US 7,063,864 B1 · Morphine sulphate microgranules, method for preparing same and compositions containing same

Abstract

The present invention concerns a novel sustained-release oral formulation of morphine sulphate in the form of microgranules. Each microgranule comprises a neutral support grain coated with an active layer and with a sustained-release layer, characterized in that the sustained-release layer contains a copolymer of methacrylic acid and of methyl methacrylate ester, the relative proportion of the free carboxyl groups and of the ester groups of which is equal to 0.5 approximately, and a silica exhibiting a hydrophobic character. The present invention also concerns a process for preparing these microgranules which is carried out entirely in aqueous medium by emplacing on neutral support grains.

Claims16

Dependent claims

Sustained-release morphine sulphate microgranules each comprising a neutral support grain coated with an active layer and with a sustained-release layer, said sustained-release layer containing:

a copolymer of poly(ethylacrylate, methyl methacrylate, trimethylammonioethyl methacrylate chloride) 1:2:0.1;
a plasticizer;
and
a lubricant;
wherein said sustained-release layer further comprises a hydrophobic silica which represents 0.2 to 1% by weight of the microgranules and wherein said microgranules are devoid of any outer protective film.

2 more elements

Dependencies are inferred from the claim text.

Facts

Application

10/009,341Filed 8 Jun 2000

Priority

FR 99 072599 Jun 1999

Granted

20 Jun 2006

Term ends

Not estimatedThe source records don’t support an estimate.

Classification12 codes

A61K 9/5026
Organic macromolecular compounds: obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, polyacrylates
A61K 9/501
Wall or coating material: inorganic compounds
A61K 9/5078
Having two or more different coatings optionally including drug-containing subcoatings: with drug-free core
A61K 31/485
Quinolines; Isoquinolines: morphinan derivatives, e.g. morphine, codeine

Morphine sulphate microgranules, method for preparing same and compositions containing same

Life of this patent

Morphine sulphate microgranules, method for preparing same and compositions containing same

Life of this patent

Abstract

Claims16