Stable and soluble formulations of receptor tyrosine kinase inhibitors, and methods of preparation thereof
AssigneeForSight Vision4, Inc.
InventorsJudit Horvath, Irina Astafieva, Signe Erickson, Kathleen Cogan Farinas
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Abstract
The present disclosure relates to stable formulations of receptor tyrosine kinase inhibitors (TKI), e.g., pazopanib; methods of preparation thereof; and use of the disclosed formulations in sustained delivery of the active agent to a target site. The disclosure further relates to methods of converting one polymorphic Form of a TKI to another polymorphic Form and/or an amorphous form.
Claims20
A method of treating an ophthalmic disease or disorder in a subject in need thereof, the method comprising administering to an eye of the subject an effective amount of a pharmaceutical solution comprising:
- (i) β-cyclodextrin sulfobutyl ether, hydroxypropyl β-cyclodextrin, or a combination thereof;
- (ii) about 0.2% to about 1.0% of polyvinylpyrrolidone;
- and
- (iii) about 30 mg/mL to about 60 mg/mL of an ophthalmic therapeutic agent or a pharmaceutically acceptable salt thereof having a solubility of less than 1 mg/mL in water.
A method of treating an ophthalmic disease or disorder in a subject in need thereof, the method comprising administering to an eye of the subject an effective amount of a pharmaceutical solution comprising:
- (i) hydroxypropyl-β-cyclodextrin, methyl-β-cyclodextrin, randomly methylated-β-cyclodextrin, ethylated-β-cyclodextrin, triacetyl-β-cyclodextrin, peracetylated-β-cyclodextrin, carboxymethyl-β-cyclodextrin, hydroxyethyl-β-cyclodextrin, 2-hydroxy-3-(trimethylammonio)propyl-β-cyclodextrin, glucosyl-β-cyclodextrin, maltosyl-β-cyclodextrin, sulfobutyl ether-β-cyclodextrin, branched-β-cyclodextrin, hydroxypropyl-γ-cyclodextrin, randomly methylated-γ-cyclodextrin, trimethyl-γ-cyclodextrin, or a combination of two or more thereof,
- (ii) about 0.1% to about 5.0% of trehalose, methylcellulose, ethylcellulose, sodium carboxymethylcellulose, sodium hyaluronate, sodium alginate, polyethylene glycol, glycerin, propylene glycol, triacetin, N,N-dimethylacetamide, polyvinylpyrrolidone, pyrrolidone, or a combination of two or more thereof;
- and
- (iii) about 30 mg/mL to about 70 mg/mL of an ophthalmic therapeutic agent or a pharmaceutically acceptable salt thereof having a solubility of less than 1 mg/mL in water.
A method of treating an ophthalmic disease or disorder in a subject in need thereof, the method comprising administering to an eye of the subject an effective amount of a pharmaceutical solution comprising:
- (i) a cyclodextrin, and (ii) about 30 mg/mL to about 90 mg/mL of an ophthalmic therapeutic agent or a pharmaceutically acceptable salt thereof having a solubility of less than 1 mg/mL in water.
Dependencies are inferred from the claim text.