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ISBN: 9780853699804 | 0853699801

Edition: 2ndFormat: Paperback

Publisher: PHARMACEUTICAL PRESS

Pub. Date: 4/1/2012

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Basic Pharmacokinetics provides an understanding of the principles of pharmacokinetics and biopharmaceutics and of how these principles can be applied to achieve successful drug therapy.

Sunil S Jambhekar is Professor and Associate Dean, LECOM-Bradenton School of Pharmacy, Florida, USA. Phillip J Breen is Associate Professor of Pharmaceutics, Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, USA.

Preface | p. xi |

About the authors | p. xiii |

Introduction and overview | p. 1 |

Use of drugs in disease states | p. 1 |

Important definitions and descriptions | p. 2 |

Sites of drug administration | p. 4 |

Review of ADME processes | p. 5 |

Pharmacokinetic models | p. 7 |

Rate processes | p. 12 |

Mathematical review | p. 17 |

Introduction | p. 17 |

A brief history of pharmacokinetics | p. 18 |

Hierarchy of algebraic operations | p. 18 |

Exponents and logarithms | p. 18 |

Variables, constants, and parameters | p. 19 |

Significant figures | p. 20 |

Units and their manipulation | p. 21 |

Slopes, rates, and derivatives | p. 21 |

Time expressions | p. 24 |

Construction of pharmacokinetic sketches (profiles) | p. 25 |

Intravenous bolus administration (one-compartment model) | p. 29 |

Introduction | p. 29 |

Useful pharmacokinetic parameters | p. 30 |

The apparent volume of distribution (V) | p. 32 |

The elimination half life (t_{1/2}) | p. 36 |

The elimination rate constant (K or K_{el}) | p. 38 |

Plotting drug concentration versus time | p. 40 |

Intravenous bolus administration of drugs: summary | p. 41 |

Intravenous bolus administration: monitoring drug in urine | p. 42 |

Use of urinary excretion data | p. 43 |

Clearance concepts | p. 55 |

Introduction | p. 55 |

Clearance definitions | p. 56 |

Clearance: rate and concentration | p. 58 |

Clearance: tank and faucet analogy | p. 58 |

Organ clearance | p. 60 |

Physiological approach to clearance | p. 61 |

Estimation of systemic clearance | p. 65 |

Calculating renal clearance (Cl_{r}) and metabolic clearance (cl_{m}) | p. 66 |

Determination of the area under the plasma concentration versus time curve: application of the trapezoidal rule | p. 67 |

Elimination mechanism | p. 69 |

Use of creatinine clearance to determine renal function | p. 69 |

Recently developed equations for estimating creatinine clearance and glomerular filtration rate | p. 76 |

Problem set 1 | p. 79 |

Drug absorption from the gastrointestinal tract | p. 95 |

Gastrointestinal tract | p. 95 |

Mechanism of drug absorption | p. 98 |

Factors affecting passive drug absorption | p. 100 |

pH-partition theory of drug absorption | p. 101 |

Extravascular routes of drug administration | p. 105 |

Introduction | p. 106 |

Drug remaining to be absorbed, or drug remaining at the site of administration | p. 106 |

Determination of elimination half life (t_{1/2}) and elimination rate constant (K or K_{el}) | p. 109 |

Absorption rate constant (K_{a}) | p. 110 |

Wagner-Nelson method (one-compartment model) and Loo-Riegelman method (two-compartment model) | p. 111 |

Lag time (t_{0}) | p. 115 |

Some important comments on the absorption rate constant | p. 116 |

The apparent volume of distribution (V) | p. 116 |

Time of maximum drug concentration, peak time (t_{max}) | p. 117 |

Maximum (peak) plasma concentration (C_{p})_{max} | p. 118 |

Some general comments | p. 120 |

Example for extravascular route of drug administration | p. 121 |

Flip-flop kinetics | p. 126 |

Problem set 2 | p. 127 |

Bioavailability/bioequivalence | p. 137 |

Introduction | p. 138 |

Important definitions | p. 138 |

Types of bioavailability | p. 139 |

Bioequivalence | p. 141 |

Factors affecting bioavailability | p. 141 |

The first-pass effect (presystemic clearance) | p. 142 |

Determination of the area under the plasma concentration-time curve and the cumulative amount of drug eliminated in urine | p. 143 |

Methods and criteria for bioavailability testing | p. 145 |

Characterizing drug absorption from plasma concentration versus time and from urinary data following the administration of a drug via different extravascular routes and/or dosage forms | p. 155 |

Equivalency terms | p. 157 |

Food and Drug Administration codes | p. 157 |

Fallacies on bioequivalence | p. 158 |

Evidence of generic bioinequivalence or of therapeutic inequivalence for certain formulations approved by the FDA | p. 159 |

Problem set 3 | p. 161 |

Factors affecting drug absorption: Physicochemical factors | p. 175 |

Dissolution rate | p. 175 |

Dissolution process | p. 175 |

Noyes-Whitney equation and drug dissolution | p. 176 |

Factors affecting the dissolution rate | p. 177 |

Gastrointestinal absorption: Role of the dosage form | p. 187 |

Introduction | p. 187 |

Solution (elixir, syrup, and solution) as a dosage form | p. 188 |

Suspension as a dosage form | p. 188 |

Capsule as a dosage form | p. 189 |

Tablet as a dosage form | p. 189 |

Dissolution methods | p. 191 |

Formulation and processing factors | p. 191 |

Correlation of in vivo data with in vitro dissolution data | p. 194 |

Continuous intravenous infusion (one-compartment model) | p. 203 |

Introduction | p. 203 |

Monitoring drug in the body or blood (plasma/serum) | p. 205 |

Sampling drug in body or blood during infusion | p. 205 |

Sampling blood following cessation of infusion | p. 220 |

Use of post-infusion plasma concentration data to obtain half life, elimination rate constant and the apparent volume of distribution | p. 222 |

Rowland and Tozer method | p. 225 |

Problem set 4 | p. 227 |

Multiple dosing: Intravenous bolus administration | p. 237 |

Introduction | p. 237 |

Useful pharmacokinetic parameters in multiple dosing | p. 241 |

Designing or establishing the dosage regimen for a drug | p. 248 |

Concept of drug accumulation in the body (R) | p. 249 |

Determination of fluctuation (¿): intravenous bolus administration | p. 251 |

Number of doses required to reach a fraction of the steady-state condition | p. 254 |

Calculation of loading and maintenance doses | p. 254 |

Maximum and minimum drug concentration at steady state | p. 255 |

Multiple dosing: extravascular routes of drug administration | p. 257 |

Introduction | p. 257 |

The peak time in multiple dosing to steady state (t′_{max}) | p. 259 |

Maximum plasma concentration at steady state | p. 260 |

Minimum plasma concentration at steady state | p. 261 |

"Average" plasma concentration at steady state: extravascular route | p. 262 |

Determination of drug accumulation: extravascular route | p. 263 |

Calculation of fluctuation factor (¿) for multiple extravascular dosing | p. 264 |

Number of doses required to reach a fraction of steady state: extravascular route | p. 264 |

Determination of loading and maintenance dose: extravascular route | p. 265 |

Interconversion between loading, maintenance, oral, and intravenous bolus doses | p. 266 |

Problem set 5 | p. 271 |

Two-compartment model | p. 285 |

Introduction | p. 285 |

Intravenous bolus administration: two-compartment model | p. 287 |

Determination of the post-distribution rate constant (ß) and the coefficient B | p. 292 |

Determination of the distribution rate constant (¿) and the coefficient A | p. 292 |

Determination of micro rate constants: the inter-compartmental rate constants (K_{21} and K_{12}) and the pure elimination rate constant (K_{10}) | p. 295 |

Determination of volumes of distribution (V) | p. 296 |

How to obtain the area under the plasma concentration-time curve from time zero to time t and time ∞ | p. 298 |

General comments | p. 299 |

Example | p. 300 |

Further calculations to perform and determine the answers | p. 302 |

Extravascular dosing of a two-compartment model drug | p. 303 |

Problem set 6 | p. 305 |

Multiple intermittent infusions | p. 309 |

Introduction | p. 309 |

Drug concentration guidelines | p. 311 |

Example: determination of a multiple intermittent infusion dosing regimen for an aminoglycoside antibiotic | p. 311 |

Does to the patient from a multiple intermittent infusion | p. 313 |

Multiple intermittent infusion of a two-compartment drug: vancomycin "peak" at 1 hour post infustion | p. 313 |

Vancomycin dosing regimen problem | p. 314 |

Adjustment for early or late drug concentrations | p. 315 |

Problem set 7 | p. 319 |

Nonlinear pharmacokinetics | p. 323 |

Introduction | p. 323 |

Capacity-limited metabolism | p. 325 |

Estimation of Michaelis-Menten parameters (V_{max} and K_{m}) | p. 327 |

Relationship between the area under the plasma concentration versus time curve and the administered dose | p. 330 |

Time to reach a given fraction of steady state | p. 332 |

Example: calculation of parameters for phenytoin | p. 333 |

Problem set 8 | p. 337 |

Drug interactions | p. 341 |

Introduction | p. 341 |

The effect of protein-binding interactions | p. 342 |

The effect of tissue-binding interactions | p. 348 |

Cytochrome P450-based drug interactions | p. 349 |

Drug interactions linked to transporters | p. 355 |

Problem set 9 | p. 357 |

Pharmacokinetic and pharmacodynamic relationships | p. 359 |

Introduction | p. 359 |

Generation of a pharmacokinetic- pharmacodynamic (PKPD) equation | p. 361 |

Pharmacokinetic and pharmacodynamic drug interactions | p. 364 |

Problem set 10 | p. 367 |

Metabolite pharmacokinetics | p. 369 |

Introduction | p. 369 |

General model | p. 370 |

Single intravenous bolus of drug conforming to a one-compartment model | p. 370 |

Single oral dose of drug conforming to a one-compartment model | p. 382 |

Intravenous infusion of a one-compartment model parent drug | p. 384 |

Chronic dosing to steady state | p. 385 |

Study design required to obtain various metabolite pharmacokinetic parameters | p. 388 |

Computer-aided simulation and fitting of metabolite pharmacokinetic data | p. 388 |

Case in point: meperidine and normeperidine | p. 388 |

Active metabolites in renal dysfunction | p. 388 |

Sample metabolite pharmacokinetics calculations | p. 393 |

Pharmacokinetic data fitting | p. 395 |

Introduction | p. 395 |

Pharmacokinetic parameter determination | p. 395 |

Nonlinear regression | p. 397 |

Goodness of fit indices | p. 398 |

Ways to improve fit | p. 401 |

Evaluation of program output | p. 401 |

How are the values of the parameters determined? | p. 404 |

Problems that may occur during a nonlinear regression run | p. 407 |

Weighting of data points | p. 408 |

Simulation | p. 409 |

Initial estimates | p. 411 |

Conclusion | p. 412 |

Pharmacokinetics and pharmacodynamics of biotechnology drugs | p. 413 |

Introduction | p. 413 |

Proteins and peptides | p. 413 |

Monoclonal antibodies | p. 419 |

Oligonucleotides | p. 423 |

Vaccines (immunotherapy) | p. 424 |

Gene therapies | p. 425 |

p. 427 | |

Introduction | p. 427 |

Statistical moment theory | p. 428 |

Applications | p. 439 |

Glossary | p. 443 |

References | p. 453 |

Index | p. 461 |

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