Model drug

Concerning the distribution of a drug, models have been published for log BB blood/brain partition coefficient) for CNS-active drugs (CNS, central nervous system) crossing the blood-brain barrier (BBB) [38-45] and binding to human serum albumin (HSA) [46]. 

W. Wierenga "DNA-Minor Groove Binding Anticancer Agents" in Cytotoxic Mnticancer Drugs Models and Conceptsfor Drug Discovey and Development, Kluwer Academic PubHshers, Boston, Mass., 1992, p. 105. 

With the advent of computer-aided-drug modeling (CADM) the critical, scientific and faster approach to newer drug entities based on the biologically active prototypes, combinatorial chemistry, chiral chemistry and biotechnology has paved the way towards more specific, potent and above all less toxic drugs to improve the ultimate quality of life in humans. 

Francis PT, Pangalos MM, Bowen DM Animal and drug modelling for Alzheimer synaptic pathology. Prog Neurobiol 39 517-545, 1992 Frank E, Kupfer DJ, Perel JM, et al Three-year outcomes for maintenance therapies in recurrent depression. Arch Gen Psychiatry 47 1093-1099, 1990 Frank E, Prien R, Jarrett RB, et al Conceptualization and rationale for consensus definitions of terms in major depressive disorder. Arch Gen Psychiatry 48 851-855, 1991... 

The relationship between the structure of the oligopeptide sequences and the rate of enzymatically catalyzed release of a drug or drug model was studied in detail. Over 50 different oligopeptide sequences were introduced into HPMA copolymers and their degradability by different enzymes studied. First, model enzymes, chymotrypsin [235, 238,239, 243,244], trypsin [245], and papain... 

Oral ModiLed-Release Product Designs forV feter-lnsoluble Drugs Models, Theories,... 

ORAL MODIFIED-RELEASE PRODUCT DESIGNS FOR WATER-INSOLUBLE DRUGS MODELS, THEORIES,... 

Ammoury, N., et al. 1989. Physiochemical characterization of polymeric nanocapsules and in vitro release evaluation of indomethacin as drug model. STP Pharma 5 647. 

C. R. Clark and L. E. Garcia-Roura, Liquid chromatographic studies on the aqueous solution conformation of substituted ben-zamide drug models, J. Chromatogr. Sci., 27 111 (1989). 

Neuse EW (2005) Macromolecular ferrocene compounds as cancer drug models. J Inorg Organomet Polym Mater 15 3-32... 

Amyloid Fibers in Disease Several small aromatic molecules, such as phenol red (used as a nontoxic drug model), have been shown to inhibit the formation of amyloid in laboratory model systems. A goal of the research on these small aromatic compounds is to find a drug that would efficiently inhibit the formation of amyloid in the brain in people with incipient Alzheimer s disease. 

FIGURE 48 SEM micrograph of matrix tablet containing potassium chloride as drug model and commercial acrylic-metacrylic copolymer. The white KCI particles are surrounded by an almost continuous dark gray mass of excipient. (Courtesy of M. Millan.)... 

The placebo model assumes an endogenous response, influenced by baseline (BL), and two exponential functions. For ai > U2, P(t) increases over time above BL then declines back to BL for sufficiently large t. The drug model is a stimulus model, a function of plasma concentration C(t), maximal effect Pmax, and LCso, the concentration that produces 50% of the maximal effect. In this example, C(t) is generated without measurement error but is influenced by subject random effects in K, K, and V, as discussed in the previous section. Additional subject random effects are considered for BL and Pmax-... 

Based on prior information collected in a patients study (31) and on the data collected, a one-compartment model with a first-order absorption with or without a lag time was tested for the choice of the structural model for nellinavir. As an extension of the parent drug model, a one-compartment model with first-order absorption and elimination was tested for the metabolite. The structure of the PK model used is presented in Figure 44.1. 

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