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Generated: December 13, 2017

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Title: Microencapsulated 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles
Abstract:Sustained-release microparticle composition. The microparticle composition can be formulated to provide multi-phasic release. In one aspect, the composition includes microparticles having more than one rate of release. In another aspect, the composition includes microparticles that exhibit diffusional release and microparticles that exhibit biodegradation release.
Inventor(s): Mesens; Jean (Wechelderzande, BE), Rickey; Michael E. (Loveland, OH), Atkins; Thomas J. (York, PA)
Assignee: Alkermas Controlled Therapeutics Inc. II (Cambridge, MA) Janssen Pharmaceutica (Beerse, BE)
Filing Date:Feb 06, 2003
Application Number:10/359,226
Claims:1. A sustained-release microparticle composition, comprising: a microparticle comprising a 1,2 benzazole of the formula ##STR15## and the pharmaceutically acceptable acid addition salts thereof, wherein R is hydrogen or alkyl of 1 to 6 carbon atoms; R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen, halo, hydroxy, alkyloxy of 1 to 6 carbon atoms, and C alkyl of 1 to 6 carbon atoms; X is O or S; Alk is C.sub.1-4 alkanediyl; and Q is a radical of formula ##STR16##

wherein R.sup.3 is hydrogen or alkyl of 1 to 6 carbon atoms; Z is --S--, --CH.sub.2 --, or --CR.sup.4.dbd.CR.sup.5 --; where R.sup.4 and R.sup.5 are independently selected from the group consisting of hydrogen or alkyl of 1 to 6 carbon atoms; A is a bivalent radical --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 -- or CR.sup.6.dbd.CR.sup.7 --; where R.sup.6 and R.sup.7 are independently selected from the group consisting of hydrogen, halo, amino or alkyl of 1 to 6 carbon atoms; and R.sup.8 a hydrogen or hydroxyl; and a biodegradable and biocompatible polymeric matrix that exhibits diffusional release of said 1,2 benzazole; and a microparticle comprising a 1,2 benzazole of the formula ##STR17## and the pharmaceutically acceptable acid addition salts thereof, wherein R is hydrogen or alkyl of 1 to 6 carbon atoms; R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen, halo, hydroxy, alkyloxy of 1 to 6 carbon atoms, and C alkyl of 1 to 6 carbon atoms; X is O or S; Alk is C.sub.14 alkanediyl; and Q is a radical of formula ##STR18##

wherein R.sup.3 is hydrogen or alkyl of 1 to 6 carbon atoms; Z is --S--, --CH.sub.2 --, or --CR.sup.4.dbd.CR.sup.5 --; where R.sup.4 and R.sup.5 are independently selected from the group consisting of hydrogen or alkyl of 1 to 6 carbon atoms; A is bivalent radical --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 -- or CR.sup.6.dbd.CR.sup.7 --; where R.sup.6 and R.sup.7 are independently selected from the group consisting of hydrogen, halo, amino or alkyl of 1 to 6 carbon atoms; and R.sup.8 is hydrogen or hydroxyl; and a biodegradable and biocompatible polymeric matrix that exhibits biodegradation release of said 1,2 benzazole;.

2. The sustained-release microparticle composition of claim 1, wherein said 1,2 benzazole is selected from the group consisting of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetr ahydro-2-methyl-4H-pyrido-[1,2-a]pyrimidin-4-one and the pharmaceutically acceptable acid addition salts thereof.

3. The sustained-release microparticle composition of claim 1, wherein said 1,2 benzazole is selected from the group consisting of 3-[2-[4-(6-fluoro-1,2,-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tet rahydro-2-hydroxy-2-methyl-4H-pyridol(1,2-a]pyrimidin-4-one and the pharmaceutically acceptable acid addition salts thereof.
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