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Details for Patent: 5,891,471

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Details for Patent: 5,891,471

Title: Pharmaceutical multiparticulates
Abstract:A process for the manufacture of particles comprises mechanically working a mixture of a drug and a hydrophobic and/or hydrophilic fusible carrier in a high speed mixture so as to form agglomerates, breaking the agglomerates to give controlled release particles and optionally continuing the mechanical working with the optional addition of a low percentage of the carrier or diluent.
Inventor(s): Miller; Ronald Brown (Basel, CH), Leslie; Stewart Thomas (Cambridge, GB2), Malkowska; Sandra Therese Antoinette (Cambridge, GB2), Knott; Treavor John (Essex, GB2), Challis; Deborah (Kent, GB2), Prater; Derek Allan (Cambridge, GB2), Heafield; Joanne (Cambridge, GB2)
Assignee: Euro-Celtique, S.A. (Luxembourg, LU)
Filing Date:Feb 27, 1996
Application Number:08/607,851
Claims:1. Pharmaceutical particles of an opioid analgesic, which provide a time to peak plasma level of said opioid in about 2 to about 6 hours after administration, produced by a process comprising the steps of:

(a) mechanically working in a high-speed mixer, a mixture of said opioid analgesic in particulate form and a particulate, hydrophobic and/or hydrophilic 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 agglomerates;

(b) breaking down the agglomerates to give controlled release particles; and optionally

(c) continuing mechanically working optionally with the addition of a low percentage of the carrier or diluent.

2. Pharmaceutical particles according to claim 1 wherein said particles have a size range of about 0.5 to about 2 mm.

3. Pharmaceutical particles according to claim 1, wherein said hydrophobic carrier is at least 25 percent by weight of the total amount of ingredients added.

4. Pharmaceutical particles according to claim 1, wherein said hydrophobic carrier is at least about 45 percent by weight of the total amount of ingredients added.

5. Pharmaceutical particles according to claim 1, wherein during the mechanical working, step (c), heat is supplied thereto by microwave radiation.

6. Pharmaceutical particles according to claim 5, wherein only part of the heating is supplied by microwave radiation.

7. Pharmaceutical particles according to claim 1, wherein said opioid analgesic is morphine, tramadol, hydromorphone, oxycodone, diamorphine or a pharmaceutically acceptable salt thereof.

8. Pharmaceutical particles according to claim 1, wherein said particles provide a plasma concentration of said opioid analgesic effective to provide an analgesic effect for about 24 hours after administration.

9. Pharmaceutical particles according to claim 1, wherein said opioid analgesic comprises from about 1% to about 90% of said particles.

10. Pharmaceutical particles according to claim 9, wherein the hydrophobic fusible carrier comprises from about 10% to about 99% of said particles.

11. Pharmaceutical particles according to claim 10, wherein said opioid analgesic is morphine sulphate and said hydrophobic fusible carrier is hydrogenated vegetable oil, said morphine and said hydrogenated vegetable oil being present in a ratio of about 1.1:1 to about 1.25:1.

12. The pharmaceutical particles according to claim 10, wherein said hydrophilic agent is PEG which comprises from about 0.047% to about 0.6% of said mixture.

13. Pharmaceutical particles according to claim 10, wherein said opioid analgesic is tramadol hydrochloride and said hydrophobic fusible carrier is hydrogenated vegetable oil, said tramadol and said hydrogenated vegetable oil being present in a ratio of about 3:1.

14. Pharmaceutical particles according to claim 10, wherein said opioid analgesic is diamorphine hydrochloride and said hydrophobic fusible carrier is hydrogenated vegetable oil, said diamorphine and said hydrogenated vegetable oil being present in a ratio of about 1:1.

15. Pharmaceutical particles according to claim 1, wherein said release control component is selected from the group consisting of polyethylene glycol, dicalcium phosphate, calcium sulfate, talc, colloidal anhydrous silica, lactose, poloxamers, microcrystalline cellulose, starch, hydroxypropyl-cellulose and hydroxypropylmethylcellulose.

16. Pharmaceutical particles according to claim 1, wherein the particles further comprise a release control component selected from the group consisting of a water soluble fusible material, a particulate soluble organic material, a particulate soluble inorganic material, a particulate insoluble organic material, a particulate insoluble inorganic material, and mixtures thereof.

17. Pharmaceutical particles according to claim 1, wherein said particles are compressed into a tablet.

18. Pharmaceutical particles according to claim 1, wherein said particles are contained in a capsule.

19. Pharmaceutical particles according to claim 1, wherein said agglomerates further comprise a release control component comprising a water-soluble fusible material or a particulate, soluble or insoluble organic or inorganic material.

20. Pharmaceutical particles according to claim 1, wherein said process further comprises the step of repeating steps (c) one or more times.

21. Pharmaceutical particles according to claim 1, wherein said high-speed mixer is a high-shear mixer.

22. Pharmaceutical particles according to claim 1, wherein said high-speed mixer is a Collette Vactron Mixer or equivalent.

23. Pharmaceutical particles according to claim 1, wherein said process further comprises the step of repeating steps (b) one or more times.
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