Microemulsion containing indolocarbazole compound and dosage forms containing the same
AssigneeCephalon, Inc.
InventorsAnthony S. Drager, Bradley T. Mclntyre, Piyush R. Patel
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Abstract
The invention described herein provides a pharmaceutical composition and oral dosage forms containing the same, having high concentrations of solubilized indolocarbazole compounds as the active ingredient in microemulsion form. The invention also provides a process for increasing the solubilized concentration of indolocarbazole compounds such as lestaurtinib using the addition of water in combination with a hydrophilic component as part of the microemulsion formation process.
Claims22
A pharmaceutical composition comprising:
- an indolocarbazole compound present in a solubilized concentration ranging from about 3% up to about 9% by weight of the total composition;
- a hydrophilic polymer component;
- and water;
- wherein said composition is a microemulsion.
An oral capsular dosage form comprising a pharmaceutical fill composition encapsulated within a capsule material, said composition comprising:
- a) indolocarbazole compound present in an amount ranging from about 3% to about 9% per total composition weight;
- b) a hydrophilic polymer component present in an amount ranging from about 30% to about 95% per total composition weight;
- and
- c) water present in an amount ranging from about 0.8% to about 50% by weight of total composition weight;
- wherein said composition is a microemulsion formulated for encapsulation with a hard capsule material.
A pharmaceutical composition comprising a microemulsion having an indolocarbazole compound as an active ingredient present in a solubilized concentration ranging from about 3% up to about 9% of the total composition weight, said composition being prepared by:
- a) combining an indolocarbazole compound, hydrophilic polymer component, and surfactant;
- b) adding water to the combined ingredients from step a) in an amount sufficient to increase the solubilized concentration of said indolocarbazole compound to the desired concentration amount;
- wherein steps a) and b) are performed at a temperature sufficient to form a molten liquid of the combined ingredients, facilitate solubilization of said indolocarbazole compound and form a microemulsion.
A process for increasing the solubilized concentration of an indolocarbazole compound in a microemulsion for a given fill volume, said process comprising:
- a) combining an indolocarbazole compound, hydrophilic polymer component, and surfactant;
- b) adding water to the combined ingredients from step a) in an amount sufficient to increase the solubilized concentration of said indolocarbazole compound to the desired concentration amount;
- wherein steps a) and b) are performed at a temperature sufficient to form a molten liquid of the combined ingredients, facilitate solubilization of said indolocarbazole compound and form a microemulsion;
- wherein said indolocarbazole is present in an amount of up to about 9% total composition weight.
A method of inhibiting receptor-tyrosine kinase in a recipient comprising orally administering to a recipient in need of such treatment an oral dosage form having a pharmaceutical composition comprising:
- a) lestaurtinib present in a solubilized concentration of from about 3% to about 9% by weight of the total composition;
- b) a hydrophilic polymer component comprising polyethylene glycol;
- c) a surfactant;
- and
- d) water;
- wherein said composition is a microemulsion.
An oral tablet dosage form comprising a pharmaceutical composition, said composition comprising:
- a) indolocarbazole compound present in an amount ranging from about 3% to about 9% per total composition weight;
- b) a hydrophilic polymer component;
- c) water;
- and
- d) additional pharmaceutically acceptable excipients;
- wherein said composition is a microemulsion formulated for compression into a tablet dosage form.
Dependencies are inferred from the claim text.