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Claims for Patent: 8,545,884

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Claims for Patent: 8,545,884

Title:Solid pharmaceutical formulations comprising BIBW 2992
Abstract: The present invention relates to a pharmaceutical dosage form containing the active substance BIBW 2992 as the dimaleate salt, providing an immediate release profile of the active substance, further, the invention relates to compacted intermediates comprising BIBW 2992 dimaleate salt (BIBW 2992 MA.sub.2) in form of a powder prepared using a combined roller compaction and sieving step from BIBW 2992 MA.sub.2, intermediate blends prepared from said compacted intermediate as well as solid oral formulations providing an immediate release profile of the active substance, made from said compacted intermediate or from said intermediate blends ready for use/ingestion, e.g. capsule and tablet formulations such as uncoated or film-coated tablets prepared by direct-compression, and methods for their production.
Inventor(s): Messerschmid; Roman (Biberach, DE), Friedl; Thomas (Ochsenhausen, DE)
Assignee: Boehringer Ingelheim International GmbH (Ingelheim am Rhein, DE)
Application Number:12/995,715
Patent Claims: 1. A compacted intermediate consisting of BIBW 2992 MA.sub.2 (API salt) and an amount of 0 to 1.0% of a lubricant, calculated on the amount of API salt by weight, in form of a powder with a particle size distribution of x10<200 .mu.m, 1 .mu.m<x50<300 .mu.m, 75 .mu.m<x90<600 .mu.m, obtainable by roller compaction, combined with at least one sieving step after compaction.

2. The compacted intermediate of claim 1 characterized by a poured density (.rho..sub.p) in the range of 0.2 g/mL<.rho..sub.p<1.0 g/mL and/or a Hausner Factor (HF) in the range of 1.00<HF<1.30.

3. An intermediate or final blend prepared from the compacted intermediate according to claim 1.

4. The intermediate or final blend according to claim 3, further characterized by contents selected from components (a) to (g): (a) compacted intermediate of BIBW 2992 MA.sub.2 in an amount of about 1 to 99% by weight, (b) optionally one or more carriers in an amount of about 10 to 99% by weight, (c) one or more binders in an amount of about 0 to 99% by weight, (d) one or more glidants in an amount of about 0 to 10% by weight, (e) one or more disintegrants in an amount of about 0 to 10% by weight, (f) one or more lubricants in an amount of about 0 to 10% by weight, and (g) 0 to 10% by weight of further excipients and/or adjuvants, wherein presence of at least one of components (b) to (g) is mandatory but also two up to at most all six of the optional components (b) to (g) are allowed to be present in addition to component (a) in the intermediate and final blend, the sum of all components adding to 100%.

5. A solid oral formulation ready for use/ingestion prepared from the compacted intermediate of BIBW 2992 MA.sub.2 according to claim 1.

6. The solid oral formulation according to claim 5 selected from powders, granules, pellets, tablets, capsules, chewable tablets, dispersible tablets, troches and lozenges.

7. A solid oral formulation, wherein the formulation is a tablet and obtained by direct compression of a final blend according to claim 3 or by tableting of pellets or granules obtained by conventional wet-, dry or hot-melt granulation of an intermediate blend according to claim 3.

8. The tablet of claim 7, said tablet being uncoated or coated.

9. The tablet of claim 8, comprising 1 to 150 mg of the API, based on BIBW 2992 (the free base).

10. The tablet of claim 9, further comprising 50 to 500 mg of carrier, binder or a combination thereof, 0.1 to 5 mg of a glidant, 1 to 15 mg of a disintegrant, and 1 to 15 mg of a lubricant.

11. The solid formulation of claim 5, packaged in PVC-blisters, PVDC-blisters or a moisture-proof packaging material such as aluminium foil blister packs, alu/alu blister, transparent or opaque polymer blister with pouch, polypropylene tubes, colored blister materials, tubes, brown glass bottles glass bottles and HDPE bottles optionally containing a child-resistant feature, optionally comprising a desiccant such as molecular sieve or silica gel.

12. A method for producing the compacted intermediate of BIBW 2992 MA.sub.2 according to claim 1 in form of a powder comprising compacting by roller compaction combined with at least one sieving step.

13. The method of claim 12, wherein the roller compaction step is carried out with BIBW 2992 MA.sub.2 alone or, optionally, with a pre-blend of BIBW 2992 MA.sub.2 with 0 to 1.0% of a lubricant in a freefall or tumble blender to prevent major sticking on the compaction rolls.

14. The method of claim 13, wherein the roller compaction step is carried out on a roller compactor optionally with horizontally, vertically or 45.degree. angle alignment of the compaction rolls, which may be smooth or shaped on their surface; using a compaction force varying between 1 kN/cm and 20 kN/cm, at a compaction speed of the compaction rolls between 1 rpm and 30 rpm, and a gap width between the compaction rolls between 1 mm and 10 mm.

15. A solid oral formulation ready for use/ingestion prepared from an intermediate blend according to claim 3.

16. The solid oral formulation according to claim 15 selected from powders, granules, pellets, tablets, capsules, troches and lozenges.

17. The solid formulation of claim 15, packaged in PVC-blisters, PVDC-blisters or a moisture-proof packaging material such as aluminium foil blister packs, alu/alu blister, transparent or opaque polymer blister with pouch, polypropylene tubes, colored blister materials, tubes, brown glass bottles glass bottles and HDPE bottles optionally containing a child-resistant feature, optionally comprising a desiccant such as molecular sieve or silica gel.

18. The solid oral formulation according to claim 16 which is in the form of a tablet selected from chewable tablet and dispersible tablet.

19. The tablet of claim 18, characterized by a composition selected from formulations A, B, C, D and E: TABLE-US-00016 Formulation A B C D E mg per mg per mg per mg per mg per Ingredient tablet tablet tablet tablet tablet BIBW 2992 MA.sub.2, unmilled 29.5600 44.3400 59.1200 73.9000 103.4600 (=BIBW 2992 base) (20.0000) (30.0000) (40.0000) (50.0000) (70.0000) Lactose monohydrate 123.8600 185.7900 247.7200 309.6500 433.5100 Microcrystalline cellulose 18.4800 27.7200 36.9600 46.2000 64.6800 Crospovidone 3.6000 5.4000 7.2000 9.0000 12.6000 Colloidal anhydrous silica 0.9000 1.3500 1.8000 2.2500 3.1500 Magnesium stearate 3.6000 5.4000 7.2000 9.0000 12.6000 Total 180.0000 270.0000 360.0000 450.0000 630.0000

which optionally are coated with a film-coat characterized by the following compositions selected for formulations A, B, C, D and E: TABLE-US-00017 Coating for Formulation A B C D E Ingredient mg per tablet Hypromellose 2.5000 3.5000 4.0000 5.0000 6.0000 Polyethylene 0.5000 0.7000 0.8000 1.0000 1.2000 glycol 400 Titanium dioxid 1.1300 0.6825 1.8080 0.9750 1.1700 Indigo Carmine 0.0700 0.2450 0.1120 0.3500 0.4200 aluminum lacquer Talcum 0.6500 1.6625 1.0400 2.3750 2.8500 Polysorbate 80 0.1500 0.2100 0.2400 0.3000 0.3600 Purified water -- -- -- -- -- (volatile component) Total 5.0000 7.0000 8.0000 10.0000 12.0000.

20. The tablet of claim 18, characterized by a composition selected from formulations F, G, H, I, J and K: TABLE-US-00018 Formulation F G H I J K mg per mg per mg per mg per mg per mg per Ingredient tablet tablet tablet tablet tablet tablet BIBW 2992 MA.sub.2, unmilled 7.390 29.560 147.800 7.390 29.560 147.800 (=BIBW 2992 base) (5.00) (20.0000) (100.0000) (5.00) (20.0000) (100.00) Lactose monohydrate 58.048 232.190 550.200 65.435 261.740 616.200 Microcrystalline cellulose 7.500 30.000 80.000 -- -- -- Crospovidone 0.750 3.000 8.000 0.750 3.000 16.000 Colloidal anhydrous silica 0.375 1.500 4.000 0.300 1.200 8.000 Magnesium stearate 0.937 3.750 10.000 1.125 4.500 12.000 Total 75.00 300.00 800.00 75.00 300.00 800.00

formulations F, G and H optionally being coated with a film-coat characterized by the following compositions: TABLE-US-00019 Coating for Formulation F G H Ingredient mg per tablet Hypromellose 1.500 5.000 10.000 Polyethylene glycol 400 0.150 0.500 1.000 Titanium dioxid 0.750 2.500 5.000 Talcum 0.600 2.000 4.000 Purified water -- -- -- (volatile component) Total 3.000 10.000 20.000.
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