Pharmaceutical compositions of 5,7,14-triazatetracyclo [10.3.1.0(2,11).0(4,9)]-hexadeca-2(11)3,5,7,9-pentaene

摘要

Disclosed is a controlled release dosage form suitable for administration to a subject comprising 5,8,14-triazatetra-cyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene, and a means for administering the compound to the subject at a rate of less than about 6 mg/hour, whereby the controlled release dosage form is formulated such that at least about 0.1 mg of the compound is administered over a 24 hour period. Also disclosed is a controlled release dosage form formulated such that, when dosed to a subject the dosage form results in a time for maximum plasma concentration (Tmax) that is increased for the drug in an initial administration to the subject by an average of 50% of the corresponding Tmax determined for an equal does of the pentaene in the form of an immediate release bolus. Also disclosed is a controlled release dosage form formulated such that the dosage releases the pentaene at a rate of less than 6 mgA/hr in vitro when dissolution tested in a USP-2 apparatus, such that the time for dissolution of 50 w/w% of the drug is between 1 and 15 hours.