This document discusses biopharmaceutics and the barriers and mechanisms of drug transport. It begins with an introduction to biopharmaceutics and the factors that influence bioavailability of drugs. It then describes the barriers to drug transport, including cell membranes and epithelia. Finally, it outlines the main mechanisms of drug transport across membranes, including passive diffusion, carrier-mediated transport, endocytosis, and para-cellular transport.
This power point is dedicated to deliver history of transfusion, its biology, Procedures for safe transfusion, Indications ,complications and their management.
This power point is dedicated to deliver history of transfusion, its biology, Procedures for safe transfusion, Indications ,complications and their management.
Overview of movement of drug molecules across cell membrane.pptxAwais irshad
After completion of the lecture, students will be able to:
Describe and distinguish passive diffusion and transporter-mediated passage
Distinguish transcellular and paracellular transport
Identify membrane and drug factors that control diffusion
Distinguish uptake and efflux transporters
Understand how transporters affect pharmacokinetics
PHARMACOKINETIC- ABSORPTION, DISTRIBUTION (1) [Autosaved].pptxShaikh Abusufyan
At the end of this presentation you will able to
1. Know the processes involved in ADME of drugs
2. Explain how these processes may affect the action of xenobiotics
3. Discuss how these processes can affect the outcome of the treatment of patients with drugs
4. Describe how differences in these processes between patients can affect therapy
5. Explain the use of this processes to improve therapy
Dear all,
May Peace Be Upon You!
I am happy to share lecture series on different topics of Pharmacology experiments, Pharmacy
practice, Clinical pharmacy and Pharmacology. Wish you all happy learning.
For 30+ video lecture series on Pharmacology Experiment as per PCI B Pharm
Syllabus refer link given below:
https://www.youtube.com/playlist?list=PLBVbJ9HCa1Ba6WSJjeBaK0HMF79hdad3g
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For 5+ video lecture series on Drug discovery refer link given below:
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For 26+ video lecture series on Drugs act on central nervous system refer link given
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Biopharmaceutics: Mechanisms of Drug AbsorptionSURYAKANTVERMA2
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.
Health Care Essay Topics. Personal Health Care Essaydavih0fytav3
Essay on the Importance of Health Social Group Public Health. Impressive Health Care Essay Thatsnotus. Essay on Health Education Health Education Essay for Students and .... Health Essay Sample Telegraph. HEALTH CARE SYSTEM ESSAY EXAMPLE Nexthanpa1963 Blog. Sample On Psychology for Health and Social care By Instant Essay Writ. Argumentative essay about universal healthcare. Universal Health Care Essay - Docsity. Health And Wellness Essay Paper Moreover, There Is Nothing More .... argumentative essay about universal healthcare. Public Health Essay Public Health Preventive Healthcare. Personal Health Care Essay. health essays. Health care essay. Importance of Health Essay In English The Importance of Good Health .... The Health of the Peop
Parameters to be Considered in A Bioequivalence Study of Drugharshalshelke4
Bioequivalence is a word used to describe the biological equivalency of two proprietary medication preparations. When two medications are bioequivalent, it indicates they are expected to be the same. Pharmacokinetic studies are used to determine bioequivalence between two medications, such as a reference drug (FDA approved drug) and a potential test drug (marketed generic drug), by administering each drug to volunteers in a cross-over research (healthy individuals). To prepare a drug many aspects need to take into consideration such as in vivo and in vitro study, pharmacokinetics, pharmacodynamics and bioavailability of the drug. While designing a drug fasting, oral, crossover study of the drug needs to perform.
Overview of movement of drug molecules across cell membrane.pptxAwais irshad
After completion of the lecture, students will be able to:
Describe and distinguish passive diffusion and transporter-mediated passage
Distinguish transcellular and paracellular transport
Identify membrane and drug factors that control diffusion
Distinguish uptake and efflux transporters
Understand how transporters affect pharmacokinetics
PHARMACOKINETIC- ABSORPTION, DISTRIBUTION (1) [Autosaved].pptxShaikh Abusufyan
At the end of this presentation you will able to
1. Know the processes involved in ADME of drugs
2. Explain how these processes may affect the action of xenobiotics
3. Discuss how these processes can affect the outcome of the treatment of patients with drugs
4. Describe how differences in these processes between patients can affect therapy
5. Explain the use of this processes to improve therapy
Dear all,
May Peace Be Upon You!
I am happy to share lecture series on different topics of Pharmacology experiments, Pharmacy
practice, Clinical pharmacy and Pharmacology. Wish you all happy learning.
For 30+ video lecture series on Pharmacology Experiment as per PCI B Pharm
Syllabus refer link given below:
https://www.youtube.com/playlist?list=PLBVbJ9HCa1Ba6WSJjeBaK0HMF79hdad3g
For 2+ video lecture series on Pharmacoeconomics refer link given below:
https://www.youtube.com/playlist?list=PLBVbJ9HCa1BY8U1TnlcHttsRB8hwpoJRL
For 5+ video lecture series on Pharmacoepidemiology refer link given below:
https://www.youtube.com/playlist?list=PLBVbJ9HCa1BbqIaLoMmuF0Bf66SMFZtnb
For 5+ video lecture series on Drug discovery refer link given below:
https://www.youtube.com/playlist?list=PLBVbJ9HCa1Bbn9IE6c4MagVHZMNNinJov
For 5+ video lecture series on Drugs used in Special population use link given below:
https://www.youtube.com/playlist?list=PLBVbJ9HCa1BZAed7zkXxyrgomJx2sSwHR
For 5+ video lecture series on Adverse Drug Reaction use link given below:
https://www.youtube.com/playlist?list=PLBVbJ9HCa1BbWpd06N6RcV2q0K3JT29Wv
For 2+ video lecture series on Therapeutic drug monitoring refer link given below:
https://www.youtube.com/playlist?list=PLBVbJ9HCa1BZQtOerZuDjx4yo0eOeTHIy
For 26+ video lecture series on Drugs act on central nervous system refer link given
below:
https://www.youtube.com/playlist?list=PLBVbJ9HCa1BY9xHaplYCYG26ALtIQp5aC
For 6+ video lecture series on drugs act on Gastrointestinal tract refer link given below:
https://www.youtube.com/playlist?list=PLBVbJ9HCa1BYgHRHwuarKTt96bu_2L5WK
To support this channel you can through UPI ID: abushaikh07-
yahoo.com@okhdfcbank
For More Such Learning You Can Subscribe to My YouTube Channel:
https://www.youtube.com/channel/UC5o-
WkzmDJaF7udyAP2jtgw/featured?sub_confirmation=1
Facebook Page: https://www.facebook.com/asacademylearningforever
Website Blog: https://itasacademy.blogspot.com/
Biopharmaceutics: Mechanisms of Drug AbsorptionSURYAKANTVERMA2
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.
Health Care Essay Topics. Personal Health Care Essaydavih0fytav3
Essay on the Importance of Health Social Group Public Health. Impressive Health Care Essay Thatsnotus. Essay on Health Education Health Education Essay for Students and .... Health Essay Sample Telegraph. HEALTH CARE SYSTEM ESSAY EXAMPLE Nexthanpa1963 Blog. Sample On Psychology for Health and Social care By Instant Essay Writ. Argumentative essay about universal healthcare. Universal Health Care Essay - Docsity. Health And Wellness Essay Paper Moreover, There Is Nothing More .... argumentative essay about universal healthcare. Public Health Essay Public Health Preventive Healthcare. Personal Health Care Essay. health essays. Health care essay. Importance of Health Essay In English The Importance of Good Health .... The Health of the Peop
Parameters to be Considered in A Bioequivalence Study of Drugharshalshelke4
Bioequivalence is a word used to describe the biological equivalency of two proprietary medication preparations. When two medications are bioequivalent, it indicates they are expected to be the same. Pharmacokinetic studies are used to determine bioequivalence between two medications, such as a reference drug (FDA approved drug) and a potential test drug (marketed generic drug), by administering each drug to volunteers in a cross-over research (healthy individuals). To prepare a drug many aspects need to take into consideration such as in vivo and in vitro study, pharmacokinetics, pharmacodynamics and bioavailability of the drug. While designing a drug fasting, oral, crossover study of the drug needs to perform.
A Strategic Approach: GenAI in EducationPeter Windle
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it describes the bony anatomy including the femoral head , acetabulum, labrum . also discusses the capsule , ligaments . muscle that act on the hip joint and the range of motion are outlined. factors affecting hip joint stability and weight transmission through the joint are summarized.
Delivering Micro-Credentials in Technical and Vocational Education and TrainingAG2 Design
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3. Introduction
3
Biopharmaceutics
a branch of pharmaceutical sciences that concerns the
interrelationship b/n
the physicochemical properties of a drug
the dosage form in which the drug is given
the route of administration
on the rate and extent of systemic drug absorption
8/11/2020
By: Sintayehu A
4. Introduction…
For a drug to be effective,
enough amount needs to reach its site(s) of action
stay at site(s) of action long enough
This depends upon;
the route of administration
the form in which it is administered
the rate at which it is delivered
8/11/2020
By: Sintayehu A
4
6. Introduction…
8/11/2020
By: Sintayehu A
6
In intravenous route,
a drug is introduced directly into the bloodstream
complete (100%) systemic drug availability
All other routes of administration involve the
absorption of the drug into the blood from the ROA
does not guarantee that the whole dose will reach
systemic circulation intact
7. Introduction…
By: Sintayehu A
7
Fig.: Drug ADME
Drug at site of
administration
(extravascular)
DISTRIBUTION
A
B
S
O
R
P
T
I
O
N
IV injection E
L
I
M
I
N
A
T
I
O
N
Unchanged
drug
excreted
Drug in tissues (including blood
cells) & other fluid of distribution
Bound drug unbound drug
Clinical effect
Metabolites excreted
DISTRIBUTION
Drug at site (s) of
action
metabolism
8/11/2020
8. Introduction…
The relative amount of drug that reaches the systemic
circulation intact and the rate at which this occurs is
known as bioavailability
Bioavailability is therefore defined as the rate and extent
of drug absorption
8/11/2020
By: Sintayehu A
8
9. Introduction…
9
it is often difficult to access the drug at its site(s) of
action
its concentration in the plasma is often taken as a
surrogate for its concentration at its site(s) of action
Unbound drug in the plasma would give a better
estimate of the concentration of the drug at its site(s)
of action
8/11/2020
By: Sintayehu A
10. Introduction…
For extravascularly administered drug to be 100%
bioavailable,
completely released from DF
fully dissolved in body fluids
stable in solution in body fluids
pass through physiologic barriers into surrounding
circulation without metabolism
reach into systemic circulation intact
8/11/2020
By: Sintayehu A
10
11. Introduction…
Whenever a drug is administered by any non-vascular
route, rapid and complete absorption into bloodstream is
sought:
there is relationship between drug concentration in body and
magnitude of therapeutic response
the greater concentration achieved, the greater magnitude
of response
it is desired to obtain these concentrations rapidly
8/11/2020
By: Sintayehu A
11
12. Introduction…
The concentration of the drug in blood plasma
depends on numerous factors
These include,
the amount of an administered dose that is absorbed and
reaches the systemic circulation;
the extent of distribution of the drug b/n the systemic
circulation and other tissues and fluids;
the rate of elimination of the drug from the body
8/11/2020
By: Sintayehu A
12
13. Introduction…
The study and characterization of the time course of
drug ADME is termed pharmacokinetics
8/11/2020
By: Sintayehu A
13
14. Introduction…
Physicochemical properties
of drug
Type of Dosage form
Dose and frequency of
administration
Route of administration
Site(s) of absorption
Food
Disease state
Co-administration
Age of patient
Others
Bioavailability of drug may be influenced by many factors
8/11/2020
14
By: Sintayehu A
15. Introduction…
Factors affecting BA can broadly grouped into:
Biological/Physiological factors
Physicochemical factors
Dosage form factors
8/11/2020
By: Sintayehu A
15
16. Introduction…
Emphasis is on factors influencing oral drug absorption
Oral route is most popular route of drug administration
The vast majority of drug dosage forms are designed for
oral ingestion:
Natural and convenient route
Relatively easy to manufacture
need not be sterilized, compact, produced in bulk
8/11/2020
By: Sintayehu A
16
18. Barriers to Drug Transport…
8/11/2020
By: Sintayehu A
18
The cytoplasm is held as an intact unit by a cell
membrane,
which surrounds it and prevents it from mixing with its
surroundings
allow penetration of some substances and not
others
selectively permeable
acts as a permeability barrier
19. Barriers to Drug Transport…
8/11/2020
By: Sintayehu A
19
Organs and tissues are collections of cells
surrounded by specialized cell structures called
epithelia,
which can be thought of as the organ’s ‘outer
membrane’ in an analogous fashion to the membrane
that surrounds the individual cell
Like cell membranes, epithelia are the site for a
wide range of transport, barrier and secretory
processes
20. Barriers to Drug Transport…
8/11/2020
By: Sintayehu A
20
In order for a drug to reach a site of action,
it must pass from an external site to an internal
site
pass through a number of tissues and epithelia
Overcoming these barriers to absorption is one of the
most important considerations in the drug delivery
process
21. Barriers to Drug Transport…
The barrier has the characteristics of a
semipermeable membrane,
allowing the rapid transit of some materials
impeding or preventing the passage of others
8/11/2020
By: Sintayehu A
21
22. Barriers to Drug Transport…
8/11/2020
By: Sintayehu A
22
Epithelia
With a few exceptions, all internal and external body
surfaces are covered with epithelium
This consists of a layer of structural protein, normally
collagen, called the basal lamina, on
which sit one or more layers of epithelial cells
23. Barriers to Drug Transport…
8/11/2020
By: Sintayehu A
23
Epithelia…
There are several morphologically distinct common
epithelial types
Simple squamous epithelium
Simple columnar epithelium
Transitional epithelium
Stratified squamous epithelium
24. Barriers to Drug Transport…
8/11/2020
By: Sintayehu A
24
Simple squamous epithelium
This forms a thin layer of flattened cells and
consequently is relatively permeable
This type of epithelium lines most of the blood
vessels
25. Barriers to Drug Transport…
8/11/2020
By: Sintayehu A
25
Simple columnar epithelium
A single layer of columnar cells is found in the
epithelium of organs such as the stomach and small
intestine
26. Barriers to Drug Transport…
8/11/2020
By: Sintayehu A
26
Transitional epithelium
This is composed of several layers of cells of
different shapes and it lines epithelia which are
required to stretch
27. Barriers to Drug Transport…
8/11/2020
By: Sintayehu A
27
Stratified squamous epithelium
These membranes are several cells thick and are
found in areas which have to withstand large
amounts of wear and tear, e.g. the inside of the
mouth and oesophagus and the vagina
29. Mechanisms…
There are two main mechanisms of drug transport
across the gastrointestinal epithelium:
Trans-cellular
Para-cellular
Fig. Mechanisms of absorptive
8/11/2020
By: Sintayehu A
29
30. Mechanisms…
The trans-cellular pathway is further divided into
Simple passive diffusion
Carrier-mediated transport
Endocytosis
8/11/2020
By: Sintayehu A
30
31. Mechanisms…
Trans-cellular pathways
Passive diffusion:
transport for relatively small lipophilic molecules
many drugs transported via this route
drug molecules pass across cell membrane via a region
of high concentration to a region of lower concentration
i.e. from lumen to blood
8/11/2020
By: Sintayehu A
31
32. Mechanisms…
Trans-cellular pathways…
Carrier-mediated transport:
The drug require carrier or transporter to cross
membrane
carrier-mediated transport
Two main types carrier-mediated transport
Active transport and
Facilitated diffusion
8/11/2020
By: Sintayehu A
32
33. Mechanisms…
Trans-cellular pathways…
Active transport: materials transported against a
concentration gradient
active transport is an energy consuming process
A carrier or membrane transporter is responsible for
binding a drug and transporting it across the membrane
8/11/2020
By: Sintayehu A
33
35. Mechanisms…
Trans-cellular pathways…
Facilitated diffusion:
Drugs are transported down the concentration gradient
does not require an energy
but does require a concentration gradient
8/11/2020
By: Sintayehu A
35
36. Mechanisms…
Trans-cellular pathways…
Endocytosis:
Endocytosis is the process by which the plasma membrane
of the cell invaginates and the invaginations become
pinched off, forming small intracellular membrane-bound
vesicles that enclose a volume of material
Thus material can be transported into the cell
8/11/2020
By: Sintayehu A
36
37. Mechanisms…
Trans-cellular pathways…
Endocytosis can be further subdivided into four main
processes:
pinocytosis
receptor-mediated endocytosis
phagocytosis
transcytosis
8/11/2020
By: Sintayehu A
37
38. Mechanisms…
Trans-cellular pathways…
Pinocytosis:
the engulfment of small droplets of extracellular fluid by
membrane vesicles
The cell will internalize material regardless of its metabolic
importance to that cell
The fat-soluble vitamins A, D, E and K are absorbed via
pinocytosis
8/11/2020
By: Sintayehu A
38
39. Mechanisms…
Trans-cellular pathways…
Receptor-mediated endocytosis
Many cells within the body have receptors on their cell
surfaces that are capable of binding with suitable ligands to
form ligand-receptor complexes on the cell surface
These complexes cluster on the cell surface and then
invaginate and break off from the membrane to form
coated vesicles
8/11/2020
By: Sintayehu A
39
40. Mechanisms…
Trans-cellular pathways…
Phagocytosis Phagocytosis
can be defined as the engulfment by the cell membrane
of particles larger than 500 nm.
This process is important for the absorption of polio
and other vaccines from the gastrointestinal tract
8/11/2020
By: Sintayehu A
40
41. Mechanisms…
Trans-cellular pathways…
Transcytosis
the process by which the material internalized by the
membrane domain is transported through the cell and
secreted on the opposite side
8/11/2020
By: Sintayehu A
41
42. Mechanisms…
Para-cellular pathway
transport of materials in the aqueous pores b/n the cells
transport ions such as calcium and for the transport of
sugars, amino acids and peptides at concentrations above
the capacity of their carriers
8/11/2020
By: Sintayehu A
42
43. Mechanisms…
8/11/2020
By: Sintayehu A
43
Efflux of drugs from the intestine
there are counter-transport efflux proteins that expel
specific drugs back into the lumen of the GIT after they
have been absorbed
efflux have a detrimental effect on drug BA
One of the key counter-transport proteins is P-
glycoprotein