Alcohol-resistant sustained-release oral pharmaceutical form based on microgranules
Inventors
Herry, Catherine • Trichard-Trolet, Laury
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-9492397-B2
Publication Date
2016-11-15
Expiration Date
Abstract
Oral pharmaceutical form containing microgranules for the sustained release of at least one active principle, including a neutral carrier that is insoluble in water or in an alcohol solution, or a neutral carrier rendered insoluble in water or an alcohol solution, comprising at least one first mounting layer containing at least one active principle and optionally a pharmaceutically acceptable binding agent, wherein the whole comprises at least one coating based on at least one hydrophobic polymer.
Core Innovation
The invention relates to preventing or delaying release of an active principle from a pharmaceutical composition in the presence of alcohol with concomitant consumption of alcohol. It delivers the active principle in an oral pharmaceutical form containing sustained-release microgranules constructed to resist alcohol-triggered release, thereby addressing dose dumping concerns.
Each microgranule comprises a neutral core rendered insoluble in water and in an alcohol solution, where the neutral core consists essentially of materials that are soluble in water and in an alcohol solution and are directly covered with one or more layers of material selected from cellulose, microcrystalline cellulose, phosphate derivatives, silica and silicate derivatives, titanium dioxide, waxes, shellac, polyvinyl acetate and/or phthalate, and lactic and glycolic acid polymers. The microgranule also includes an active layer containing the active principle and a pharmaceutically acceptable binder.
The microgranule further includes a coating layer comprising a hydrophobic polymer. The invention defines a performance criterion for preventing alcohol-enhanced release: the percentage of active principle released after 2 h in an acid-alcohol medium of 0.1 N HCl containing alcohol and a quantity of ethanol between 4% and 30% must be not more than 15 points, 15% in absolute value, greater than that released in an acid medium of 0.1 N HCl, while the neutral carrier is a spherical or quasi spherical inert carrier of size between 50 μm and 3 mm.
Claims Coverage
Independent claim clm-00001 provides one inventive feature set for preventing or delaying release in alcohol consumption conditions using sustained-release microgranules with a specifically structured neutral insoluble core, an active layer with binder, and a hydrophobic polymer coating, together with defined release performance in a 0.1 N HCl plus ethanol (4%–30%) acid-alcohol medium.
Alcohol-resistant sustained-release microgranule method using insoluble neutral core and hydrophobic coating
A method for preventing or delaying release of an active principle from a pharmaceutical composition in the presence of alcohol with concomitant consumption of alcohol, by delivering the active principle in an oral pharmaceutical form containing sustained-release microgranules, each microgranule comprising a neutral core rendered insoluble in water and in an alcohol solution; an active layer comprising the active principle and a pharmaceutically acceptable binder; and a coating layer comprising a hydrophobic polymer; wherein the percentage of active principle released after 2 h in an acid-alcohol medium of 0.1 N HCl containing alcohol and ethanol between 4% and 30% is not more than 15 points (15% in absolute value) greater than that released in 0.1 N HCl acid alone; and the neutral carrier is spherical or quasi spherical inert carrier of size between 50 μm and 3 mm.
The provided independent claim coverage centers on an alcohol-resistant sustained-release approach in oral microgranules that combines an insoluble neutral core, an active layer with binder, and a hydrophobic polymer coating, with a quantitative release limitation after 2 h in a 0.1 N HCl/ethanol (4%–30%) acid-alcohol medium relative to acid alone.
Stated Advantages
Prevents or delays release of the active principle in the presence of alcohol during concomitant alcohol consumption.
Limits alcohol-enhanced release after 2 h in an acid-alcohol medium (0.1 N HCl with ethanol 4%–30%) to not more than 15 points (15% absolute) greater than release in acid medium alone.
Documented Applications
Oral pharmaceutical use of sustained-release microgranules to manage active principle release when alcohol is present and consumed.
Interested in licensing this patent?