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Claims for Patent: 8,263,600

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Claims for Patent: 8,263,600

Title:Antifungal composition with enhanced bioavailability
Abstract: A liquid suspension comprising an antifungally effective amount of the micronized compound represented by the chemical structural formula I: ##STR00001## at least one thickening agent, a non-ionic surfactant, and a pharmaceutically acceptable liquid carrier is disclosed.
Inventor(s): Sharpe; Stefan (Jersey City, NJ), Sequeira; Joel (Edison, NJ), Harris; David (New Providence, NJ), Mahashabde; Shashank (Kendall Park, NJ)
Assignee: Merck Sharp & Dohme Corp. (Rahway, NJ)
Application Number:13/161,097
Patent Claims: 1. A liquid suspension comprising: 40 mg/ml of a micronized compound represented by the chemical structural formula I: ##STR00008## wherein the micronized compound of formula I has a mean particle size of about 1800 nm; Polysorbate 80; an effective amount of a buffer system comprising sodium citrate and citric acid sufficient to maintain a pH in the range of about 4.0 to about 6.0; a combination of thickening agents comprising xanthan gum and liquid sugar; and a pharmaceutically acceptable liquid carrier comprising glycerin.

2. A liquid suspension comprising: 40 mg/ml of a micronized compound represented by the chemical structural formula I: ##STR00009## wherein the micronized compound of formula I has a mean particle size of about 1000 nm to about 1800 nm; Polysorbate 80; an effective amount of a buffer system comprising sodium citrate and citric acid sufficient to maintain a pH in the range of about 4.0 to about 6.0; a combination of thickening agents comprising xanthan gum and liquid sugar; and a pharmaceutically acceptable liquid carrier comprising glycerin.

3. A liquid suspension comprising: posaconazole (micronized), represented by the chemical structural formula I: ##STR00010## wherein the micronized compound of formula I has a mean particle size of about 1000 nm to about 1800 nm in an amount of about 40 mg/ml; Polysorbate 80, in an amount between about 5 mg/ml and about 50 mg/ml; sodium citrate, in an amount between about 0.4 and about 0.8 mg/ml; citric acid, in an amount between about 0.36 and about 0.6 mg/ml; simethicone, in an amount between about 2 mg/ml and about 4 mg/ml; xanthan gum, in an amount between about 1 mg/ml and about 5 mg/ml; sodium benzoate, in an amount between about 0.5 mg/ml and about 3 mg/ml; liquid glucose, in an amount between about 200 mg/ml and about 500 mg/ml; and glycerin, in an amount between about 50 mg/ml and about 150 mg/ml.

4. The liquid suspension of claim 1, wherein the suspension further comprises purified water.

5. The liquid suspension of claim 1, wherein the suspension further comprises: artificial cherry flavor, in an amount between about 2 mg/ml and about 10 mg/ml; and titanium dioxide, in an amount about 2 mg/ml and about 6 mg/ml.
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