Pharmacokinetics evaluation

M Mayersohn, The xylose test to assess gastrointestinal absorption in the elderly a pharmacokinetic evaluation of the literature. J Gerontol 37 300-305, 1982. 

N Ammoury, H Fessi, JP Devissaguet, M Du-brasquet, S Benita. Jejunal absorption, pharmacological activity, and pharmacokinetic evaluation of indomethacin-loaded poly(d,l-lactide) and poly(-isobutyl-cyanoacrylate) nanocapsules in rats. Pharm Res 8 101-105, 1991. 

Where the drug studied is a racemate, the pharmacokinetics, including potential interconversion, of the individual enantiomers should be investigated in Phase I clinical studies. Phase I or II data in the target population should indicate whether an achiral assay, or monitoring of only one optical isomer where a fixed ratio is confirmed, will be adequate for pharmacokinetic evaluation. If the racemate has already been marketed and the sponsor wishes to develop the single enantiomer, additional studies should include determination of any conversion to the other isomer and whether there is any difference in pharmacokinetics between the single enantiomer administered alone or as part of the racemate. 

A novel class of tricyclic lymphocyte specific kinase (Lck) inhibitors containing the 9,10-dihydro-8//-pyrazolo[l,2-tf]pyrimido[4,5-c]pyridazin-8-one moiety has been reported <2006BML4257, 2006H(68)2037>. The most promising compound, 708, advanced to pharmacokinetic evaluation <2006BML4257>. 

Table 6.26. PHARMACOKINETIC EVALUATION OF 7-(IMIDAZOL-l-YL)QUINOLONES IN MICE [102]...

Studies are often one to two weeks in duration and routinely include body weight determinations, clinical observations, and gross necropsy findings. Additional antemortem studies may be performed as appropriate, especially in large animals (e.g., observation of local reactogenicity, pharmacokinetic evaluations, hematological and/or clinical biochemistry measurements). Histological evaluations may also be performed. 

Includes satellite animals for pharmacokinetic evaluation. bNumber of animals/group includes several animals. 

As bioanalysis plays a key role during drug discovery and toxico-kinetic/pharmacokinetic evaluation of drug candidates, several improvements have been made in minimizing the time spent in performing bioanalysis and for the evaluation of drug efficacy. 

Wasserman V. Development, Characterization, Optimization, and Pharmacokinetic Evaluation of Liposome-Based Piperidine Nitroxide Formulation for Treatment of Pathological Conditions Tumor and Rheumatoid Arthritis. Ph.D. thesis, 2002. 

Matsumura Y, Hamaguchi T, Ura T, Muio K, Yamada Y, Shimada Y, Shitao K, Okusaka T, Ueno H, Ikeda M, Watanahe N. Phase I clinical trial and pharmacokinetic evaluation of NK911, a micelle-encapsulated doxorubicin. Br J Cancer 2004 91 1775-1781. 

Lo M.W., J.B. McCrea, C.R. Shadle, M. Hesney, R. Chiou, D. Cylc, A.S. Yuan, and M.R. Goldberg (2000). Enalapril in RAPIDISC (wafer formulation) Pharmacokinetic evaluation of a novel, convenient formulation. International Journal of Clinical Pharmacology and Therapeutics 38 327-332. 

Battino D, Crod D, Rossini A, et al. Serum carbamazepine concentrations in elderly patients a case-matched pharmacokinetic evaluation based on therapeutic drug monitoring data. Epilepsia 2003 44 923-929. 

Schmider J, von Moltke LL, Shader Rl, et al. Extrapolating in vitro data on drug metabolism to in vivo pharmacokinetics evaluation of the pharmacokinetic interaction between amitriptyline and fluoxetine. Drug Metab Rev 1999 31 545-560. 

Biobatch The lot of drug product formulated for purposes of pharmacokinetic evaluation in a bioavailabUity/bioequivalency study. For modified release solid oral, this batch should be 10% or greater than the proposed commercial production batch or at least 100,000 units, whichever is greater. 

Nishikawa, M., Takakura, Y. and Hashida, M. (1996) Pharmacokinetic evaluation of polymeric carriers. Adv. Drug Deliv. Rev., 21, 135-155. 

Mamidi, R.N., et al. 2002. Pharmacological and pharmacokinetic evaluation of celecoxib prodrugs in rats. Biopharm Drug Dispos 23 273. 

Loo, J.C., et al. 1981. Pharmacokinetic evaluation of betamethasone and its water soluble phosphate ester in humans. Biopharm Drug Dispos 2 265. 

A. Wiegand, K. Bauer, R. Bonn, et al. Pharmacodynamic and pharmacokinetic evaluation of a new transdermal delivery system with a time-dependent release of glyceryl trinitrate. J. Clin. Pharmacol. 32 77—84, 1992. 

Human FcRn Transgenic Mice for Pharmacokinetic Evaluation of Therapeutic Antibodies... 

Therapeutic monoclonal antibodies are widely recognized to be a most promising means to treat an increasing number of human diseases, including cancers and autoimmunity. To a large extent, the efficacy of monoclonal antibody treatment is because IgG antibodies have greatly extended persistence in vivo. However, conventional rodent models do not mirror human antibody pharmacokinetics. The key molecule responsible for the extended persistence antibodies is the major histocompatibility complex class I family Fc receptor, FcRn. We describe human FcRn transgenic mouse models and how they can be exploited productively for the preclinical pharmacokinetic evaluation of therapeutic antibodies. 

M. Saah, W.-M. Wu, K. Eberst, E. Marvanyos, and N. Bodor, Design, synthesis, and pharmacokinetic evaluation of a chemical delivery system for drug targeting to lung tissue, J. Pharm. Sci. 85 496 (1996). 

Crooke, S.T., L.R. Grillone, A. Tendolkar, A. Garrett, M.J. Fratkin, J. Leeds, and W.H. Barr. 1994. A pharmacokinetic evaluation of 14C-labeled afovirsen sodium in patients with genital warts. Clin. Pharmacol. Ther. 56 641—646. 

Bioanalytical Methods Used for Pharmacokinetic Evaluations of Biotech Macromolecule Drugs Issues, Assay Approaches, and Limitations... 

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