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The bioavailability of flufenamic acid and its dissolution rate from capsules
International Journal of Clinical Pharmacology, Therapy, and Toxicology
|February 1, 1983
Summary
Bioavailability of flufenamic acid (FA) capsules varied significantly between products in humans and dogs. Dissolution tests using acidic pretreatment better predicted human bioavailability than standard methods.
Area of Science:
- Pharmacokinetics
- Drug formulation and delivery
- Biopharmaceutics
Background:
- Flufenamic acid (FA) is a non-steroidal anti-inflammatory drug (NSAID) with variable oral bioavailability.
- Assessing the in vivo performance of generic drug products is crucial for therapeutic equivalence.
Purpose of the Study:
- To compare the bioavailability of five commercial flufenamic acid capsules in humans and beagle dogs.
- To evaluate various in vitro dissolution methods for predicting in vivo drug performance.
- To assess the utility of beagle dogs as animal models for predicting human drug bioavailability.
Main Methods:
- Human and beagle dog studies were conducted to determine flufenamic acid bioavailability.
- In vitro dissolution testing of FA capsules was performed using multiple methods, including acidic pretreatment, rotating basket, and paddle methods.
- In vitro-in vivo correlations (IVIVC) were established to evaluate dissolution test predictivity.
Main Results:
- Significant inter-capsule variability in flufenamic acid bioavailability was observed in both species.
- Human and dog bioavailability results showed discrepancies.
- Dissolution methods involving acidic pretreatment demonstrated significant correlation with in vivo bioavailability in both humans and dogs.
- Standard dissolution methods (rotating basket, paddle) without surfactants did not correlate with in vivo data.
Conclusions:
- The bioavailability of flufenamic acid capsules differs significantly among commercial products.
- Dissolution testing with acidic pretreatment is a more reliable predictor of human flufenamic acid bioavailability compared to standard methods.
- Beagle dogs may not be ideal models for predicting the bioavailability of weak acid drugs like flufenamic acid in humans due to species-specific differences.