Physio Release® technology to improve oral absorption and bioavailability of active ingredients
The oral absorption of active ingredients (AIs) depends on several physiological and technological factors that determine how much of a compound reaches systemic circulation.
Dissolution rate, gastrointestinal permeability, release profile, gastric emptying time, and intestinal metabolism all affect bioavailability and therapeutic performance.
During gastrointestinal transit — from the esophagus to the colon — actives may undergo chemical and enzymatic transformations. Controlling these factors is essential to design optimized oral formulations capable of achieving steady, efficient absorption.
Physiology of Oral Absorption
- Esophagus: peristaltic movements deliver the compound to the stomach, where residence time ranges from 5 minutes to 2 hours, depending on particle size.
- Stomach: dissolution begins but is influenced by particle size and food intake.
- Small intestine: the primary site for nutrient and drug absorption, with a transit time of 3–4 hours, crucial for extended-release formulations.
- Colon: transit time varies between 12 and 36 hours; absorption is limited, so avoiding premature release here is key.
Case Study: Alpha-Lipoic Acid (ALA)
Alpha-lipoic acid (ALA) is a potent antioxidant with proven clinical applications, yet its oral bioavailability is only about 30% due to extensive first-pass metabolism and chemical instability.
Although ALA is absorbed rapidly, food intake reduces its absorption efficiency. Once absorbed, it crosses the blood-brain barrier, acting as a direct and indirect antioxidant and a metal-chelating agent, while also inducing heme-oxygenase-1 (HO-1) expression with potential anti-inflammatory effects.
Improving ALA bioavailability requires:
- Controlled release along the small intestine;
- Chemical stabilization to prevent polymerization;
- Sustained plasma levels for optimal pharmacodynamic activity.
What Physio Release® Technology Is and How It Works
The Physio Release® Technology represents a major advancement in controlled-release systems for oral delivery of active ingredients.
Unlike conventional modified-release tablets, Physio Release® combines the active ingredient with specific inert excipients in a compressed matrix designed to regulate release rate, timing, and site within the gastrointestinal tract.
1. Release Rate
The system allows the slowing down of the release profile to extend therapeutic coverage and reduce dosing frequency.
2. Release Timing
Physio Release® can delay activation, initiating drug release only after a defined period post-ingestion.
3. Release Site
The active ingredient can be target-released in the small intestine, maximizing absorption while avoiding gastric degradation.
Mechanism of Action
When taken on an empty stomach, the Physio Release® tablet reaches the small intestine in approximately 30 minutes, where dissolution begins.
The process continues for about 4 hours, ensuring:
- Complete and gradual release of the active;
- Optimal absorption in highly permeable intestinal segments;
- Prevention of degradation by avoiding release in the colon.
This results in steady plasma concentrations, enhanced bioavailability, and improved therapeutic predictability.
Advantages of Physio Release® Technology
- Consistent and prolonged absorption over time.
- Precise control of release rate, timing, and location.
- Reduced dosing frequency and improved patient compliance.
- Enhanced bioavailability and chemical stability of the active.
- Minimized gastric degradation for predictable therapeutic effects.
Conclusion
Physio Release® Technology is an innovative controlled-release oral system that optimizes absorption, stability, and bioavailability of active ingredients.
It enables precise modulation of release rate and site, ensuring that the compound is absorbed only where it is most effective.
PJ Pharma, the ready-to-market line of Gruppo FarmaImpresa, develops Physio Release® oral formulations available both ready to commercialize and in private label, with full regulatory and technical support for national and international markets.
