Method and composition for stable and controlled delivery of...

A - Human Necessities – 61 – K

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A61K 9/20 (2006.01)

Patent

CA 2527133

The present invention provides stable encapsulated (-)-hydroxycitric acid ("HCA")~containing compositions and methods of making the same. A method is provided by which the hygroscopic salts of HCA in their relatively pure and active forms, including especially the potassium salt, but also including the sodium salt, are rendered non-hygroscopic and stable (that is, not prone to lactonization, not readily subject to attachment to ligands which inhibit absorption or lead to excretion, and so forth) such that these HCA salts might be included in dry delivery formats, liquid delivery and in controlled-release vehicles. The nonhygroscopic salts of HCA and its derivatives likewise may be protected against acid degradation, lactonization and undesirable ligand binding when exposed to acidic environments or other challenging conditions. The method taught herein can be employed to reduce the polar/ionic qualities of HCA salts and derivatives when presented to the intestinal lumen to provide advantages in absorption.

La présente invention concerne des compositions contenant un acide (-)-hydroxycitrique stable et encapsulé ("HCA") et des procédés de fabrication desdites compositions. Un procédé consiste à rendre les sels hygroscopiques de HCA dans leurs formes relativement pures et actives, spécialement le sel de potassium, mais également le sel de sodium, non hygroscopiques et stables, (à savoir ne risquant pas la lactonisation, et n'étant pas complètement soumis à une fixation à des ligands inhibant l'absorption ou entraînant l'excrétion) de manière que ces sels HCA puissent être inclus dans des formats d'administration secs, dans l'administration liquide et dans des excipients à libération contrôlée. Les sels non hygroscopiques de HCA et leurs dérivés peuvent être protégés contre la dégradation acide, la lactonisation et la liaison à des ligands indésirable lors de leur exposition à des environnements acides ou dans d'autres conditions difficiles. Le procédé de cette invention peut être mis en oeuvre pour réduire les qualités polaires/ioniques des sels HCA et leurs dérivés lors de leur présentation à la lumière intestinale afin d'apporter des avantages en termes d'absorption.

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