Pharmaceutical compositions with enhanced performance
View Patent ↗Pharmaceutical compositions of a low-solubility drug and lower alkanoate-, phthalate- and trimellitate esters of hydroxypropyl methyl cellulose and lower alkanoate- and succinate esters of cellulose and methyl cellulose are disclosed that provide enhanced concentrations of the drug in a use environment.
1. A composition comprising
(a) a low-solubility drug, said drug having a minimum aqueous solubility of 0.5 mg/mL or less, and
(b) a cellulose alkanyl succinate polymer having a degree of substitution of alkanyl groups of at least 1.0 and a degree of substitution of succinyl groups of at least 0.2;
wherein said polymer and said drug are in the form of a solid amorphous dispersion.
2. The composition of claim 1 wherein the degree of substitution of alkanyl groups is at least 1.25 and the degree of substitution of succinyl groups is at least 0.25.
3. The composition of claim 1 wherein the ratio of the degree of substitution of alkanyl groups to the degree of substitution of succinyl groups is less than 7.
4. A composition comprising
(a) a low-solubility drug, said drug having a minimum aqueous solubility of 0.5 mg/mL or less, and
(b) a methyl cellulose alkanyl succinate polymer having a combined degree of substitution of methoxy groups and alkanyl groups of at least 1.0 and a degree of substitution of succinyl groups of at least 0.2;
wherein said polymer and said drug are in the form of a solid amorphous dispersion.
5. The composition of claim 4 wherein said combined degree of substitution is at least 1.25 and said degree of substitution of alkanyl groups is at least 0.25.
6. The composition of claim 4 wherein the ratio of (i) the combined degree of substitution of methoxy groups and alkanyl groups to (ii) the degree of substitution of succinyl groups is less than 7.
7. The composition of claim 1 or 4 wherein said alkanyl groups are selected from the group consisting of acetyl, propionyl and butyryl.
8. The composition of claim 1 or 4 wherein at least a major portion of said drug is amorphous.