligands. At least one of the ligands preferably includes an oxygen, nitrogen, carbon, or sulfur atom, and preferably all four ligands include at least one such atom. Preferred ligands are saccharides and amino acids, including fructose, sorbitol, mannitol, xylitol, sorbose, serine and threonine. Especially preferred ligands have a conformation with at least two hydroxyl groups, or one hydroxyl group and one amino group in a 1,2- and a 1,3-position relative to each other, providing a high association constant in the range of about 3,000 and about 20,000. The compounds/complexes are preferably provided in formulations which provide good transdermal delivery, including appropriate solvent systems, microemulsions, liposomes. Particularly targeted inflammations are those of the joints and skin, including bums such as sunburn.
一种含硼化合物/复合物的局部应用会影响炎症,其中一个中心四面体硼原子与四个配体共价结合。至少一个配体最好包括氧、氮、碳或硫原子,而且最好所有四个配体都包含至少一个这样的原子。优选的配体是糖类和氨基酸,包括果糖、山梨醇、甘露醇、木糖醇、山梨糖、丝氨酸和苏氨酸。特别优选的配体具有至少两个羟基或一个羟基和一个氨基在1,2-和1,3-位置相对排列的构象,提供约3,000至约20,000范围内的高关联常数。这些化合物/复合物最好以提供良好经皮递送的配方形式提供,包括适当的溶剂体系、微乳液、脂质体。特别针对的炎症是关节和皮肤的炎症,包括晒伤等。