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Claims for Patent: 6,582,728

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Claims for Patent: 6,582,728

Title: Spray drying of macromolecules to produce inhaleable dry powders
Abstract:According to the subject invention, dispersible dry powder pharmaceutical-based compositions are provided, including methods for their manufacture and dry powder dispersion devices. A dispersible dry powder pharmaceutical-based composition is one having a moisture content of less than about 10% by weight (%w) water, usually below about 5%w and preferably less than about 3%w; a particle size of about 1.0-5.0 .mu.m mass median diameter (MMD), usually 1.0-4.0 .mu.m MMD, and preferably 1.0-3.0 .mu.m MMD; a delivered dose of about >30%, usually >40%, preferably >50%, and most preferred >60%; and an aerosol particle size distribution of about 1.0-5.0 .mu.m mass median aerodynamic diameter (MMAD), usually 1.5-4.5 .mu.m MMAD, and preferably 1.5-4.0 MMAD. Such composition are of pharmaceutical grade purity.
Inventor(s): Platz; Robert M. (Half Moon Bay, CA), Patton; John S. (San Carlos, CA), Foster; Linda (Sunnyvale, CA), Eljamal; Mohammed (San Jose, CA)
Assignee: Inhale Therapeutic Systems, Inc. (San Carlos, CA)
Application Number:08/423,515
Patent Claims: 1. A method for preparing a dry powder composition for pulmonary administration, said method comprising the following steps performed sequentially: (a) providing an aqueous solution comprising a pharmaceutically active macromolecule and a pharmaceutically acceptable carrier selected from the group consisting of human serum albumin, carbohydrates, amino acids, polypeptides, buffers, and salts; and (b) spray drying said aqueous solution from step (a) at a temperature in the range from 50.degree. C. to 200.degree. C. to produce a non-liposomal dry powder composition suitable for pulmonary administration comprising a therapeutically effective amount of said pharmaceutically active macromolecule and said pharmaceutically acceptable carrier and having a moisture content below 10% by weight, wherein said pharmaceutically active macromolecule retains its activity upon spray drying.

2. The method of claim 1, wherein said composition is substantially free from penetration enhancers.

3. The method of claim 1, wherein said pharmaceutically acceptable carrier is human serum albumin.

4. The method of claim 1, wherein said pharmaceutically acceptable carrier comprises a carbohydrate.

5. The method of claim 4, wherein said carbohydrate is selected from the group consisting of monosaccharides, disaccharides, cyclodextrins, polysaccharides, maltodextrins, dextrans, and alditols.

6. The method of claim 4, wherein said carbohydrate is selected from the group consisting of monosaccharides, disaccharides, polysaccharides, and alditols.

7. The method of claim 4, wherein said carbohydrate is selected from the group consisting of galactose, D-mannose, sorbose, lactose, trehalose, raffinose, mannitol, and xylitol.

8. The method of claim 4, wherein sad carbohydrate is mannitol.

9. The method of claim 1, wherein said pharmaceutically acceptable carrier comprises an amino acid.

10. The method of claim 1, wherein 95% of the mass of said dry powder composition has a particle size less than 10 .mu.m.

11. The method of claim 1, wherein said dry powder composition is of homogeneous constitution.

12. The method of claim 1, wherein said dry powder composition, when pulmonarily administered to a patient in need thereof, is systemically absorbed in a rapid manner.

13. The method of claim 1, wherein said dry powder composition comprises particles having an average particle size less, than about 10 .mu.m in diameter.

14. The method of claim 1, wherein said pharmaceutically active macromolecule is selected from the group consisting of polypeptides, proteins and nucleic acids.

15. The method of claim 1, wherein at least about 80% of the mass of said dry powder composition comprises particles having a diameter of less than about 5 .mu.m.

16. The method of claim 1, wherein said dry powder composition contains less than about 5% macromolecule degradation products.

17. The method of claim 1, wherein said moisture content in said dry powder composition is less than about 5% by weight.

18. The method of claim 1, wherein said dry powder composition comprises particles having an aerosol particle size distribution of about 1-5 .mu.m MMAD.

19. The method of claim 1, wherein said dry powder composition has a delivered dose of greater than 30%.

20. The method of claim 19, wherein said dry powder composition has a delivered dose of greater than about 50%.

21. The method of claim 1, wherein said dry powder composition is aerosolizable in a dry powder inhaler.

22. The method of claim 1, further comprising: (c) dispersing an amount of said dry powder composition in a gas stream to form an aerosol.

23. The method of claim 1, wherein said aqueous solution consists essentially of water as the solvent.

24. The method of claim 1, wherein said pharmaceutically active macromolecule retains at least about 74% of its activity upon spray drying.

25. A dry powder composition for pulmonary administration produced by the method of claim 1.

26. A method for preparing a dry powder composition for pulmonary administration, said method comprising the following steps performed sequentially: (a) providing an aqueous mixture comprising a pharmaceutically active macromolecule and a pharmaceutically acceptable carder selected from the group consisting of human serum albumin, carbohydrates, amino acids, polypeptides, buffers, and salts; and (b) spray drying said aqueous solution from step (a) at a temperature in the range from 50.degree. C. to 200.degree. C. to produce a non-liposomal dry powder composition suitable for pulmonary administration comprising a therapeutically effective amount of said pharmaceutically active macromolecule and said pharmaceutically acceptable carrier and having a moisture content below 10% by weight, wherein said pharmaceutically active macromolecule retains its activity upon spray drying.

27. The method of claim 4, wherein said pharmaceutically acceptable carrier comprises a carbohydrate selected from the group consisting of monosaccharides, disaccharides, cyclodextrins, maltodextrins, dextrans and alditols.
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