Rifaximin Beta Polymorph Delayed Release Tablet
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Solution Overview
Problem
Current oral dosage forms of rifaximin require high doses and multiple administrations for treating Crohn's disease, leading to poor patient compliance due to high solubility in the stomach, which reduces efficacy, and are burdened by excessive enteric coating weights.
Innovation Solution
An oral dosage form containing rifaximin in polymorphic form β, without enteric release coating, designed for delayed release, ensuring less than 10% of the drug is released in the stomach and more than 50% is released in the intestinal tract, thereby maintaining low solubility in acidic conditions and reducing excipient amounts.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If rifaximin is provided with enteric coating to reduce solubility in stomach, then delayed release is improved, but tablet weight and excipient amount increase excessively
Solution Approach 1:
The patent extracts and removes the enteric coating layer from the tablet formulation, relying instead on the inherent delayed-release properties of rifaximin form β itself to achieve gastric resistance without adding excessive weight from coating materials
Solution Approach 2:
The patent changes the polymorphic form parameter of rifaximin from conventional forms to form β, which inherently exhibits low solubility in acidic gastric conditions, thereby achieving delayed release without requiring additional enteric coating excipients
2Reliability
If high dose of rifaximin is administered to treat Crohn's disease, then treatment efficacy is improved, but patient compliance deteriorates due to multiple administrations required
Solution Approach 1:
The patent enables sustained therapeutic action throughout the day with a single dose by ensuring the drug remains undissolved in the stomach and is released continuously in the intestine, maintaining effective concentrations without requiring multiple administrations
3Quantity of substance
If rifaximin shows high solubility in stomach, then absorption is improved, but efficacy at intestinal site of action deteriorates
Solution Approach 1:
The patent changes the solubility parameter of rifaximin in gastric conditions by utilizing form β, which maintains low solubility in acidic pH, preventing premature dissolution and absorption in the stomach while ensuring availability at the intestinal site of action
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The formulation allows for a once-daily administration of rifaximin with enhanced bioavailability and reduced excipient load, improving patient compliance and treatment efficacy for gastrointestinal inflammatory diseases like Crohn's disease.
Implementation Method 1
An oral dosage form for delayed release comprising (A) rifaximin in polymorphic form β
Implementation Method 2
the rifaximin exhibits a low solubility of the API, especially under acidic conditions such as in the stomach
Implementation Method 3
the oral dosage form provides delayed release of the active pharmaceutical agent
Implementation Method 4
more than 50% is released in the intestinal tract
Data Source
AI summary
The present invention relates to an oral dosage form containing rifaximin in form beta, wherein the oral dosage form provides delayed release of the active pharmaceutical agent. Further, the invention relates to the preparation of an oral dosage form, preferably a tablet.