Contribution of intestinal transporters to drug absorption and the implications for drug discovery and development (2) : efflux transporters
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منابع مشابه
Segmental intestinal transporters and metabolic enzymes on intestinal drug absorption.
Recently, a physiologically-based, segregated flow model that incorporates separate intestinal tissue and flow to both a nonabsorptive and an absorptive outermost layer (enterocytes) was shown to better describe the observations on route-dependent morphine glucuronidation in the rat small intestine than a traditional physiologically-based model. These theoretical models were expanded, as the se...
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INTRODUCTION There are many factors that can affect the absorption process of orally administered drugs. Intestinal transporters play an important role in drug absorption. These transporters are divided into two major classes: the solute carriers and the ATP-binding cassette (ABC) transporters. P-glycoprotein (P-gp), belonging to the ABC transporter superfamily, flushes out the substrate drugs ...
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The absorption of drugs via the oral route is a subject of intense and continuous investigation in the pharmaceutical industry since good bioavailability implies that the drug is able to reach the systemic circulation by mouth. Oral dry absorption is affected by both drug properties and the physiology of the gastrointestinal tract (GIT), or patient properties, including drug dissolution from th...
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Transporters play important roles in tissue distribution and urinary- and biliary-excretion of drugs and transporter molecules involved in those processes have been elucidated well. Furthermore, an involvement of efflux transporters such as P-glycoproteins, multidrug resistance associated protein 2, and breast cancer resistance protein as the intestinal absorption barrier and/or intestinal lumi...
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Administered drugs interact with membrane transporters of epithelia, Blood Brain Barrier and other districts influencing their delivery and efficacy. Drugs can also be used as inhibitors of transporters involved in human pathology. Drug-transporter interactions are responsible of off-target effects contributing to toxicity. High Throughput Screening technologies increased the potential applicat...
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ژورنال
عنوان ژورنال: Drug Delivery System
سال: 2006
ISSN: 0913-5006,1881-2732
DOI: 10.2745/dds.21.142