Rifaximin Multilayer Tablet Bioadhesion
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Solution Overview
Problem
Conventional rifaximin dosage forms have a short residence time in the gastrointestinal tract due to stomach emptying and intestinal peristalsis, requiring frequent administration to maintain therapeutic effectiveness, especially during pathological conditions like diarrhea.
Innovation Solution
A pharmaceutical composition with a multilayer tablet design, incorporating a release controlling polymer and a bioadhesive polymer, which extends the residence time of rifaximin in the gastrointestinal tract through controlled release and bioadhesion, allowing for once-daily administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If conventional dosage forms are used, then the drug can be administered orally, but the residence time in the gastrointestinal tract is short due to stomach emptying and intestinal peristalsis
Solution Approach 1:
The patent applies preliminary action by incorporating mucoadhesive polymers into the dosage form before administration. These polymers are pre-positioned to interact with the gastrointestinal mucosa upon contact, ensuring immediate adhesion when the dosage form reaches the target site. This preliminary preparation of the dosage form structure allows it to automatically adhere to mucosal surfaces, extending residence time without requiring post-administration intervention or frequent redosing.
Solution Approach 2:
The patent employs composite materials by formulating the dosage form with a combination of mucoadhesive polymers (such as carbomers, cellulose derivatives, chitosan) and the antibiotic rifaximin. This composite structure integrates the drug with polymers that have specific bioadhesive properties, creating a material that both delivers the therapeutic agent and simultaneously anchors itself to the gastrointestinal mucosa, thereby resolving the contradiction between maintaining therapeutic presence and avoiding frequent administration.
2Speed
If the drug is released quickly, then therapeutic effect is achieved rapidly, but the residence time at the site of action is insufficient
Solution Approach 1:
The patent applies dynamics by creating a dosage form with time-dependent release characteristics. The mucoadhesive matrix structure allows the drug to be released at a controlled rate over time as the polymer gradually hydrates, swells, and erodes in the gastrointestinal environment. This dynamic release profile ensures that rifaximin is progressively released while the dosage form maintains its adhered state, coordinating the speed of drug release with the duration of mucosal residence.
Solution Approach 2:
The patent implements continuity of useful action through the sustained mucoadhesive interaction between the polymer matrix and gastrointestinal mucosa. As the dosage form remains adhered to the mucosal surface, it continuously releases rifaximin over an extended period. This continuous release mechanism ensures that therapeutic concentrations are maintained at the site of action throughout the residence time, eliminating the need for rapid re-dosing while preserving therapeutic efficacy.
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 composition achieves a prolonged release profile, with 20-50% of rifaximin released in 8 hours, 30-70% in 12 hours, and over 70% in 24 hours, and maintains adhesive strength, effectively eradicating pathogens and extending the time for last unformed stools in patients, improving patient compliance and treatment efficacy.
Implementation Method 1
a bioadhesive polymer, which extends the residence time of rifaximin in the gastrointestinal tract through controlled release and bioadhesion
Data Source
Figure 1
AI summary
A pharmaceutical composition comprising therapeutically effective amount of rifaximin or pharmaceutically acceptable salt or enantiomer or polymorph thereof, pharmaceutically acceptable excipient(s) and release controlling agent(s). Pharmaceutical composition of rifaximin comprising: at least two entities wherein one entity is an immediate release or fast release and the other is controlled release. The pharmaceutical composition in the form of multilayer tablet comprising, at least one layer comprising, therapeutically effective amount of rifaximin or pharmaceutically acceptable salt or enantiomer or polymorph thereof, pharmaceutically acceptable excipient(s); said layer providing controlled release rifaximin; and at least one layer which provides increased residence time of the dosage form in the gastrointestinal tract. The pharmaceutical formulation comprising rifaximin having an in vitro dissolution profile, wherein about 70% of rifaximin is released in about 24 hours. The composition comprising therapeutically effective amount of rifaximin or pharmaceutically acceptable salt(s) or enantiomer(s) or polymorph(s) thereof, one or more release controlling agent(s) and pharmaceutically acceptable excipient(s) causing pathogenic eradication.