Zaleplon gastroretentive drug delivery system
Inventors
Masri, Suher • Moor, Eytan • Kirmayer, David • Kluev, Elena • Carni, Giora • Navon, Nadav
Assignees
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Publication Number
US-9693981-B2
Publication Date
2017-07-04
Expiration Date
Abstract
A biodegradable, multi-layered controlled release gastroretentive dosage form which is optionally divided into a first dosage of zaleplon for controlled release and a second dosage of zaleplon for immediate release in the stomach and gastrointestinal tract of a patient, folded into a capsule which disintegrates upon contact with gastric juice and the gastroretentive dosage form unfolds rapidly upon contact with gastric juice. The biodegradable, multi-layered gastroretentive dosage forms of the invention provide efficient sleep induction with good sleep maintenance and minimal next day residual effects.
Core Innovation
The invention describes an oral dosage unit for administration of zaleplon that includes a capsule disintegrating upon contact with gastric medium and a coated immediate-release dose of zaleplon. After the capsule disintegrates, a biodegradable multi-layered gastroretentive dosage form, compacted or folded into the capsule, unfolds rapidly upon contact with the gastric medium.
The biodegradable multi-layered gastroretentive dosage form includes an inner layer comprising a dose of zaleplon for controlled release, where the zaleplon is substantially uniformly dispersed in a polymer or forms a solid solution with the polymer. The controlled-release zaleplon is released from the inner layer upon contact with gastric medium, while the dosage form further includes a rigid frame layer providing mechanical strength.
Two outer layers are provided, and at least one outer layer comprises orifices in one or more places adjacent to the inner layer containing zaleplon, with the outer layers permitting the passage of gastric medium from the environment. The oral dosage unit is constructed and dosed such that a pharmacologically effective blood plasma level of zaleplon is maintained from about one half hour following administration through about four to about twelve hours.
Claims Coverage
The independent claim is clm-00001. It contains inventive coverage centered on a disintegrating immediate-release capsule combined with a biodegradable, rapidly unfolding multi-layer gastroretentive dosage form that includes a uniformly dispersed/solid-solution controlled-release inner layer, a rigid frame for mechanical strength, and outer layers with orifices, configured to maintain a specified blood plasma exposure window.
Disintegrating capsule with immediate-release zaleplon coating and rapid unfolding gastroretentive dosage form
An oral dosage unit for administration of zaleplon comprising a capsule that disintegrates upon contact with gastric medium and is coated with a dose of zaleplon for immediate release, and a biodegradable multi-layered gastroretentive dosage form compacted or folded into said capsule that unfolds rapidly upon disintegration of the capsule upon contact with the gastric medium.
Controlled-release inner layer with substantially uniform dispersion or solid solution of zaleplon in a polymer
A biodegradable multi-layered gastroretentive dosage form comprising an inner layer including a dose of zaleplon for controlled release, wherein the zaleplon is substantially uniformly dispersed in a polymer or forming a solid solution therewith, and wherein the zaleplon is released from the inner layer upon contact of the gastroretentive dosage form with gastric medium.
Rigid frame layer for mechanical strength
A biodegradable multi-layered gastroretentive dosage form comprising a rigid frame layer providing said dosage form with mechanical strength.
Outer layers with orifices permitting passage of gastric medium adjacent the controlled-release inner layer
A biodegradable multi-layered gastroretentive dosage form comprising two outer layers, wherein at least one outer layer comprises orifices adjacent to said inner layer containing zaleplon, and wherein said outer layers permit the passage of gastric medium from the environment.
Dosing to maintain pharmacologically effective blood plasma level from about one half hour through about four to about twelve hours
The oral dosage unit is constructed and dosed such that, upon administration to a subject, a pharmacologically effective blood plasma level of zaleplon is maintained from about one half hour following administration through about four to about twelve hours.
Overall, the claim coverage combines an immediate-release disintegrating capsule with a biodegradable multi-layer gastroretentive system that unfolds rapidly in gastric medium, featuring an inner controlled-release layer with substantially uniform dispersion or a solid solution of zaleplon in a polymer, a rigid frame for mechanical strength, and outer layers with orifices that allow gastric-medium passage, all configured to maintain a pharmacologically effective blood plasma level over the specified post-administration time window.
Stated Advantages
Maintains a pharmacologically effective blood plasma level of zaleplon from about one half hour following administration through about four to about twelve hours.
Documented Applications
Not explicitly described in patent.
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