Pharmaceutical preparations and methods for their regional administration

• US 6,652,874 B2
• Filed: 05/16/2002
• Issued: 11/25/2003
• Est. Priority Date: 01/24/1997
• Status: Expired due to Term

• Current Assignee: FemmePharma, Inc.
• Original Assignee: FemmePharma Co.
• Inventors: Ragavan, Vanaja V., DiPiano, Gerianne M.
• Primary Examiner(s): Spear, James M.
• Application Number:
  US10/147,762
• Publication Number:
  US 20020172714A1
• Time in Patent Office: 558 Days
• Field of Search: 424/422, 424/426, 424/430, 424/433, 424/489
• US Class Current: 424/430
• 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

Abstract

Formulations have been developed for regional delivery of drugs, for example, into a cavity such as the pelvic region, peritoneal region, or directly on organs of interest. Regional delivery increases comfort and bioavailability of the drug, resulting in rapid and relatively high blood levels in the regions to be treated in the substantial absence of side effects due to the high levels required for efficacy following systemic delivery. In the preferred embodiment, 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 drug 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 drug formulation, comprising drug particles suitable for local or regional administration of an effective amount of the drug to provide relief from symptoms in a region in patients in need thereof, wherein the effective amount is less than the effective amount when the drug is administered systemically and

wherein the drug is selected from the group consisting of anticancer drugs, cytotherapeutic drugs, anti-proliferative drugs, and antiviral drugs.

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 drug is in the form of micro or nano particulates.

6. The formulation of claim 4 wherein the micro or nano particulates adhere to mucosal tissue.

7. The formulation of claim 4 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.

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.

16. The formulation of claim 1, wherein the region is selected from the group consisting of uterus, fallopian tubes, peritoneal space, pelvic cul-de-sac, ovaries, and urinogenital tract.

17. The formulation of claim 1, wherein the formulation is in a carrier promoting quick uptake of the drug into the blood stream, a carrier manipulating release of drug, or a carrier promoting adhesion of the drug, wherein the carrier is selected from the group consisting of a liquid suspension or dispersion, a hydrogel suspension or dispersion, a topical ointment, a cream, a lotion, and a foam.

5. A method of treating a patient comprising the step of administering to the patient an effective amount of a drug formulation, comprising drug particles suitable for local or regional administration of an effective amount of the drug to provide relief from symptoms 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 and

wherein the drug is selected from the group consisting of anticancer drugs, cytotherapeutic drugs, anti-proliferative drugs, and antiviral drugs.

9. The method of claim 5 wherein the region is the female reproductive organs.

12. The method of claim 9 wherein the patient has a disorder located in the reproductive organs.

13. The method of claim 9 which can be administered vaginally, intraperitoneally, or directly on the reproductive organs of interest.

14. The method of claim 5 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.

15. The method of claim 5 wherein the drug is an antiviral agent effective for treatment of viral infections selected from genital herpes and genital papilloma viral infections.

18. The method of claim 5, wherein the region is selected from the group consisting of uterus, fallopian tubes, peritoneal space, pelvic cul-de-sac, ovaries, and urinogenital tract.

19. The method of claim 5, wherein the formulation is in a carrier promoting quick uptake of the drug into the blood stream, a carrier manipulating release of drug, or a carrier promoting adhesion of the drug, wherein the carrier is selected from the group consisting of a liquid suspension or dispersion, a hydrogel suspension or dispersion, a topical ointment, a cream, a lotion, and a foam.

20. The method of claim 5, wherein the drug is in the form of micro or nano particulates.