BIOPHARMACEUTICS AND PHARMACOKINETICS

Name: Chiu, Cheryl S. Date: 09/09/2021

Section: BSPH 2-Y1-1 Score: _________________

Assignment No. 1
The LADMER System

In order to design a rational dosage regimen, a pharmacist must be familiar with the
concepts of the LADMER system (Liberation, Absorption, Distribution, Metabolism, Excretion and
Response). With the principles of this complex system on hand, one can make a suitable
treatment routine for a specific patient or group of patients with altered physiologic states.

1. Select one particular drug of interest. Illustrate a schematic diagram showing the LADMER
system that the selected drug undertakes inside the body. Specify the processes which the drug
goes through in each step of the complex LADMER system and the factors affecting these
processes. You may use product inserts and books as your reference.

IBUPROFEN
LIBERATION
ABSORPTION DISTRIBUTION
Once Ibuprofen reaches the
digestive system, particularly the After being turned into tiny After the filtration, the
stomach, after taken orally, it molecules, the drug will proceed bloodstream, together with the
will start to disintegrate after to the small intestine which has drug, will continue to go through
reacting with the acidic fluids villi that are responsible for the different organs such as the
found there. absorbing it into the heart, brain, and the kidneys.
bloodstream.

RESPONSE
EXCRETION METABOLISM
When the Ibuprofen molecules
encounter the site where pain The filtered-out metabolites and While it passes through the
response is active, they will bind the used-up Ibuprofen will be different organs, the body
to the molecules that are part of excreted by the kidneys through naturally filters the blood. For
the reaction. Ibuprofen the urinary system. instance, there are enzymes
specifically blocks the found in the liver that will try to
production of compounds that neutralize the drug and turn it
transmit pain signals. into a metabolite.

Source: How does your body process medicine? - Céline Valéry

https://www.youtube.com/watch?v=uOcpsXMJcJk
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2. What are the pharmacotechnical factors affecting drug liberation? Discuss the significance of
liberation in drug’s bioavailability.

● Drug Dissolution
● Drug Solubility
● Particle Size and Surface Area
● Partition Coefficient and Extent of Ionization
● Salt Formation
● Polymorphism
● Chirality
● Hydrates
● Complex Formation

Liberation will be the one that determines the extent and rate at which the drug will enter the
blood circulation. Since the body will try to eliminate the drug, the amount of drug or the
bioavailability of it will decrease after time passes.

Source: Introduction to Biopharmaceutics PDF

3. Give at least three (3) dosage forms in which liberation is altered?

● Capsules - consist of a white powder held in a hard gelatin shell. The gelatin shell
dissolves slowly, meaning that it can pass through the stomach to regions of higher pH
before the bulk of the drug is liberated.

● Dispersible tablets - the effervescence as carbon dioxide gas is released helps break
up
○ the tablets, releasing small particles of the drug. The smaller the particles, the
more quickly they dissolve and are absorbed.

● Injectable solutions - do not undergo liberation.

Source: Fox, S. C. (2014). Pharmaceutics. London: Pharmaceutical Press.

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4. Define the following terms:

a. Absorption
It is the process wherein the liberated drug is absorbed into the systemic circulation of
blood.

b. Bioavailability
The rate and extent to which the active ingredient or active moiety is absorbed from a drug
product and becomes available at the site of action.

c. Disposition
Description of drug distribution and elimination (fate of the drug).

d. Volume of distribution
Theoretical volume that the drug uniformly distributes to immediately after being injected
into the body.

e. Biliary recycling
Drugs are excreted via bile into the small intestine, but can be reabsorbed from the distal
intestinal lumen.

f. Excretion
Excretion of a drug is understood to be any one of a number of processes by which a drug
is eliminated from an organism either in an unaltered form or modified as a metabolite.

g. Protein binding
Affects drug activity in one of two ways: either by changing the effective concentration of
the drug at its site of action or by changing the rate at which the drug is eliminated, thus
affecting the length of time for which effective concentrations are maintained.

h. Enzyme inhibitor
A molecule that disrupts the normal reaction pathway between an enzyme and a
substrate.

i. Enzyme inducer
Type of drug that increases the metabolic activity of an enzyme either by binding to the
enzyme and activating it, or by increasing the expression of the gene coding for the
enzyme.

j. Extravascular administration
Any route other than intravenous route (intradermal, topical, oral). There is more
absorption at the site of administration and not too much drug in the systemic circulation.

k. Intravascular administration
Administering fluids from a container to a patient's vascular system through a needle or
catheter inserted into a vein.
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l. Pharmacokinetics
Science of the kinetics of drug absorption, distribution, and elimination (i.e, metabolism
and excretion).

m. Gastric emptying time

Measures the time it takes for food to empty from the stomach and enter the small
intestine.

n. Prodrug
A biologically inactive compound which can be metabolized in the body to produce a drug.

o. Pharmacodynamics
Study of the biochemical and physiological effects of drugs on the body.

p. Biopharmaceutics
Examines the interrelationship of the physical/chemical properties of the drug, the drug
product in which the drug is given, and the route of administration on the rate and extent
of systemic drug absorption.

Source:
The Free Dictionary: Medical Dictionary. (n.d.). Retrieved August 27, 2020, from https://medical-
dictionary.thefreedictionary.com/
Shargel, L., & Yu, A. B. (2016). Applied biopharmaceutics & pharmacokinetics. Singapore:
McGraw-Hill Education.