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Publication Number
US-11291629-B2
Publication Date
2022-04-05
Expiration Date
Abstract
An object of the invention is to provide a mucoadhesive oral preparation having high drug absorption rate and rapid drug release rate. The means for solving the problem is a mucoadhesive oral preparation having (a) a basal layer substantially consisting of a water-insoluble material, (b) a drug layer locating above the basal layer and containing a drug but not containing mucoadhesive material, and (c) an adhesive portion locating on a portion of the surface of the drug layer side of the oral formulation and containing mucoadhesive material.
Core Innovation
The invention provides a mucoadhesive oral drug delivery preparation in a capsule shape with a larger length than width. The preparation has a three-portion structure including a basal layer substantially consisting of water-insoluble material, a drug layer locating above the basal layer containing a drug but not containing mucoadhesive material, and an adhesive portion locating on an outer periphery at the surface of the drug-layer side and containing mucoadhesive material.
The area of the adhesive portion is larger than the area of the drug layer. The three-portion spatial arrangement localizes the mucoadhesive adhesive portion on a portion of the outer periphery of the drug-layer-side surface rather than throughout the drug layer or surface.
The document further discloses variants of the mucoadhesive oral preparation, including tablet, film, and capsule-shaped forms, and discusses GI site targeting strategies such as enteric coating and multi-unit approaches.
Claims Coverage
The coverage is centered on one independent claim defining the three-portion mucoadhesive oral preparation geometry, including layer composition constraints, positioning on the drug-layer side surface, and an area relationship between the adhesive portion and the drug layer. Dependent claims further refine the basal-layer and mucoadhesive-material selections and specify tablet and film agent variants within the capsule-shaped form.
Three-portion mucoadhesive capsule with localized peripheral adhesive
A mucoadhesive oral preparation in a capsule shape having a larger length than width, comprising a basal layer substantially consisting of water-insoluble material, a drug layer locating above the basal layer containing a drug but not containing mucoadhesive material, and an adhesive portion locating on an outer periphery at the surface of the drug layer side and containing mucoadhesive material, wherein an area of the adhesive portion is larger than an area of the drug layer.
Enumerated basal water-insoluble material selection
The water-insoluble material of the basal layer is selected from specific polymers, cellulose derivatives, lipid/wax-like excipients, and related water-insoluble compounds as enumerated in the dependent claim.
Enumerated mucoadhesive material selection for the adhesive portion
The mucoadhesive material of the adhesive portion is selected from carboxyvinyl polymer, polyacrylic acid and its salts, alginic acid and its salts, or propylene glycol alginate ester as enumerated in the dependent claim.
Tablet-in-capsule-shaped oral preparation drug class
An oral preparation in which the capsule-shaped tablet form contains at least one drug selected from insulin and insulin derivatives, GLP-1 receptor agonists, sleep inducers, steroids, or anti-inflammatory drugs.
Film-agent-in-capsule-shaped oral preparation drug class
An oral preparation in which the film agent in a capsule-shaped form contains a drug selected from insulin and insulin derivatives, GLP-1 passive agonists, sleep inducers, steroids, and anti-inflammatory drugs.
Overall, the claim set focuses on a localized-peripheral adhesive configuration in a capsule-shaped three-portion structure, requiring a water-insoluble basal layer, a central drug layer lacking mucoadhesive material, and an outer-periphery adhesive portion containing mucoadhesive material with adhesive-area larger than drug-layer area. Dependent claims further restrict basal and mucoadhesive material types and specify capsule-form variants together with enumerated drug-class examples.
Stated Advantages
Improves drug absorption.
Enables rapid drug release.
Avoids trapping of drug within a swellable mucoadhesive gel.
Produces faster in vitro permeation when the mucoadhesive portion is localized on the outer periphery versus formulated throughout the drug layer or surface.
Documented Applications
GI tract absorption of drugs using a mucoadhesive oral preparation with a localized outer-periphery adhesive portion to support rapid drug release.
In vitro permeation evaluation using Franz cell comparisons between a localized peripheral mucoadhesive portion and a dispersed mucoadhesive formulation across the drug layer or surface.
GI site targeting strategies discussed using enteric coating and multi-unit approaches in connection with the oral preparation.
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