Pharmaceutical compositions
A pharmaceutical composition in solid form containing at least a therapeutically effective amount of one or more statins in the free acid form is disclosed.
1 . A pharmaceutical composition in solid form comprising a therapeutically effective amount of one or more statins in the free acid form.
2 . The pharmaceutical composition of claim 1 , wherein the statin in the free acid form is rosuvastatin free acid.
3 . The pharmaceutical composition of claim 1 , further comprising one or more pharmaceutically acceptable excipients.
4 . The pharmaceutical composition of claim 2 , comprising one or more pharmaceutically acceptable excipients.
5 . The pharmaceutical composition of claim 1 , comprising a solid composite comprising a therapeutically effective amount of the one or more statins in the free acid form and at least one pharmaceutically acceptable excipient.
6 . The pharmaceutical composition of claim 5 , wherein the pharmaceutically acceptable excipient is N-methylpyrrolidone.
7 . A pharmaceutical composition in solid form comprising a statin in the free acid form and one or more pharmaceutically acceptable excipients, wherein the statin in the free acid form retains at least about 97.5% of its initial purity after two months, and at least about 97% of its initial purity after three months when stored at a temperature of about 2° C. to about 8° C.
8 . The pharmaceutical composition of claim 7 , wherein the pharmaceutically acceptable excipient is a diluent.
9 . The pharmaceutical composition of claim 7 , wherein the statin in the free acid form is rosuvastatin free acid.
10 . The pharmaceutical composition of claim 7 , wherein the pharmaceutically acceptable excipient is selected from the group consisting of sugar alcohol, disaccharide, N-methylpyrrolidone, colloidal silicon dioxide, cellulose derivative and mixtures thereof.
11 . The pharmaceutical composition of claim 7 , wherein the pharmaceutically acceptable excipient is N-methylpyrrolidone.
12 . The pharmaceutical composition of claim 7 , having a content of the lactone form of the rosuvastatin free acid of no more than about 3%.
13 . The pharmaceutical composition of claim 7 , having a content of the lactone form of the rosuvastatin free acid of no more than about 2.5%.
14 . A solid composite comprising rosuvastatin in the free acid form and one or more pharmaceutically acceptable excipients, wherein the rosuvastatin in the free acid form retains at least about 97.5% of its initial purity after two months, and at least about 97% of its initial purity after three months when stored at a temperature of about 2° C. to about 8° C.
15 . The solid composite of claim 14 , wherein the pharmaceutically acceptable excipient is a diluent.
16 . The solid composite of claim 14 , wherein the pharmaceutically acceptable excipient is N-methylpyrrolidone.
17 . The solid composite of claim 14 , having a content of the lactone form of the rosuvastatin free acid of no more than about 3%.
18 . The solid composite of claim 14 , having a content of the lactone form of the rosuvastatin free acid of no more than about 2.5%.
19 . A process for preparing a free acid form of rosuvastatin, the process comprising (a) dissolving rosuvastatin salt into one or more solvents; (b) adjusting the pH of the solution to about 3.0 to about 3.5; and (c) isolating the free acid of rosuvastatin.
20 . The process of claim 19 , wherein the solvent is diethyl ether or ethyl acetate.
21 . The process of claim 19 , wherein the step of isolating comprises extracting the free acid form of rosuvastatin from the solution.