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Publication Number
US-9877925-B2
Publication Date
2018-01-30
Expiration Date
Abstract
A sustained release oral pharmaceutical form suitable for single daily dose administration has a neutral microgranule coated with a mounting layer of active ingredient and pharmaceutically acceptable binder; and a coating layer of a hydrophobic coating polymer of a non-water soluble cellulose derivative, and at least 20% of inert load in relation to dry weight of hydrophobic coating polymer. The pharmaceutical form has improved resistance to rapid release of active ingredient, particularly in the presence of alcohol.
Core Innovation
A once a day sustained release pharmaceutical formulation is provided in granules having a neutral carrier and a center toward the periphery structure. From the center toward the periphery, the granules comprise a neutral carrier, at least one mounting layer comprising an active ingredient and a pharmaceutically acceptable binder, and a sustained-release coating layer.
The sustained-release coating layer comprises a hydrophobic coating polymer selected from non-water soluble cellulose derivatives. The formulation further requires at least 20% of talk in relation to the dry weight of the hydrophobic coating polymer, such that immediate release induced by consumption of alcohol during administration is avoided or limited.
The formulation is defined in terms of alcohol-induced release limitation during administration of a once a day sustained release pharmaceutical formulation. The described granule construction, including the hydrophobic non-water soluble cellulose-derivative polymer and the specified talk content relative to hydrophobic coating polymer dry weight, is presented as maintaining sustained release across ethanol-containing conditions.
Claims Coverage
The independent claim covers a method for avoiding or limiting immediate release induced by alcohol during administration of a once-a-day sustained-release formulation, with granules structured as a neutral core, an active-ingredient mounting layer with a binder, and a sustained-release coating layer. The main inventive requirements include a hydrophobic coating polymer selected from non-water soluble cellulose derivatives and a talk requirement of at least 20% relative to the hydrophobic coating polymer dry weight.
Alcohol during administration limiting immediate release in once-a-day sustained release formulation
A method for avoiding or limiting immediate release of an active ingredient induced by the consumption of alcohol during the administration of a once a day sustained release pharmaceutical formulation, comprising consuming alcohol during the administration of the pharmaceutical formulation.
Center-to-periphery granule structure with neutral carrier and mounting layer
The pharmaceutical formulation comprises granules which comprise, from the center toward the periphery: a neutral carrier; at least one mounting layer comprising an active ingredient and a pharmaceutically acceptable binder.
Sustained-release coating layer with non-water soluble cellulose derivatives and talk threshold
A sustained-release coating layer comprising a hydrophobic coating polymer selected from non-water soluble cellulose derivatives, and at least 20% of talk in relation to the dry weight of the hydrophobic coating polymer.
Overall, the claim requires combining alcohol during administration with a once-a-day sustained-release granule architecture (neutral carrier plus active-ingredient mounting layer with binder) and a sustained-release coating that uses non-water soluble cellulose-derivative hydrophobic polymer together with a specified talk content relative to hydrophobic polymer dry weight.
Stated Advantages
Avoiding or limiting immediate release of an active ingredient induced by the consumption of alcohol during administration of the once a day sustained release pharmaceutical formulation.
Documented Applications
Administration of a once a day sustained release pharmaceutical formulation to avoid or limit alcohol-induced immediate release of an active ingredient.
Morphine sulfate microgranules presented in the document as alcohol-resistant sustained release examples.
Diltiazem microgranules presented in the document as ethanol resistance dependent on meeting the talk-related coating requirements.
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