Principles and Practice of Pharmaceutical Medicine
maximal rate of metabolism) for each metabolic reaction, using substrate saturation plots (using the familiar algebra and, becau ...
and/or microsomal protein binding). Using this well-stirred model, it has proved possible to predict the hepatic clearance fromi ...
microsomes will be sufficient. However, if the potential for non-microsomal biotransformation exists, then a differentin vitrosy ...
Elementary aspects of oral bioavailability The oral bioavailability (F) of a drug is dependent on (a) the absorption of the drug ...
relationship between Fa and Caco-2 cell perme- ability, expressed as the apparent permeability constant (Papp), as follows: ifwP ...
and cats. This method could be expected to save time and money in the drug discovery process by enabling us to do the following: ...
expected to achieve a neuroprotective plasma con- centration of 1500 ng ml^1. To do this, we pre- dicted the volume of distribu ...
half-life would be 14.5 h, the plasma clearance be 0.138 l h^1 kg^1 and theV 1 ,VdssandVdbbe 1.01, 2.37 and 2.56 l kg^1 , res ...
amongst different agonists, describing response size for a standard degree of receptor occupation (Jenkinsonet al., 1995). When ...
then this may be added to the right-hand side of the equation: E¼E 0 þ EmaxC EC 50 þC Alternatively, the relationship between co ...
and is analogous to the ‘plasma disappearance’ curve (above): XIV¼DIVeKt The amount of drug in a single hypothetical com- partm ...
one-compartment model with bolus input of dose (D) is: Ae¼ kleD ke0K ½eKteke0t whereKis the elimination rate constant. The ...
In this equation,kdis the apparent first-order degra- dation rate constant (also calledkout). This constant can be obtained expe ...
P 0 ¼130 s andtlag¼ 0 h. The computer fitting gave 0.2629.46 for the IC 50 , 0.03317.9 for kd,2.6839.6 fornand 12158 forP 0 ...
are made in discussions among committee members and may not necessarily be based on hard and fast criteria. Also, unlike a compu ...
Medicinal chemistry New chemical entity (NCE) Binding IC 50 Functional assay EC 50 Criteria met Criteria met In vitro intrinsic ...
pharmacological screening to general pharmacol- ogy and toxicology, all with pharmacokinetic sup- port, which involves the devel ...
Colburn WA. 1995. ‘Clinical markers and endpoints in bioequivalence assessment’.Drug Inf. J. 29 : 917. Curry SH. 1980.Drug Dispo ...
Pitsui M, Parker E, Aarons L, Rowland M. 1993. ‘Population pharmacokinetics and pharmacody- namics of warfarin in healthy young ...
9 Phase II and Phase III Clinical Studies Anthony W. Fox 9.1 The phases of drug development: an obsolete model In former times,i ...
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