Antisense compositions and methods of making and using same
AssigneeNogra Pharma Limited
InventorsSergio Baroni, Salvatore Bellinvia, Francesca Viti
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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.
Claims9
An oral dosage form comprising an amount of anti-SMAD7 antisense oligonucleotide comprising the nucleotide sequence of SEQ ID NO:1, wherein all internucleoside linkages in the anti-SMAD7 antisense oligonucleotide are O,O-linked phosphorothioates, or a pharmaceutically acceptable salt thereof, wherein about 10% to about 30% of the amount of the anti-SMAD7 antisense oligonucleotide is released in an environment of pH of 6.6 from the oral dosage form over a period of 30 minutes in an HPLC dissolution method and substantially none of the amount of anti-SMAD7 antisense oligonucleotide is released from the oral dosage form in an environment of pH of 1.0 over a period of 120 minutes in an HPLC dissolution method.
An oral dosage form comprising an amount of anti-SMAD7 antisense oligonucleotide comprising the nucleotide sequence of SEQ ID NO:1, wherein all internucleoside linkages in the anti-SMAD7 antisense oligonucleotide are O,O-linked phosphorothioates, or a pharmaceutically acceptable salt thereof, wherein not more than about 50% of the amount of the anti-SMAD7 antisense oligonucleotide is released in an environment of pH of 6.6 from the oral dosage form over a period of 30 minutes in an HPLC dissolution method and substantially none of the amount of anti-SMAD7 antisense oligonucleotide is released from the oral dosage form in an environment of pH of 1.0 over a period of 120 minutes in an HPLC dissolution method.
An oral dosage form comprising an amount of anti-SMAD7 antisense oligonucleotide comprising the nucleotide sequence of SEQ ID NO:1, wherein all internucleoside linkages in the anti-SMAD7 antisense oligonucleotide are O,O-linked phosphorothioates, or a pharmaceutically acceptable salt thereof, wherein substantially none of the amount of the anti-SMAD7 antisense oligonucleotide is released in an environment of pH of 1.0 from the oral dosage form over a period of 120 minutes in an HPLC dissolution method.
Dependencies are inferred from the claim text.