Cyclosporin compositions and process therefor
AssigneeNovartis AG
InventorsMatthias Olbrich, Heinrich Potter
Life of this patent
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Abstract
The invention relates to formulations of cyclosporin with high bioavailability for oral administration, which contain about 1 part by weight of one or more cyclosporin(s), preferably cyclosporin A and/or cyclosporin G, 7.5 to 7.8 parts by weight of one or more polyethylene glycol esters of saturated C10-C22hydroxy fatty acids, 0.7 to 0.85 part by weight of a monohydric alcohol as co-solvent, and 0.7 to 0.8 part by weight of a polyhydric alcohol as co-solvent. The drug form is produced by initially dissolving the cyclosporin in ethanol and, while stirring, adding propylene glycol and SOLUTOL® HS 15 until a clear, viscous solution results, bottled as drinkable solution or packed into capsules.
Claims17
A formulation comprising:
- a) about 1 part by weight cyclosporin;
- b) 7.5 to 7.8 parts by weight of a polyethylene glycol monoester of a saturated C10-C22 hydroxy fatty acid;
- c) 0.7 to 0.85 part by weight of a monohydric alcohol as co-solvent;
- and
- d) 0.7 to 0.8 part by weight of a polyhydric alcohol as co-solvent.
A process for the production of a clear cyclosporin solution comprising:
- a) dissolving about 1 part by weight cyclosporin in from 0.7 to 0.85 part by weight of a monohydric alcohol as co-solvent with continuous stirring at room temperature;
- and
- b) adding from 0.7 to 0.8 part by weight of a polyhydric alcohol as co-solvent and from 7.5 to 7.8 parts by weight of a polyethylene glycol monoester of saturated C10-C22 hydroxy fatty acid with continuous stirring at room temperature.
Dependencies are inferred from the claim text.