Research and Development Centre, Sun Pharmaceutical Industries Ltd, Gurgaon, Haryana, India.
Acta Derm Venereol. 2020 Feb 5;100(4):adv00049. doi: 10.2340/00015555-3381.
Two open-label, crossover studies compared the bioavailability of Micronized-isotretinoin 32 mg and Lidose-isotretinoin 40 mg in healthy adults. In the fed bioequivalence/food-effect study, participants (n = 71) received single doses of fed-state Micronized-isotretinoin 32 mg, fed-state Lidose-isotretinoin 40 mg and fasted-state Micronized-isotretinoin 32 mg. In the fasting study, participants (n = 18) received single doses of fasted-state Micronized-isotretinoin 32 mg and fasted-state Lidose-isotretinoin 40 mg. Bioavailability was assessed by isotretinoin LnAUC0–t, LnAUC0–∞ and LnCmax in blood samples taken pre-dosing and over 96 h post-dosing. The 90% confidence intervals for baseline-adjusted least squares geometric mean ratios for LnAUC0–t, LnAUC0–∞ and LnCmax fell within the 80–125% range for bioequivalence for fed-state Micronized-isotretinoin 32 mg vs. fed-state Lidose-isotretinoin 40 mg. Fasted-state Micronized-isotretinoin 32 mg had ~2 times higher bioavailability than fasted-state Lidose-isotretinoin 40 mg. Food had no effect on the rate and a marginal effect on the extent of absorption of Micronized-isotretinoin 32 mg.
两项开放性、交叉研究比较了健康成年人中单剂量 Micronized-isotretinoin（32mg）和 Lidose-isotretinoin（40mg）的生物利用度。在进食状态下的生物等效性/食物效应研究中，71 名参与者单次服用 Micronized-isotretinoin（32mg）、Lidose-isotretinoin（40mg）和 Micronized-isotretinoin（32mg）禁食状态。在禁食研究中，18 名参与者单次服用 Micronized-isotretinoin（32mg）和 Lidose-isotretinoin（40mg）禁食状态。通过测定血样中异维 A 酸 LnAUC0-t、LnAUC0-∞和 LnCmax 的浓度，评估生物利用度，这些血样是在给药前和给药后 96 小时内采集的。经基线调整的最小二乘几何均数比值的 90%置信区间，用于比较 Micronized-isotretinoin（32mg）进食状态与 Lidose-isotretinoin（40mg）进食状态的生物等效性，均落在 80%-125%范围内。与 Lidose-isotretinoin（40mg）禁食状态相比，Micronized-isotretinoin（32mg）禁食状态的生物利用度约高 2 倍。食物对 Micronized-isotretinoin（32mg）的吸收速率没有影响，但对吸收程度有轻微影响。
