Reduced-odor thiol compositions

Abstract

The present invention provides compositions for and methods of delivering a therapeutically-effective dose of a malodorous, sulfide or disulfide group-containing compound, for example glutathione (reduced) and / or glutathione disulfide, in a vehicle that is effective to reduce the unpleasant odor and / or taste of the compound. The invention further provides methods for reducing the amount of oxidation occurring when sulfide group-containing compounds, such as glutathione, are incorporated into sugar and or sugar-free hard candies without subjecting the glutathione to thermal and or moisture degradation where degradation is expressed as oxidation. The invention further provides vehicle compositions including the protected sulfide group-containing compounds and their use as medicaments. The sulfide group-containing compounds are protected from degradation by their dispersion into fats, oils, and / or fractionated or partially hydrogenated oils prior to their blending into the vehicle.

Description

FIELD OF THE INVENTION[0001]This invention relates to compositions for and methods of delivering a therapeutically-effective dose of a malodorous, sulfide (thiol) or disulfide group-containing compound, for example glutathione (reduced) and / or glutathione disulfide, in a vehicle that is effective to reduce the unpleasant odor and / or taste of the compound. The invention further relates to methods for reducing the amount of oxidation occurring when sulfide group-containing compounds, or thiols, such as glutathione, are incorporated into sugar and or sugar-free hard or soft candy vehicles.BACKGROUND OF THE INVENTION[0002]Glutathione (L-α-glutamyl-L-cysteinyl-glycine; GSH) is a well-known tri-peptide thiol found in virtually all cells. Glutathione disulfide (GSSG) is the oxidized dimer of glutathione. Glutathione functions to reduce the disulfide linkages of proteins and other molecules, as an antioxidant, and is an essential compound in the gamma-glutamyl cycle, which is thought to eff...

AI Technical Summary

Benefits of technology

[0012]The present invention further provides a method for preventing oxidation of thiol groups in thiol compounds, comprising blending a thiol compound for which oxidation is to be prevented into a fluidized fat or oil; and preventing the oxidation of the thiol compound. Preferably, the thiol compound is glutathione, ascorbate-2-phosphate, N-acetyl-L-cysteine, or derivatives or pharmaceutically acceptable salts of any of the foregoing, in any combination as described above.

[0016]Blends prepared as described may be used for preparing thiol compound-containing compositions having reduced sulfur odor and flavor. In one embodiment, a composition according to the present invention is prepared by blending a thiol compound into a fluidized fat or oil to produce a blend; adding the blend to a composition in preparation; and completing the preparation of the composition to produce a prepared thiol compound-containing composition having reduced sulfur odor and flavor.

[0020]The present invention further provides compound-containing compositions having reduced sulfur odor and flavor, comprising blends including one or more thiol compounds dispersed into fat or oil as described herein. In a preferred embodiment, the composition is a medicament and may be a cough drop or lozenge. The composition may be a hard or soft candy. In a preferred embodiment, the composition is a hard candy, the thiol compound is glutathione, the oil or fat is Paramount C, the ratio of glutathione to Paramount C is from about 55:45 to about 45:55, the glutathione has a particle size range of about 80 to about 120 microns, the carbohydrate is isomalt, and the residual water content is about 3.5% or less.

Problems solved by technology

Thiol-containing compounds, however, are notorious for their unpleasant odor and taste and so the use of thiol compounds such as glutathione in oral and nasal formulations has not been well received.

Furthermore, the sulfurous taste and smell of thiol compounds like glutathione increases with the amount of oxidation.

However, such compounds are highly prone to oxidative degradation.

This fact prevents the easy incorporation of thiol compounds into oral or nasal vehicles in highly reduced form.

Glutathione cannot be added to a candy product vehicle during production in a water solution do to its instability in water.

The thiol compounds tend to become oxidized during the product preparation phase and are thus not available in the final product to the patient in their more effective, highly reduced form.