Determination of Acitretin in the Skin, in the Suction Blister, and in Plasma of Human Volunteers after Multiple Oral Dosing

Laugier, Jean‐Philippe; Bun, H.; Durand, Alain; Surber, Christian; Geiger, J M; Wilhelm, Klaus‐Peter; Maibach, Howard I.

doi:10.1002/jps.2600830505

Cited by 17 publications

(4 citation statements)

References 25 publications

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“…In the skin, concentrations of the compound and metabolites were found until 168 h following administration. Both observations are consistent with previous observations for second-generation retinoids (acitretin), but with lower values of accumulation [28]. After administration of 50 mg/day of acitretin in healthy volunteers for 21 or 28 days, plasma half life was 38 h, and there were remnant concentrations of acitretin and metabolite (13-cis-acitretin) in skin (7-14 days).…”

Section: Discussionsupporting

confidence: 81%

Kinetics of Plasma and Tissue Distribution of 9-<i>cis</i>-Retinoic Acid in Rat

Disdier¹,

Marchetti²,

Bun³

et al. 2000

Skin Pharmacol Physiol

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The biotransformation and tissue distribution of 9-cis-retinoic acid was investigated in hairless rats. Indeed, only limited information is available about the pharmacokinetics of 9-cis-retinoic acid. Assuming that the target site for retinoids is the skin, tissue distribution study is therefore particularly justified. Following single oral administration of 30 mg/kg of 9-cis-retinoic acid, the parent drug and five metabolites were detected in plasma. Additionally, concentrations of 9-cis-retinoic acid and metabolites were determined in the skin and seven other tissues. The distribution of 9-cis-retinoic acid was rapid in all of the organs studied (T_max ≤2 h). In skin, unchanged 9-cis-retinoic acid was still measurable up to 168 h after administration and was undetectable in other organs and plasma after 48 h.

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Section: Discussionsupporting

confidence: 81%

Kinetics of Plasma and Tissue Distribution of 9-<i>cis</i>-Retinoic Acid in Rat

Disdier¹,

Marchetti²,

Bun³

et al. 2000

Skin Pharmacol Physiol

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“…These data could also be used in further refinement of the formulation, if it was thought that MK‐0873 concentrations in the skin were not adequate. It should be noted that the use of biopsy to assess skin PKs for topical and transdermal products has been published previously. However, in this report, we demonstrate the application of skin biopsy data in preclinical and clinical PK studies for rational design of topical formulation.…”

Section: Introductionmentioning

confidence: 99%

Use of Minipig Skin Biopsy Model as an Innovative Tool to Design Topical Formulation to Achieve Desired Pharmacokinetics in Humans

Mitra

Leyes

Manser

et al. 2015

Journal of Pharmaceutical Sciences

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“…The organic layer was removed, evaporated and residue dissolved in 200 mL of methanol. The methanolic solution was filtered by 0.45 m m filters (HV‐Millipore), evaporated in a Speed Vac SC 100 (Savant, IL, USA) and the residue dissolved in 50 mL of methanol and utilized for high‐performance liquid chromatography analysis 10 …”

Section: Methodsmentioning

confidence: 99%

Acitretin and treatment of the oral leucoplakias. A model to have an active molecules release

Gombos

Femiano

et al. 2000

Acad Dermatol Venereol

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At the end of the study 71% (groups A and B) of patients showed clinical remission or marked improvement. No improvement was noted in the control subjects (group C). These results were further confirmed by histological findings. There were no significant changes in laboratory values in the three groups. The acitretin concentration in plasma and tissue ranged from 0 to 50 mg with no difference between groups A and B, and it was very high in saliva (ranging from 4.9 to 43 mg) with higher concentrations in group A than in group B (due to a longer adhesion time in group A). Patients' compliance was excellent. The results show that mucoadhesive tablets of topical acitretin are efficacious in the treatment of oral leucoplakia without systemic side-effects.

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Determination of Acitretin in the Skin, in the Suction Blister, and in Plasma of Human Volunteers after Multiple Oral Dosing

Cited by 17 publications

References 25 publications

Kinetics of Plasma and Tissue Distribution of 9-<i>cis</i>-Retinoic Acid in Rat

Kinetics of Plasma and Tissue Distribution of 9-<i>cis</i>-Retinoic Acid in Rat

Use of Minipig Skin Biopsy Model as an Innovative Tool to Design Topical Formulation to Achieve Desired Pharmacokinetics in Humans

Acitretin and treatment of the oral leucoplakias. A model to have an active molecules release

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