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[Bioavailability of phloroglucinol in man]
G Dollo1, F Chevanne, P Le Corre
1Laboratoire de Pharmacie Galénique et Biopharmacie, Université de Rennes I, Faculté des Sciences Pharmaceutiques et Biologiques, France. Dollo@univ.rennes1.fr
Journal De Pharmacie De Belgique
|August 4, 1999
Summary
This study compared two oral phloroglucinol dosage forms in healthy volunteers. Both forms demonstrated bioequivalence, indicating similar absorption and pharmacokinetic profiles after sublingual administration.
Area of Science:
- Pharmacokinetics and Drug Metabolism
- Pharmaceutical Sciences
- Clinical Pharmacology
Background:
- Phloroglucinol is an active compound used in various oral dosage forms.
- Understanding its pharmacokinetic behavior and bioavailability is crucial for therapeutic efficacy.
- Comparative studies of different oral formulations are essential for pharmaceutical development.
Purpose of the Study:
- To evaluate and compare the bioavailability of two oral phloroglucinol dosage forms.
- To elucidate the pharmacokinetic profile of phloroglucinol following sublingual administration.
- To establish bioequivalence between a flash liberation tablet and a freeze-dried reference tablet (lyoc).
Main Methods:
- A randomized, cross-over study involving twelve healthy volunteers.
- Sublingual administration of two oral dosage forms containing 125.2 mg of active phloroglucinol.
- Development and application of a high-performance liquid chromatographic (HPLC) method for quantifying free and conjugated phloroglucinol.
- Analysis of pharmacokinetic parameters including T1/2 alpha, T1/2 beta, AUC, Tmax, Cmax, and MRT.
- Statistical analysis using ANOVA, Westlake, and two one-sided t-tests for bioequivalence assessment.
Main Results:
- The HPLC method accurately quantified phloroglucinol and its metabolites.
- Phloroglucinol exhibits significant metabolism, poor systemic bioavailability after oral administration, and primarily urinary elimination in metabolized form.
- Pharmacokinetic profiles and key parameters (T1/2 alpha, T1/2 beta, AUC, Tmax, Cmax, MRT) were determined for both dosage forms.
- Comparative analysis revealed equivalent performance between the flash liberation tablet and the freeze-dried reference tablet.
Conclusions:
- The two studied oral dosage forms of phloroglucinol are bioequivalent.
- The findings support the use of both formulations interchangeably based on demonstrated equivalent performance.
- The study clarifies phloroglucinol's pharmacokinetic behavior, highlighting its metabolism and bioavailability characteristics in humans.