Pharmaceutical compositions

• US 9,775,837 B2
• Filed: 10/28/2015
• Issued: 10/03/2017
• Est. Priority Date: 01/09/2008
• Status: Active Grant

• Current Assignee: Charleston Laboratories, Inc.
• Original Assignee: Charleston Laboratories, Inc.
• Inventors: Bosse, Paul, Ameling, John, Schachtel, Bernard, Takigiku, Ray
• Primary Examiner(s): TRAN, SUSAN T
• Application Number:
  US14/925,669
• Publication Number:
  US 20160106755A1
• Time in Patent Office: 706 Days
• Field of Search: None
• CPC Class Codes: A61K 31/165 having aromatic rings, e.g. colchicine, atenolol, progabide
• CPC Class Codes: A61K 31/167 having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• CPC Class Codes: A61K 31/24 having an amino or nitro group
• CPC Class Codes: A61K 31/403 condensed with carbocyclic rings, e.g. carbazole
• CPC Class Codes: A61K 31/404 Indoles, e.g. pindolol
• CPC Class Codes: A61K 31/4196 1,2,4-Triazoles
• CPC Class Codes: A61K 31/422 not condensed and containing further heterocyclic rings
• CPC Class Codes: A61K 31/437 the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
• CPC Class Codes: A61K 31/454 containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 31/515 Barbituric acids; Derivatives thereof, e.g. sodium pentobarbital
• CPC Class Codes: A61K 31/522 having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• CPC Class Codes: A61K 31/5415 ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 47/36 Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• CPC Class Codes: A61K 9/0024 Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue compositions for intravenous administration, normal injectable solutions or dispersions for, e.g. subcutaneous administration A61K9/0019; brain implants A61K9/0085; (coated) prostheses, catheters or stents A61L
• CPC Class Codes: A61K 9/0056 Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• CPC Class Codes: A61K 9/1694 resulting in granules or microspheres of the matrix type containing more than 5% of excipient
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/2054 : Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2086 : Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat active cores with a complete drug-free outer coat A61K9/28
• CPC Class Codes: A61K 9/209 : containing drug in at least two layers or in the core and in at least one outer layer
• CPC Class Codes: A61K 9/4808 : characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release capsules filled with granules or microparticles A61K9/16; filled with microcapsules or coated microparticles A61K9/50; with mixture of different granules, microcapsules, (coated) microparticles A61K9/5084
• CPC Class Codes: A61K 9/5084 : Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs tablets containing such a mixture A61K9/2077
• CPC Class Codes: A61P 1/08 : for nausea, cinetosis or vertigo; Antiemetics
• CPC Class Codes: A61P 25/04 : Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/06 : Antimigraine agents
• CPC Class Codes: A61P 25/08 : Antiepileptics; Anticonvulsants
• CPC Class Codes: A61P 29/00 : Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 29/02 : without antiinflammatory effect
• CPC Class Codes: A61P 39/00 : General protective or antinoxious agents
• CPC Class Codes: A61P 43/00 : Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 7/02 : Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
• CPC Class Codes: A61P 9/00 : Drugs for disorders of the cardiovascular system

Abstract

Methods and compositions are provided which comprise effective amounts of analgesic to treat a subject, including reducing or eliminating an adverse effect associated with the analgesic.

Claims

1. A solid oral pharmaceutical composition that comprises only two active ingredients and one or more pharmaceutically acceptable excipients, wherein the solid oral pharmaceutical composition comprises:

a first plurality of particulates that comprises a first active ingredient that is a triptan; and

a second plurality of particulates that comprises a second active ingredient that is an antiemetic, wherein the plurality of second particulates is formulated for rapid release.

2. The solid oral pharmaceutical composition of claim 1, wherein the antiemetic is promethazine or a pharmaceutically acceptable salt thereof.

3. The solid oral pharmaceutical composition of claim 2, wherein the promethazine or the pharmaceutically acceptable salt thereof is provided in an amount of from about 0.5 mg to about 60 mg.

4. The solid oral pharmaceutical composition of claim 2, wherein the promethazine is present in an amount of about 22 mg or about 44 mg.

5. The solid oral pharmaceutical composition of claim 2, wherein the pharmaceutically acceptable salt of promethazine is promethazine hydrochloride.

6. The solid oral pharmaceutical composition of claim 5, wherein the promethazine hydrochloride is present in an amount of about 25 mg or about 50 mg.

7. The solid oral pharmaceutical composition of claim 1, wherein the first plurality of particulates or the second plurality of particulates are beads, spheres, or pellets.

8. The solid oral pharmaceutical composition of claim 1, wherein the first plurality of particulates and the second plurality of particulates are contained within a capsule.

9. The solid oral pharmaceutical composition of claim 1 that further comprises a coating material.

10. The solid oral pharmaceutical composition of claim 1 that further comprises polyvinyl alcohol.

11. The solid oral pharmaceutical composition of claim 1 that further comprises hydroxypropyl methylcellulose.

12. The solid oral pharmaceutical composition of claim 11, wherein the hydroxypropyl methylcellulose is hydroxypropyl methylcellulose 2910.

13. The solid oral pharmaceutical composition of claim 1, wherein the triptan is sumatriptan or a pharmaceutically acceptable salt thereof.

14. The solid oral pharmaceutical composition of claim 13, wherein the pharmaceutically acceptable salt of sumatriptan is sumatriptan succinate.

15. The solid oral pharmaceutical composition of claim 1, wherein the antiemetic is provided as:

from about 12.5 mg to about 50 mg of promethazine, or a pharmaceutically acceptable salt of promethazine; and

wherein the triptan is provided as;

from about 25 mg to about 100 mg of sumatriptan, or a pharmaceutically acceptable salt of sumatriptan.

16. The solid oral pharmaceutical composition of claim 1, wherein the triptan is naratriptan or a pharmaceutically acceptable salt thereof.

17. The solid oral pharmaceutical composition of claim 1, wherein the triptan is almotriptan or a pharmaceutically acceptable salt thereof.

18. The solid oral pharmaceutical composition of claim 1, wherein the triptan is zolmitriptan or a pharmaceutically acceptable salt thereof.

19. The solid oral pharmaceutical composition of claim 1, wherein the triptan is frovatriptan or a pharmaceutically acceptable salt thereof.

20. The solid oral pharmaceutical composition of claim 1, wherein the triptan is rizatriptan or a pharmaceutically acceptable salt thereof.

21. The solid oral pharmaceutical composition of claim 1, wherein about 90% to about 100% of the triptan is released by about 60 minutes in a dissolution test as measured with a USP Apparatus 2 (Paddle Apparatus), and about 90% to about 100% of the antiemetic is released by about 40 minutes in a dissolution test as measured with a USP Apparatus 2 (Paddle Apparatus).

22. A method of treating or preventing pain in a subject, comprising administering to the subject the solid oral pharmaceutical composition of claim 1.

23. The method of claim 22, wherein the pain is a headache.

24. The method of claim 23, wherein the headache is a migraine headache, a cluster headache, a hemicrania continua headache, a chronic headache, a tension headache, a chronic tension headache, or any combination thereof.

25. The method of claim 23, wherein the headache is a migraine headache with or without an aura.

26. The method of claim 23, wherein the headache is acute.

27. The method of claim 22, wherein the solid oral pharmaceutical composition reduces nausea or vomiting.

28. The method of claim 22, wherein the solid oral pharmaceutical composition prevents nausea or vomiting.

29. A method of treating or preventing photophobia in a subject, comprising administering to the subject the solid oral pharmaceutical composition of claim 1.

30. The method of claim 29, wherein the photophobia is associated with a migraine headache.