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INTRODUCTION TO BIOPHARMACEUTICS
Biopharmaceutics:
Biopharmaceutics is defined as the study of factors influencing the rate and amount of drug
that reaches the systemic circulation and the use of this information to optimise the therapeutic
efficacy of the drug products.
Absorption:
• The process of movement of drug from its site of administration to the systemic
circulation is called as absorption.
• The concentration of drug in plasma and hence the onset of action, and the intensity
and duration of response depend upon the bioavailability of drug from its dosage form.
Bioavailability:
• Bioavailability is defined as the rate and extent (amount) of drug absorption.
• Any alteration in the drugs bioavailability is reflected in its pharmacological effects.
Drug Disposition:
• Other processes that play a role in the therapeutic activity of a drug are distribution and
elimination. Together, they are known as drug disposition.
Drug Distribution:
• The movement of drug between one compartment and the other (generally) blood and
the extravascular tissues) is referred to as drug distribution.
• Since the site of action is usually located in the extravascular tissues, the onset, intensity
and sometimes duration of action depend upon the distribution behaviour of the drug.
• The magnitude (intensity) and the duration of action depend largely upon the effective
concentration and the time period for which this concentration is maintained at the site
of action which in turn depend upon the elimination processes.
Elimination:
• Elimination is defined as the process that tends to remove the drug from the body and
terminate its action.
• Elimination occurs by two processes – biotransformation (metabolism), which usually
inactivates the drug, and excretion which is responsible for the exit of drug/ metabolites
from the body.
• In order to administer drugs optimally, knowledge is needed not only of the
mechanisms of drug absorption, distribution, metabolism and excretion (ADME) but
also of the rate (kinetics) at which they occur i.e. pharmacokinetics.
Pharmacokinetics:
• Pharmacokinetics is defined as the study of time course of drug ADME and their
relationship with its therapeutic and toxic effects of the drug.
• Simply speaking, pharmacokinetics is the kinetics of ADME or KADME.
Clinical Pharmacokinetics:
• The use of pharmacokinetic principles in optimising the drug dosage to suit individual
patient needs and achieving maximum therapeutic utility is called as clinical
pharmacokinetics.
Drug administration and therapy can now be conveniently divided into four phases or
processes:
1. The Pharmaceutical phase:
It is concern with:
o Physiochemical properties of the drug
o Design and manufacture of an effective drug product for administration by a
suitable route.
2. The Pharmacokinetic phase:
It is concerned with the ADME of drugs are elicited by the plasma drug concentration
– time profile and its relationship with the dose, dosage form and frequency and route
of administration. In short, it is the sum of all the processes inflicted by the body on
drug.
3. The Pharmacodynamic phase:
It is concerned with the biochemical and physiologic effects of the drug and its
mechanism of action. It is characterized by the concentration of drug at the site of action
and its relation to the magnitude of effects observed. Thus, in comparison –
▪ Pharmacokinetics is a study of what the body does to the drug, whereas
▪ Pharmacodynamics is a study of what the drug does to the body.
▪ Pharmacokinetics relates changes in concentration of drug within the body with
time after its administration, whereas
▪ Pharmacodynamics relates response to concentration of drug in the body.
4. The Therapeutic phase:
It is concerned with the translation of pharmacological effect into clinical benefit.
The various processes involved in the therapy with a drug is given in below fig.
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INTRODUCTION TO BIOPHARMACEUTICS , pharmacokinetics, pharmacodynamics and therapeutical outcomes

  • 1. INTRODUCTION TO BIOPHARMACEUTICS Biopharmaceutics: Biopharmaceutics is defined as the study of factors influencing the rate and amount of drug that reaches the systemic circulation and the use of this information to optimise the therapeutic efficacy of the drug products. Absorption: • The process of movement of drug from its site of administration to the systemic circulation is called as absorption. • The concentration of drug in plasma and hence the onset of action, and the intensity and duration of response depend upon the bioavailability of drug from its dosage form. Bioavailability: • Bioavailability is defined as the rate and extent (amount) of drug absorption. • Any alteration in the drugs bioavailability is reflected in its pharmacological effects. Drug Disposition: • Other processes that play a role in the therapeutic activity of a drug are distribution and elimination. Together, they are known as drug disposition. Drug Distribution: • The movement of drug between one compartment and the other (generally) blood and the extravascular tissues) is referred to as drug distribution. • Since the site of action is usually located in the extravascular tissues, the onset, intensity and sometimes duration of action depend upon the distribution behaviour of the drug. • The magnitude (intensity) and the duration of action depend largely upon the effective concentration and the time period for which this concentration is maintained at the site of action which in turn depend upon the elimination processes. Elimination: • Elimination is defined as the process that tends to remove the drug from the body and terminate its action. • Elimination occurs by two processes – biotransformation (metabolism), which usually inactivates the drug, and excretion which is responsible for the exit of drug/ metabolites from the body. • In order to administer drugs optimally, knowledge is needed not only of the mechanisms of drug absorption, distribution, metabolism and excretion (ADME) but also of the rate (kinetics) at which they occur i.e. pharmacokinetics. Pharmacokinetics: • Pharmacokinetics is defined as the study of time course of drug ADME and their relationship with its therapeutic and toxic effects of the drug.
  • 2. • Simply speaking, pharmacokinetics is the kinetics of ADME or KADME. Clinical Pharmacokinetics: • The use of pharmacokinetic principles in optimising the drug dosage to suit individual patient needs and achieving maximum therapeutic utility is called as clinical pharmacokinetics. Drug administration and therapy can now be conveniently divided into four phases or processes: 1. The Pharmaceutical phase: It is concern with: o Physiochemical properties of the drug o Design and manufacture of an effective drug product for administration by a suitable route. 2. The Pharmacokinetic phase: It is concerned with the ADME of drugs are elicited by the plasma drug concentration – time profile and its relationship with the dose, dosage form and frequency and route of administration. In short, it is the sum of all the processes inflicted by the body on drug. 3. The Pharmacodynamic phase: It is concerned with the biochemical and physiologic effects of the drug and its mechanism of action. It is characterized by the concentration of drug at the site of action and its relation to the magnitude of effects observed. Thus, in comparison – ▪ Pharmacokinetics is a study of what the body does to the drug, whereas ▪ Pharmacodynamics is a study of what the drug does to the body. ▪ Pharmacokinetics relates changes in concentration of drug within the body with time after its administration, whereas ▪ Pharmacodynamics relates response to concentration of drug in the body.
  • 3. 4. The Therapeutic phase: It is concerned with the translation of pharmacological effect into clinical benefit. The various processes involved in the therapy with a drug is given in below fig.