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Details for Patent: 6,258,341

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Details for Patent: 6,258,341

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 from 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; Sheila R. (Sunnyvale, CA)
Assignee: Inhale Therapeutic Systems, Inc. (San Carlos, CA)
Filing Date:Oct 17, 1996
Application Number:08/733,225
Claims:1. An aerosolized powder composition for pulmonary administration that, prior to aerosolization, has been stored for a minimum period of 3 weeks at a storage temperature (Ts) that is at least 10.degree. C. lower than the glass transition temperature (T.sub.g) of said composition,

said composition comprising a pharmaceutically-acceptable glassy matrix and a pharmacologically active material within the glassy matrix, and characterized by an MMAD between about 1-5 microns both before and after storage.

2. The composition of claim 1, wherein the difference between T.sub.g and T.sub.s is at least about 20.degree. C.

3. The composition of claim 1, wherein the difference between T.sub.g and T.sub.s is at least about 30.degree. C.

4. The composition of claim 1, wherein the T.sub.g is about 35.degree. C. to about 200.degree. C.

5. The composition of claim 4, wherein the T.sub.g is greater than about 45.degree. C.

6. The composition of claim 5, wherein the T.sub.g is greater than about 55.degree. C.

7. The composition of claim 1, wherein T.sub.s is about 2.degree. C. to about 30.degree. C. and T.sub.g is about 22.degree. C. to about 200.degree. C.

8. The composition 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 polyamino acids.

9. The composition of claim 1, wherein the glass former is selected from the group consisting of sodium citrate, raffinose, lactose, trehalose, maltotriose, maltodextrin, maltose, glucopyranosyl-sorbitol, glucopyranosyl-mannitol, polydextrose, sucrose, cycloclodextrin, casein, HSA, hydroxyethyl starch, stachyose, magnesium gluconate, and celloboise.

10. The composition of claim 9, wherein the glass former is selected from the group consisting of sodium citrate, raffinose, lactose, trehalose, maltodextrin, maltose, sucrose, stachyose, magnesium gluconate, and gluocopyranosyl-mannitol.

11. The composition of claim 1, which prior to aerosolization, is in unit dosage form.

12. The combination of claim 11, wherein the unit dosage form includes a moisture barrier.

13. The composition of claim 1, aerosolized in a current of air.

14. A process for maintaining the aerosol performance of a powder composition over time, said process comprising:

(a) removing solvent from a solution comprising a solvent, a glass former and a pharmacologically active material under conditions effective to form a glassy matrix composition suitable for pulmonary administration, said composition having (i) the pharmacologically active material within the matrix, (ii) a glass transition temperature (T.sub.g), and (iii) an MMAD from 1-5 microns, and

(b) storing the composition at a storage temperature (T.sub.s) that is at least 10.degree. C. lower than said T.sub.g, such that the composition maintains an MMAD from 1-5 microns when stored at said T.sub.s for a minimum period of 3 weeks, and

(c) aerosolizing said composition.

15. The process of claim 14, wherein the solvent is removed by spray drying.

16. The process of claim 14, wherein the solvent is removed by evaporative drying.

17. The process of claim 14, wherein the solvent is removed by chemical precipitation.

18. The process of claim 14, wherein the solvent is water.

19. The process of claim 14, wherein the solvent is ethanol.

20. The process of claim 14, wherein the difference between T.sub.g and T.sub.s is at least about 20.degree. C.

21. The process of claim 20 wherein the difference between T.sub.g and T.sub.s is at least about 30.degree. C.

22. The process of claim 14, wherein the T.sub.g is about 35.degree. C. to about 200.degree. C.

23. The process of claim 22 wherein the T.sub.g is greater than about 45.degree. C.

24. The process of claim 23, wherein the T.sub.g is greater than about 55.degree. C.

25. The process of claim 14, wherein T.sub.s is about 2.degree. C. to about 30.degree. C. and T.sub.g is about 22.degree. C. to about 200.degree. C.

26. The process of claim 14, wherein the glassy matrix comprises a glass former chosen from the group consisting of carbohydrates, carbohydrate derivatives, carbohydrate polymers, organic carboxylic salts, synthetic organic polymers, proteins, peptides, amino acids and polyamino acids.

27. The process of claim 26, wherein the glass former is selected from the group consisting of sodium citrate, raffinose, lactose, trehalose, maltotriose, maltodextrin, maltose, glucopyranosyl-sorbitol, glucopyranosyl-mannitol, polydextrose, sucrose, cyclodextrin, casein, HSA, hydroxyethyl starch, stachyose, magnesium gluconate, and cellubiose.

28. The process of claim 14, wherein said aerosolizing step comprises aerosolizing said composition in a current of air.

29. An aerosolized powdered, dispersible composition having stable aerosol performance over time, which composition comprises:

(a) a first, respirable powdered component comprising the composition of claim 1, and

(b) a second, non-respirable powdered component comprising a powdered, pharmaceutically-acceptable carrier.

30. The composition of claim 29, wherein the difference between T.sub.g and T.sub.s of that first component is at least about 20.degree. C.

31. The composition of claim 30, wherein the difference between T.sub.g and T.sub.s is at least about 30.degree. C.

32. The composition of claim 29, wherein the largest particle size of the first component is about 10 microns, with the majority of the particles between about 1 micron to about 5 microns, and the particle size of the second component is between about 15 microns to about 100 microns.
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