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In addition to covering various aspects of design of dosage regimens and application of pharmacokinetic principles in clinical situations, the text contains a final chapter on Controlled Release Medication to familiarize the students with the principles involved in the design of innovative formulations. We feel that a concept is more readily appreciated and understood when illustrated by a simple figure or a table.
In order to exemplify the text, illustrations have been used liberally throughout the book. We acknowledge the contribution of hundreds of scientists who are dedicated to improvement of drug therapy.
We are also indebted to the authors of the various books and articles mentioned in bibliography which became a major source of information for writing this text. Special thanks are due to Professor W. Ritschel for his timely help and inspiration. Further, we are appreciative of the publishers who graciously volunteered to make the publication of this book a reality. Nagpur May 15, Brahmankar Sunil B. Absorption of Drugs.
Factors Affecting Protein-Drug Binding. Drug related factors. Drug interactions. Patient related factors. Kinetics of Protein— Drug Binding. Chemical Pathways of Drug Biotransforriiation. Phase 1 Reactions.
Oxidative reactions. Reductive reactions. Hydrolytic reactions. Phase II Reactions. Conjugation with glucuronic acid. Conjugation with sulfate moieties. Conjugation with alpha-amino acids. Miscellaneous conjugation reactions.
Factors Affecting Biotransformation Physicochemical properties of the. Chemical factors. Biological factors. Bioactivation and Tissue Toxicity. Prodrugs Applications of Prodrug Design Improvement of taste.
Change of physical form of the drug. Enhancement'of bioavailability lipophilicity Prevention of presystemic metabolism Prolongation of duration of action Reduction of toxicity Siie-specific drug delivery drug targeting Limitations of Prodrug Design. Excretion of Drugs. Renal Excretion o f Drugs. Glomerular filtration.
Active tubular secretion. Tubular reabsorption. Concept of clearance. Factors affecting renal excretion. Dose adjustment in renal failure. Dialysis and hemoperfusion. Nonrenal Routes of Drug Excretion. Biliary excretion o f drugs-enterohepatic cycling. Pulmonary excretion. Salivary excretion. Pharmacokinetic Drug Interactions. Mechanisms o f Drug Interactions. Pharmacokinetics: Basic Considerations. Plasma Drug Concentration-Time profile.
Rates, Rate Constants and Orders of Reaction. Zero-Order Kinetics. First-Order Kinetics. Mixed-Order Kinetics. Pharmacokinetic Models. Compartment models. Noncompartmental analysis. Physiologic models. Compartment Modeling.
One-Compartment Open Model. Intravenous bolus administration. Intravenous infusion. Extravascular administration. Urinary Excretion Data. Multicompartment Models. Two-Compartment Open Model. Nonlinear Pharmacokinetics. Causes o f Nonlinearity. Michaelis-Menten Equation. Estimation o f Km and Vmax. Bioavailability and Bioequivalence.
Measurment o f Bioavailability. Plasma level-time studies. Urinary excretion studies. In vitro Drug Dissolution Testing Models. In vitro-in vivo Correlation. Bioequivalence Studies. Methods for Enhancement o f Bioavailability.
Applications of Pharmacokinetic Principles. Design of Dosage Regimens. Monitoring Drug Therapy. Drug Concentration and Pharmacologic Response. Therapeutic Concentration Range. Concentration-Response Relationships. Intensity o f Effect-Concentration Relationship. Controlled Release Medication. Design o f Controlled Drug Delivery Systems. Oral Controlled Release Systems. Parenteral Controlled Release Systems. Transdermal Drug Delivery Systems. Ophthalmic Drug Delivery Systems. Intravaginal and Intrauterine Drug Delivery Systems.
Bioavailability Testing o f Controlled Release Formulations. Drugs, whether obtained from plant, animal or mineral sources or synthesized chemically, are rarely administered in their pure chemical form. Earlier, it was believed that the therapeutic response to a drug is an attribute of its intrinsic pharmacologic activity. Variations are also observed when the same drug is administered as different dosage forms or similar dosage forms produced by different manufacturers, which in turn depend upon the physicochemical properties of the drug, the excipients present in the dosage form, the method of formulation and the manner of administration.
A new and separate discipline called biopharmaceutics has therefore been developed to account for all such factors that influence the therapeutic effectiveness of a drug. The process of movement of drug from its site o f administration to the systemic circulation is called as absorption. The concentration of.
BHRAMANKAR - Biopharmaceutics
If your institution subscribes to this resource, and you don't have a MyAccess Profile, please contact your library's reference desk for information on how to gain access to this resource from off-campus. Drugs are substances intended for use in the diagnosis, cure, mitigation, treatment, or prevention of disease. Drugs are given in a variety of dosage forms or drug products such as solids tablets, capsules , semisolids ointments, creams , liquids, suspensions, emulsions, etc, for systemic or local therapeutic activity. Drug products can be considered to be drug delivery systems that release and deliver drug to the site of action such that they produce the desired therapeutic effect and are also designed specifically to meet the patient's needs including palatability, convenience, and safety. Drug product performance is defined as the release of the drug substance from the drug product either for local drug action or for drug absorption into the plasma for systemic therapeutic activity. Advances in pharmaceutical technology and manufacturing have focused on developing quality drug products that are safer, more effective, and more convenient for the patient. The importance of the drug substance and the drug formulation on absorption, and in vivo distribution of the drug to the site of action, is described as a sequence of events that precede elicitation of a drug's therapeutic effect.
Biopharmaceutics and Pharmacokinetics
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