Formulation
AssigneeAstraZeneca AB
InventorsJohn R. Evans, Rosalind U. Grundy
Life of this patent
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Abstract
The invention relates to a novel sustained release pharmaceutical formulation adapted for administration by injection containing the compound 7α-[9-(4,4,5,5,5-pentafluoropentylsulphinyl)nonyl]oestra-1,3,5(10)-triene-3,17β-diol, more particularly to a formulation adapted for administration by injection containing the compound 7α-[9-(4,4,5,5,5-pentafluoropentylsulphinyl)nonyl]oestra-1,3,5(10)-triene-3,17β-diol in solution in a ricinoleate vehicle which additionally comprises at least one alcohol and a non-aqueous ester solvent which is miscible in the ricinoleate vehicle.
Claims17
A pharmaceutical formulation adapted for intra-muscular injection comprising fulvestrant, 30% or less weight of a pharmaceutically-acceptable alcohol per volume of formulation, at least 1% weight of a pharmaceutically-acceptable non-aqueous ester solvent miscible in a ricinoleate vehicle per volume of formulation and a sufficient amount of a ricinoleate vehicle so as to prepare a formulation which is capable after injection of attaining a therapeutically significant blood plasma fulvestrant concentration of at least 2.5 ngml−1 for at least 2 weeks.
A pharmaceutical formulation adapted for intra-muscular injection comprising fulvestrant, 30% or less weight of a pharmaceutically-acceptable alcohol per volume of formulation, at least 1% weight of a pharmaceutically-acceptable non-aqueous ester solvent miscible in a ricinoleate vehicle per volume of formulation and a sufficient amount of a ricinoleate vehicle so as to prepare a formulation of at least 45 mgml−1 of fulvestrant.
A pharmaceutical formulation as claimed in any claim from 1 to 6 which contains 60% w/v or less of a pharmaceutically-acceptable non-aqueous ester solvent.
A pharmaceutical formulation as claimed in any claim from 1 to 13 wherein the pharmaceutically-acceptable alcohol is a mixture of ethanol and benzyl alcohol.
A pharmaceutical formulation as claimed in any claim from 1 to 14 wherein the pharmaceutically-acceptable non-aqueous ester solvent is selected from benzyl benzoate, ethyl oleate, isopropyl myristate, isopropyl palmitate or a mixture of any thereof.
A pharmaceutical formulation as claimed in any claim from 1 to 15 wherein the pharmaceutically-acceptable non-aqueous ester solvent is benzyl benzoate.
A pharmaceutical formulation as claimed in any claim from 1 to 16 wherein the total volume of the formulation is 6 ml, or less, and the concentration of fulvestrant is at least 4 mgml−1.
Dependencies are inferred from the claim text.