Pharmaceutical preparations and methods for their administration

• US 5,993,856 A
• Filed: 11/17/1997
• Issued: 11/30/1999
• Est. Priority Date: 01/24/1997
• Status: Expired due to Term

• Current Assignee: FemmePharma, Inc.
• Original Assignee: FemmePharma Co.
• Inventors: DiPiano, Gerrianne M., Ragavan, Vanaja V.
• Primary Examiner(s): Mosley, Terressa
• Application Number:
  US08/971,346
• Time in Patent Office: 743 Days
• Field of Search: 424/489, 424/430, 424/433, 424/422
• US Class Current: 424/489
• CPC Class Codes: A61K 31/58 containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin digitoxin A61K31/7048
• CPC Class Codes: A61K 9/0034 Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
• 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 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/02 for disorders of the vagina
• CPC Class Codes: A61P 31/04 Antibacterial agents
• CPC Class Codes: A61P 31/10 Antimycotics
• CPC Class Codes: A61P 31/12 Antivirals
• CPC Class Codes: A61P 31/20 for DNA viruses
• CPC Class Codes: A61P 31/22 for herpes viruses
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: Y10S 977/775 Nanosized powder or flake, e.g. nanosized catalyst
• CPC Class Codes: Y10S 977/795 Composed of biological material
• CPC Class Codes: Y10S 977/906 Drug delivery
• CPC Class Codes: Y10S 977/915 Therapeutic or pharmaceutical composition

Abstract

Formulations which have been developed for topical or local delivery intrapelvically, intraperitoneally or directly on reproductive organs of interest administration to a region such as the female reproductive system, provide for increased comfort, increased bioavailability, rapid and relatively high blood levels in the regions to be treated in the substantial absence of systemic levels of drug which might cause side effects. These formulations consist of drug micro or nanoparticles, which may be formed of drug alone or in combination with an excipient or polymeric carrier. The excipient or polymer may be used to manipulate release rates and to increase adhesion to the affected region. The particulate formulation can be applied as a dried powder, a liquid suspension or dispersion, or as a topical ointment, creme, lotion, foam or suppository.

Claims

1. A micro or nanoparticulate drug formulation for local or regional topical administration of an effective amount to provide relief from symptoms associated with a disease or disorder in a region in patients in need thereof, wherein the effective amount is less than the effective amount when the drug is administered systemically.

2. The formulation of claim 1 wherein the region is the female reproductive organs.

3. The formulation of claim 2 wherein the patients have a disorder located in the reproductive organs.

4. The formulation of claim 1 wherein the formulation comprises drug particles.

5. The formulation of claim 3 wherein the drug is for treatment of endometriosis.

6. The formulation of claim 1 wherein the micro or nano particulates adhere to mucosal tissue.

7. The formulation of claim 1 where the micro or nano particulates comprise polymer altering rates of drug absorption in the region to be treated.

8. The formulation of claim 1 which can be administered vaginally, intraperitoneally, or directly on the reproductive organs of interest.

9. The formulation of claim 8 wherein the drug is danazol and wherein the formulation is suitable for vaginal administration in patients in need thereof and is in a dosage effective for treatment of endometriosis.

10. The formulation of claim 1 wherein the drug is an anticancer drug, cytotherapeutic or anti-proliferative drug in a dosage effective for treatment of cancer in the region of the patient where administered.

11. The formulation of claim 1 wherein the drug is an antiviral agent effective for treatment of viral infections selected from genital herpes and genital papilloma viral infections.

12. The formulation of claim 1 wherein the drug is an antifungal agent effective for treatment of vaginal fungal infections.

13. The formulation of claim 1 wherein the drug is an antibacterial agent effective for treatment of vaginal and endometrial bacterial infections.

14. The formulation of claim 1 wherein the drug is a steroid or steroid-like product suitable for treatment of endocrine conditions.

15. The formulation of claim 14 wherein the drug is effective for treatment of menopause, infertility, contraception, dysfunctional uterine bleeding, dysmenorrhea, adenomyosis, or assisted reproductive technologies.

16. A method of treating a patient comprising the step of topically administering to the patient an effective amount of a micro or nanoparticulate drug formulation suitable for local or regional topical administration of an effective amount to provide relief from symptoms associated with a disease or disorder in a region in the patient in need thereof, wherein the effective amount is less than the effective amount when the drug is administered systemically.

17. The method of claim 16 wherein the region is the female reproductive organs.

18. The method of claim 16 wherein the patients have a disorder located in the reproductive organs.

19. The method of claim 18 wherein the drug is for treatment of endometriosis and the patient has endometriosis.

20. The method of claim 17 which can be administered vaginally, intraperitoneally, or directly on the reproductive organs of interest.

21. The method of claim 16 wherein the drug is danazol and wherein the formulation is vaginally administered in patients in need thereof in a dosage effective for treatment of endometriosis.

22. The method of claim 16 wherein the drug is an anticancer drug, cytotherapeutic or anti-proliferative drug in a dosage effective for treatment of cancer in the region of the patient where administered.

23. The method of claim 16 wherein the drug is an antiviral agent effective for treatment of viral infections selected from genital herpes and genital papilloma viral infections.

24. The method of claim 16 wherein the drug is an antifungal agent effective for treatment of vaginal fungal infections.

25. The method of claim 16 wherein the drug is an antibacterial agent effective for treatment of vaginal and endometrial bacterial infections.

26. The method of claim 16 wherein the drug is a steroid or steroid-like product suitable for treatment of endocrine conditions.

27. The method of claim 26 wherein the drug is effective for treatment of menopause, infertility, contraception, dysfunctional uterine bleeding, dysmenorrhea, adenomyosis, or assisted reproductive technologies.

28. A method for treating endometriosis by decreasing the discomfort associated with endometriosis comprising administering to the mucosal membranes of the female reproductive tract danazole in a form promoting quick uptake into the blood stream, wherein the danazole is administered in an effective amount which is less than the effective amount when the drug is administered systemically.

29. The method of claim 28 wherein the danazole is in a form selected from the group consisting of foams, tablets, and creams.

30. The method of claim 28 wherein the danazole is in a form suitable for application to the uterus.

31. A composition for treating endometriosis comprising danazole in a form promoting quick uptake into the blood stream when applied to the mucosal membranes of the female reproductive tract, wherein danazole is in a form delivering an effective amount to decrease the discomfort of endometriosis which is less than the effective amount when the drug is administered systemically.

32. The composition of claim 31 wherein the danazole is in a form selected from the group consisting of foams, tablets, and creams.

33. The composition of claim 32 wherein the danazole is in a form suitable for application to the uterus.