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US 8,026,276 B2Granted
Parenteral CCI-779 formulations containing cosolvents, an antioxidant, and a surfactant
AssigneeWyeth
InventorsJoseph T. Rubino, Victoria Siskavich, Maureen M. Harrison, Pooja Gandhi
Life of this patent
Estimating the term…
Abstract
Parenteral formulations of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl) -2-methylpropionic acid (CCI-779) are provided. One parenteral formulation contains CCI-779, an alcoholic co-solvent, and an antioxidant. Another parenteral formulation contains CCI-779, an alcoholic solvent, an antioxidant, a diluent solvent, and a surfactant. Processes for preparing parenteral CCI-779 formulations using a co-solvent concentrate are also provided.
Claims24
A parenteral composition comprising:
- (i) a first mixture of about 1 to about 25 mg/mL of CCI-779, about 15 to about 60% w/v of dehydrated ethanol, about 0.01 to about 0.1% w/v of d,1-α-tocopherol, about 0.001 to about 0.005% w/v of citric acid, and about 15 to about 60% w/v of propylene glycol, and
- (ii) a second mixture of about 15 to about 60% w/v of polysorbate 80, 15 to 60% w/v of polyethylene glycol 400, and about 15 to about 60% w/v of dehydrated ethanol.
A parenteral composition comprising:
- (i) a first mixture of about 1 to about 25 mg/mL of CCI-779, about 15 to about 60% w/v of dehydrated ethanol, about 0.01 to about 0.1% w/v of d,1-α-tocopherol, and about 15 to about 60% w/v of propylene glycol, and
- (ii) a second mixture of about 15 to about 60% w/v of polysorbate 80, 15 to 60% w/v of polyethylene glycol 400, and about 15 to about 60% w/v of dehydrated ethanol.
A parenteral composition consisting of:
- (i) a concentrate of about 1 to about 25 mg/mL of CCI-779, about 0.01 to 0.1% w/v of d,1-α-tocopherol, about 0.001 to about 0.005% w/v of citric acid, and about 15 to about 60% w/v of dehydrated ethanol and propylene glycol, and
- (ii) a diluent of about 15 to about 60% w/v of polysorbate 80, 15 to 60% w/v of polyethylene glycol 400, and about 15 to about 60% w/v of dehydrated ethanol.
A parenteral composition consisting of
- (i) a concentrate of about 1 to about 25 mg/mL of CCI-779, about 0.01 to 0.1% w/v of d,1-α-tocopherol, and about 15 to about 60% w/v of dehydrated ethanol and propylene glycol, and
- (ii) a diluent of about 15 to about 60% w/v of polysorbate 80, 15 to 60% w/v of polyethylene glycol 400, and about 15 to about 60% w/v of dehydrated ethanol.
A parenteral composition comprising:
- (i) about 1 to about 25 mg/mL of CCI-779,
- (ii) about 0.01 to 0.1% w/v of d,1-α-tocopherol,
- (iii) about 0.001 to about 0.005% w/v of citric acid,
- (iv) about 15 to about 60% w/v of a combination of dehydrated ethanol and propylene glycol, and
- (v) about 15 to about 60% w/v of a combination of polysorbate 80 and polyethylene glycol 400.
2 more elements
A parenteral composition comprising:
- (i) about 1 to about 25 mg/mL of CCI-779,
- (ii) about 0.01 to 0.1% w/v of d,1-α-tocopherol,
- (iii) about 0.001 to about 0.005% w/v of citric acid,
- (iv) about 15 to about 60% w/v of a combination of dehydrated ethanol and propylene glycol, wherein the ratio of dehydrated ethanol to propylene glycol is about 1.4:1, and
- (v) about 15 to about 60% w/v of a combination of polysorbate 80 and polyethylene glycol 400, wherein the ratio of polysorbate 80 to polyethylene glycol 400 is about 1:1;
- wherein:
- the ratio of mixture (iv) to (i) is about 50:1;
- and
- the ratio of mixture (v) to (i) is about 50:1.
6 more elements
A parenteral composition comprising:
- (i) about 1 to about 25 mg/mL of CCI-779,
- (ii) about 0.01 to 0.1% w/v of d,1-α-tocopherol,
- (iii) about 15 to about 60% w/v of a combination of dehydrated ethanol and propylene glycol, wherein the ratio of dehydrated ethanol to propylene glycol is about 1.4:1, and
- (iv) about 15 to about 60% w/v of a combination of polysorbate 80 and polyethylene glycol 400, wherein the ratio of polysorbate 80 to polyethylene glycol 400 is about 1:1;
- wherein:
- the ratio of mixture (iii) to (i) is about 50:1;
- and
- the ratio of mixture (iv) to (i) is about 50:1.
5 more elements
A parenteral composition comprising:
- (i) about 2.5% w/v of CCI-779, about 0.075% w/v of d,1-α-tocopherol, about 0.0025% w/v of citric acid, about 40% w/v of dehydrated ethanol, and about 50% w/v of propylene glycol, and
- (ii) about 40% w/v of polysorbate 80, about 20% w/v of dehydrated ethanol, and about 43% w/v of polyethylene glycol 400.
A parenteral composition comprising:
- (i) about 1% w/v of CCI-779,
- (ii) about 0.03% w/v of d,1-α-tocopherol,
- (iii) about 0.001% w/v of citric acid,
- (iv) about 28% w/v of dehydrated ethanol,
- (v) about 20% w/v propylene glycol,
- (vi) about 24% w/v of polysorbate 80 and
- (vii) about 26% w/v of polyethylene glycol 400.
4 more elements
Dependencies are inferred from the claim text.