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Claims for Patent: 6,899,890

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Claims for Patent: 6,899,890

Title: Bioadhesive drug delivery system
Abstract:The present invention relates to a novel essentially pH neutral vaginal drug delivery system suitable for modified delivery of a therapeutically active material in the vaginal cavity. The vaginal drug delivery system comprises an essentially pH neutral emulsion having globules having two phases, an internal water soluble phase and an external water-insoluble phase or film, wherein the water-soluble interior phase contains a therapeutically active drug or drugs. One novel aspect of the vaginal drug delivery system is that the internal water soluble phase comprises an acidic buffered phase.
Inventor(s): Kirschner; Mitchell I. (St. Louis, MO), Levinson; R. Saul (Chesterfield, MO), Riley; Thomas C. (Manchester, MO), Hermelin; Marc S. (St. Louis, MO)
Assignee: KV Pharmaceutical Company (St. Louis, MO)
Application Number:10/101,014
Patent Claims: 1. An essentially pH neutral vaginal drug delivery system, which comprises: an essentially pH neutral emulsion having globules having two phases, an internal water-soluble phase and an external water-insoluble phase or film; said internal water-soluble phase comprises an acidic buffered phase containing a therapeutically active drug or drugs, wherein the acidic buffered phase comprises said therapeutically active drug or drugs either alone or in combination with an additional buffering agent; wherein the acidic buffered phase is isotonic, hypertonic, or hypotonic; and wherein the globules have a particle size ranging from about 0.1 microns to about 100 microns.

2. The composition of claim 1, wherein the therapeutically active drug or drugs is micronized and has a particle size ranging from about 0.1 microns to less than 60 microns.

3. The composition of claim 2, wherein the therapeutically active drug or drugs has a particle size ranging from about 0.1 microns to about 15 microns.

4. The composition of claim 1, wherein the globules have a particle size ranging from about 0.1 microns to about 60 microns.

5. The composition of claim 4, wherein the globules have a particle size ranging from about 0.5 microns to about 55 microns.

6. The composition of claim 1, wherein the acidic buffered phase has an internal pH of less than 6.0.

7. The composition of claim 6, wherein the acidic buffered phase has an internal pH of between about 2.5 to about 5.5.

8. The composition of claim 7, wherein the acidic buffered phase has an internal pH of between about 3.5 to about 5.0.

9. The composition of claim 1, wherein the therapeutically active drug is selected from the group consisting of antifungal agents, antibacterial agents, antimicrobial agents, antiviral agents, spermicides, hormone agents, antitrichomonial agents, antiprotozoan agents, antimycoplasm agents, antiretroviral agents, nucleoside analogues, reverse transcriptase inhibitors, protease inhibitors, contraceptive agents, sulfadrugs, sulfonamides, sulfones, hygiene agents, probiotic agents, vaccine agents, antibody agents, peptide agents, protein agents, polysaccharide agents, nucleic acids, plasmids, liposomes, carbohydrate polymers, transgenic bacteria, yeast, chemotherapeutic agents, steroid agents, growth enhancing agents, libido enhancers, androgenic substances, chitin derivatives, environment modifying agents, pH modifiers, and mixtures and combinations thereof.

10. The composition of claim 9, wherein the therapeutically active drug is a growth enhancing agent selected from the group consisting of cytokines.

11. The composition of claim 1, further comprising an excipient selected from the group consisting of lubricants, cleansing agents, deodorizers, humectants, emollients, plasticizers, binders, emulsifying agents, stabilizing agents, solvents, bioabsorbable materials, antioxidants, solubilizing agents, antimicrobial preservatives, diluents, glidants, suspending agents, extended-release agents, coating agents, adsorbents, disintegrants, chelating agents, and mixtures and combinations thereof.

12. The composition of claim 9, wherein the therapeutically active drug is an antifungal agent selected from the group consisting of butoconazole nitrate, clotrimazole, ketoconazole nitrate, miconizole, polyene antifungals, nystatin, amphotericin B, pimaricin, oxiconazole nitrate, terconazole nitrate, tioconazole, flutrimazole, intraconizole, allylamines, terbenafine, butenafine, amorolfine, naftifine, gluconazole, azoles, econazole, voriconizole, fluconazole, posaconazole, sulconazole, diction bis-benzimidazoles, glucan synthesis inhibitor, echinacandins, anidulafungin, caspofungin, micafugin, anti-tb drugs, diaphenylsulfone, ciclopirox olamine, haloprogin, tolnatane, undecylenate, and mixtures and combinations thereof.

13. The composition of claim 9, wherein the therapeutically active drug is an antibacterial agent selected from the group consisting of clindamycin, sulfonamides, erythromycin, clarithromycin, azythromycin, tetracycline, doxacline, metronidazole, macrolides, ketolides, quinolones, cephalosporins, carbapenmens, penicillins, gentamicin, magainin peptides, dalbavancin, ramoplanin, iseganan, cefoxitin, ceftriaxone, trichloroacetic acid, and mixtures and combinations thereof.

14. The composition of claim 9, wherein the therapeutically active drug is an antiviral agent selected from the group consisting of penciclovir, acylovir, ganciclovir, foscarnet, valaciclovir, pleconaril, and mixtures and combinations thereof.

15. The composition of claim 9, wherein the therapeutically active drug is the spermicide nonoxyl-9.

16. The composition of claim 9, wherein the androgenic substances are selected from the group consisting of danazol, testosterone, and mixtures and combinations thereof.

17. The composition of claim 1, wherein the external water-insoluble phase or film contains an additional therapeutically active drug outside of the acidic buffered phase.

18. The composition of claim 17, wherein the additional therapeutically active drug in the external phase or film is micronized and has a particle size ranging from about 0.5 microns to less than 60.0 microns.

19. The composition of claim 17, wherein the additional therapeutically active drug in the external phase or film is non-micronized.

20. The composition of claim 17, wherein the additional therapeutically active drug in the external phase or film is both micronized and non-micronized.

21. The composition of claim 20, wherein the ratio of the micronized drug in the acid buffered phase and the micronized drug outside of the acid buffered phase to the nonmicronized drug is about 0.1 to about 1,000; and wherein the release rate of the therapeutically active drug is from about 0.1 hours to about 168 hours.

22. The composition of claim 1, wherein the acidic buffered phase has an osmotic pressure greater than 300.+-.10 milliosmol/liter.

23. The composition of claim 1, wherein the acidic buffered phase has an osmotic pressure less than 300.+-.10 milliosmol/liter.

24. The composition of claim 1, wherein the acidic buffered phase has an osmotic pressure equal to 300.+-.10 milliosmol/liter.

25. The composition of claim 1, wherein the therapeutically active drug is a surface active drug.

26. The composition of claim 25, wherein the surface active drug is clindamycin phosphate.

27. An essentially pH neutral vaginal drug delivery system, which comprises: an essentially pH neutral emulsion having globules having two phases, an internal water-soluble phase and an external water-insoluble phase or film; said internal water-soluble phase comprises an acidic buffered phase containing a micronized therapeutically active drug or drugs, wherein the acidic buffered phase comprises said micronized therapeutically active drug or drugs either alone or in combination with an additional buffering agent; wherein the acidic buffered phase is isotonic, hypertonic, or hypotonic; and wherein the micronized therapeutically active drug has a particle size ranging from about 0.1 microns to less than 60.0 microns; wherein the efficacy of the therapeutically active drug is maximized by the acidic buffered phase; and wherein the acidic buffered phase is present in an amount sufficient to provide a cessation of symptoms of irritation and itching of the vaginal mucosa.

28. The composition of claim 27, wherein the acidic buffered phase is positively charged and has an internal pH of between about 2.5 to about 5.0.

29. The composition of claim 27, wherein the therapeutically active drug is selected from the group consisting of antifungal agents, antibacterial agents, antimicrobial agents, antiviral agents, spermicides, hormone agents, antitrichomonial agents, antiprotozoan agents, antimycoplasm agents, antiretroviral agents, nucleoside analogues, reverse transcriptase inhibitors, protease inhibitors, contraceptive agents, sulfadrugs, sulfonamides, sulfones, hygiene agents, probiotic agents, vaccine agents, antibody agents, peptide agents, protein agents, polysaccharide agents, nucleic acids, plasmids, liposomes, carbohydrate polymers, transgenic bacteria, yeast, chemotherapeutic agents, steroid agents, growth enhancing agents, libido enhancers, androgenic substances, chitin derivatives, environment modifying agents, pH modifiers, and mixtures and combinations thereof.

30. The composition of claim 29, wherein the therapeutically active drug is a growth enhancing agent selected from the group consisting of cytokines.

31. The composition of claim 27, further comprising an excipient selected from the group consisting of lubricants, cleansing agents, deoderizers, humectants, emollients, plasticizers, binders, emulsifying agents, stabilizing agents, solvents, bioabsorbable materials, antioxidants, solubilizing agents, antimicrobial preservatives, diluents, glidants, suspending agents, extended-release agents, coating agents, adsorbents, disintegrants, chelating agents, and mixtures and combinations thereof.

32. The composition of claim 29, wherein the therapeutically active drug is an antifungal agent selected from the group consisting of butoconazole nitrate, clotrimazole, ketoconazole nitrate, miconizole, polyene antifungals, nystatin, amphotericin B, pimaricin, oxiconazole nitrate, terconazole nitrate, tioconazole, flutrimazole, intraconizole, allylamines, terbenafine, butenafine, amorolfine, naftifine, gluconazole, azoles, econazole, voriconizole, fluconazole, posaconazole, sulconazole, diction bis-benzimidazoles, glucan synthesis inhibitor, echinacandins, anidulafungin, caspofungin, micafugin, anti-tb drugs, diaphenylsulfone, ciclopirox olamine, haloprogin, tolnatane, undecylenate, and mixtures and combinations thereof.

33. The composition of claim 29, wherein the therapeutically active drug is an antibacterial agent selected from the group consisting of clindamycin, sulfonamides, erythromycin, clarithromycin, azythromycin, tetracycline, doxacline, metronidazole, macrolides, ketolides, quinolones, cephalosporins, carbapenmens, penicillins, gentamicin, magainin peptides, dalbavancin, ramoplanin, iseganan, cefoxitin, ceftriaxone, trichloroacetic acid, and mixtures and combinations thereof.

34. The composition of claim 29, wherein the therapeutically active drug is an antiviral agent selected from the group consisting of penciclovir, acylovir, ganciclovir, foscarnet, valaciclovir, pleconaril, and mixtures and combinations thereof.

35. The composition of claim 29, wherein the therapeutically active drug is the spermicide nonoxyl-9.

36. The composition of claim 29, wherein the androgenic substance is selected from the group consisting of danazol, testosterone, and mixtures and combinations thereof.

37. The composition of claim 27, wherein the external water-insoluble phase or film contains an additional therapeutically active drug outside of the acidic buffered phase.

38. The composition of claim 37, wherein the additional therapeutically active drug in the external phase or film is micronized and has a particle size ranging from about 0.5 microns to less than 60.0 microns.

39. The composition of claim 37, wherein the additional therapeutically active drug in the external phase or film is non-micronized.

40. The composition of claim 37, wherein the additional therapeutically active drug in the external phase or film is both micronized and non-micronized.

41. The composition of claim 40, wherein the ratio of the micronized drug in the acid buffered phase and the micronized drug outside of the acid buffered phase to the nonmicronized drug is about 0.1 to about 1,000; and wherein the release rate of the therapeutically active drug is from about 0.1 hours to about 72 hours.

42. The composition of claim 27, wherein the acidic buffered phase has an osmotic pressure greater than 300.+-.10 milliosmol/liter.

43. The composition of claim 27, wherein the acidic buffered phase has an osmotic pressure less than 300.+-.10 milliosmol/liter.

44. The composition of claim 27, wherein the acidic buffered phase has an osmotic pressure equal to 300.+-.10 milliosmol/liter.

45. The composition of claim 27, wherein the therapeutically active drug is a surface active drug.

46. The composition of claim 45, wherein the surface active drug is clindamycin phosphate.

47. An essentially pH neutral vaginal drug delivery system, which comprises: an essentially pH neutral emulsion having globules having two phases, an internal water-soluble phase and an external water-insoluble phase or film; said internal water-soluble phase comprises an acidic buffered phase having an internal pH of about 2.0 to about 6.0 and a therapeutically active drug or drugs, wherein the acidic buffered phase comprises said therapeutically active drug or drugs either alone or in combination with an additional buffering agent; and wherein the globules have a particle size ranging from about 0.1 microns to about 100 microns.

48. The composition of claim 47, wherein the acidic buffered phase has an internal pH of between about 2.5 to about 5.5.

49. Method for treating a vaginal disorder comprising: administering to a patient an essentially pH neutral vaginal drug delivery system, which comprises: an essentially pH neutral emulsion having globules having two phases, an internal water-soluble phase and an external water-insoluble phase or film; said internal water-soluble phase comprises an acidic buffered phase containing a therapeutically active drug or drugs, wherein the acidic buffered phase comprises said therapeutically active drug or drugs either alone or in combination with an additional buffering agent; wherein the acidic buffered phase is isotonic, hypertonic, or hypotonic; and wherein the therapeutically active drug has a particle size ranging from about 0.1 microns to less than 60.0 microns.

50. The method of claim 49, wherein the vaginal disorder is selected from the group consisting of infection caused by a Candida species, Enterococci species, Streptococci species, Staphylococci species, uropathogens, E. coli, Kelbsiella, Clostridia species, Mobiluncus species, Gardnerella, Prevotella species, bacteria pseudomonas, protozoans, mycoplasm, Chlamydia, HIV, HPV, herpes, N. gonorrhoeae, Trichomonas vaginalis, C. trachomatis, and mixtures and combinations thereof.

51. The method of claim 49, wherein the isotonic acidic buffered phase releases the therapeutically active drug or drugs from the globule by diffusion.

52. The method of claim 49, wherein the therapeutically active drug is delivered to the area of action within about 0.1 hour to about 168 hours after administration.

53. The method of claim 49, wherein the hypertonic acidic buffered phase releases the therapeutically active drug or drugs from the globule by rupture of the globule.

54. The method of claim 53, wherein the therapeutically active drug is delivered to the area of action within about 5 minutes to about 60 minutes after administration.

55. The method of claim 49, wherein the hypotonic acidic buffered phase releases the therapeutically active drug or drugs from the globule by diffusion and permeation.

56. The method of claim 55, wherein the therapeutically active drug is delivered to the area of action for about at least 1 hour after administration.

57. The method of claim 49, wherein the vaginal disorder is nonspecific vaginitis.
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