Claims for Patent: 5,688,529

Summary for Patent: 5,688,529

Title:	Mycophenolate mofetil high dose oral suspensions
Abstract:	High dose, dry granulations or powder blends and aqueous oral suspensions of mycophenolate mofetil or mycophenolic acid, contain: active compound (7.5-30%), suspending/viscosity agent, sweetener, flavor, buffer (to a pH of 5-7.5), and optionally contain flavor enhancer, wetting agent, antimicrobial agent and color.
Inventor(s):	Lidgate; Deborah Marilyn (Los Altos, CA), Wang-Kessler; Li-hua (Palo Alto, CA), Joshi; Bindu (Milpitas, CA), Hegde; Sayee Gojanan (Los Angeles, CA), Gu; Leo (Saratoga, CA)
Assignee:	Syntex (U.S.A) Inc. (Palo Alto, CA)
Application Number:	08/412,645
Patent Claims:	1. A pharmaceutical formulation comprising: as a liquid suspension suitable for oral administration. 2. A pharmaceutical formulation consisting essentially of: adjusted to a pH of 7, as a liquid suspension suitable for oral administration. 3. A pharmaceutical formulation comprising: as a liquid suspension suitable for oral administration. 4. The pharmaceutical formulation of claim 3, consisting essentially of: adjusted to a pH of 7, as a liquid suspension suitable for oral administration. 5. A process for the preparation of a pharmaceutical formulation comprising: as a liquid suspension for oral administration, the process comprising: I. a. adding and dispersing the antimicrobial agent to heated water, followed by adding the suspending and/or viscosity agent(s); b. dissolving, with mixing, the buffer(s), followed by adding the sweetener(s), wetting agent(s), dye(s), flavor enhancer(s), and flavor(s); and c. adding the active compound to the mixture from step b, followed by mixing the liquids well to form a suspension; or II. a. adding and dissolving with mixing the antimicrobial agent and water; b. dispersing the suspending and/or viscosity increasing agent(s) in the dispersion of step a; c. adding with mixing the sweetener(s) to the dispersion of step b; followed by adding the suspending and/or viscosity agent(s) with mixing; followed by adding the sweetener(s) with mixing; d. dissolving the buffer(s) in water, followed by adding and dissolving sweetener(s), followed by adding and dispersing the wetting agent(s), followed by adding and dispersing the active compound; e. combining the dispersions of steps c and d with mixing; f. adding the dye(s) and flavor(s) to the dispersion of step e; and g. bringing the dispersion of step f to volume with purified water. 6. A pharmaceutical formulation comprising: as a dry granulation or powder blend suitable, when constituted with water, for forming a suspension for oral administration, where mg/mL represents concentration after constitution with water. 7. The pharmaceutical formulation of claim 6 provided in a container marked to be filled with purified water to a final predetermined volume. 8. The pharmaceutical formulation of claim 7, comprising: in a container marked to be filled with purified water to a final predetermined volume of 450 mL. 9. The pharmaceutical formulation of claim 7, comprising: in a container marked to be filled with purified water to a final predetermined volume of 450 mL. 10. The pharmaceutical formulation of claim 7, comprising: in a container marked to be filled with purified water to a final predetermined volume of 450 mL. 11. The pharmaceutical formulation of claim 7, comprising: in a container marked to be filled with purified water to a final predetermined volume of 450 mL. 12. The pharmaceutical formulation of claim 7, comprising in a container marked to be filled with purified water to a final predetermined volume of 240 mL. 13. The pharmaceutical formulation of claim 7, comprising in a container marked to be filled with purified water to a final predetermined volume of 120 mL. 14. The pharmaceutical formulation of claim 7, comprising: in a container marked to be filled with purified water to a final predetermined volume of 450 mL. 15. A pharmaceutical formulation, comprising: as a dry granulation or powder blend suitable, when constituted with water, for forming a suspension for oral administration, where mg/mL represents concentration after constitution with water. 16. The pharmaceutical formulation of claim 15 provided in a container marked to be filled with purified water to a final predetermined volume. 17. The pharmaceutical formulation of claim 16, comprising: in a container marked to be filled with purified water to a final predetermined volume of 450 mL. 18. A process for the preparation of a pharmaceutical formulation comprising: as a dry granulation or powder blend suitable, when constituted with water, for forming a suspension for oral administration, where mg/mL represents concentration after constitution with water, the process comprising: I. a. combining the active compound, sweetener(s), wetting agent(s), suspending and/or viscosity increasing agent(s), flavor(s) and antimicrobial agent(s) in a mixer; b. dissolving the dye(s) and buffer(s) in water; c. combining the solution of step (b) to the mixer bowl of step (a) and mixing until a desired granulation size is obtained; d. drying the granulation then milling to reduce particle size; e. adding the suspending and/or viscosity increasing agent(s) to the granulation of step (d) using a blender; or II. a. combining the active compound, sweetener(s), wetting agent(s), suspending and/or viscosity increasing agent(s), dye(s), and buffer(s) and mixing to form a powder blend.