Posaconazole intravenous solution formulations stabilized by substituted beta-cyclodextrin
AssigneeMerck Sharp & Dohme Corp.
InventorsSusan K. Heimbecher, David Monteith
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Abstract
The present invention relates to aqueous solutions useful as pharmaceutical compositions of posaconazole for intravenous administration. These compositions include a solubilizing agent, such as a modified β-cyclodextrin in an acidified solution, which can also include a chelating agent such as disodium edetate (EDTA). In clinical trials, a 200 mg posaconazole dose of the selected composition was found to achieve acceptable pharmacokinetic properties.
Claims21
A pharmaceutical composition for intravenous administration comprising:
- posaconazole, or a pharmaceutically acceptable salt thereof;
- and,
- a modified β-cyclodextrin,
- in aqueous solution, wherein the pH of said composition is between about 2.0 and about 3.5.
A pharmaceutical composition for intravenous administration comprising components and the quantities of each as follows:
- Components
- Quantity
- Posaconazole
- about 5 to about 25 mg/mL
- Captisol ® (sulfobutylether-β-
- about 25 mM to about
- cyclodextrin)
- 200 mM
- Disodium Edetate (EDTA)
- about 0.1 to about 1.0 mg/mL
- 1N Hydrochloric Acid
- sufficient quantity to
- adjust to pH of about
- 2.0 to about 3.0
- 1N Sodium Hydroxide
- sufficient quantity to
- adjust to pH of about
- 2.0 to about 3.0
- Water
- q.s. ad 1 mL
Dependencies are inferred from the claim text.