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Development and evaluation of enteric-coated penicillamine tablets
Journal of Pharmaceutical Sciences
|September 1, 1984
Summary
Enteric-coated penicillamine tablets significantly reduced gastrointestinal bleeding in pigs compared to uncoated tablets. This novel formulation may decrease GI irritation caused by penicillamine, offering a safer drug delivery option.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Gastroenterology
Background:
- Penicillamine is used to treat various conditions but can cause gastrointestinal (GI) irritation.
- Developing an enteric-coated formulation aims to mitigate GI side effects.
Purpose of the Study:
- To develop and evaluate an enteric-coated penicillamine tablet.
- To assess the safety and efficacy of the enteric-coated formulation in a preclinical model.
Main Methods:
- Commercially available penicillamine tablets were enteric-coated using cellulose acetate phthalate.
- In vitro dissolution and disintegration tests were performed.
- In vivo studies were conducted in weanling pigs comparing enteric-coated and uncoated tablets, monitoring for GI bleeding and plasma concentrations.
Main Results:
- Enteric-coated tablets resisted disintegration in simulated gastric fluid and disintegrated in simulated intestinal fluid.
- Significantly less GI tract bleeding was observed in pigs receiving enteric-coated penicillamine compared to uncoated tablets.
- Plasma concentration-time curves in pigs showed similarities to human data, with a relative bioavailability of 67% for the enteric-coated form.
Conclusions:
- Enteric-coated penicillamine tablets effectively reduce GI irritation and bleeding in a preclinical model.
- The enteric coating appears to be a viable strategy for improving the gastrointestinal safety of penicillamine.
- Further studies are warranted to confirm these findings and explore clinical applications.