Absorption and Drug Development by Avdeef, Alex;

Short description:

Many times drugs work fine when tested outside the body, but when they are tested in the body they fail. One of the major reasons a drug fails is that it cannot be absorb by the body in a way to have the effect it was intended to have.

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Long description:

Many times drugs work fine when tested outside the body, but when they are tested in the body they fail. One of the major reasons a drug fails is that it cannot be absorb by the body in a way to have the effect it was intended to have. Permeability, Solubility, Dissolution, and Charged State of Ionizable Molecules:

• Helps drug discovery professionals to eliminate poorly absorbable molecules early in the drug discovery process, which can save drug companies millions of dollars.


• Extensive tabulations, in appendix format, of properties and structures of about 200 standard drug molecules.

Profiling compounds for drug-like properties

Of the hundreds of thousands of compounds synthesized each year, most have almost no chance of becoming drugs. This problem exists because most molecules lack eht drug-like poperties necessary to enable them to be effective in vivo. To address this issue, Alex Avdeef s Absorption and Drug Development shows the reader how to examine a compound s pharmaceutical properties, emphasizing oral absorption. This book explains the different physiochemical methods currently used to analyze drug candidates and how to interpret these methods. Topics discussed include:

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  The physicochemical needs of pharmaceutical research and development
  


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  The flux model in terms of solubility, permeability, and charge state (pH)
  


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  Ionization constants
  


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  Experimental methods of measuring partition coefficients, log P and log D
  


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  Partition coefficients where the lipid phase is made of liposomes formed from vesicles of bilayers of phospholipids
  


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  PAMPA (parallel artificial membrane permeability assays)
  

Also included are physicochemical data for over 200 commercial drugs. With over 600 references and 100 drawings, this book is suitable for the practical pharmaceutical chemist and those seeking a better understanding of physiochemical measurements.

...a useful book for anyone interested in the measurement of physiochemical parameters that relate to drug permeability. (
Journal of Medicinal Chemistry, Vol. 47, No. 7)

"...useful compilations of data...of use to those working in the agrochemical and environmental industries..." (Chemistry & Industry, 19 January 2004)

...a useful book for anyone interested in the measurement of physiochemical parameters that relate to drug permeability. (
Journal of Medicinal Chemistry, Vol. 47, No. 7)

"...useful compilations of data...of use to those working in the agrochemical and environmental industries..." (Chemistry & Industry, 19 January 2004)

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Table of Contents:

Preface.

Acknowledgments.

Definitions.

1. Introduction.

2. Transport Model.

3. Charge State.

4. Partitioning Into Octanol.

5. Partitioning Into Liposomes.

6. Solubility.

7. Permeability.

8. Summary and Some Simple Rules.

References.

Index.

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