POLYETHYLENE GLYCOL-COATED SODIUM CARBONATE AS A PHARMACEUTICAL EXCIPIENT AND COMPOSITIONS PRODUCED FROM THE SAME

• US 20100266682A1
• Filed: 04/21/2010
• Published: 10/21/2010
• Est. Priority Date: 12/10/2008
• Status: Abandoned Application

• Current Assignee: Transcept Pharmaceuticals Incorporated
• Original Assignee: Transcept Pharmaceuticals Incorporated
• Inventors: Davar, Nipun, Pather, Indiran, Ghosh, Sangita, Kavalakatt, Pauly
• Application Number:
  US12/764,489
• Publication Number:
  US 20100266682A1
• Time in Patent Office: Days
• US Class Current: 424/451
• 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 31/4748 forming part of bridged ring systems strychnine A61K31/475; morphinan derivatives A61K31/485
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 9/0031 Rectum, anus
• CPC Class Codes: A61K 9/0036 Devices retained in the vagina or cervix for a prolonged period, e.g. intravaginal rings, medicated tampons, medicated diaphragms
• 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 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• CPC Class Codes: A61K 9/14 Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles microspheres A61K9/16; microcapsules A61K9/50; nanocapsules, nanoparticles of the matrix type A61K9/51
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives

Abstract

Non-effervescent pharmaceutical compositions having at least one particle of carbonate coated by a layer of polyethylene glycol that substantially covers the at least one carbonate particle are described. Compositions are also described where the compositions include a weakly basic therapeutic agent, a first pH-modifying agent having at least one particle of carbonate coated by a layer of polyethylene glycol, and a second pH-modifying agent. The weakly basic therapeutic agent could be, but is not limited to, zolpidem or scopolamine. Compositions including zolpidem and scopolamine are used to treat insomnia and depression, respectively.

Claims

1. A pharmaceutical composition comprising:

zolpidem;

a first pH-modifying agent comprising at least one particle of a carbonate salt coated by a layer of polyethylene glycol that substantially covers the at least one carbonate salt particle; and

a second pH-modifying agent selected from the group consisting of sodium bicarbonate, sodium phosphate dibasic, potassium phosphate dibasic, sodium citrate, potassium citrate, sodium acetate, and sodium tartrate.

2. The pharmaceutical composition of claim 1, wherein the pharmaceutical composition is a non-effervescent composition.

3. The pharmaceutical composition of claim 1, wherein the pharmaceutical composition is selected from the group consisting of a lozenge, disk, film, bead, wafer, compressed core, tablet, capsule, and powder formulation.

4. The pharmaceutical composition of claim 1, wherein the zolpidem is present in amount of less than 10 mg of zolpidem hemitartrate or a molar equivalent amount of a pharmaceutically acceptable form of zolpidem.

5. The pharmaceutical composition of claim 1, wherein the second pH-modifying agent is sodium bicarbonate.

6. The pharmaceutical composition of claim 1, wherein, after storage in an open dish at 30°

C. and 65% relative humidity for at least two weeks, upon administration, the composition releases at least 20% of the zolpidem in a period of 5 minutes.

7. The pharmaceutical composition of claim 1, wherein, after storage in an open dish at 30°

C. and 65% relative humidity for at least two weeks, upon administration, the composition releases at least 30% of the zolpidem in a period of 5 minutes.

8. The pharmaceutical composition of claim 1, wherein, after storage in an open dish at 30°

C. and 65% relative humidity for at least two weeks, upon administration, the composition releases at least 40% of the zolpidem in a period of 10 minutes.

9. The pharmaceutical composition of claim 1, wherein, after storage in an open dish at 30°

C. and 65% relative humidity for at least two weeks, upon administration, the composition releases at least 60% of the zolpidem in a period of 10 minutes.

10. A method for treating insomnia in a subject, comprising the steps of:

administering to the subject a solid pharmaceutical composition comprising;

zolpidem;

a first pH-modifying agent comprising at least one particle of a carbonate salt coated by a layer of polyethylene glycol that substantially covers the carbonate salt particle; and

a second pH-modifying agent,

wherein the first and second pH-modifying agents are present in an amount sufficient to raise the pH of the subject'"'"'s saliva to at least about 7.9.

11. The method of claim 10, wherein the solid pharmaceutical composition is a non-effervescent composition.

12. The method of claim 10, wherein the insomnia is middle-of-the-night insomnia.

13. The method of claim 10, wherein the composition is administered by a route selected from the group consisting of oral, sublingual, buccal, and intranasal.

14. The method of claim 10, wherein the composition is administered intracavity.

15. The method of claim 14, wherein the cavity is selected from the group consisting of oral, rectal, vaginal, and nasal.

16. The method of claim 10, wherein less than 10 mg of zolpidem hemitartrate or a molar equivalent amount of a pharmaceutically acceptable form of zolpidem is administered.

17. The method of claim 10, wherein the second pH-modifying agent is sodium bicarbonate.

18. The method of claim 10, wherein, after storage in an open dish at 30°

C. and 65% relative humidity for at least two weeks, the composition releases at least 20% of the zolpidem in a period of 5 minutes following administration.

19. The method of claim 10, wherein, after storage in an open dish at 30°

C. and 65% relative humidity for at least two weeks, the composition releases at least 40% of the zolpidem in a period of 10 minutes following administration.

20. A pharmaceutical composition comprising:

scopolamine;

a first pH-modifying agent comprising at least one particle of a carbonate salt coated by a layer of polyethylene glycol that substantially covers the at least one carbonate salt particle; and

a second pH-modifying agent.

21-25. -25. (canceled)

26. A method for treating depression in a subject, comprising the steps of:

administering to the subject an orally dissolving film comprising;

scopolamine;

a first pH-modifying agent comprising a particle of a carbonate salt coated by a layer of polyethylene glycol that substantially covers the carbonate salt particle; and

a second pH-modifying agent,

wherein the first and second pH-modifying agents are present in an amount sufficient to raise the pH of the subject'"'"'s saliva to at least about 8.8.

27-33. -33. (canceled)

34. A pharmaceutical composition comprising:

a weakly basic therapeutic agent;

a first pH-modifying agent comprising at least one particle of a carbonate salt coated by a layer of polyethylene glycol that substantially covers the at least one carbonate salt particle; and

a second pH-modifying agent.

35-38. -38. (canceled)

39. A non-effervescent pharmaceutical composition comprising a pH-modifying agent including at least one particle of a carbonate salt coated by a layer of polyethylene glycol that substantially covers the at least one carbonate salt particle.

40-49. -49. (canceled)

50. A layered composition comprising:

carbonate and a pharmaceutically acceptable counter ion; and

polyethylene glycol,

wherein the carbonate and counter ion are coated by a layer of polyethylene glycol that substantially covers the carbonate and counter ion.

51-54. -54. (canceled)

55. A layered composition comprising:

a granule comprising carbonate and a pharmaceutically acceptable counter ion; and

polyethylene glycol,

wherein the polyethylene glycol is arranged in a layer that substantially covers the granule.

56-63. -63. (canceled)

64. A layered composition comprising:

a particle comprising carbonate and a pharmaceutically acceptable counter ion; and

a layer of polyethylene glycol substantially surrounding the particle.

65-70. -70. (canceled)