Microencapsulated 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles

DETAILED DESCRIPTION The present invention relates to microencapsulated 1,2-benzazoles and their use in the treatment of warm blooded animals suffering from mental disease.
In a preferred embodiment, the invention relates to a pharmaceutical composition designed for the controlled release of an effective amount of a drug over an extended period of time, prepared in microparticle form.
This composition comprises at least one antipsychotic agent and at least one biocompatible, biodegradable encapsulating polymer.
More particularly, the present invention relates to a method of treating warm blooded animals suffering from psychotic disorders comprising the administration thereto of a pharmaceutically effective amount of a biodegradable and biocompatible microparticle composition comprising a 1,2-benzazole of the formula ##STR2## 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 ##STR3## 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 is hydrogen or hydroxyl; within a polymeric matrix.
In another aspect, the present invention relates to a pharmaceutical composition comprising a biodegradable and biocompatible microparticle composition comprising a 1,2-benzazole of Formula I within a polymeric matrix.
In still another aspect, the present invention relates to a method of inhibiting serotonergic or dopaminergic overstimulation in animals wherein said method comprises administration of a biodegradable and biocompatible microparticle composition comprising a 1,2-benzazole of Formula I within a polymeric matrix