Delivery of drugs to mucosal surfaces

• US 20020197324A1
• Filed: 07/15/2002
• Published: 12/26/2002
• Est. Priority Date: 04/18/1997
• Status: Abandoned Application

• Current Assignee: Archimedes Development Limited (Kirin Holdings Company Limited)
• Original Assignee: West Pharmaceutical Drug Delivery and Research Centre Limited
• Inventors: Illum, Lisbeth, Watts, Peter James
• Application Number:
  US10/196,590
• Publication Number:
  US 20020197324A1
• Time in Patent Office: Days
• US Class Current: 424/488
• 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 9/0043 Nose
• CPC Class Codes: A61K 9/06 Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels composition of ointments, creams or gels A61K47/00
• CPC Class Codes: A61K 9/12 Aerosols; Foams A61K9/0043, A61K9/0056, A61K9/006, A61K9/0073 take precedence; spray-films A61K9/7015
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 11/02 Nasal agents, e.g. decongestants
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 15/02 for disorders of the vagina
• CPC Class Codes: A61P 15/18 Feminine contraceptives
• CPC Class Codes: A61P 23/02 Local anaesthetics
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/16 Anti-Parkinson drugs
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• 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 31/04 Antibacterial agents
• CPC Class Codes: A61P 31/14 for RNA viruses
• CPC Class Codes: A61P 31/16 for influenza or rhinoviruses
• CPC Class Codes: A61P 37/08 Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 9/06 : Antiarrhythmics
• CPC Class Codes: A61P 9/08 : Vasodilators for multiple indications
• CPC Class Codes: A61P 9/12 : Antihypertensives

Abstract

Liquid pharmaceutical compositions for administration to a mucosal surface, comprising a therapeutic agent and a pectin with a low degree of esterification are described. Such compositions gel, or can be adapted to gel, at the site of application in the absence of an extraneous source of divalent metal ions.

Claims

1. A single component liquid pharmaceutical composition for administration to a mucosal surface comprising a therapeutic agent, a pectin with a low degree of esterification and an aqueous carrier, that gels or can be adapted to gel at the site of application.

2. A composition as claimed in claim 1, wherein the mucosal surface is the nasal cavity.

3. A composition as claimed in claim 1, wherein the mucosal surface is the vagina.

4. A composition as claimed in claim 1, wherein the mucosal surface is the rectum.

5. A composition as claimed in claim 1, wherein the mucosal surface is the back of the throat.

6. A composition as claimed in claim 1, where the mucosal surfaces is the eye.

7. A composition as claimed in claim 1, which is administered as a spray or a liquid free flowing system.

8. A composition as claimed in claim 1, wherein the degree of esterification is less than 50%.

9. A composition as claimed in claim 1, wherein the pectin concentration in the composition is from 1 to 100 g/L.

10. A composition as claimed in claim 1, wherein the pH of the composition is between 2 and 9.

11. A composition as claimed in claim 1, for use in the delivery of an antiviral agent to the nose or the vagina.

12. A composition as claimed in claim 1, for use in the delivery of a vaccine to the nose, the rectum or the vagina.

13. A composition as claimed in claims 1, for use in the delivery of a decongestant agent.

14. A composition as claimed in claims 1, for use in the delivery of a contraceptive agent.

15. A composition as claimed in claim 1, for use as a vaginal lubricating agent.

16. A composition as claimed in claim 1, for use in the delivery of an anti-allergic agent.

17. A pharmaceutical formulation in a form suitable for administration to a mucosal surface, which formulation comprises a composition according to claim 1 in a pharmaceutically acceptable dosage form.

18. A formulation as claimed in claim 17, which is in the form of a spray or a liquid free flowing system.

19. The use of a composition according to claim 1, as a means of delivery of therapeutic agents to the nose, the vagina, the rectum, the back of the throat or the eye.

22. A kit of parts comprising a composition according to claim 1, which kit of parts is packaged and presented with instructions to administer the composition or formulation to a mucosal surface in the absence of an extraneous source of divalent metal ions.

25. A pharmaceutical gel composition obtainable by administering a composition according to claim 1, to a mucosal surface of a mammalian patient in the absence of extraneous application of a solution of divalent metal ions to the surface.

28. A method for delivering a therapeutic agent in a liquid formulation to the nose, eye, rectum, back of throat or vagina which comprises the delivery of the agent in a composition according to claim 1.

29. A method of treatment of a mammalian patient which comprises administration of a composition according to claim 1 to such a patient.

30. A method for the delivery of therapeutic agents to a mucosal surface in a mammal, which comprises administering a composition, as defined in claim 1 to the surface.

31. The use of a composition according to claim 1, as a means of delivery of therapeutic agents to the nose, vagina, rectum, back of the throat, or eye.

32. The use of a composition according to claim 1, in the manufacture of a medicament for the delivery of a therapeutic agent to the nose, vagina, rectum, back of the throat, or eye.

33. The use of a composition according to claim 1, in the manufacture of a medicament for the treatment or prophylaxis of a disease which comprises administration of the composition, including a therapeutic agent which is effective against the disease, to a mucosal surface of a patient in need of such treatment or prophylaxis, in the absence of extraneous application of a solution of divalent metal ions to the surface.

35. The use of a composition according to claim 1, in the manufacture of a medicament for use in a method of treatment according to any one of claims 26 to 30.

38. A process for the preparation of a composition according to claim 1, which comprises mixing together the therapeutic agent and the pectin in the aqueous carrier.

39. A product obtainable by a process according to claim 38.

20. A kit of parts comprising a liquid pharmaceutical composition for administration to a mucosal surface, comprising a therapeutic agent, a pectin with a low degree of esterification and an aqueous carrier, which composition gels or is adapted to gel at the site of application, provided that the kit does not comprise a solution of divalent metal ions to be added extraneously to the surface.

21. A kit of parts comprising a liquid pharmaceutical composition for administration to a mucosal surface, which composition comprises a therapeutic agent, a pectin with a low degree of esterification and an aqueous carrier, which composition gels or is adapted to gel at the site of application, and which kit of parts is packaged and presented with instructions to administer the composition to the surface in the absence of an extraneous source of divalent metal ions.

23. A pharmaceutical gel composition obtainable by applying a liquid composition, comprising a therapeutic agent, a pectin with a low degree of esterification and an aqueous carrier, to a mucosal surface of a mammalian patient in the absence of extraneous application of a solution of divalent metal ions to the surface.

24. A pharmaceutical gel composition comprising a therapeutic agent and a pectin with a low degree of esterification, which gel is obtainable by applying a liquid composition, comprising the therapeutic agent and pectin in an aqueous carrier, to a mucosal surface, and which gel is substantially free of divalent metal ions derived from an extraneous source applied to the mucosal surface before, or at the same time as, the liquid composition is applied.

26. A method of treatment of a patient which comprises the administration of a liquid pharmaceutical composition, comprising a therapeutic agent, a pectin with a low degree of esterification and an aqueous carrier, which composition gels or is adapted to gel at the site of application, to a mucosal surface of the patient in the absence of extraneous application of a solution of divalent metal ions to the surface.

27. A method of treatment or prophylaxis of a disease which comprises administration of a liquid pharmaceutical composition, comprising a therapeutic agent which is effective against the disease, a pectin with a low degree of esterification and an aqueous carrier, which composition gels or is adapted to gel at the site of application, to a mucosal surface of a patient in need of such treatment, in the absence of extraneous application of a solution of divalent metal ions to the surface.

34. The use of a pectin with a low degree of esterification in the manufacture of a single component liquid composition for the delivery of therapeutic agents to mucosal surfaces.

36. A composition comprising a therapeutic agent, a pectin with a low degree of esterification and an aqueous carrier, which composition is packaged and presented for use in the treatment of a patient, which treatment comprises the administration of the composition to a mucosal surface of the patient in the absence of extraneous application of a solution of divalent metal ions to the surface.

37. The use of a pectin with a low degree of esterification in the manufacture of an aqueous liquid pharmaceutical composition for the treatment of a patient comprising the administration of the composition to a mucosal surface of the patient in the absence of extraneous application of a solution of divalent metal ions to the surface.