Pharmaceutical formulation
AssigneeF2G Limited
InventorsDerek Law, Graham Edward Morris Sibley
Life of this patent
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Abstract
A pharmaceutical composition suitable for oral administration comprising particles of 2-(1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)-N-(4-(4-(5-fluoropyrimidin-2-yl)piperazin-1-yl)phenyl)-2- oxoacetamideis provided. Also provided is a pharmaceutical composition suitable for parenteral administration wherein the composition comprises 2-(1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)-N-(4-(4-(5-fluoropyrimidin-2-yl)piperazin-1-yl)phenyl)-2-oxoacetamide. The compositions are useful in the treatment of fungal infection in a subject in need thereof.
Claims17
A pharmaceutical composition suitable for oral administration comprising (i) spray-dried particles of a compound of Formula I or a pharmaceutically acceptable salt thereof
- 2-(1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)-N-(4-(4-(5-fluoropyrimidin-2-yl)piperazin-1-yl)phenyl)-2-oxoacetamide, and (ii) one or more excipients comprising hydroxypropyl methyl cellulose acetate succinate (HPMCAS).
A pharmaceutical composition suitable for oral administration comprising (i) spray-dried particles of a compound of Formula I or a pharmaceutically acceptable salt thereof
- 2-(1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)-N-(4-(4-(5-fluoropyrimidin-2-yl)piperazin-1-yl)phenyl)-2-oxoacetamide, wherein the particles are obtained by spray-drying from a solution comprising an organic solvent selected from the group consisting of dichloromethane, methanol, and mixtures thereof.
A pharmaceutical composition suitable for parenteral administration comprising:
- (i) a compound of Formula I or a pharmaceutically acceptable salt thereof
- 2-(1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)-N-(4-(4-(5-fluoropyrimidin-2-yl)piperazin-1-yl)phenyl)-2-oxoacetamide
- (ii) cyclodextrin or modified cyclodextrin;
- and
- (iii) polyethylene glycol.
A method of producing a pharmaceutical composition comprising a compound of Formula I or a pharmaceutically acceptable salt thereof
- 2-(1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)-N-(4-(4-(5-fluoropyrimidin-2-yl)piperazin-1-yl)phenyl)-2-oxoacetamide,
- wherein said method comprises:
- i) dissolving one or more excipients in a solvent;
- ii) adding the compound of Formula I, or the pharmaceutically acceptable salt thereof, to the solution produced in step (i);
- and
- iii) spray drying the solution produced in step (ii),
- wherein:
- the one or more excipients comprises hydroxypropyl methyl cellulose acetate succinate (HPMCAS);
- the solvent is a mixture of dichloromethane and methanol, wherein the volume ratio of dichloromethane to methanol is from 5:1 to 1:1;
- the concentration of hydroxypropyl methyl cellulose acetate succinate (HPMCAS) in the solvent is from 5% to 20% w/v;
- and
- the compound of Formula I, or the pharmaceutically acceptable salt thereof, is added to the solution produced in step (i) to give a concentration of 0.5% to 10% by mass.
A pharmaceutical composition comprising (i) spray-dried particles of a compound of Formula I or a pharmaceutically acceptable salt thereof
- 2-(1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)-N-(4-(4-(5-fluoropyrimidin-2-yl)piperazin-1-yl)phenyl)-2-oxoacetamide, and (ii) a cyclodextrin or modified cyclodextrin, wherein said pharmaceutical composition is in the form of a solution, syrup, emulsion or suspension.
Dependencies are inferred from the claim text.