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Details for Patent: 6,589,560

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Details for Patent: 6,589,560

Title: Stable glassy state powder formulations
Abstract:A powdered, dispersible composition having stable dispersibility over time is provided. The composition exhibits a characteristic glass transition temperature (T.sub.g) and a recommended storage temperature (T.sub.s), wherein the difference between T.sub.g and T.sub.s is at least about 10.degree. C. (i.e. T.sub.g -T.sub.s is greater than 10.degree. C.). The composition comprises a mixture of a pharmaceutically-acceptable glassy matrix and at least one pharmacologically active material within the glassy matrix. It may be further mixed with a powdered, pharmaceutically-acceptable carrier. It is particularly valuable in unit dosage form having a moisture barrier, in combination with appropriate labelling instructions. A process for producing a powdered dispersible composition is also provided, wherein the process comprises removing the solvent from a solution comprising a solvent, a glass former and a pharmacologically active material under conditions sufficient to form a glassy matrix having the pharmacologically active material within the matrix.
Inventor(s): Foster; Linda C. (Mountain View, CA), Kuo; Mei-chang (Palo Alto, CA), Billingsley; Shelia R. (Sunnyvale, CA)
Assignee: Nektar Therapeutics (San Carlos, CA)
Filing Date:Jun 11, 2001
Application Number:09/879,853
Claims:1. A method for maintaining the dispersibility of a powdered composition over time, said method comprising: (i) providing a powder suitable for pulmonary administration, said powder comprising a pharmaceutically acceptable glassy matrix and a pharmacologically active material, (ii) determining the glass transition temperature, Tg, of said powder, and (iii) storing the powder in unit dosage form at a storage temperature, Ts, that is at least 10.degree. C. less than the Tg of said powder.

2. The method of claim 1, wherein said storing step comprises storing the powder at said Ts for a period of at least one month.

3. The method of claim 1, wherein said powder is characterized by a dispersibility of at least 40% both before and after said storing.

4. The method of claim 1, wherein said powder is characterized by a dispersibility of at least 50% both before and after said storing.

5. The method of claim 1, wherein said powder is characterized by a dispersibility of at least 60% both before and after said storing.

6. The method of claim 1, wherein the dispersibility of said powder does not change appreciably over the course of said storing.

7. The method of claim 2, wherein said storing is carried out at a storage temperature that is at least 20.degree. C. less than the Tg of said powder.

8. The method of claim 1, wherein said providing step comprises forming a mixture comprising a solvent, a glass former capable of forming a glassy matrix, and a pharmacologically active material, and removing the solvent from said mixture by spray drying to thereby provide a powder suitable for pulmonary administration.

9. The method of claim 8, wherein said mixture comprises an aqueous solution.

10. The method of claim 1, wherein said pharmacologically active material is selected from the group consisting of small molecules, peptides, proteins, glycoproteins, RNA sequences, DNA sequences, genes and gene vectors.

11. The method of claim 1, wherein said storing step comprises storing said powder for a period of six months to about two years.

12. The method of claim 1, wherein said storing step comprises storing said powder for a period of two weeks to about three years.

13. The method of claim 3, wherein said storing step comprises storing said powder for a period of two weeks to about three years.

14. The method of claim 4, wherein said storing step comprises storing said powder for a period of two weeks to about three years.

15. The method of claim 5, wherein said storing step comprises storing said powder for a period of two weeks to about three years.

16. The method of claim 6, wherein said storing step comprises storing said powder for a period of two weeks to about three years.

17. The method of claim 1, wherein said powder has a moisture content of less than about 10 percent by weight.

18. The method of claim 1, wherein said powder has a moisture content of less than about 5 percent by weight.

19. The method of claim 1, wherein said powder has a moisture content of less than about 2% by weight.

20. The method of claim 1, wherein said storing is carried out at a storage temperature that is at least 30.degree. C. less than the Tg of said powder.

21. The method of claim 1, wherein the Tg of said powder in step (ii) is greater than 45.degree. C.

22. The method of claim 1, wherein the Tg of said powder in step (ii) is greater than 55.degree. C.

23. The method of claim 1, wherein the glassy matrix comprises a glass former selected from the group consisting of carbohydrates, carbohydrate derivatives, carbohydrate polymers, organic carboxylic acid salts, synthetic organic polymers, proteins, peptides, amino acids, and mixtures thereof.

24. The method of claim 1, wherein the glassy matrix comprises a glass former selected from the group consisting of carbohydrates, peptides, and amino acids.

25. The method of claim 1, wherein the glassy matrix comprises a glass former selected from the group consisting of sodium citrate, raffinose, lactose, trehalose, maltotriose, maltodextrin, maltose, glucopyranosyl-sorbitol, glucopyranosyl-mannitol, polydextrose, sucrose, cyclodextrin, casein, human serum albumin, hydroxyethyl starch, stachyose, magnesium gluconate, cellobiose, and mixtures thereof.

26. The method of claim 1, further comprising aerosolizing said powder.

27. The method of claim 26, wherein said aerosolizing is carried out by actuating a dry powder inhaler.
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