Comparative pharmacokinetic profiles of a novel isotretinoin formulation (isotretinoin-Lidose) and the innovator isotretinoin formulation: A randomized, 4-treatment, crossover study - 23/10/13
Abstract |
Background |
A high-fat meal is needed for optimal absorption of isotretinoin. A new formulation of isotretinoin, which enhances absorption of isotretinoin in the absence of dietary fat, has recently been approved by the Food and Drug Administration (FDA).
Objective |
We sought to compare the pharmacokinetic profiles of a new formulation of isotretinoin (isotretinoin-Lidose) with the innovator isotretinoin formulation.
Methods |
This study was an open-label, single-dose, randomized, 4-treatment, crossover comparative trial between a new and innovator formulation of isotretinoin in the fasting and fed states.
Results |
Both formulations were bioequivalent under fed conditions. As expected in a fasting state, absorption of both formulations was reduced. A considerable difference between the 2 drugs occurred under fasted conditions–there was a marked improvement in overall bioavailability of the isotretinoin-Lidose formulation. Mean plasma levels of the isotretinoin-Lidose formulation during fasting reached 66.8% of that observed with a fatty meal, and those of the isotretinoin formulation only reached 39.6% of that observed with a fatty meal.
Limitations |
Only the FDA-stipulated standard high-fat, high-calorie meal of 50-g fat was studied in the fed state.
Conclusion |
Isotretinoin-Lidose formulation is bioequivalent to the innovator formulation under fed conditions with regard to its pharmacokinetic profile but delivers twice as much isotretinoin and 4-oxo-isotretinoin when administered after an overnight fast.
Le texte complet de cet article est disponible en PDF.Key words : acne, area under the curve, bioavailability, fasting, fed, isotretinoin, maximum measured plasma concentration over sampling time period, systemic exposure, time of maximum measured plasma concentration
Abbreviations used : AUCt, AUCi, BA, BE, Cmax, FDA, Tmax
Plan
Funding sources: None. |
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Disclosure: Dr Leyden is a consultant to Cipher Pharmaceuticals Inc and Ranbaxy Pharmaceutical Inc. Dr Webster is a consultant to Ranbaxy, Cipher Pharmaceuticals Inc, Galderma, Valeant, Dermira, and Cutanea. Dr Gross is an employee of Cipher Pharmaceuticals Inc. |
Vol 69 - N° 5
P. 762-767 - novembre 2013 Retour au numéroBienvenue sur EM-consulte, la référence des professionnels de santé.
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