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Bilayer tablets based on poly (epsilon-caprolactone) and polymethylmethacrilates as controlled-release systems for
Vanna Sanna1, Elisabetta Gavini, Paolo Giunchedi
1Dipartimento di Scienze del Farmaco, University of Sassari, Sassari, Italy.
Pharmaceutical Development and Technology
|October 2, 2004
Summary
New bilayer tablets protect folic acid from rumen degradation in ruminants. These rumen-stable delivery systems ensure controlled release in the intestine, improving nutrient bioavailability.
Area of Science:
- Veterinary Pharmacology
- Drug Delivery Systems
- Ruminant Nutrition
Background:
- Rumen degradation limits the efficacy of orally administered active ingredients in ruminants.
- Rumen-stable delivery systems are needed to protect active ingredients and ensure postruminal bioavailability.
- Controlled release mechanisms are crucial for targeted delivery in the gastrointestinal tract.
Purpose of the Study:
- To prepare and evaluate bilayer tablets as rumen-stable delivery systems for folic acid in ruminants.
- To ensure protection against ruminal degradation and achieve controlled release in the intestinal tract.
- To assess the retention of these tablets in the ruminant reticulum-rumen.
Main Methods:
- Preparation of bilayer tablets with a high-density layer (poly(epsilon-caprolactone) and iron powder) and a release layer (poly(epsilon-caprolactone) or Eudragit RS/RL with folic acid).
- In vitro testing of rumen-protection stability in buffer systems (pH 5.5 and 2.0).
- In vitro release studies at pH 7.4 to simulate intestinal conditions.
- Preliminary in vivo radiographic evaluation in sheep to assess reticulum-rumen retention.
Main Results:
- Bilayer tablets achieved a density of approximately 2.3 g/cm³, sufficient to prevent rumination.
- Tablets with poly(epsilon-caprolactone) or Eudragit RS release layers demonstrated stability in simulated ruminal and abomasal environments (pH 5.5 and 2.0).
- Sustained release of folic acid was observed at pH 7.4, and radiographic studies confirmed tablet retention in the reticulum-rumen.
Conclusions:
- Bilayer tablets are effective rumen-stable delivery systems for folic acid in ruminants.
- The designed tablets protect active ingredients from degradation and ensure controlled intestinal release.
- These systems hold promise for improving nutrient delivery and therapeutic outcomes in ruminant medicine.