Formulation
OwnerPaul Richard Gellert, Alison Margaret Pottsinventors
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Abstract
The invention relates to a pharmaceutical formulation, preferably adapted for administration by injection, containing the compound 7a-[9-(4,4,5,5,5-pentafluoropentylsulphinyl)nonyl]oestra-1,3,5(10)-triene-3,17β-diol and an antioxidant, more particularly to a formulation adapted for administration by injection containing the compound 7a-[9-(4,4,5,5,5-pentafluoropentyl-sulphinyl)nonyl]oestra-1,3,5(10)-triene-3,17β-diol in solution in a ricinoleate vehicle which comprises an antioxidant.
Claims17
A pharmaceutical formulation comprising fulvestrant and an antioxidant selected from:
- thiourea;
- tocopherol optionally in the presence of lecithin or ascorbyl palmitate;
- ascorbyl palmitate;
- propyl gallate optionally in the presence of butylated hydroxyanisole or butylated hydroxytoluene;
- dithiothreitol;
- butylated hydroxytoluene;
- dithioerythreitol;
- acetyl cysteine;
- thioglycerol;
- and
- thioglycolic acid.
A formulation according to any preceding claim wherein the formulation is adapted for intramuscular administration.
A pharmaceutical formulation according to any preceding claim wherein the formulation comprises a ricinoleate excipient, a pharmaceutically acceptable non-aqueous ester solvent and a pharmaceutically acceptable alcohol.
A unit dose of a pharmaceutical formulation as claimed in any claim from 1 to 11 wherein the total amount of fulvestrant in the formulation is 250 mg, or more, and the total volume of the formulation is 6 ml, or less.
A pharmaceutical formulation as defined in any preceding claim for use in medical therapy.
Use of fulvestrant in the preparation of a pharmaceutical formulation as defined in any preceding claim for the treatment of a benign or malignant disease of the breast or reproductive tract.
A pharmaceutical formulation adapted for intramuscular administration comprising fulvestrant and an antioxidant selected from ascorbyl palmitate, butylated hydroxyanisole, butylated hydroxytoluene, malic acid, propyl gallate, sodium bisulfite, sodium sulfite, sodium metabisulfite, potassium metabisulfite, potassium bisulfite, sodium thiosulfate, sodium formaldehyde sulfoxylate, L-ascorbic acid, D-ascorbic acid, acetylcysteine, cysteine, thioglycerol, thioglycollic acid, thiolactic acid, thiourea, dithiothreitol, dithioerythreitol, glutathione, nordihydroguaiaretic acid, tocopherol and fumaric acid.
Dependencies are inferred from the claim text.