Analgesic composition for treatment of migraine headaches

• US 5,914,129 A
• Filed: 07/23/1996
• Issued: 06/22/1999
• Est. Priority Date: 07/23/1996
• Status: Expired due to Term

• Current Assignee: Alexander Mauskop
• Original Assignee: Alexander Mauskop
• Inventors: Mauskop, Alexander
• Primary Examiner(s): Dees, Jose' G.
• Assistant Examiner(s): Shelborne, Kathryne E.
• Application Number:
  US08/685,078
• Time in Patent Office: 1,064 Days
• Field of Search: 424/44, 424/682, 424/692, 424/464.5, 514/165, 514/224.5, 514/350, 514/568, 514/728, 514/812
• US Class Current: 424/464
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61P 25/06 Antimigraine agents

Abstract

Magnesium-containing analgesic compositions used for the alleviation of pain, in particular, migraine headache pain, and methods for using the same are described herein. The compositions consist essentially of an analgesic agent, a magnesium salt, a stimulant, optionally an effervescing agent, and a pharmacetically acceptable carrier or vehicle. The symptoms of migraine headache intended to be alleviated include nausea, unilateral pain, dizziness, pulsatile pain, worsening of pain by light physical activity, photophobia and phonophobia.

Claims

1. A pharmaceutical composition for the alleviation of pain, associated with migraine headache consisting essentially of a therapeutically effective amount of one or more magnesium salt, one or more stimulant selected from the group consisting of methamphetamine, deoxamphetamine, methylphenidate, pemoline, caffeine and mixtures thereof, and one or more analgesic agent selected from the group consisting of acetylsalicylic acid, acetaminophen, paracetamol, ibuprofen, ketoprofen, ketoconazole, indomethacin, diflunisol, naproxen, ketorolac, dichlophenac, tolmetin, sulindac, phenacetin, piroxicam. mefamanic acid, dextromethorphan, codeine, morphine, hydromorphine, levophanol, meperidine, meptazinol, propoxyphene, yropiram, buprenorphine, pentazocine, nalbuphine, butorphanol, tramadol, hydrocodone, oxycodone and methadone, pharmaceutically acceptable salts thereof, and mixtures thereof;

and a pharmaceutically acceptable carrier or vehicle, wherein the composition is orally administered.

2. The composition of claim 1, wherein at least one of the one or more analgesic agent is a non-opioid analgesic agent.

3. The composition of claim 2, wherein the non-opioid analgesic agent is selected from the group consisting of acetylsalicylic acid, acetaminophen, paracetamol, ibuprofen, ketoprofen, ketoconazole, indomethacin, diflunisol, naproxen, ketorolac, dichlophenac, tolmetin, sulindac, phenacetin, piroxicam, mefamanic acid, dextromethorphan, salicylates, pharmaceutically acceptable salts thereof, and mixtures thereof.

7. The composition of claim 1, wherein at least one of the one or more magnesium salt is a magnesium salt of an analgesic agent.

8. The composition of claim 7, wherein the magnesium salt of the analgesic agent is magnesium acetylsalicylate.

9. The composition of claim 1, wherein the one or more magnesium salt is present at a level ranging from about 5 to about 30 wt. %, and the one or more stimulant is present at a level ranging from about 1 to about 25%.

10. The composition of claim 1, wherein at least one of the one or more analgesic agent is a non-opioid analgesic agent and is present at a level ranging from about 10 to about 90 wt. %.

4. A pharmaceutical composition for the alleviation of pain, associated with migraine headache consisting essentially of a therapeutically effective amount of one or more magnesium salt, one or more stimulant, and one or more analgesic agent selected from the group consisting of acetylsalicylic acid, acetaminophen, paracetamol, ibuprofen, ketoprofen, ketoconazole, indomethacin, diflunisol, naproxen, ketorolac, dichlophenac, tolmetin, sulindac, phenacetin, piroxicam, mefamanic acid, dextromethor-han, codeine, morphine, hydromorohine, levophanol, meperidine, meptazinol, propoxyphene, propiram, buprenorphine, pentazocine, nalbuphine, butorphanol, tramadol, hydrocodone, oxycodone and methadone, pharmaceutically acceptable salts thereof, and mixtures thereof, wherein at least one of the one or more analgesic agent is an opioid analgesic agent;

and a pharmaceutically acceptable carrier or vehicle, wherein the composition is orally administered.

5. The composition of claim 4, wherein the opioid analgesic agent is selected from the group consisting of codeine, morphine, hydromorphine, levophanol, meperidine, meptazinol, propoxyphene, propiram, buprenorphine, pentazocine, nalbuphine, butorphanol, tramadol, hydrocodone, oxycodone and methadone, pharmaceutically acceptable salts thereof, and mixtures thereof.

11. The composition of claim 4, wherein the opioid analgesic agent is present at a level ranging from about 0.5 to about 20 wt. %.

6. A pharmaceutical composition for the alleviation of pain, associated with migraine headache consisting essentially of a therapeutically effective amount of one or more magnesium salt, one or more stimulant, and one or more analgesic agent selected from the group consisting of acetylsalicylic acid, acetaminophen, paracetamol, ibuprofen, ketoprofen, ketoconazole, indomethacin, diflunisol, na-roxen, ketorolac, dichlophenac, tolmetin, sulindac, phenacetin, piroxicam, mefamanic acid, dextromethorphan, codeine, morphine, hydromorphine, levophanol, meperidine, meptazinol, propoxyphene, propiram, buprenorphine, pentazocine, nalbuphine, butorphanol, tramadol, hydrocodone, oxycodone and methadone, pharmaceutically acceptable salts thereof, and mixtures thereof, wherein the one or more analgesic agent is a combination of a non-opioid analgesic agent and an opioid analgesic agent;

and a pharmaceutically acceptable carrier or vehicle, wherein the composition is orally administered.

12. The composition of claim 6, wherein the non-opioid analgesic agent is present at a level ranging from about 10 to about 90 wt. %, and the opioid analgesic agent that is present at a level ranging from about 0.5 to about 20 wt. %.

13. A pharmaceutical composition for the alleviation of pain, associated with migraine headache consisting essentially of a therapeutically effective amount of one or more magnesium salt, one or more stimulant selected from the group consisting of methamphetamine, deoxamphetamine, methylphenidate, pemoline, caffeine and mixtures thereof, one or more analgesic agent selected from the group consisting of acetylsalicylic acid, acetaminophen, paracetamol, ibuprofen, ketoprofen, ketoconazole, indomethacin, diflunisol, naproxen, ketorolac, dichlophenac, tolmetin, sulindac, phenacetin, piroxicam, mefamanic acid, dextromethorphan, codeine, morphine, hydromorphine, levophanol, meperidine, meptazinol, propoxyphene, propiram, buprenorphine, pentazocine, nalbuphine, butorphanol, tramadol, hydrocodone, oxycodone and methadone, pharmaceutically acceptable salts thereof, and mixtures thereof and one or more effervescing agent;

and a pharmaceutically acceptable carrier or vehicle, wherein the composition is orally administered.

14. The composition of claim 13, wherein at least one of the one or more analgesic agent is a non-opioid analgesic agent.

15. The composition of claim 14, wherein the non-opioid analgesic agent is selected from the group consisting of acetylsalicylic acid, acetaminophen, paracetamol, ibuprofen, ketoprofen, ketoconazole, indomethacin, diflunisol, naproxen, ketorolac, dichlophenac, tolmetin, sulindac, phenacetin, piroxicam, mefamanic acid, dextromethorphan, salicylates, pharmaceutically acceptable salts thereof, and mixtures thereof.

19. The composition of claim 13, wherein at least one of the one or more magnesium salt is a magnesium salt of an analgesic agent.

20. The composition of claim 19, wherein the magnesium salt of the analgesic agent is magnesium acetylsalicylate.

21. The composition of claim 13, wherein the one or more effervescing agent is selected from the group consisting of alkali or alkaline earth metal carbonates, bicarbonates and mixtures thereof.

22. The composition of claim 13, wherein at least one of the one or more magnesium salt is present at a level ranging from about 5 to about 30 wt. %, and the one or more stimulant is present at a level ranging from about 1 to about 25 wt. %.

23. The composition of claim 13, wherein at least one of the one or more analgesic agent is a non-opioid analgesic agent and is present at a level ranging from about 10 to about 90 wt. %.

26. The composition of claim 13, wherein the one or more effervescing agent is present at a level ranging from about 20 to about 80 wt. %.

16. A pharmaceutical composition for the alleviation of pain, associated with migraine headache consisting essentially of a therapeutically effective amount of one or more magnesium salt;

one or more stimulant;

one or more analgesic agent selected from the group consisting of acetylsalicylic acid, acetaminophen, paracetamol, ibuprofen, ketoprofen, ketoconazole, indomethacin, diflunisol, naproxen, ketorolac, dichlophenac, tolmetin, sulindac, phenacetin, piroxicam, mefamanic acid, dextromethorphan, codeine, morphine, hydromorphine, levophanol, meperidine, meptazinol, propoxypmhene, propiram, buprenorphine, pentazocine, nalbuphine, butorphanol, tramadol, hydrocodone, oxycodone and methadone, pharmaceutically acceptable salts thereof, and mixtures thereof, wherein at least one of the one or more analgesic agent is an opioid analgesic agent;

one or more effervescing agent; and

a pharmaceutically acceptable carrier or vehicle, wherein the composition is orally administered.

17. The composition of claim 16, wherein the opioid analgesic agent is selected from the group consisting of codeine, morphine, hydromorphine, levophanol, meperidine, meptazinol, propoxyphene, propiram, buprenorphine, pentazocine, nalbuphine, butorphanol, tramadol, hydrocodone, oxycodone and methadone, pharmaceutically acceptable salts thereof, and mixtures thereof.

24. The composition of claim 16, wherein the opioid analgesic agent is present at a level ranging from about 0.5 to about 20 wt. %.

18. A pharmaceutical composition for the alleviation of pain, associated with migraine headache consisting essentially of a therapeutically effective amount of one or more magnesium salt;

one or more stimulant;

one or more analgesic agent selected from the group consisting of acetylsalicylic acid, acetaminophen, paracetamol, ibuprofen, ketoprofen, ketoconazole, indomethacin, diflunisol, naproxen, ketorolac, dichlophenac, tolmetin, sulindac, phenacetin, piroxicam, mefamanic acid, dextromethorphan, codeine, morphine, hydromorphine, levophanol, meperidine, meptazinol, propoxyphene, propiram, buprenorphine, pentazocine, nalbuphine, butorphanol, tramadol, hydrocodone, oxycodone and methadone, pharmaceutically acceptable salts thereof, and mixtures thereof, wherein at least one of the one or more analgesic agent is a non-opioid analgesic agent, and at least one of the one or more analgesic agent is an opioid analgesic agent;

one or more effervescing agent; and

a pharmaceutically acceptable carrier or vehicle, wherein the composition is orally administered.

25. The composition of claim 18, wherein the non-opioid analgesic agent is present at a level ranging from about 10 to about 90 wt. %, and the opioid analgesic agent is present at a level ranging from about 0.5 to about 20 wt. %.

27. A pharmaceutical composition for the alleviation of pain, associated with migraine headache consisting essentially of from about 5 to about 30 wt. % of one or more magnesium salt, from about 1 to about 25 wt. % of one or more stimulant selected from the group consisting of methamphetamine, deoxamphetamine, methylphenidate, pemoline, caffeine and mixtures thereof, and analgesic agent selected from the group consisting of an opioid analgesic agent, an non-opioid analgesic agent and mixtures thereof, the non-opioid analgesic agent being selected from the group consisting of acetylsalicylic acid, acetaminophen, paracetamol, ibuprofen, ketoprofen, ketoconazole, indomethacin, diflunisol, naproxen, ketorolac, dichlophenac, tolmetin, sulindac, phenacetin, piroxicam, mefamanic acid and dextromethorphan, and pharmaceutically acceptable salts thereof;

and the opioid analgesic agent being selected from the group consisting of codeine, morphine, hydromorphine, levophanol, meperidine, meptazinol, propoxyphene, propiram, buprenorphine, pentazocine, nalbuphine, butorphanol, tramadol, hydrocodone, oxycodone and methadone, and pharmaceutically acceptable salts thereof, wherein the opioid analgesic agent is present in an amount of from about 0.5 to about 20 wt. %, and the non-opioid analgesic agent is present in an amount from about 10 to about 90 wt. %; and

a pharmaceutically acceptable carrier or vehicle, wherein the composition is orally administered.

28. A pharmaceutical composition for the alleviation of pain, associated with migraine headache consisting essentially of from about 5 to about 30 wt. % of one or more magnesium salt, from about 1 to about 25 wt. % of one or more stimulant selected from the group consisting of methamphetamine, deoxamphetamine, methylphenidate, pemoline, caffeine and mixtures thereof, from about 20 to about 80 wt. % of one or more effervescing agent, and analgesic agent selected from the group consisting of an opioid analgesic agent, an non-opioid analgesic agent and mixtures thereof, the non-opioid analgesic agent being selected from the group consisting of acetylsalicylic acid, acetaminophen, paracetamol, ibuprofen, ketoprofen, ketoconazole, indomethacin, diflunisol, naproxen, ketorolac, dichlophenac, tolmetin, sulindac, phenacetin, piroxicam, mefamanic acid and dextromethorphan, and pharmaceutically acceptable salts thereof;

the opioid analgesic agent being selected from the group consisting of codeine, morphine, hydromorohine, levophanol, meperidine, mentazinol, propoxhene, propiram, buprenorohine, pentazocine, nalbuphine, butorphanol, tramadol, hydrocodone, oxycodone and methadone, and pharmaceutically acceptable salts thereof, wherein the opioid analgesic agent is present in an amount of from about 0.5 to about 20 wt. %, and the non-opioid analgesic agent is present in an amount from about 10 to about 90 wt. % and a pharmaceutically acceptable carrier or vehicle, wherein the composition is orally administered.