Progesterone formulations having a desirable pk profile
US-2024358839-A1 · Oct 31, 2024 · US
US9907756B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9907756-B2 |
| Application number | US-201615204277-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jul 7, 2016 |
| Priority date | Jun 6, 2008 |
| Publication date | Mar 6, 2018 |
| Grant date | Mar 6, 2018 |
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The present invention relates to a suspension formulation containing the active substance 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate, to a capsule pharmaceutical dosage form containing said suspension formulation, to a process for preparing said suspension formulation, to a process for preparing said capsule comprising said suspension formulation and to the packaging material for the finished capsule.
Opening claim text (preview).
The invention claimed is: 1. A formulation of the active substance 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate which comprises a lipid suspension of the active substance in 1 to 90 wt. % of medium chain triglycerides, 1 to 30 wt. % of hard fat and 0.1 to 10 wt. % of lecithin. 2. A capsule comprising a capsule shell and a capsule formulation, wherein the capsule formulation comprises the formulation in accordance with claim 1 . 3. The capsule according to claim 2 , wherein the capsule is a soft gelatin capsule. 4. The capsule according to claim 2 , wherein the capsule shell comprises glycerol as plasticizing agent. 5. The capsule according to claim 2 , wherein the capsule is a hard gelatin or a hydroxypropylmethylcellulose (HPMC) capsule, a polyvinyl alcohol polymer capsule or a pullulan capsule, optionally with a sealing or banding. 6. A lipid suspension consisting essentially of 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate, medium chain triglycerides, hard fat and lecithin, wherein the medium chain triglycerides, hard fat and lecithin are present in the lipid suspension in the following amounts: 1 to 90 wt. % of medium chain triglycerides, 1 to 30 wt. % of hard fat, and 0.1 to 10 wt. % of lecithin. 7. A capsule comprising a capsule shell and a capsule formulation, wherein the capsule formulation comprises the lipid suspension in accordance with claim 6 . 8. The capsule according to claim 7 , wherein the capsule is a soft gelatin capsule.
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