Rapidly disintegrating solid oral dosage forms containing dasatinib
Inventors
Andersson, Per • Meijer, Thomas • Söderberg, Victor
Assignees
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Publication Number
US-10894018-B1
Publication Date
2021-01-19
Expiration Date
Abstract
The instant application relates to the field of pharmaceutical compositions comprising dasatinb. Furthermore, the instant application relates to a method of treating proliferative disorders in a patient in need thereof, comprising administering a therapeutically effective amount of said compositions.
Core Innovation
The invention relates to rapid-disintegrating solid oral dosage forms for oral administration that include dasatinib in the form of dasatinib (S)-1,2-propanediol solvate. The tablet includes at least one pharmaceutically acceptable excipient and a coating layer, and is configured to release dasatinib with rapid dissolution performance under defined test conditions.
The disclosed tablet is designed to meet fast dissolution requirements while supporting pharmacokinetic and bioequivalence acceptance criteria relative to a reference listed drug that comprises dasatinib monohydrate (Sprycel). The document ties formulation performance to dissolution behavior and to bioequivalence decision criteria.
The approach includes selecting a specific dasatinib solvate form and incorporating a coating layer together with pharmaceutically acceptable excipients in a tablet dosage form. Dissolution performance is defined by releasing at least 80% of dasatinib within 20 minutes when tested in a USP Type 2 apparatus under specified hydrochloric acid conditions with controlled temperature and agitation.
Claims Coverage
The provided content identifies one independent claim. The inventive features include the specific dasatinib (S)-1,2-propanediol solvate tablet composition, defined rapid dissolution performance by USP Type 2 testing, and an amount of dasatinib equivalent to 140 mg.
Dasatinib (S)-1,2-propanediol solvate tablet composition
A tablet for oral administration comprising dasatinib (S)-1,2-propanediol solvate, at least one pharmaceutically acceptable excipient, and a coating layer.
Rapid dissolution release by USP Type 2 in 0.01 M hydrochloric acid
The tablet releases at least 80% of the dasatinib within 20 minutes when tested in a USP Type 2 apparatus in 500 mL of 0.01 M hydrochloric acid at about 37° C. and about 75 RPM.
Dasatinib amount equivalent to 140 mg
The amount of dasatinib is equivalent to 140 mg dasatinib.
Across the provided independent claim, the core claim coverage is directed to a tablet that combines dasatinib (S)-1,2-propanediol solvate with an excipient system and a coating layer, and that satisfies a defined rapid dissolution threshold under USP Type 2 testing conditions, while using a dasatinib dose amount equivalent to 140 mg.
Stated Advantages
Provides rapid dissolution performance, with at least 80% dasatinib released within 20 minutes under the specified USP Type 2 conditions.
Supports bioequivalence characteristics versus a reference listed drug comprising dasatinib monohydrate, using 90% confidence interval ratio criteria for AUC and Cmax.
Includes reference-scaled average bioequivalence (RSABE) for highly variable drugs as part of the bioequivalence acceptance approach.
Documented Applications
Treatment using a therapeutically effective amount of a composition according to claim 1 for Philadelphia chromosome-positive (Ph+) leukemia populations, including newly diagnosed adult chronic phase CML and adults with resistance or intolerance to prior therapy including imatinib, or Ph+ ALL with resistance or intolerance to prior therapy.
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