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Details for Patent: 7,186,401

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Details for Patent: 7,186,401

Title:Dry powder for inhalation
Abstract: The aim of the invention is to improve the moisture resistance of dry powder formulations for inhalation which contain a pharmaceutically ineffective carrier of not-inhalable particle size and a finely divided pharmaceutically active compound of inhalable particle size and to also improve the storage stability of said formulations. To this end, magnesium stearate is used in said formulations. One of the features of the inventive dry powder is that a high fine particle dosage or fine particle fraction can be maintained also under relatively extreme temperature and humidity conditions.
Inventor(s): Keller; Manfred (Bad Krozingen, DE), Muller-Walz; Rudi (Schopfheim, DE)
Assignee: Jagotec AG (Muttenz, CH)
Filing Date:Jul 28, 2003
Application Number:10/628,965
Claims:1. A method of producing a dry powder formulation for inhalation, said formulation having a fine particle fraction (FPF) with reduced sensitivity to penetrating moisture, and comprising a pharmaceutically inactive carrier comprising particles of noninhalable size and a pharmaceutically active component comprising at least one finely-divided pharmaceutically active compound comprising particles of inhalable size; said method comprising: mixing together (i) said pharmaceutically inactive carrier; (ii) said pharmaceutically active component; and (iii) pulverulent magnesium stearate, in an amount of 0.1 to 2% by weight, based on the total weight of the formulation, said amount being effective to provide the FPF with reduced sensitivity to penetrating moisture and to stabilize the dry powder formulation.

2. The method of claim 1, comprising mixing by tumble blending.

3. The method of claim 1, comprising first mixing the carrier with the magnesium stearate and then admixing the pharmaceutically active component therewith.

4. The method of claim 1, comprising first mixing the carrier with the pharmaceutically active component and then admixing the magnesium stearate therewith.

5. The method of claim 1, wherein the pharmaceutically active compound is a hygroscopic compound capable of absorbing at least 0.5% by weight of its own weight of absorptively bound water when stored in air having a relative humidity of 50%.

6. The method of claim 1, wherein the pharmaceutically active compound is a hydrophilic compound having a wetting angle of less than 90.degree..

7. The method of claim 1, wherein the pharmaceutically active compound is a hydrophilic compound having a wetting angle of less than 70.degree..

8. The method of claim 1, wherein the pharmaceutically active compound is formoterol or a pharmaceutically acceptable salt thereof.

9. The method of claim 1, wherein the pharmaceutically active compound is selected from the group consisting of formoterol fumarate, formoterol tartrate, ipratropium bromide and tiotropium bromide.

10. The method of claim 1, wherein the pharmaceutically active component further comprises a second pharmaceutically active compound having particles of inhalable size.

11. The method of claim 10, wherein the pharmaceutically active component comprises a) a compound selected from the group consisting of formoterol fumarate, formoterol tartrate, levalbuterol sulfate and salmeterol xinafoate, and b) a corticosteroid.

12. The method of claim 1, wherein the pharmaceutically active compound has a mean particle size of 1 to 10 .mu.m.

13. The method of claim 1, wherein the pharmaceutically active compound has a mean particle size of 1 to 6 .mu.m.

14. The method of claim 1, wherein the magnesium stearate is present in an amount of 0.25 to 1% by weight, based on the total weight of the formulation.

15. The method of claim 1, wherein the magnesium stearate is present in an amount of 0.4 to 0.8% by weight, based on the total weight of the formulation.

16. The method of claim 1, wherein the carrier is selected from the group consisting of monosaccharides, disaccharides, sugar alcohols, polylactic acid and cyclodextrin.

17. The method of claim 1, wherein the carrier is selected from the group consisting of glucose, lactose monohydrate and trehalose.

18. The method of claim 1, wherein the carrier particles have a mass mean aerodynamic diameter of 10 to 500 .mu.m.

19. The method of claim 1, wherein the carrier particles have a mass mean aerodynamic diameter of 50 to 200 .mu.m.

20. The method of claim 1, further comprising admixing particles of micronized lactose monohydrate wherein at least 50% of the particles thereof have a maximum particle size of 10 .mu.m, with said carrier, said pharmaceutically active component and said magnesium stearate.

21. A method of stabilizing a fine particle fraction (FPF) of a dry powder formulation for inhalation, said formulation comprising a pharmaceutically inactive carrier and a finely-divided pharmaceutically active compound; said method comprising: mixing said carrier having particles of noninhalable particle size, said pharmaceutically active compound having particles of inhalable particle size and pulverulent magnesium stearate, an amount of 0.1 to 2% by weight, based on the total weight of the formulation, said amount being effective to stabilize the FPF of the formulation against penetrating moisture.

22. A dry powder formulation for inhalation, comprising: a) a pharmaceutically inactive carrier having particles of noninhalable particle size, b) at least two finely divided pharmaceutically active compounds having particles of inhalable particle size, and c) magnesium stearate adhering to said particles of said pharmaceutically inactive carrier, the magnesium stearate being in an amount of 0.1 to 2% by weight, based on the total weight of the formulation, said amount being sufficient to provide the formulation with an improved resistance to moisture.

23. The formulation of claim 22, wherein one pharmaceutically active compound is selected from the group consisting of formoterol fumarate, formoterol tartrate, levalbuterol sulfate and salmeterol xinafoate, and a second pharmaceutically active compound is a corticosteroid.

24. The formulation of claim 22, wherein the magnesium stearate is present in an amount of 0.25 to 1% by weight, based on the total weight of the formulation.

25. The formulation of claim 22, further comprising particles of micronized lactose monohydrate wherein at least 50% of the particles thereof have a maximum particle size of 10 .mu.m.

26. The method of claim 1, wherein said formulation exhibits a reduction in FPF by at least 50% within 10 days of storage at 40.degree. C. and 75% relative atmospheric humidity.

27. The method of claim 21, wherein said formulation exhibits a reduction in FPF by at least 50% within 10 days of storage at 40.degree. C. and 75% relative atmospheric humidity.

28. The formulation of claim 22, said formulation comprising a fine particle fraction (FPF) and exhibiting a reduction in said FPF by at least 50% within 10 days of storage at 40.degree. C. and 75% relative atmospheric humidity.
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