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Details for Patent: 6,572,885

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Details for Patent: 6,572,885

Title: Orally administrable opioid formulations having extended duration of effect
Abstract:Sustained release oral solid dosage forms of opioid analgesics are provided as multiparticulate systems which are bioavailable and which provide effective blood levels of the opioid analgesic for at least about 24 hours. A unit dose of the opioid analgesic contains a plurality of substrates including the opioid analgesic in sustained release form. The substrates have a diameter from about 0.1 mm to about 3 mm.
Inventor(s): Oshlack; Benjamin (New York, NY), Chasin; Mark (Manalapan, NJ)
Assignee: Euro-Celtique, S.A. (Luxembourg, LU)
Filing Date:Jun 26, 2001
Application Number:09/891,882
Claims:1. An oral analgesic dosage form for once-a-day administration, comprising (a)(i) inert pharmaceutically acceptable beads having a diameter from about 0.1 mm to 3 mm (ii) morphine or a pharmaceutically acceptable salt thereof disposed about the beads, and (iii) hydrophobic sustained-release material disposed about the morphine or pharmaceutically acceptable salt thereof, and (b) morphine or a pharmaceutically acceptable salt thereof in immediate release form; said dosage form providing a therapeutic effect for about 24 hours or more after oral administration to a human patient.

2. The dosage form of claim 1, wherein said hydrophobic material comprises an acrylic polymer.

3. The dosage form of claim 2, which comprises from about 5 mg to about 800 mg morphine.

4. The dosage form of claim 1, wherein the sustained-release beads release said morphine or pharmaceutically acceptable salt thereof at a rate that is independent of pH between pH 1.6 and 7.2.

5. The dosage form of claim 4, wherein the hydrophobic sustained-release material consists essentially of one or more ammonio methacrylate copolymers.

6. The dosage form of claim 5, wherein said hydrophobic sustained-release material is applied onto said beads as an aqueous dispersion of said ammonio methacrylate copolymers, and said beads are cured in order to obtain a stabilized release rate of said morphine or pharmaceutically acceptable salt thereof.

7. The dosage form of claim 1, wherein said beads and said morphine in immediate release form are contained in a gelatin capsule.

8. The dosage form of claim 1, which releases said morphine or pharmaceutically acceptable salt thereof at a rate such that after oral administration to a human, blood plasma levels of said morphine are maintained within the therapeutic range for about 24 hours.

9. The dosage form of claim 1, which provides effective steady-state blood plasma levels of said morphine for at least about 24 hours.

10. The dosage form of claim 1, wherein said morphine in immediate release form is 10% of said dosage form.

11. The dosage form of claim 6, wherein said morphine in immediate release form is 10% of said dosage form, and said dosage form provides effective steady-state blood plasma levels of said morphine for at least about 24 hours.

12. An oral analgesic dosage form for once-a-day administration, comprising (a) sustained release substrates comprising morphine or a pharmaceutically acceptable salt thereof and a hydrophobic material, said substrates having a diameter from about 0.1 mm to about 3 mm; and (b) morphine or a pharmaceutically acceptable salt thereof in immediate release form; said dosage form providing a therapeutic effect for about 24 hours or more after oral administration to a human patient.

13. The dosage form of claim 12, which provides effective steady-state blood plasma levels of said morphine for at least about 24 hours.

14. The dosage form of claim 12, wherein said immediate release portion of said morphine or pharmaceutically acceptable salt thereof is 10% of said unit dosage form.

15. The dosage form of claim 12, wherein said sustained-release substrates comprise (i) inert pharmaceutically acceptable beads having a diameter from about 0.1 mm to 3 mm (ii) morphine or a pharmaceutically acceptable salt thereof disposed about the beads, and (iii) said hydrophobic material being selected from the group consisting of one or more ammonio methacrylate copolymers, a hydrophobic cellulosic material, and mixtures thereof, said sustained-release substrates releasing said morphine or pharmaceutically acceptable salt thereof at a rate that is independent of pH between pH 1.6 and 7.2.

16. The dosage form of claim 15, wherein said hydrophobic material consists of one or more ammonio methacrylate copolymers.

17. The dosage form of claim 12, wherein said sustained release substrates comprise pharmaceutically acceptable matrices comprising said morphine or pharmaceutically acceptable salt thereof and a hydrophobic material.

18. A method for preparing an oral analgesic dosage form comprising (i) preparing sustained-release morphine multiparticulates by coating inert pharmaceutically acceptable beads having a diameter from about 0.1 mm to about 3 mm with morphine or a pharmaceutically acceptable salt thereof and thereafter overcoating said morphine-coated beads with sustained-release coating comprising a hydrophobic material; and (ii) combining an effective amount of said sustained-release morphine multiparticulates with an effective amount of said morphine or pharmaceutically acceptable salt thereof in immediate release form to obtain a dosage form which, upon oral administration to a human patient, provides a therapeutic effect for about 24 hours.

19. A method for treating a patient for pain, the method comprising administering to a patient once-a-day an oral analgesic dosage form comprising (a)(i) inert pharmaceutically acceptable beads having a diameter from about 0.1 mm to about 3 mm, (ii) morphine or a pharmaceutically acceptable salt thereof disposed about the beads, and (iii) hydrophobic sustained-release material disposed about the morphine; and (b) morphine or a pharmaceutically acceptable salt thereof in immediate release form; said dosage form providing a therapeutic effect for about 24 hours or more after oral administration to a human patient.

20. A method for treating a patient for pain, the method comprising administering to a patient once-a-day an oral analgesic dosage form comprising (a) sustained release substrates comprising morphine or a pharmaceutically acceptable salt thereof and a hydrophobic material, said substrates having a diameter from about 0.1 mm to about 3 mm; and (b) morphine or a pharmaceutically acceptable salt thereof in immediate release form; said dosage form providing a therapeutic effect for about 24 hours or more after oral administration to a human patient.

21. An oral analgesic dosage form for once-a-day administration, comprising (a) a therapeutically effective amount of morphine or a pharmaceutically acceptable salt thereof; (b) means for providing sustained release of a portion of said morphine or pharmaceutically acceptable salt thereof; and (c) means for providing immediate release of the remaining portion of said morphine or pharmaceutically acceptable salt thereof; said dosage form providing a therapeutic effect for about 24 hours or more after oral administration to a human patient.

22. A method for treating a patient for pain, the method comprising administering to a patient once-a-day an oral analgesic dosage form comprising: (a) a therapeutically effective amount of morphine or a pharmaceutically acceptable salt thereof; (b) means for providing sustained release of a portion of said morphine or said pharmaceutically acceptable salt thereof; and (c) means for providing immediate release of the remaining portion of said morphine or pharmaceutically acceptable salt thereof; said dosage form providing a therapeutic effect for about 24 hours or more after oral administration to a human patient.
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