The role of formulation on the pharmacokinetics of antiretroviral drugs

Introduction: A multitude of antiretroviral drug formulations are now available for HIV-infected adults and children. These formulations include individual and co-formulated drugs, many of which are also supplied in generic versions. Many antiretroviral drugs have a low aqueous solubility and poor b...

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Main Authors: Diane Et Bastiaans, Tim R. Cressey, Herman Vromans, David M. Burger
Format: Journal
Published: 2018
Online Access:https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=84902481899&origin=inward
http://cmuir.cmu.ac.th/jspui/handle/6653943832/45772
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Institution: Chiang Mai University
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spelling th-cmuir.6653943832-457722018-01-24T06:17:16Z The role of formulation on the pharmacokinetics of antiretroviral drugs Diane Et Bastiaans Tim R. Cressey Herman Vromans David M. Burger Introduction: A multitude of antiretroviral drug formulations are now available for HIV-infected adults and children. These formulations include individual and co-formulated drugs, many of which are also supplied in generic versions. Many antiretroviral drugs have a low aqueous solubility and poor bioavailability. Drug formulation can significantly affect bioavailability, and given the increasing number of new formulations and drug combinations, it is important to be aware that formulation can influence the pharmacokinetics of antiretroviral drugs.Areas covered: This review provides an overview of studies assessing the pharmacokinetics of different antiretroviral drug formulations in adults and children, including fixed-dose combinations. For some antiretroviral drugs, differences in pharmacokinetics have been described, with largest differences in exposure when a liquid formulation is compared to a tablet or capsule formulation. Biopharmaceutical properties of antiretroviral drugs relevant to bioavailability are discussed.Expert opinion: Antiretroviral drug formulations and their excipients can significantly impact drug exposure. However, this is not yet fully recognized. It is important to realize that children use different formulations than adults. Effort should be made to ensure that adequate drug exposures are achieved to treat HIV-infected children. In addition, manipulation of drug formulations may lead to differences in pharmacokinetics.© 2014 Informa UK, Ltd. 2018-01-24T06:17:16Z 2018-01-24T06:17:16Z 2014-01-01 Journal 17447607 17425255 2-s2.0-84902481899 10.1517/17425255.2014.925879 https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=84902481899&origin=inward http://cmuir.cmu.ac.th/jspui/handle/6653943832/45772
institution Chiang Mai University
building Chiang Mai University Library
country Thailand
collection CMU Intellectual Repository
description Introduction: A multitude of antiretroviral drug formulations are now available for HIV-infected adults and children. These formulations include individual and co-formulated drugs, many of which are also supplied in generic versions. Many antiretroviral drugs have a low aqueous solubility and poor bioavailability. Drug formulation can significantly affect bioavailability, and given the increasing number of new formulations and drug combinations, it is important to be aware that formulation can influence the pharmacokinetics of antiretroviral drugs.Areas covered: This review provides an overview of studies assessing the pharmacokinetics of different antiretroviral drug formulations in adults and children, including fixed-dose combinations. For some antiretroviral drugs, differences in pharmacokinetics have been described, with largest differences in exposure when a liquid formulation is compared to a tablet or capsule formulation. Biopharmaceutical properties of antiretroviral drugs relevant to bioavailability are discussed.Expert opinion: Antiretroviral drug formulations and their excipients can significantly impact drug exposure. However, this is not yet fully recognized. It is important to realize that children use different formulations than adults. Effort should be made to ensure that adequate drug exposures are achieved to treat HIV-infected children. In addition, manipulation of drug formulations may lead to differences in pharmacokinetics.© 2014 Informa UK, Ltd.
format Journal
author Diane Et Bastiaans
Tim R. Cressey
Herman Vromans
David M. Burger
spellingShingle Diane Et Bastiaans
Tim R. Cressey
Herman Vromans
David M. Burger
The role of formulation on the pharmacokinetics of antiretroviral drugs
author_facet Diane Et Bastiaans
Tim R. Cressey
Herman Vromans
David M. Burger
author_sort Diane Et Bastiaans
title The role of formulation on the pharmacokinetics of antiretroviral drugs
title_short The role of formulation on the pharmacokinetics of antiretroviral drugs
title_full The role of formulation on the pharmacokinetics of antiretroviral drugs
title_fullStr The role of formulation on the pharmacokinetics of antiretroviral drugs
title_full_unstemmed The role of formulation on the pharmacokinetics of antiretroviral drugs
title_sort role of formulation on the pharmacokinetics of antiretroviral drugs
publishDate 2018
url https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=84902481899&origin=inward
http://cmuir.cmu.ac.th/jspui/handle/6653943832/45772
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