Claims for Patent: 6,106,864

Summary for Patent: 6,106,864

Title:	Pharmaceutical formulations containing darifenacin
Abstract:	There is provided a pharmaceutical dosage form adapted for administration to the gastrointestinal tract of a patient, comprising darifenacin, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable adjuvant, diluent or carrier, characterized in that the dosage form is adapted to deliver at least 10% by weight of the darifenacin, or the pharmaceutically acceptable salt thereof, to the lower gastrointestinal tract of the patient. The formulation minimizes unwanted side-effects and increases the bioavailability of darifenacin.
Inventor(s):	Dolan; Thomas Francis (Sandwich, GB), Humphrey; Michael John (Sandwich, GB), Nichols; Donald John (Sandwich, GB)
Assignee:	Pfizer Inc. (New York, NY)
Application Number:	09/029,072
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 6,106,864
Patent Claims:	1. A pharmaceutical dosage form adapted for administration to the gastrointestinal tract of a patient, comprising darifenacin, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable adjuvant, diluent, or carrier; characterized in that the dosage form is adapted to release in the lower gastrointestinal tract at least 10% by weight of the darifenacin, or the pharmaceutically acceptable salt thereof. 2. A dosage form as claimed in claim 1, which is adapted to release at least 50% by weight of the darifenacin, or the pharmaceutically acceptable salt thereof, to the lower gastrointestinal tract. 3. A dosage form as claimed in claim 1, which is adapted to release the darifenacin, or the pharmaceutically acceptable salt thereof, to the gastrointestinal tract of the patient over or after a sustained period of time following administration of the dosage form to the patient. 4. A dosage form as claimed in claim 3, wherein no more than 90% by weight of the darifenacin, or the pharmaceutically acceptable salt thereof, is released 4 hours after dosing. 5. A dosage form as claimed in claim 4, wherein no more than 90% by weight of the darifenacin, or the pharmaceutically acceptable salt thereof, is released 8 hours after dosing. 6. A dosage form as claimed in claim 5, wherein no more than 90% by weight of the darifenacin, or the pharmaceutically acceptable salt thereof, is released 16 hours after dosing. 7. A dosage form as claimed in claim 1, wherein the darifenacin is in the form of its hydrobromide salt. 8. A dosage form as claimed in claim 1, which is adapted for oral administration. 9. A dosage form as claimed in claim 1, wherein the darifenacin, or the pharmaceutically acceptable salt thereof, is embedded in a matrix from which it is released by diffusion. 10. A dosage form as claimed in claim 9, wherein the matrix material is high molecular weight hydroxypropyl methylcellulose. 11. A dosage form as claimed in claim 1, which is adapted for rectal administration. 12. A dosage form as claimed in claim 11, which is a suppository. 13. A dosage form as claimed in claim 1, which is adapted to release at least 25% by weight of the darifenacin, or the pharmaceutically acceptable salt thereof, to the lower gastrointestinal tract. 14. A dosage form as defined in claim 1, comprising darifenacin hydrobromide, anhydrous dibasic calcium phosphate, hydroxypropyl methylcellulose, and magnesium stearate. 15. A dosage form as defined in claim 14, wherein said hydroxypropyl methycellulose has a number average molecular weight of 89,000, a methoxy content of 19-24%, and a hydroxypropoxy content of 7-12%. 16. A pharmaceutical dosage form adapted for administration to the gastrointestinal tract of a patient, comprising darifenacin, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable adjuvant, diluent or carrier; characterized in that the dosage form is adapted to release the darifenacin, or the pharmaceutically acceptable salt thereof, in Apparatus 1 described in USP XXII at page 1578, having baskets of 40 mesh (381 .mu.m apertures), a rotation speed of 100 rpm and a dissolution medium of water 37.degree. C., over a sustained period of time. 17. A dosage form as claimed in claim 16, wherein no more than 90% by weight of the darifenacin, or the pharmaceutically acceptable salt thereof, is released after 4 hours. 18. A dosage form as claimed in claim 16, wherein no more than 90% by weight of the darifenacin, or the pharmaceutically acceptable salt thereof, is released after 8 hours. 19. A dosage form as claimed in claim 16, wherein no more than 90% by weight of the darifenacin, or the pharmaceutically acceptable salt thereof, is released after 16 hours. 20. A dosage form as claimed in claim 16, wherein the darifenacin is in the form of its hydrobromide salt. 21. A dosage form as claimed in claim 16, which is adapted for oral administration. 22. A dosage form as claimed in claim 16, wherein the darifenacin, or the pharmaceutically acceptable salt thereof, is embedded in a matrix from which it is released by diffusion. 23. A dosage form as claimed in claim 22, wherein the matrix material is high molecular weight hydroxypropyl methylcellulose. 24. A dosage form as claimed in claim 16, which is adapted for rectal administration. 25. A dosage form as claimed in claim 24, which is a suppository. 26. A method of treatment of irritable bowel syndrome or urinary incontinence, which comprises administering darifenacin, or a pharmaceutically acceptable salt thereof, to the lower gastrointestinal tract of a patient in need of such treatment. 27. A method as claimed in claim 26, which comprises administering a dosage form as defined in claim 1 to the gastrointestinal tract of a patient in need of such treatment. 28. A method as claimed in claim 26, which comprises administering a dosage form as defined in claim 16 to the gastrointestinal tract of a patient in need of such treatment.