Microcapsules for the controlled release of acetylsalicylic acid in the gastrointestinal environment
AssigneeFlamel Technologies
InventorsOlga Burguiere, Ahmad Yassine, Jean-Philippe Selles
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Abstract
The present invention relates to controlled-release microcapsules of acetylsalicylic acid which comprise particles of acetylsalicylic acid with a size of between 100 and 1000 .mu.m, coated with a coating material consisting of a mixture of a cellulosic film-forming polymeric derivative, an antiadherent, a plasticizer, a lubricant and a vinylic film-forming polymeric derivative. The invention further relates to a process for the preparation of said microcapsules.
Claims24
A process for the preparation of microcapsules for the controlled release of acetylsalicylic acid (ASA) in the gastrointestinal environment, said microcapsules being orally ingestible in a dose (D) and comprising particles of acetylsalicylic acid with a size of between 100 and 1000 .mu.m which are coated and designed so that, when ingested orally in a single administration of a dose D of between 75 and 320 mg of ASA, they induce moderate ASA absorption kinetics in vivo in man, extending over at least 24 hours, said ASA absorption being:
- less than or equal to 10% by weight of the absorbed fraction of D at a time t after ingestion of 0.4 hour,
- less than or equal to 50% by weight of the absorbed fraction of at t=3.9 hours, and
- less than or equal to 90% by weight of the absorbed fraction of D at t=23 hours, t being given to within .+-.10%, which process consists essentially in:
- a) preparing a coating composition by mixing a film-forming polymer (P.sub.1) insoluble in the gastrointestinal environment, a water-soluble polymer (P.sub.2), a solid lubricating filler and a hydrophobic plasticizer in a solvent system,
- b) applying the composition/solvent system mixture to particles of acetylsalicylic acid, and
- c) drying the resulting microcapsules.
Dependencies are inferred from the claim text.