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Etretinate: effect of milk intake on absorption.
The Journal of Investigative Dermatology
|June 1, 1984
Summary
Administering etretinate with a fat load, such as milk, significantly increases its absorption and serum concentration compared to taking it with water. This fat-enhanced absorption impacts etretinate and its metabolite levels for psoriasis and skin disorder treatments.
Area of Science:
- Pharmacology
- Dermatology
- Drug Metabolism
Background:
- Etretinate, an aromatic retinoid, is used for skin disorders like psoriasis.
- Its lipid-soluble nature suggests absorption may depend on dietary fat intake.
Purpose of the Study:
- To investigate the effect of a fat load on etretinate and its metabolite serum concentrations.
- To compare etretinate absorption with and without a fat load.
Main Methods:
- Ten patients (6 with Darier's disease, 4 with psoriasis) received etretinate (1 mg/kg) with water or milk after fasting.
- Serum concentrations of etretinate and its metabolite Ro 10-1670 were measured.
Main Results:
- Milk administration increased peak serum etretinate concentrations by 260% compared to water.
- Overall 24-h etretinate levels increased by 296% with milk.
- Conversely, Ro 10-1670 peak concentrations decreased by 17% with milk.
- Etretinate became the dominant serum retinoid with milk, unlike with water where Ro 10-1670 predominated.
Conclusions:
- A fat load significantly enhances etretinate absorption and serum levels.
- This alters the etretinate/Ro 10-1670 ratio in serum.
- Further clinical trials are needed to determine the clinical significance of these findings.