Controlled release pharmaceutical dosage forms of a cholesteryl ester transfer protein inhibitor
OwnerWilliam J. Curatolo, Steven C. Sutton +1inventors
InventorsWilliam J. Curatolo, Steven C. Sutton, Leah E. Appel
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Abstract
The present invention relates to controlled release pharmaceutical dosage forms of a cholesteryl ester transfer protein inhibitor, (CETPI) methods of using and methods of making same. In particular, it relates to a controlled release form of the CETPI [2R,4S] 4-[(3,5-bis-trifluoromethyl-benzyl)-methoxycarbonyl-amino]-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid ethyl ester.
Claims63
A controlled release dosage form comprising:
- (a) a solubility-enhanced form of a cholesteryl ester transfer protein inhibitor (CETPI);
- and
- (b) a controlled release means for delivering said CETPI;
- wherein following administration to an in vivo use environment said controlled release dosage form provides at least one of:
- (i) at least 50% inhibition of plasma cholesteryl ester transfer protein for at least 12 hours;
- (ii) a maximum drug concentration in the blood that is less than or equal to 80% of the maximum drug concentration in the blood provided by an immediate release dosage form consisting of the same amount of the solubility-enhanced form of said CETPI;
- (iii) a mean HDL cholesterol level after dosing for 8 weeks that is at least about 1.2-fold that obtained prior to dosing;
- and
- (iv) a mean LDL cholesterol level after dosing for 8 weeks that is less than or equal to 90% that obtained prior to dosing.
A controlled release dosage form comprising:
- (a) a solubility-enhanced form of a cholesteryl ester transfer protein inhibitor (CETPI);
- and
- (b) a controlled release means for delivering said CETPI;
- wherein following administration to a use environment said controlled release dosage form releases at least 80 wt % of said CETPI after about at least 2 hours.
The controlled release dosage form of claim 41 wherein said period of time is greater than 2 hours.
Dependencies are inferred from the claim text.