Predicting Passive Intestinal Drug Absorption: An Interesting Relationship between Fraction Absorbed and Melting Point

Persistent Link:
http://hdl.handle.net/10150/195503
Title:
Predicting Passive Intestinal Drug Absorption: An Interesting Relationship between Fraction Absorbed and Melting Point
Author:
Chu, Katherine A.
Issue Date:
2009
Publisher:
The University of Arizona.
Rights:
Copyright © is held by the author. Digital access to this material is made possible by the University Libraries, University of Arizona. Further transmission, reproduction or presentation (such as public display or performance) of protected items is prohibited except with permission of the author.
Abstract:
Oral drug administration remains the most popular route of drug delivery. Absorption of the dissolved drug through the intestinal epithelial membrane is a prerequisite to systemic bioavailability and drug efficacy. In efforts to reduce the long lead times, attrition rates, and costs of drug discovery and development, computational models have been developed to predict the membrane permeability and absorption efficiency of a dosed drug. Many models utilize various molecular descriptors to correlate with in vitro permeability or human intestinal absorption data. It is widely accepted that the two most significant physicochemical properties that control a compound's passive transport process are its aqueous solubility and lipophilicity characteristics.This work will discuss the theoretical background of passive transport, a number of computational models developed to predict in vitro permeability, other models that predict human fraction of dose absorbed, and predicting absorption efficiency relative to a maximum dose. A newly developed prediction method is also presented, that reveals an interesting relationship between fraction absorbed and the melting point of the drug.
Type:
text; Electronic Dissertation
Keywords:
absorption; cyclodextrin; formulation; melting point; partition; solubility
Degree Name:
Ph.D.
Degree Level:
doctoral
Degree Program:
Pharmaceutical Sciences; Graduate College
Degree Grantor:
University of Arizona
Advisor:
Yalkowsky, Samuel H.
Committee Chair:
Yalkowsky, Samuel H.

Full metadata record

DC FieldValue Language
dc.language.isoENen_US
dc.titlePredicting Passive Intestinal Drug Absorption: An Interesting Relationship between Fraction Absorbed and Melting Pointen_US
dc.creatorChu, Katherine A.en_US
dc.contributor.authorChu, Katherine A.en_US
dc.date.issued2009en_US
dc.publisherThe University of Arizona.en_US
dc.rightsCopyright © is held by the author. Digital access to this material is made possible by the University Libraries, University of Arizona. Further transmission, reproduction or presentation (such as public display or performance) of protected items is prohibited except with permission of the author.en_US
dc.description.abstractOral drug administration remains the most popular route of drug delivery. Absorption of the dissolved drug through the intestinal epithelial membrane is a prerequisite to systemic bioavailability and drug efficacy. In efforts to reduce the long lead times, attrition rates, and costs of drug discovery and development, computational models have been developed to predict the membrane permeability and absorption efficiency of a dosed drug. Many models utilize various molecular descriptors to correlate with in vitro permeability or human intestinal absorption data. It is widely accepted that the two most significant physicochemical properties that control a compound's passive transport process are its aqueous solubility and lipophilicity characteristics.This work will discuss the theoretical background of passive transport, a number of computational models developed to predict in vitro permeability, other models that predict human fraction of dose absorbed, and predicting absorption efficiency relative to a maximum dose. A newly developed prediction method is also presented, that reveals an interesting relationship between fraction absorbed and the melting point of the drug.en_US
dc.typetexten_US
dc.typeElectronic Dissertationen_US
dc.subjectabsorptionen_US
dc.subjectcyclodextrinen_US
dc.subjectformulationen_US
dc.subjectmelting pointen_US
dc.subjectpartitionen_US
dc.subjectsolubilityen_US
thesis.degree.namePh.D.en_US
thesis.degree.leveldoctoralen_US
thesis.degree.disciplinePharmaceutical Sciencesen_US
thesis.degree.disciplineGraduate Collegeen_US
thesis.degree.grantorUniversity of Arizonaen_US
dc.contributor.advisorYalkowsky, Samuel H.en_US
dc.contributor.chairYalkowsky, Samuel H.en_US
dc.contributor.committeememberMyrdal, Paul Ben_US
dc.contributor.committeememberMayersohn, Michaelen_US
dc.identifier.proquest10747en_US
dc.identifier.oclc659753571en_US
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