Previously submitted to: JMIR Dermatology (no longer under consideration since Jun 30, 2025)
Date Submitted: Aug 13, 2024
Warning: This is an author submission that is not peer-reviewed or edited. Preprints - unless they show as "accepted" - should not be relied on to guide clinical practice or health-related behavior and should not be reported in news media as established information.
Comparative Bioavailability of Low-dose Micronized-isotretinoin 16 mg & Conventional Isotretinoin 20 mg Under Fasting Condition in Healthy Adult Male Subjects: A Randomized, Single-dose, Two-way, Cross-over Study
ABSTRACT
Background:
Isotretinoin, the first line therapy for the treatment of severe nodular acne, is recommended to be administered with meals to optimize its bioavailability and efficacy. To overcome this limitation, low-dose micronized-isotretinoin is formulated by using an optimized micronization technology that enhances the rate of dissolution and bioavailability of isotretinoin.
Objective:
To assess the comparative bioavailability of low-dose micronized-isotretinoin 16mg (Test;T) and conventional isotretinoin 20mg (Reference;R) under fasting condition.
Methods:
An open label, randomized, two-treatment, two-period, two-sequence, single-dose, cross-over comparative bioavailability study. Study period involved fasting for at least 10hours prior to administration and 4hours after a single oral dose of either test or reference product. The interval between dosing (washout period) was 18days.
Results:
Total 15 participants completed the study. The Cmax was 439.58±169.99ng/mL and 149.64±26.91ng/mL; and AUC0–∞ was 6181.90 ± 2240.75ng·h/mL and 2479.83 ± 975.90ng·h/mL for test and reference, respectively. The ratio of T/R [90 %CI] were 277.78% (238.11-324.06) for Cmax, and 246.95% (228.93-266.39) for AUC0–∞. The Median Tmax was 3.25hrs and 2.75hrs test and reference formulation respectively. Both the formulations were well tolerated.
Conclusions:
Low-dose micronized-isotretinoin 16mg had ~2.5 folds higher bioavailability as compared to conventional isotretinoin 20mg under fasting conditions.
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