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Details for Patent: 5,843,480

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Details for Patent: 5,843,480

Title: Controlled release diamorphine formulation
Abstract:A controlled-release pharmaceutical preparation comprising diamorphine, or a pharmaceutically acceptable salt thereof.
Inventor(s): Miller; Ronald Brown (Basel, CH), Leslie; Stewart Thomas (Cambridge, GB2), Prater; Derek Allan (Milton, GB2), Knott; Trevor John (Wickford, GB2), Mohammad; Hassan (Haslingfield, GB2)
Assignee: Euro-Celtique, S.A. (Luxembourg, LU)
Filing Date:Dec 27, 1996
Application Number:08/774,229
Claims:1. A controlled release, storage stable solid pharmaceutical preparation comprising a controlled release matrix comprised of a particulate, hydrophobic, fusible carrier or diluent having a melting point ranging from about 35.degree. to 150.degree. C., and an effective amount of diamorphine or a pharmaceutically acceptable salt thereof, said controlled release matrix in a form selected from the group consisting of multiparticulates, granules and controlled release seeds, that is suitable for administration at time intervals ranging from about 12 to about 24 hours, said pharmaceutical preparation being prepared without water and retaining substantially all of the incorporated diamorphine after at least six months of storage at 30.degree. C., relative to a preparation that has not undergone said storage, said preparation exhibiting no substantial difference in in-vitro dissolution rate, as measured by Ph. European Paddle method at 100 rpm in 900 ml of aqueous buffer at pH 4.5 at 37.degree. C., relative to said preparation that has not undergone said storage.

2. The controlled release, storage stable solid pharmaceutical preparation of claim 1, further comprising conventional capsulating excipients.

3. The controlled release, storage stable solid pharmaceutical preparation of claim 1 comprising a tablet comprising said multiparticulates, granules or controlled-release seeds in compressed form.

4. The preparation of claim 3, comprising conventional tableting excipients.

5. The controlled-release, storage stable solid pharmaceutical preparation according to claim 1 which has a dissolution rate as follows:

6. The controlled release, storage stable solid pharmaceutical preparation according to claim 1, wherein the release rate is as follows:

7. The controlled release, storage stable solid pharmaceutical preparation according to claim 1, wherein the release rate is as follows:

8. A preparation according to claim 1, comprising an amount of diamorphine or salt thereof sufficient for up to 24 hours dosing.

9. A preparation according to claim 1, which provides for controlled-release of the diamorphine or salt such that it is suitable for 12 hourly administration.

10. A preparation according to claim 1, which provides for controlled-release of the diamorphine or salt such that it is suitable for 24 hourly administration.

11. A storage stable sustained-release diamorphine pharmaceutical preparation prepared by a process comprising the steps of mechanically working, in a high shear mixer, and without water, a mixture of diamorphine or pharmaceutically active salt thereof in particulate form and a particulate, hydrophobic, fusible carrier or diluent having a melting point from 35.degree. to 150.degree. C., at a speed and energy input which allows the carrier or diluent to melt or soften whereby it forms a matrix of hydrophobic fusible carrier or diluent containing an effective amount of diamorphine or salt thereof dispersed therein to produce a storage stable, sustained-release pharmaceutical preparation.

12. The pharmaceutical preparation of claim 11, wherein said process further comprises the step of adding to said mixture a release modifying component comprising a water soluble, fusible material or a particulate, soluble or insoluble organic or inorganic material.

13. Pharmaceutical sustained-release multiparticulates containing diamorphine or a salt thereof prepared by a process comprising the steps of:

(a) mechanically working in a high-shear mixer, a mixture of an effective amount of diamorphine or a salt thereof in particulate form and a particulate, hydrophobic, fusible carrier or diluent having a melting point from 35.degree. to 150.degree. C., without water, at a speed and energy input which allows the carrier or diluent to melt or soften, whereby it forms agglomerates; and

(b) breaking down from step (a) said agglomerates into a plurality of sustained-release multiparticulates.

14. A process according to claim 13, wherein said mixture further comprises a release modifying component comprising a water soluble fusible material, or a particulate soluble or insoluble organic or inorganic material.

15. A process according to claim 13, further comprising continuing mechanically working optionally with a further addition of low percentage of the carrier or diluent.

16. A process according to claim 13, comprising repeating step (b) up to five times.

17. A process according to claim 11, wherein the product is sieved or milled to obtain multiparticulates, granules or controlled-release seeds or particles of a desired size range.

18. A process according to claim 13, wherein said multiparticulates or granules are further processed by filling into capsules.

19. A process according to claim 13, wherein said multiparticulates, granules or controlled-release seeds or particles are compressed into tablets.

20. A process according to claim 13, comprising mixing said multiparticulates, granules or controlled-release seeds or particles, with conventional tableting excipients.

21. A method of treating a patient suffering from pain which comprises administering to the patient a storage stable, controlled release preparation comprising an effective amount of diamorphine or a pharmaceutically acceptable salt thereof and a controlled release matrix in a form selected from the group consisting of multiparticulates, granules and controlled release seeds, that is suitable for administration at time intervals ranging from about 12 to about 24 hours, said pharmaceutical preparation being prepared without water and retaining substantially all of the incorporated diamorphine after at least six months of storage at 30.degree. C., relative to a preparation that has not undergone said storage, said preparation exhibiting no substantial difference in in-vitro dissolution rate, as measured by Ph. European Paddle method at 100 rpm in 900 ml of aqueous buffer at pH 4.5 at 37.degree. C., relative to said preparation that has not undergone said storage.

22. A method of treating a heroin addict by maintenance therapy, which comprises administering to the addict a storage stable preparation comprising an effective amount of diamorphine or a pharmaceutically acceptable salt thereof and a controlled release matrix in a form selected from the group consisting of multiparticulates, granules and controlled release seeds, that is suitable for administration at time intervals ranging from about 12 to about 24 hours, said pharmaceutical preparation being prepared without water and retaining substantially all of the incorporated diamorphine after at least six months of storage at 30.degree. C., relative to a preparation that has not undergone said storage, and that shows no substantial difference in in-vitro dissolution rate, as measured by Ph. European Paddle method at 100 rpm in 900 ml of aqueous buffer at pH 4.5 at 37.degree. C., relative to said preparation that has not undergone said storage.

23. The storage stable, controlled release preparation of claim 1 wherein the preparation is storage stable for at least three months.

24. The storage stable, controlled release preparation of claim 1 wherein the preparation shows no substantial change in the content of a substance selected from the group consisting of diamorphine, 6-O-acetylmorphine, morphine or a salt thereof, during storage at 30.degree. C. for at least six months.

25. The preparation of claim 1, wherein said preparation comprises a release modifying component selected from the group consisting of a water-soluble fusible material, a particulate soluble and an insoluble organic or inorganic material.

26. The preparation of claim 1, comprising said controlled release matrix enclosed in a capsule suitable for oral administration.
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