Interstitial therapy for immediate symptom relief and chronic therapy in interstitial cystitis

• US 7,414,039 B2
• Filed: 01/27/2005
• Issued: 08/19/2008
• Est. Priority Date: 01/28/2004
• Status: Active Grant

• Current Assignee: Regents of the University of California (University of California)
• Original Assignee: Regents of the University of California (University of California)
• Inventors: Parsons, C. Lowell
• Primary Examiner(s): Maier; Leigh C
• Application Number:
  US11/045,411
• Publication Number:
  US 20050234013A1
• Time in Patent Office: 1,300 Days
• Field of Search: None
• US Class Current: 514/57
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/167 having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• CPC Class Codes: A61K 31/24 having an amino or nitro group
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61K 31/727 Heparin; Heparan
• CPC Class Codes: A61K 31/728 Hyaluronic acid
• CPC Class Codes: A61K 31/737 Sulfated polysaccharides, e.g. chondroitin sulfate, dermatan sulfate A61K31/727 takes precedence
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 9/0034 Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
• CPC Class Codes: A61K 9/08 Solutions composition of solutions A61K47/00
• CPC Class Codes: A61P 13/02 of urine or of the urinary tract, e.g. urine acidifiers
• CPC Class Codes: A61P 13/10 of the bladder

Abstract

The present invention relates to a disorder of the lower urinary tract, and in particular, reducing the symptoms (including treatment) of interstitial cystitis in vivo. In a preferred embodiment, the present invention relates to treatment formulations and methods for reducing interstitial cystitis in patients.

Claims

1. A method for inhibiting Interstitial Cystitis and its symptoms in a subject in need thereof, said method comprising administering to said subject an effective amount of a composition comprising a heparinoid, a local anesthetic agent and a buffering compound, thereby inhibiting Interstitial Cystitis and its symptoms in the subject.

2. The method of claim 1 further comprising administering to said subject an effective amount of an osmolar component.

3. The method of claim 2, wherein the composition is in solution and the osmolar component is present in a sufficient amount so that the final solution is isotonic or near isotonic.

4. The method of claim 3, wherein the osmolar component is at least one of sodium chloride, dextrose, dextran 40, dextran 60, starch and mannitol or a combination thereof.

5. The method of claim 1, wherein the local anesthetic agent is at least one of lidocaine, bupivacaine, and mepivacaine.

6. The method of claim 1, wherein the heparinoid comprises at least one of a heparin, a pentosan polysulfate sodium, a heparan sulfate, a heparin sodium, a hyaluronic acid, and a chondroitin sulfate.

7. The method of claim 6, wherein the heparinoid comprises at least one of a heparin, a heparan sulfate, a heparin sodium, a hyaluronic acid, and a chondroitin sulfate, and the method further comprises the administration to said subject of an effective amount of sodium pentosan polysulfate to inhibit Interstitial Cystitis.

8. The method of claim 7, wherein the sodium pentosan polysulfate is administered orally.

9. The method of claim 8, wherein the sodium pentosan polysulfate is in a quantity from about 100 mg/day to about 600 mg/day.

10. The method of claim 9, wherein the sodium pentosan polysulfate is in a quantity from about 100 mg/day to about 300 mg/day.

11. A method for repairing a mucin layer of bladder tissue by the method of claim 1 thereby inhibiting Interstitial Cystitis.

12. The method of claim 1, wherein the buffering compound comprises at least one of sodium bicarbonate and THAM (tromethamine or Tris hydroxymethylpropyl).

13. The method of claim 1, wherein the effective amount of the buffering compound is 3 ml of 8.4% sodium bicarbonate (w/v) per unit dose.

14. The method of claim 1, wherein the effective amount of the heparinoid is

(i) about 0.5 mg to about 1000 mg of heparin per unit dose;

(ii) about 1 mg to about 600 mg of pentosan polysulfate sodium per unit dose;

(iii) about 0.5 mg to about 10,000 mg of heparan sulfate per unit dose;

(iv) about 5 mg to about 600 mg of hyaluronic acid per unit dose;

(v) about 1 mg to about 10,000 mg of chondroitin sulfate per unit dose;

or

(vi) about 10 mg to about 600 mg of heparin sodium per unit dose.

15. The method of claim 1, wherein the effective amount of the anesthetic agent is 10 ml of 1% lidocaine or 16 ml of 2% lidocaine per unit dose.

16. The method of claim 1, wherein the heparinoid, the anesthetic agent, and the buffering compound are administered concomitantly or in sequence.

17. The method of claim 2, wherein the heparinoid, the anesthetic agent, the buffering compound and the osmolar component are administered concomitantly or in sequence.

18. The method of claim 1, wherein the subject is selected from the group consisting of human, monkey, ape, dog, cat, cow, horse, rabbit, mouse and rat subjects.

19. The method of claim 1, wherein administration to said subject is effected by intravesicular administration, administration using liposomes, administration using biodegradable polymers, or administration using a hydrogel.

20. The method of claim 2, wherein the heparinoid, the anesthetic agent, the buffering compound and the osmolar component are in solution.

21. The method of claim 20, wherein the solution has a pH from about 7 to 12.

22. A method for monitoring the course of Interstitial Cystitis in a subject, said method comprising

intravesicularly administering a solution containing an amount of potassium that would elicit pain in a subject that has a compromised urothelium, wherein the subject has been administered the composition, comprising a heparinoid, a local anesthetic agent, and a buffering compound, and

monitoring the pain response of the subject at different points in time,

whereby a difference in the amount of pain determined is indicative of the course of the Interstitial Cystitis condition.