Application of biopharmaceutics

A company is going to market a new dosage form of a certain drug. The dose is known.
When this dosage form is administered to a healthy human the drug may not release
quickly. In this case the action of the drug will be delayed. In another case if the drug is
released all at a time then the duration of action of the drug will be very short. So with the
knowledge of biopharmaceutics we can change various formulation factors to obtain
optimum onset of action and duration of action.

A company is marketing tablets of a certain drug. Now it wants to change a few

ingredients or some formulation factors. The new tablets may not behave similarly as the
previous one. So the bioavailability of new tablets is compared with the old tablets. If it is
found that the bioavailability of the newer tablets are equivalent (i.e bioequivalent) to
that of older tablets then the new tablets will be permitted to market (by FDA).

A company is marketing the tablets of a certain drug. Now they have planned to make
transdermal dosage form of the same drug. To establish its efficacy the bioavailability of
the transdermal dosage form is compared to that of the established tablet dosage form. If
both are found to be closer than the transdermal dosage form will be accepted by FDA.

Application of pharmacokinetics
1

The bioavailability of a dosage form is calculated by pharmacokinetic equations.

The frequency of dosing is calculated from pharmacokinetic equations.

To calculate the dose of a controlled release dosage form pharmacokinetic equations are
required.

In case of patients with kidney failure the dose of a drug should be calculated very
cautiously. If the rate of absorption of the drug is greater than the elimination rate of the
drug from that patient then the drug will be accumulated in the body and may show toxic
effect. The rate of elimination of the drug from the body of that patient is calculated with
the help of pharmacokinetic equations.

When a potent anticancer drug is administered to a patient the plasma concentration of the
drug must be very close to minimum effective concentration. Since the therapeutic index
of the drug is very narrow in case of potent drugs so rate of administration must also be
very slow. This rate of administration is calculated by pharmacokinetic principles.

SIGNIFICANCE OF PLASMA DRUG

CONCENTRATION MEASUREMENT.
N.B. Measurement of drug concentration in blood, serum, or

Whole blood
Centrifugation

plasma is the most direct method to assess the pharmacokinetics

of the drug in the body.

Sediment

Supernatant liquid

Whole blood contains cellular elements (red blood

RBC
WBC
Platelets

Plasma

corpuscles, white blood corpuscles and platelets) and various

proteins (albumin, globulin, prothrombin and fibrinogen,

Clotting
Serum

etc.).
To obtain plasma, the whole blood preserved with some anticoagulant (e.g. citrate or heparin)
is centrifuged and the supernatant liquid is collected as plasma.
To obtain serum the whole blood is allowed to clot, then centrifuged and the serum is
collected from the supernatant.

1 The intensity of pharmacologic or toxic effect of a drug is often related to the

concentration of the drug at the receptor site. Receptor sites are usually
located in the tissue cells. Most of the tissue cells are perfused with tissue
fluids or plasma. Hence, the biological effect of a drug at its receptor site
can be controlled by controlling the concentration of the drug in the blood.
2 When a drug is administered to patients the individual variation of
pharmacokinetics is common. In those cases the monitoring of the plasma
drug concentration is required for delivering potent drugs like anticancer
agents. Plasma drug concentration allows for the adjustment of the dose so
that the plasma concentration remains within maximum safe concentration.
3

In some diseases the normal physiological functions may change. In these

cases monitoring plasma drug concentration may provide a guide to the
progress of the disease state and enable the investigator to change the dose
accordingly.

4 Allows for the adjustment of the drug dosage in order to individualize &
optimize therapeutic drug regimen.
5 For drugs those bind irreversibly with the receptor site, pharmacodynamic
effect may not be accurately predicted from the plasma drug concentration.
For example, anticancer drugs interfere with nucleic acid or protein
biosynthesis to destroy tumor cells. For these drugs, the plasma drug
concentration does not relate directly to the pharmacodynamic response. In
this case other pathophysiologic parameters and side effects are monitored in
the patient to prevent adverse effect.
6 It

helps

in

substitutions.

determining

therapeutic

equivalents

&

therapeutic