Rapidly disintegrating solid oral dosage forms containing dasatinib
Inventors
Andersson, Per • Meijer, Thomas • Söderberg, Victor
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-11344500-B2
Publication Date
2022-05-31
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 provides orally administered dasatinib rapid-dissolving solid dosage forms in the form of tablets. The dosage forms include dasatinib 1,2-propanediol solvate, including dasatinib (R)-1,2 propanediol solvate, dasatinib (S)-1,2 propanediol solvate, or combinations thereof, together with at least one pharmaceutically acceptable excipient and a coating layer.
A primary aspect of the invention is a dissolution performance requirement designed to support rapid release. The tablet is described as releasing at least about 70% of the dasatinib within 20 minutes when tested in a USP Type 2 dissolution test in 500 mL of 0.01 M hydrochloric acid at about 37±3°C and about 75 RPM.
The invention also positions the dosage form for regulatory and scientific comparability to Sprycel (dasatinib monohydrate) through bioequivalence considerations. The disclosure includes a fed versus fasted pharmacokinetic comparison and describes dissolution testing concepts together with excipient and coating layer concepts to address dependence on gastric transit time and fed/fasted state effects.
Claims Coverage
The independent claim is directed to a tablet formulation with three inventive features focused on the specific dasatinib solvate form, the inclusion of pharmaceutically acceptable excipients and a coating layer, and a defined dissolution-release criterion under a specified USP Type 2 test condition.
Dasatinib 1,2-propanediol solvate in an oral tablet
The tablet comprises dasatinib 1,2-propanediol solvate, dasatinib (R)-1,2 propanediol solvate, dasatinib (S)-1,2 propanediol solvate, or a combination thereof.
Pharmaceutically acceptable excipient and coating layer
The tablet includes at least one pharmaceutically acceptable excipient and a coating layer.
Rapid release in USP Type 2 in 0.01 M HCl
The tablet releases at least about 70% of the dasatinib within 20 minutes when tested in a USP Type 2 in 500 mL of 0.01 M hydrochloric acid at about 37±3°C and about 75 RPM.
Overall, the independent claim is covered by formulation and performance limitations that tie the specific dasatinib 1,2-propanediol solvate selection to an excipient/coating tablet structure and a defined rapid-release dissolution requirement under a USP Type 2 test condition.
Stated Advantages
Improved dissolution/rapid release, including releasing at least about 70% of dasatinib within 20 minutes under the stated USP Type 2 conditions.
Bioequivalence positioning versus Sprycel (dasatinib monohydrate) using fed versus fasted pharmacokinetic comparisons.
Less affected by fed/fasted state and independent of gastric transit time.
Documented Applications
Oral administration of dasatinib rapid-dissolving solid dosage forms as tablets for achieving defined dissolution and bioequivalence characteristics relative to Sprycel (dasatinib monohydrate).
Interested in licensing this patent?