Process for forming amorphous atorvastatin
View Patent ↗Forming amorphous atorvastatin comprises the steps of dissolving atorvastatin in a hydroxylic solvent, followed by rapidly evaporating the solvent. In another aspect, a composition comprises particles of amorphous atorvastatin and a core.
1. A process for forming amorphous atorvastatin, comprising:
(a) dissolving atorvastatin in a solution comprising a hydroxylic solvent; and
(b) rapidly evaporating said hyroxylic solvent from said solution to form amorphous atorvastatin, wherein at least 90 wt % of said solvent is evaporated by spray drying in less than five minutes.
2. The process of claim 1 wherein said hydroxylic solvent is selected from the group consisting of methanol, ethanol, n-propanol, and iso-propanol.
3. The process of claim 2 wherein said hydroxylic solvent is methanol.
4. The process of claim 1 wherein said evaporation in step (b) is carried out such that at least 90 wt % of said solvent is removed from said solution in less than one minute.
5. The process of claim 1 wherein said solvent is evaporated by spray-coating said solution onto a core, affording an atorvastatin coated core.
6. The process of claim 5 wherein said core is selected from the group consisting of non-pareil seeds, sugar beads, wax beads, glass beads, lactose, microcrystalline cellulose, polymer beads, starch, colloidal silica, calcium carbonate and calcium phosphate.
7. The process of claim 5 wherein said core is selected from the group consisting of a tablet, pill, multiparticulate and capsule.
8. The process of claim 7 wherein said tablet, pill, multipartculate or capsule contains atorvastatin.
9. The process of claim 1 wherein said amorphous atorvastatin is in the form of particles having a mean average diameter ranging in size from 1 μm to less than 500 μm.
10. The process of claim 1 wherein said amorphous atorvastatin is in the form of particles having a mean average diameter ranging in size from 1 μm to less than 100 μm.
11. The process of claim 5 wherein evaporation is carried out such that at least 90 weight % of said solvent is removed from said solution in less than five minutes.
12. The process of claim 5 wherein evaporation is carried out such that at least 90 weight % of said solvent is removed from said solution in less than one minutes.
13. The process of claim 1 wherein said amorphous atorvastatin has a residual solvent level of less than 1 wt %.
14. The process of claim 5 wherein said atorvastatin coated core has a residual solvent level of less than 1 wt %.