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Last Updated: November 25, 2020

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Claims for Patent: 10,105,323

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Summary for Patent: 10,105,323
Title:Pharmaceutical dosage form for immediate release of an indolinone derivative
Abstract: The present invention relates to a pharmaceutical dosage form delivering an immediate release profile containing the active substance 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-a- nilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulph- onate.
Inventor(s): Messerschmid; Roman (Biberach an der Riss, DE), Lach; Peter (Ulm, DE), Sokoliess; Torsten (Neu-Ulm, DE), Stopfer; Peter (Warthausen, DE), Trommeshauser; Dirk (Warthausen, DE)
Assignee: Boehringer Ingelheim International GmbH (Ingelheim am Rhein, DE)
Application Number:15/590,487
Patent Claims: 1. A pharmaceutical dosage form which is a viscous lipid suspension formulation comprising: 10 to 50 wt. % of the active substance 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-a- nilino)-1-phenyl-methylenel]-6-methoxycarbonyl-2-indolinone-monoethanesulp- honate, 10 to 70 wt. % of medium chain triglycerides; 10 to 30 wt. % of hard fat; and 0.25 to 2.5 wt. % of lecithin, which delivers an immediate release profile in which not less than 70% (Q65%) of the active substance is dissolved in 60 minutes in vitro under the following in vitro dissolution conditions according to European Pharmacopeia 6.2: Apparatus 2 (paddle), dissolution medium with 0.1 M HCl (pH 1) and stirring speed of 50 to 150 rpm, at a temperature of 37.degree. C.

2. The pharmaceutical dosage form according to claim 1, wherein it is an orally deliverable dosage form.

3. The pharmaceutical dosage form according to claim 2, wherein it is in the form of a capsule.

4. The pharmaceutical dosage form according to claim 3 in the form of a soft gelatine capsule comprising 50 mg of active substance free base equivalent selected from the group consisting of compositions A, B and C: TABLE-US-00012 Formulation Formulation Formulation A B C mg per mg per mg per Ingredients capsule capsule capsule Active 60.20 60.20 60.20 Substance* Triglycerides, 40.95 53.70 54.00 Medium-chain Hard fat 38.25 25.50 25.50 Lecithin 0.60 0.60 0.30 Gelatin 72.25 72.25 72.25 Glycerol 85% 32.24 32.24 32.24 Titanium 0.20 0.20 0.20 dioxide Iron oxide A 0.32 0.32 0.32 Iron oxide B 0.32 0.32 0.32 Total Capsule Weight 245.33 245.33 245.33.

5. The pharmaceutical dosage form according to claim 3 in the form of a soft gelatine capsule comprising 75 mg of active substance free base equivalent selected from the group consisting of A, B and C: TABLE-US-00013 Formulation Formulation Formulation A B C mg per mg per mg per Ingredients capsule capsule capsule Active 90.3 90.3 90.3 Substance* Triglycerides, 61.425 80.55 80.1 Medium-chain Hard fat 57.375 38.25 38.25 Lecithin 0.9 0.9 1.35 Gelatin 107.11 107.11 107.11 Glycerol 85% 46.84 46.84 46.84 Titanium 0.35 0.35 0.35 dioxide Iron oxide A 0.058 0.058 0.058 Iron oxide B 0.16 0.16 0.16 Total Capsule Weight 364.518 364.518 364.518.

6. The pharmaceutical dosage form according to claim 3 in the form of a soft gelatine capsule comprising 100 mg of active substance free base equivalent selected from the group consisting of compositions A, B and C: TABLE-US-00014 Formulation Formulation Formulation A B C mg per mg per mg per Ingredients capsule capsule capsule Active 120.40 120.40 120.40 Substance* Triglycerides, 81.90 107.40 106.8 Medium-chain Hard fat 76.50 51.00 51.00 Lecithin 1.20 1.20 1.80 Gelatin 111.58 111.58 111.58 Glycerol 85% 48.79 48.79 48.79 Titanium 0.36 0.36 0.36 dioxide Iron oxide A 0.06 0.06 0.06 Iron oxide B 0.17 0.17 0.17 Total Capsule Weight 440.96 440.96 440.96.

7. The pharmaceutical dosage form according to claim 3 in form of a soft gelatine capsule comprising 125 mg of active substance free base equivalent, selected from the group consisting of compositions A, B and C: TABLE-US-00015 Formulation Formulation Formulation A B C mg per mg per mg per Ingredients capsule capsule capsule Active Substance* 150.50 150.50 150.50 Triglycerides, 102.375 134.25 133.5 Medium-chain Hard fat 95.625 63.75 63.75 Lecithin 1.50 1.50 2.25 Gelatin 142.82 142.82 142.82 Glycerol 85% 62.45 62.45 62.45 Titanium dioxide 0.47 0.47 0.47 Iron oxide A 0.08 0.08 0.08 Iron oxide B 0.22 0.22 0.22 Total Capsule Weight 556.04 556.04 556.04.

8. The pharmaceutical dosage form according to claim 3 in form of a soft gelatine capsule comprising 150 mg of active substance free base equivalent selected from the group consisting of compositions A, B and C: TABLE-US-00016 Formulation Formulation Formulation A B C mg per mg per mg per Ingredients capsule capsule capsule Active Substance* 180.60 180.60 180.60 Triglycerides, 122.85 161.10 160.20 Medium-chain Hard fat 114.75 76.50 76.50 Lecithin 1.80 1.80 2.70 Gelatin 142.82 142.82 142.82 Glycerol 85% 62.45 62.45 62.45 Titanium dioxide 0.47 0.47 0.47 Iron oxide A 0.08 0.08 0.08 Iron oxide B 0.22 0.22 0.22 Total Capsule Weight 626.04 626.04 626.04.

9. The pharmaceutical dosage form according to claim 3 in form of a soft gelatine capsule comprising 200 mg of active substance free base equivalent selected from the group consisting of compositions A, B and C: TABLE-US-00017 Formulation Formulation Formulation A B C mg per mg per mg per Ingredients capsule capsule capsule Active 240.80 240.80 240.80 Substance* Triglycerides, 163.30 214.80 216.00 Medium-chain Hard fat 153.50 102.00 102.00 Lecithin 2.40 2.40 1.20 Gelatin 203.19 203.19 203.19 Glycerol 85% 102.61 102.61 102.61 Titanium 0.57 0.57 0.57 dioxide Iron oxide A 0.90 0.90 0.90 Iron oxide B 0.90 0.90 0.90 Total Capsule Weight 868.17 868.17 868.17.

10. The pharmaceutical dosage form according to claim 1, comprising dose-range values of between 25 to 300 mg of the active substance.

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