By Han van de Waterbeemd, Bernard Testa, Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
The peroral program (swallowing) of a medication implies that the physique needs to first resorb the lively substance ahead of it will probably start to take impact. The efficacy of drug uptake is determined by the only hand at the chemical features of the lively substance, specially on its solubility and membrane permeability. nonetheless, it really is decided through the organism's skill to soak up prescription drugs in terms of particular delivery proteins or to excrete them. considering many pharmacologically energetic ingredients are poorly suited to oral consumption, a decisive criterion for the efficacy of a drugs is its so-called bioavailability.
Written by way of a global crew from academia and the pharmaceutical undefined, this ebook covers all facets of the oral bioavailability of medications. the focal point is put on tools for deciding on the parameters correct to bioavailability. those variety from sleek physicochemical recommendations through organic experiences in vitro and in vivo correct as much as computer-aided predictions. The authors particularly tackle probabilities for optimizing bioavailability throughout the early screening degree for the lively substance.
Its transparent constitution and entire assurance make this booklet both appropriate for researchers and teachers in and instructing.
Chapter 1 Physico?Chemical techniques to Drug Absorption (pages 1–20): Prof. Dr. Han van de Waterbeemd
Chapter 2 High?Throughput dimension of log D and pKa (pages 21–45): Dr. John E. A. Comer
Chapter three High?throughput dimension of Permeability Profiles (pages 46–71): Dr. Alex Avdeef
Chapter four Caco?2 and rising choices for Prediction of Intestinal Drug delivery: A normal evaluate (pages 72–89): Prof. Dr. according to Artursson and Dr. Staffan Tavelin
Chapter five mobilephone Cultures in Drug Discovery: An commercial point of view (pages 90–131): Dr. Anna?Lena Ungell and Dr. Johan Karlsson
Chapter 6 Use of Animals for the selection of Absorption and Bioavailability (pages 132–154): Dr. Chris Logan
Chapter 7 In Vivo Permeability experiences within the Gastrointestinal Tract of people (pages 155–188): Dr. Niclas Petri and Prof. Dr. Hans Lennernas
Chapter eight Gastrointestinal Dissolution and Absorption of gear (pages 189–214): Dr. Gladys E. Granero, Dr. Chandrasekharan Ramachandran and Prof. Dr. Gordon L. Amidon
Chapter nine Aqueous Solubility in Discovery, Chemistry, and Assay adjustments (pages 215–231): Dr. Chris Lipinski
Chapter 10 components Influencing the Water Solubilities of Crystalline medications (pages 232–242): Dr. James W. McFarland, Dr. Chau M. Du and Dr. Alex Avdeef
Chapter eleven Transporters within the GI Tract (pages 243–287): Dr. Ho?Chul Shin, Dr. Christopher P. Landowski, Dr. Duxin sunlight and Prof. Dr. Gordon L. Amidon
Chapter 12 Hepatic shipping (pages 288–310): Prof. Dr. Hiroshi Suzuki and Prof. Dr. Yuichi Sugiyama
Chapter thirteen the significance of intestine Wall Metabolism in settling on Drug Bioavailability (pages 311–328): Kevin Beaumont
Chapter 14 converted mobilephone strains (pages 329–338): Dr. Charles L. Crespi
Chapter 15 Intestinal Absorption: The position of Polar floor sector (pages 339–357): Prof. Dr. in step with Artursson and Dr. Christel A. S. Bergstrom
Chapter sixteen Calculated Molecular houses and Multivariate Statistical research in Absorption Prediction (pages 358–405): Dr. Ulf Norinder and Dr. Markus Haeberlein
Chapter 17 VOLSURF: a device for Drug ADME?Properties Prediction (pages 406–419): Prof. Dr. Gabriele Cruciani, Dr. Mirco Meniconi, Dr. Emanuele Carosati, Dr. Ismael Zamora and Prof. Dr. Raimund Mannhold
Chapter 18 Simulation of Absorption, Metabolism, and Bioavailability (pages 420–443): Prof. Dr. Michael B. Bolger, Dr. rainbowbalaji Agoram, Dr. Robert Fraczkiewicz and Dr. Boyd Steere
Chapter 19 Prediction of Bioavailability (pages 444–460): Dr. Arun okay. Mandagere and Dr. Barry Jones
Chapter 20 in the direction of P?Glycoprotein Structure–Activity Relationships (pages 461–492): PD Anna Seelig, Dr. Ewa Landwojtowicz, Dr. Holger Fischer and Dr. Xiaochun Li Blatter
Chapter 21 software of the Biopharmaceutic type procedure Now and sooner or later (pages 493–531): Dr. Bertil Abrahamsson and Prof. Dr. Hans Lennernas
Chapter 22 Prodrugs (pages 532–546): Prof. Dr. Bente Steffansen, Dr. Anne Engelbrecht Thomsen and Prof. Dr. Sven Frokjaer
Chapter 23 smooth supply techniques: Physiological concerns for Orally Administered medicines (pages 547–568): Prof. Dr. Clive G. Wilson
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Additional resources for Drug Bioavailability: Estimation of Solubility, Permeability, Absorption and Bioavailability
When it becomes necessary, the column is re-coated by pumping octanol through it, followed by two blank runs for reconditioning. Samples are taken directly from 10 mM DMSO-solvated stocks in 96-well plates. Typically, 2 mL of sample is aspirated, and injected on to the column – this represents about 8 mg of sample with MW ¼ 400. The retention time (Rt ) of peaks eluting from the column is related to the capacity factor log k by Eq. (8): Rt À T0 log k ¼ log T0 ð8Þ where T0 is the time required to clear the volume of the system (this is a constant value of a few seconds).
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1998, 41, 1007–1010. , High-throughput artiﬁcial membrane permeability studies in early lead discovery and development, in: Pharmacokinetic Optimization in Drug Research; Biological, Physicochemical and Computational Strategies. , Guy, R. (eds), WileyVCH, Weinheim and Verlag HCA, Zurich, 2001, pp. 447–464. , Balogh, M. , Drug absorption in vitro model: ﬁlter-immobilized artiﬁcial membranes 2. Studies of the permeability properties of lactones in Piper methysticum Forst, Eur. J. Pharm. Sci. 2001, 14, 271–280.
Drug Bioavailability: Estimation of Solubility, Permeability, Absorption and Bioavailability by Han van de Waterbeemd, Bernard Testa, Raimund Mannhold, Hugo Kubinyi, Gerd Folkers