Patent ID: 6649187
Filing Date: 2003-11-18
Classification: A61K

Abstract:
A controlled release solid dosage form comprising:a pharmaceutical composition comprising an amine drug, wherein the amine drug is the free base or salt form of [S-(R,S)]-2-[4-[[(4-methyl)piperazin-1-yl]carbonyl]phenoxy]-3,3-diethyl-N-[1-(3,4-methylenedioxyphenyl)butyl]-4-oxo-1-azetidinecarboxamide) and a polyalkylamine polymer, wherein the polyalkylamine polymer is cross-linked polymeric ammonium salt and comprises groups that link ammonium nitrogen atoms wherein: about 25% or more of the groups which link ammonium nitrogen atoms are group Y, wherein each Y is independently â€”C(R1R2)bâ€”; b is an integer of 7 to about 20; and each R1 and each R2 is independently alkylene of about 1 to 20 carbon atoms; zero to about 75% of the groups which link ammonium nitrogen atoms are group Z wherein Z is a hydrocarbylene radical containing 2 to 50 carbon atoms, the hydrocarbylene radical optionally containing or substituted with one or more hydroxyl, ether, ester, amino, thioether, keto, silyl group or helerocyclic rings; about 25% or more of the ammonium nitrogen atoms are secondary ammonium nitrogen atoms; and said cross-linked polymeric ammonium salt is insoluble in water; a coat surrounding the pharmaceutical composition and comprising a film-forming polymer and plasticizer; and plural apertures in the coat; wherein the amine drug and polyalkylamine polymer are released through the apertures when the dosage form is placed into an aqueous environment of use, and the dosage form provides a controlled release of the amine drug.