Composition for promoting vascular smooth muscle relaxation

A - Human Necessities – 61 – K

Patent

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Details

A61K 47/10 (2006.01) A61K 31/21 (2006.01)

Patent

CA 2573386

A composition for topical application to a part of the body comprises a vasodilator, for example glyceryl trinitrate, as active ingredient dissolved in a blend of volatile and non-volatile solvents of different solvating capacities for the vasodilator. The vasoldator is present in the composition at a concentration at or slightly below saturation, whereby evaporation of the volatile solvent in use will maintain the vasodilator at saturated or super- saturated concentrations in the residue, whereby the vasodilator will become saturated or supersaturated in the solvent remaining and, as the active ingredient passes through the skin and is absorbed in the bloodstream, and thus becomes depleted in the residual composition, continuing evaporation of volatile solvent will maintain the active ingredient substantially at saturation or supersaturation level in the residual composition throughout the major part of the absorption phase, thereby maximising absorption levels but at a moderate dosage level.

La présente invention concerne une composition pour application topique sur une partie du corps, ladite composition comprenant un vasodilatateur, par exemple le trinitrate de glycéryle, en tant que principe actif dissous dans un mélange de solvants volatiles et non-volatiles de différentes capacités solvantes pour le vasodilatateur. Le vasodilatateur est présent dans la composition à une concentration de ou légèrement inférieure à la saturation, moyennant quoi, en utilisation, l~évaporation du solvant volatile maintiendra le vasodilatateur à des concentrations saturées ou super-saturées dans le résidu, moyennant quoi le vasodilatateur deviendra saturé ou super-saturé dans le solvant restant et, à mesure que le principe actif passe à travers la peau et est absorbé dans le courant sanguin, et ainsi s~épuise dans la composition résiduelle, l~évaporation continuelle du solvant volatile maintiendra le principe actif pratiquement à un niveau de saturation ou de super-saturation dans la composition résiduelle tout au long de la plus grande partie de la phase d~absorption, portant au maximum les niveaux d~absorption mais à un niveau de dosage modéré.

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