Drug Metabolism in Drug Design and Development Basic Concepts and Practice

studies in human liver microsomes as a better representative of thein vivo situation. Clinical inhibition potential can be predi ...

metabolite-mediated toxicity pathway is indeed thought to be animal specific then it is necessary to demonstrate this specificit ...

tested as inhibitors of UGT1A1, 1A3, 1A4, 1A6, and 1A9 in human liver microsomes (Zhang et al., 2005). All the protease inhibito ...

9.7 IMPACT OF METABOLISM INFORMATION ON NDA FILING AND LABELING FDA and ICH guidelines (see Chapter 7 for specific guidelines) r ...

andin vivodrug–drug interaction studies: a PhRMA perspective. J Clin Pharmacol 2003;43:443–469. Cohen LH, Remley MJ, Raunig D, V ...

stable-labeled [^13 C 2 ]omapatrilat after oral administration to rats, dogs, and humans. Drug Metab Dispos 2003;31:67–75. Iyer ...

species-dependent metabolism of efavirenz produces a nephrotoxic glutathione conjugate in rats. Toxicol Appl Pharmacol 2000;169: ...

Wait JCM, Vaccharajani N, Mitroka J, Jemal M, Khan S, Bonacorsi SJ, Rinehart JK, Iyer RA. Metabolism of [^14 C]gemopatrilat afte ...

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PART III ANALYTICAL TECHNIQUES IN DRUG METABOLISM ...

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10 APPLICATIONS OF LIQUID RADIOCHROMATOGRAPHY TECHNIQUES IN DRUG METABOLISM STUDIES MINGSHEZHU,WEIPINGZHAO,ANDW. GRIFFITHHUMPHRE ...

the metabolism of the drug, and the kinetics of the metabolic reactions (Ilett et al., 2002; Lautala et al., 1999; Zhang et al., ...

limit of RFD is 250–500 disintigrations per minutes (DPM) and the limit of quantification of RFD ranges from 750 to 1500 DPM, wh ...

FIGURE 10.2 Metabolite profiles of buspirone determined by HPLC with MSC, LSC, and RFD (Zhu et al., 2005b). Buspirone metabolite ...

counting (MSC) and other recently developed liquid radiochromatographic techniques. 10.3 New Radiochromatography Techniques 10.3 ...

are generally utilized for the calculation of relative radioactivity abundance. If counting efficiencies of HPLC effluent fracti ...

10.2. Minor metabolite peaks M1, M2, M4, M10, M13 and M14 were detected in all analyses with TopCount (Fig. 10.2a), but not dete ...

10.3.1.3 Matrix Effect of Biological Samples MSC uses solid scintillators to convert radioactivity decay energy into photons. Bi ...

NEW RADIOCHROMATOGRAPHY TECHNIQUES 297 ...