Pharmaceutical compositions

• US 9,198,867 B2
• Filed: 01/10/2012
• Issued: 12/01/2015
• 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:
  US13/347,552
• Publication Number:
  US 20120201888A1
• Time in Patent Office: 1,421 Days
• Field of Search: None
• US Class Current: 1/1
• 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 pharmaceutical oral dosage form comprising only two active agents:

a controlled-release matrix comprising, an effective amount of a first active agent that is a triptan to treat a headache, wherein the triptan is provided as;

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

an immediate-release matrix comprising, an effective amount of a second active agent that is an antiemetic to treat triptan induced nausea or vomiting, wherein the antiemetic is provided as;

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

wherein about 90% to about 100% of the first active agent is released by about 60 minutes in a dissolution test as measured by USP Apparatus 2 (Paddle Apparatus), and about 90% to about 100% of the second active agent is released by about 40 minutes in a dissolution test as measured by USP Apparatus 2 (Paddle Apparatus).

2. The solid pharmaceutical oral dosage form of claim 1, wherein the controlled-release matrix comprises microcrystalline cellulose, polyvinylpyrrolidone, croscarmellose sodium, and magnesium stearate.

3. The solid pharmaceutical oral dosage form of claim 1, wherein the solid pharmaceutical oral dosage form is multiparticulates.

4. The solid pharmaceutical oral dosage form of claim 3, wherein the multiparticulates comprise:

controlled-release particulates comprising the triptan, and

immediate-release particulates comprising the antiemetic.

5. The solid pharmaceutical oral dosage form of claim 1, wherein the immediate-release matrix comprises microcrystalline cellulose and croscarmellose sodium.

6. The solid pharmaceutical oral dosage form of any one of claim 1, 3 or 4, wherein about 25 mg of the promethazine is provided.

7. The solid pharmaceutical oral dosage form of any one of claim 1, 3 or 4, wherein the triptan is the pharmaceutically acceptable salt of sumatriptan that is sumatriptan succinate.

8. The solid pharmaceutical oral dosage form of any one of claim 1, 3 or 4, wherein the antiemetic is the pharmaceutically acceptable salt of promethazine that is promethazine hydrochloride.

9. The solid pharmaceutical oral dosage form of claim 3 or 4, wherein the multiparticulates are beads, spheres, or pellets.

10. The solid pharmaceutical oral dosage form of claim 3 or 4, wherein the multiparticulates are enteric-coated.

11. The solid pharmaceutical oral dosage form of claim 3 or 4, wherein the multiparticulates are contained within a capsule.

12. The solid pharmaceutical oral dosage form of claim 11, wherein the capsule is a soft gelatin capsule or a hard gelatin capsule.

13. The solid pharmaceutical oral dosage form of claim 11, wherein the capsule comprises an inner dosage component and an outer dosage component, the outer dosage component being in the form of an envelope over the inner dosage component.

14. The solid pharmaceutical oral dosage form of claim 13, wherein the inner dosage and outer dosage components are separated by an enteric layer.

15. The solid pharmaceutical oral dosage form of claim 11, wherein the capsule has micro drilled holes.

16. A method of treating a headache in a subject, comprising administering to the subject the solid pharmaceutical oral dosage form of any one of claim 1, 3 or 4.

17. The method of claim 16, 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.

18. The method of claim 16, wherein the solid pharmaceutical oral dosage form alleviates nausea or vomiting.

19. The solid pharmaceutical oral dosage form of claim 8, wherein about 25 mg of the promethazine hydrochloride is provided.

20. The multiparticulates of claim 3 or 4, wherein the triptan is the pharmaceutical acceptable salt of sumatriptan that is sumatriptan succinate;

and the antiemetic is the pharmaceutical acceptable salt of promethazine that is promethazine hydrochloride.

21. A method of treating pain in a subject, comprising administering to the subject the solid pharmaceutical oral dosage form of any one of claim 1, 3 or 4.

22. A method of treating photophobia in a subject, comprising administering to the subject the solid pharmaceutical oral dosage form of any one of claim 1, 3 or 4.

23. The method of claim 22, wherein the photophobia is associated with a migraine headache.

24. The solid pharmaceutical oral dosage form of claim 1, further comprising a coating material.

25. The solid pharmaceutical oral dosage form of claim 1, further comprising polyvinyl alcohol.

26. The solid pharmaceutical oral dosage form of claim 1, further comprising hydroxypropyl methylcellulose.

27. The solid pharmaceutical oral dosage form of claim 26, wherein the hydroxypropyl methylcellulose is hydroxypropyl methylcellulose 2910.

28. The solid pharmaceutical oral dosage form of claim 1, wherein the triptan is provided as from about 25 mg to about 100 mg of sumatriptan.

29. The method of claim 16, wherein the headache is a migraine headache with or without aura.

30. The method of claim 16, wherein the headache is acute.