Oral pharmaceutical formulation in the form of a plurality of microcapsules for prolonged release of active principle(s) with slow solubility
US8652523B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jul 28, 2003 |
| Grant date | Feb 18, 2014 |
| Priority date | — |
| Expiry date | Nov 1, 2025 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61K9/5078
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The invention concerns microcapsules with prolonged release of active principles with low solubility, consisting of a core containing the active principle and coated with a polymer layer which controls the release of the active principle. The aim is that said oral microcapsules containing hardly soluble active principles, should have a coating film of sufficient thickness to ensure controlled permeability and should be adapted to industrial reproduction. This is achieved by the inventive microcapsules of mean diameter less than 1000 microns, and whereof the coating film contains a film-forming polymer (P1) insoluble in gastrointestinal tract fluids, a water-soluble polymer (P2), a plasticizer (PL), and optionally a lubricating surfactant (TA). Said microcapsules are characterized in that their coating films represents at least 3% p/p of dry matter, relative to their total weight and their core contains a hardly soluble active principle and a solubilizing agent (polyoxyethylene hydrogenated castor oil) which provides the core wherein it is contained with properties such that the behavior of the exposed core (non-coated) in a given dissolving test (TD), is as follows: release of 80% …
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.