Oral formulation of lipid soluble thiamine, lipoic acid,...

A - Human Necessities – 61 – K

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A61K 9/20 (2006.01) A61K 9/48 (2006.01)

Patent

CA 2541990

A formulation comprised of four active components which are a lipid soluble thiamine, lipoic acid, arginine a-ketoglutarate, and a creatine derivative for oral administration is disclosed. The active components may be combined with excipient materials in such a way that those materials provide for an immediate release of a first portion of the active ingredients from the formulation following by a gradual release of any remaining active ingredients in a manner which makes it possible to (1) quickly obtain a therapeutic level of the active ingredients; and (2) substantially increase the period of time over which therapeutic levels of the active ingredients are maintained relative to a quick release formulation. These features make it possible to use the formulation to obtain a range of beneficial effects including reducing serum glucose levels and maintaining those reduced glucose levels over time to treat diabetic polyneuropathy as well as improving circulation and increasing muscle performance.

La présente invention concerne une formulation constituée de quatre composants actifs : la thiamine liposoluble, l'acide lipoïque, l'arginine .alpha.-cétoglutarate, et un dérivé de créatine pour une administration par voie orale. Les composants actifs peuvent être combinés avec des excipients, de telle sorte que ces excipients permettent une libération immédiate d'une première partie des principes actifs de la formulation, puis une libération progressive de n'importe quel principe actif restant, de telle sorte qu'il soit possible (1) d'obtenir rapidement un niveau thérapeutique de principes actifs; et (2) d'augmenter sensiblement le laps de temps durant lequel les niveaux thérapeutiques des principes actifs sont conservés par rapport à une formulation à libération rapide. Ces caractéristiques permettent d'utiliser ladite formulation pour obtenir une gamme effets bénéfiques, parmi lesquels, la réduction des niveaux de glucose sérique et le maintien de ces niveaux de glucose réduits dans le temps, pour traiter une polyneuropathie diabétique, ainsi que pour améliorer la circulation et l'augmentation de la performance musculaire.

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