Pharmaceutical formulations comprising substituted xanthine compounds
OwnerAlfred Rudolph, Cynthia Tuthillinventors
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Abstract
The present invention provides novel pharmaceutical compositions comprising substituted xanthine compounds useful for the treatment of cystic fibrosis and other diseases, and methods of use thereof.
Claims26
A liquid pharmaceutical formulation suitable for oral administration comprising an effective amount of a therapeutically active xanthine derivative, substituted xanthine, or pharmaceutically acceptable salt of said xanthine derivative or said substituted xanthine, having the formula:
- (I), wherein
- R1 and R2 are the same or different and are C(1-6)alkyl or C(1-6)alkenyl, or hydrogen;
- R3 is C(1-6)alkyl or hydrogen, and R4 is C(48)cycloalkyl, aryl or hydrogen, wherein at least one of R1, R2 and is other than hydrogen, in admixture with a pharmaceutically acceptable oil.
The formulation of claim 1, wherein said formulation is a solution.
The formulation of claim 1, wherein said xanthine derivative, substituted xanthine, or pharmaceutically acceptable salt of said xanthine derivative or said substituted xanthine, is hydrophobic.
The formulation of claim 1, wherein said formulation is a suspension.
The formulation of claim 4, wherein said suspension is substantially homogenous.
The formulation of claim 4, wherein said therapeutically active xanthine derivative, substituted xanthine, or pharmaceutically acceptable salt of said xanthine derivative or said substituted xanthine, is in the form of particles having a mean diameter less than about 100 microns.
The formulation of claim 1 further comprising a pharmaceutically acceptable preservative.
The formulation of claim 1 further comprising a pharmaceutically acceptable antioxidant.
The formulation of claim 1 wherein said pharmaceutically acceptable oil is a vegetable oil.
The formulation of claim 1 wherein in said formula (I) R1 and R2 are the same or different and are C(1-6)alkyl or C(1-6)alkenyl;
- R3 is C(1-6)alkyl or hydrogen, and R4 is C(4-8) cycloalkyl.
The formulation of claim 1 wherein in said formula (I) R1 and R2 are the same and are methyl or allyl, R3 is ethyl, cyclopropylmethyl or hydrogen, and R4 is cyclohexyl, provided that R1 is allyl when R3 is hydrogen, and R1 is methyl when R3 is ethyl or cyclopropylmethyl.
The formulation of claim 1 wherein in said formula (I) R1 and R2 are both methyl, R3 is ethyl, cyclopropylmethyl, and R4 is cyclohexyl.
The formulation of claim 1 wherein in said formula (I) R1 and R2 are allyl, R3 is hydrogen, and R4 is cyclohexyl, cyclohexylmethyl, or cycloheptyl.
The formulation of claim 1 wherein in said formula (I) R1 is methyl, R2 is allyl, R3 is cyclopropylmethyl or ethyl, and R4 is cyclohexyl.
The formulation of claim 1 wherein in said formula (I) R1 and R2 are the same or different, and are methyl, propyl, allyl or hydrogen;
- R3 is methyl or hydrogen, and R4 is cyclohexyl or cyclopentyl.
The formulation of claim 1 wherein said substituted xanthine of formula (I) is selected from the group consisting of 1,3-dipropyl-cyclopentylxanthine (CPX), 1,3-diallyl-cyclohexylxanthine (DAX/DCHX), 1,3-dipropyl-7-methylcyclopenthylxanthine (DP-CPX), cyclohexylcaffeine (CHC), and xanthine amino congener (XAC).
Dependencies are inferred from the claim text.