Tablet for pulsed delivery
Inventors
Cao, Bruce • Wassink, Sandra E. • Treacy, Jr., Donald J. • Burnside, Beth A. • Rowlings, Colin E. • Bonck, John A.
Assignees
Publication Number
US-8715727-B2
Publication Date
2014-05-06
Expiration Date
2025-07-01
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Abstract
A pharmaceutical tablet comprising an immediate release portion containing an active ingredient and a delayed release portion, wherein the delayed release portion comprises an enteric-coated layer and within the enteric-coated layer there is at least one member selected from the group consisting of enteric-coated microparticle dosage forms containing an active ingredient and enteric-coated mini-tablet dosage forms containing an active ingredient, is disclosed.
Core Innovation
The invention discloses a pharmaceutical tablet that provides both immediate and enteric (delayed) release of an active drug agent. The tablet comprises two main portions: an immediate release portion that contains an active ingredient released without substantial delay after ingestion, and a delayed release portion containing an active ingredient whose release is substantially delayed until the tablet reaches the intestine. The delayed release portion contains an enteric-coated layer within which there can be at least one member selected from enteric-coated microparticle dosage forms and enteric-coated mini-tablet dosage forms, each containing an active ingredient.
The core tablet within the enteric-coated layer can contain particles or mini-tablets coated with an enteric layer, ensuring these do not disintegrate until they reach the intestine. Optionally, the core tablet may also include an uncoated dose of active ingredient for release upon disintegration in the intestine. The immediate release portion may be applied as a layer over the enteric-coated core, which can partially or completely engulf the core, ensuring that an initial dose is released in the stomach while subsequent sequential pulses are released in the intestine as designed.
The main problem addressed by the invention is the inability of current multi-particulate and mini-tab delivery systems to prevent pre-intestinal separation and premature release of active components in the stomach, leading to variability in pharmacokinetics and reduced efficacy. Existing systems often release all their contents rapidly upon enteric coating dissolution or provide steady rather than pulsatile blood levels. By bundling enteric-coated mini-tabs or microparticles within an enteric-coated core, this invention achieves staged, pulsatile drug delivery in the GI tract, overcoming the issues of pellet spread, dumping, and variability in absorption.
Claims Coverage
The patent contains multiple independent claims describing inventive features related to a pharmaceutical tablet for pulsed delivery of amoxicillin and related methods and processes.
Once-a-day immediate and delayed release tablet containing amoxicillin
A pharmaceutical tablet formulated for once-daily administration, comprising: - An immediate release portion containing amoxicillin - A delayed release portion that includes an enteric-coated layer - Within the enteric-coated layer, an uncoated dosage of amoxicillin and at least one member chosen from enteric-coated microparticle dosage forms or enteric-coated mini-tablet dosage forms containing amoxicillin - The tablet does not contain clavulanate
Method for preparing a once-a-day pharmaceutical tablet with immediate and delayed release of amoxicillin
A method for preparing a once-a-day pharmaceutical tablet without clavulanate that includes the steps of: 1. Formulating a delayed release portion with a core tablet and an enteric coating, where the core includes an uncoated dosage of amoxicillin and at least one member selected from enteric-coated microparticle dosage forms or enteric-coated mini-tablet dosage forms containing amoxicillin, and the enteric coating covers the core tablet. 2. Applying an immediate release portion containing amoxicillin as a layer over the delayed release portion so that the immediate release layer at least partially covers the delayed release portion.
Process for treating a bacterial infection with the once-a-day amoxicillin tablet
A process for treating a bacterial infection in a host comprising administering the once-a-day pharmaceutical tablet containing an immediate and delayed release of amoxicillin (without clavulanate), once daily.
The inventive features focus on a unique once-a-day tablet combining immediate and delayed release of amoxicillin without clavulanate, a method for its preparation, and its application in treating bacterial infections.
Stated Advantages
Decreases variability in the absorption of active drug agents, particularly antibiotics.
Prevents pre-intestinal separation and dumping of microparticles or mini-tabs, ensuring all delayed release portions enter the small intestine as a single unit.
Enables pulsatile dosing, providing sequential bursts of active ingredient to achieve distinct pharmacokinetic profiles.
Allows high dose loading and delivery of multiple pulses within a smaller tablet size compared to traditional multi-particulate tablets.
Permits delivery of multiple drugs, including incompatible drugs, from a single tablet core.
Enables targeting of different regions of the GI tract for delivery.
Supports once-a-day dosing, increasing convenience and compliance and reducing risk of overdose.
Documented Applications
Treatment of bacterial infections with once-a-day oral administration of amoxicillin in immediate and delayed release forms.
Decreasing variability of absorption of antibiotics, specifically beta-lactam antibiotics, cephalosporin antibiotics, and macrolide antibiotics.
Formulations for both amoxicillin and clarithromycin, either separately or in combination.
Decreasing absorption variability for active drug agents in general, including anti-infective agents such as antifungals and antivirals, and antineoplastic agents.
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