Depot preparation

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 491/044 (2006.01) A61K 9/107 (2006.01) A61K 31/395 (2006.01) A61K 31/40 (2006.01) A61K 47/38 (2006.01) C07D 207/00 (2006.01)

Patent

CA 2095499

Abstract of The Disclosure Disclosed are the hemipamoate and pamoate salt of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz- [2,3;6,7]oxepino-[4,5-c]pyrrole, very insoluble compounds having excellent properties for use as depot preparations. Also disclosed are pharmaceutical preparations which include the pamoate salts of trans-5- chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-z[dibenz[2,3;6,7] oxepino-[4,5-c]pyrrole, especially in crystalline form. Such preparations release therapeutically useful amounts of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H- dibenz[2,3:6,7]oxepino-[4,5-c]pyrrole for 2 to S weeks after administration. The invention also includes process of manufacturing the pharmaceutical preparations which generally involves allowing the free base of trans-5- chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz- [2,3:6,7]oxepino[4,5-c]pyrrole to react with pamoic acid to form a pamoate or hemipamoate salt.

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