Dr.U.P.

Rathnakar
MD.DIH.PGDHM
www.scribd.com
PK is the quantitative study
of drug movement in,
through and out of the
body
During these processes the
drug has to cross various
biological membranes
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Dose






Drug in the plasma



Drug at the site of action



MOA & Effect- Adverse and Beneficial



Absorption




Distribution


Metabolism





Excretion
P
H
R
M
C
O
K
I
N
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T
I
C
S
Pharmacodynamics
PK-Membrane Transport
Mechanism by which drugs cross biological membrane
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Membrane Transport..
Passive diffusion and Filtration

Specialized transport

Carrier transport
Facilitated diffusion
Active transport

Pinocytosis
Size
Lipid solubility
Ionization
Concentration
gradient
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Passive diffusion

Bidirectional process,
Movement of molecules from higher to lower conc
[Down the gradient]
Lipid soluble drugs- Passive diffusion, after dissolving
in the lipid of cell membrane


Acidic drugs are unionized in acidic medium[better diffusion]
Alkaline drugs are unionized in alkaline Medium[better diffusion]
Unionized drugs are readily absorbed
More lipid soluble Diffuses quickly
Greater the difference in concn gradient Quicker diffusion


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Filtration
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FILTRATION
Capillaries (Except in brain-Tight
junction) have large pores & most
drugs filter through these.
Lipid insoluble drugs cross
biological membranes by
filtration through these pores
Diffusion of drugs is dependent on
Rate of Blood Flow

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Specialized transport: Carrier mediated
Drug + CARRIER in the membrane complex is
transported from one side of the membrane to other.
Eg. Calcium & iron absorption
Carrier transport
1. Specific,
2. Saturable,
3. Competitively inhibited by - which utilize the same
carrier.



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Specialized transport


I. Carrier transport

1. Facilitated diffusion
2. Active transportPrimary or Secondary


II. Pinocytosis

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Specialized transport: Carrier mediated
Facilitated diffusion

No energy required
Drug + carrier[SLC Transporter] in the membrane, diffusion
across the cell membrane.

Movement ONLY higher to lower conc [ALONG].
Eg. Vit. B12 absorption
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Specialized transport: Active transport

Movements of molecules Low conc. To high conc.
Against the conc.gradient
Require energy.
P-glycoprotein

Active transport
1. Primary
2. Secondary
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ATP ADP
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By formation of vesicles

Pinocytosis;
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Absorption
[Movement from site of administration to
circulation]

ORAL:

S.c, i.m: Absorbed by capillaries or lymphatics

Topical: Lipid solubility-Hyoscine, Fentanyl, GTN,
Nicotine, Testosterone, Estradiol

Cornea

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Absorption:Factors
Aqueous solubility, particle size
Concentration
Area of absorbing surface
Vascularity
pH and ionization
Food
Other drugs
Diseases
Route
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BA=30/150
First pass metabolism
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Bio-Availability
Absorption: Bio-Availability
The fraction [F] of administered dose of a drug that
reaches systemic circulation in the unchanged form
I.V. 100% Bio-availablity
Oral-Not 100%. WHY?
1. Incompletely absorbed
2. First pass metabolism
i.m or s.c. also may be less
than 100% -Local binding
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Pharmaceutical Equivalence
Contain the same active ingredients, identical in strength, dosage form, and
route of administration.
Eg. Tab.Metacin 500 mg and T.Crocin 500mg

Bioequivalence
Bioavailability of the active ingredient in the two products are same.
Eg. Metacin and Crocin

Therapeutic equivalence
Comparable efficacy and safety

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