Single-Pass Intestinal Perfusion (SPIP) and prediction of fraction absorbed and permeability in humans: A study with antiretroviral drugs

Autor(es)

Dezani, Thaisa Marinho ^[1] ; Dezani, Andre Bersani ^[1] ; da Silva Junior, Joao Batista ^[1] ; dos Reis Serra, Cristina Helena ^[1]

Afiliação do(s) autor(es)

^[1] Univ Sao Paulo, Fac Pharmaceut Sci, Dept Pharm, Ave Prof Lineu Prestes 580, Bl-13, BR-05508900 Sao Paulo, SP - Brazil

• Tipo de documento: Artigo Científico
• Fonte: EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS; v. 104, p. 131-139, JUL 2016.
• Citações Web of Science: 14

Resumo

In recent years, the prediction of oral drug absorption in humans has been a challenge for researchers and many techniques for permeability studies have been developed for several purposes, including biowaiver processes. The Single-Pass Intestinal Perfusion (SPIP) method performed in rats can provide permeability results closest to in vivo condition. The purpose of the present study was to evaluate the intestinal permeability of the antiretroviral drugs lamivudine, stavudine and zidovudine using the SPIP method in rats and to predict their permeability (P-eff,P-humans) and fraction absorbed (F-a) in humans. Metoprolol and fluorescein were used as marker compounds of high and low permeability, respectively. The effective permeability (P-eff) results showed that stavudine and zidovudine have high permeability characteristics while lamivudine presented the lowest result. From P-eff values obtained in rats, the P-eff,P-humans and F-a were calculated. The use of SPIP in rats and calculations for absorption prediction in humans may indicate the transport mechanisms and/or pre-systemic metabolism involved on permeation processes of drugs, since this model is the closest to in vivo conditions. (C) 2016 Elsevier B.V. All rights reserved. (AU)

• Processo FAPESP: 11/09670-3 - Estudo de permeabilidade de fármacos antirretrovirais por meio do modelo de perfusão in situ. Aplicação na Classificação Biofarmacêutica.
• Beneficiário: João Batista da Silva Junior
• Linha de fomento: Bolsas no Brasil - Iniciação Científica