ACTIVE INGREDIENT CONTAINING STABILISED SOLID MEDICINAL FORMS AND METHOD FOR THE PRODUCTION THEREOF

• US 20090270515A1
• Filed: 09/14/2007
• Published: 10/29/2009
• Est. Priority Date: 09/25/2006
• Status: Active Grant

• Current Assignee: Losan Pharma GmbH
• Original Assignee: Losan Pharma GmbH
• Inventors: Spickermann, Dirk, Gruber, Peter
• Granted Patent: US 9,775,807 B2
• Time in Patent Office: Days
• US Class Current: 514/769
• CPC Class Codes: A61K 9/1611 Inorganic compounds
• CPC Class Codes: A61K 9/2009 Inorganic compounds
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

The invention relates to solid medicinal forms containing at least one active ingredient and at least one pharmaceutically compatible, water soluble drying agent which is selected from the group consisting of trimagnesium dicitrate and/or calcium chloride, the solid medicinal form having a drying loss of at most 6% and a relative equilibrium moisture content of 25% or less. The invention also relates to solid medicinal forms containing a moisture-sensitive active ingredient and trimagnesium dicitrate.

Claims

1. A solid medicinal form containing at least one active ingredient and at least one pharmaceutically compatible, water soluble drying agent, wherein said drying agent is trimagnesium dicitrate, said active ingredient is not trimagnesium dicitrate, and the solid medicinal form has a drying loss, measured at 120°

C./30 min of at most 3% and a relative equilibrium moisture, measured at 25°

C., of 20% or less.

2. The solid medicinal form according to claim 1, wherein the solid medicinal form has a relative equilibrium moisture content of 10% or less.

3. The solid medicinal form according to claim 1, wherein the concentration of the drying agent in the solid medicinal form ranges from 15 to 75% by weight.

4. The solid according to claim 1, wherein said active ingredient is sensitive to moisture.

5. The solid medicinal form according to claim 1, wherein the relative equilibrium moisture of said solid medicinal form is at most 15%.

6. The solid medicinal form according to claim 1, wherein the concentration of the active ingredient in the solid medicinal form is 5 to 50% by weight.

7. The solid medicinal form according to claim 1, wherein the active ingredient is sensitive to moisture.

8. The solid medicinal form according to claim 1, wherein the solid medicinal form comprises a tablet, capsule, granules or a powder.

14. A method of producing a solid medicinal form according to claim 1, comprising the steps of:

1) mixing at least one pharmaceutically active ingredient with a drying agent selected from the group consisting of trimagnesium dicitrate, calcium chloride and combinations thereof,

2) optionally, dry granulating the composition obtained in step a) to obtain granules,

3) compressing or encapsulating the composition obtained in step a) or the granules obtained in step b) to obtain the solid medicinal form, and

4) optionally, packing the solid medicinal form in a tight packaging means, wherein the ratio of the mass of drying agent to the mass of active ingredient in step a) is chosen and the method is carried out under conditions such that the solid medicinal form obtained in step c) has a drying loss, measured at 120°

C./30 min, of at most 6% and a relative equilibrium moisture content, measured at 25°

C., of 25% or less.

15. The method according to claim 14, wherein the drying agent is substantially anhydrous trimagnesium dicitrate.

16. The method according to claim 14, wherein the ratio of the mass of drying agent to the mass of pharmaceutical active ingredient in step a) is 0.75 to 1.5.

9. A solid medicinal form containing at least one moisture-sensitive active ingredient, 5 to 95% by weight of trimagnesium dicitrate and, optionally, further excipients, wherein said active ingredient is not trimagnesium dicitrate.

10. The solid medicinal form according to claim 9, wherein said solid medicinal form contains 30 to 40% moisture-sensitive active ingredient and 30 to 40% trimagnesium dicitrate.

11. The solid medicinal form according to claim 9, wherein said medicinal form further contains 10 to 20% by weight of microcrystalline cellulose, 0.2 to 2% lubricant and 1 to 5% sliding agent.

12. The solid medicinal form according to claim 9, wherein said solid medicinal form has a drying loss of 0.5 to 3%, measured at 120°

C./30 min, and a relative equilibrium moisture content, measured at 25°

C., of less than 10%.

13. The solid medicinal form according to claim 9, wherein said solid medicinal form is packed in a tight packaging means.

17. A method of increasing the chemical stability of a moisture-sensitive pharmaceutical active ingredient, comprising the step of mixing the active ingredient with trimagnesium dicitrate.

18. (canceled)

19. A method of protecting a moisture-sensitive pharmaceutically active ingredient against hydrolysis comprising the steps of mixing the active ingredient with trimagnesium dicitrate.

20. A method of drying a moisture-sensitive pharmaceutically active comprising the step of combining the active ingredient with trimagnesium dicitrate to yield a solid medicinal form.