Oxybutynin formulations and method of use

• US 6,087,396 A
• Filed: 01/15/1999
• Issued: 07/11/2000
• Est. Priority Date: 10/05/1998
• Status: Expired due to Fees

• Current Assignee: Situs, Inc.
• Original Assignee: Situs, Inc.
• Inventors: Roberts, Dennis H.
• Primary Examiner(s): KRASS, FREDERICK F
• Application Number:
  US09/231,139
• Time in Patent Office: 543 Days
• Field of Search: 514/534, 514/544, 514/549, 600/29, 600/30, 600/31, 604/264, 604/275, 604/285, 604/288, 604/892.1, 424/422, 424/423, 424/430
• US Class Current: 514/534
• CPC Class Codes: A61K 31/216 of acids having aromatic rings, e.g. benactizyne, clofibrate
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 9/0034 Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
• CPC Class Codes: A61P 13/10 of the bladder

Abstract

Oxybutynin chloride formulations having increased stability at body temperature, even at high concentrations. These formulations comprise oxybutynin chloride at a pH of between 3.0 and 5.0, and may include a buffer capable of providing adequate buffering capacity in this range. The OC solutions can be placed in an infuser device for treatment of bladder dysfunction.

Claims

1. A pharmaceutical composition comprising an aqueous oxybutynin chloride solution, wherein said composition has an oxybutynin concentration of about 1.0 to 30 mg/ml and a pH of 3 to 5 is stable at about 37 degrees C for at least 12 hours, when placed within the bladder.

2. The composition of claim 1, wherein the concentration of oxybutynin chloride is between about 10 mg/ml and 25 mg/ml.

3. The composition of claim 2, wherein the concentration of oxybutynin chloride is about 20 mg/ml.

4. The composition of claim 1, wherein the pH is between about 3.5 and 4.5.

5. The composition of claim 4, wherein the pH is about 4.0.

6. The composition of claim 1, further comprising a buffering agent having a concentration of between about 0.005 M and 0.1 M.

7. The composition of claim 6, wherein said buffering agent has a concentration of between about 0.01 and 0.05 M.

8. The composition of claim 6, wherein said buffering agent is acetate or citrate.

9. The composition of claim 1, further comprising a viscosity-enhancing agent.

10. The composition of claim 9, wherein said viscosity-enhancing agent is carboxymethylcellulose or hydroxypropylmethylcellulose.

11. The composition of claim 1, further in combination with an infuser capable of releasing said composition at a predetermined flow rate.

12. The composition of claim 11, wherein said infuser is an intravesical infuser.

13. The composition of claim 11, wherein said flow rate is less than about 400 μ

l/hour.

14. A method for treating a bladder disorder, comprising the steps of:

positioning an intravesical infuser in said bladder; and

introducing the pharmaceutical composition of claim 1 into said intravesical infuser.

15. The method of claim 14, wherein said bladder disorder is selected from the group consisting of secondary urge incontinence, hyperreflexive voiding dysfunction, neurogenic bladder and decreased bladder capacity.

16. The method of claim 14, further comprising the step of infusing said composition out of said infuser into the bladder at a rate not exceeding 400 1μ

/hour.