Percutaneous absorption of azelaic acid in humans

Abstract

Six healthy male volunteers received a single topical treatment with 5 g of an anti-acne cream containing 20% azelaic acid (AzA) onto the face, the chest and the upper back. One week later 1 g of AzA was given orally to the same subjects as aqueous microcrystalline suspension. Following the two treatments the renal excretion of the unchanged compound was measured. Analysis included ether extraction of the urine, derivatization of extract and HPLC with UV detection. After topical application 2.2 +/- 0.7%, and after oral administration 61.2 +/- 8.8% of the dose had been excreted unchanged with the urine. By comparing both amounts, the percutaneous absorption of AzA from the cream was assessed to 3.6% of the dermally applied dose.

S2k – Guideline on the Therapy of Acne

“…Azelaic acid Azelaic acid is a dicarboxylic acid which is naturally present in the organism [479,480] and is not teratogenic [472,475,476]. The percutaneous rate of absorption is 3.6% [481].…”

Azelaic acid 15% gel for treatment of rosacea

“…Following the single topical application of azelaic acid 20% cream to the face, chest and upper back of six healthy male volunteers, percutaneous absorption of azelaic acid was 3.6% of the dermally applied dose; 2.2% of the dose was excreted unchanged in the urine [40]. When administered orally, 61.2% of a 1-g dose was excreted unchanged in the urine of the same volunteers.…”

Gravidez, Aleitamento e Fármacos em Dermatologia: Tratamento Tópico

“…12 Após a aplicação tópica de ácido azeláico, cerca de 4% do fármaco é absorvido para a circulação sistémica, mas estudos em modelos animais não mostraram teratogenicidade (categoria de risco B pela FDA). 79 Não existem estudos relativos à sua utilização durante a amamentação, mas pela fraca absorção sistémica o seu uso parece ser seguro durante a lactação. 19,80 A aplicação local de azoto líquido e de ácido tricloroacé-tico são considerados tratamentos de eleição para verrugas víricas e condilomas acuminados em grávidas.…”