Antisense compositions and methods of making and using same
AssigneeNogra Pharma Limited
InventorsSergio Baroni, Salvatore Bellinvia, Francesca Viti
Life of this patent
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Abstract
The present invention provides pharmaceutical formulations for oral administration of antisense oligonucleotides, such as antisense oligonucleotides against SMAD7. The pharmaceutical formulations can be used to treat Crohn's disease, ulcerative colitis and chronic inflammatory bowel disease.
Claims21
A pharmaceutical tablet formulation for oral administration of an antisense oligonucleotide comprising:
- an intra-granular phase comprising an antisense oligonucleotide represented by SEQ ID NO 1 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable filler;
- an extra-granular phase comprising a disintegrant;
- and
- an enteric coating comprising an ethylacrylate-methacrylic acid copolymer.
A pharmaceutically acceptable tablet for oral use comprising:
- about 0.5% to about 10% by weight of an antisense oligonucleotide represented by SEQ ID NO 1 or a pharmaceutically acceptable salt thereof;
- about 30% to about 50% by weight mannitol;
- about 10% to about 30% by weight microcrystalline cellulose;
- and
- an enteric coating comprising an ethylacrylate-methacrylic acid copolymer.
An oral dosage form comprising about 35 mg to about 500 mg of an antisense oligonucleotide represented by SEQ ID NO 1 or a pharmaceutically acceptable salt thereof within an enteric coating comprising an ethylacrylate-methacrylic acid copolymer.
A pharmaceutically acceptable tablet for oral use comprising:
- an intra-granular phase comprising:
- about 5 to about 10% by weight antisense oligonucleotide represented by SEQ ID NO 1 or a pharmaceutically acceptable salt thereof;
- about 40% by weight mannitol,
- about 8% by weight microcrystalline cellulose,
- about 5% by weight hydropropylmethyl cellulose, and
- about 2% by weight sodium starch glycolate;
- and
- an extra-granular phase comprising:
- about 17% by weight microcrystalline cellulose,
- about 2% by weight sodium starch glycolate,
- about 0.4% by weight magnesium stearate;
- and
- an enteric coating over the tablet, comprising an ethylacrylate-methacrylic acid copolymer,
- wherein the percentages refer to the weights of the ingredients compared to the total weight of the tablet.
Dependencies are inferred from the claim text.