Pharmacokinetics
 Pharmaco-drug
 Kinetics-movement
 It is the branch of pharmacologyconcerned with the
movement of drug in the bodyor study about [ADME]
 Basicallyit is what drug does to the body.
 It involve four process;
a] Absorption
b] Distribution
c] Metabolism
d] Excretion
Absorption
❑ It is defined as the movement of drug molecules
from its site of administration to the systematic
circulation .
❑ it is first and important step of pharmacokinetics
❑ When we take any drug through oral route, it goes
into stomach in which it get disintegrate and
dissolution take place then drug reach into intestine.
❑Now , after dissolution drug absorb into blood from
intestine /stomach through membrane.
Membrane
❖ It is a biological membrane which is made up with
phospholipids and cholesterol and other groups
❖ It act as a semi permeable membrane..
❑Now, drug reaches into systematic circulation through
membrane transport
Which are following
1] Passive Transport
2] Active Transport
3] Facilitated Transport
4] Endocytosis
 Concentration gradient: when any drug/substance move
from high concentration to lower concentration.
1] passive transport
 Also known as passive diffusion
 In this transport ,drug/substance move across the cocentration
[high to low]
 Most of the drug are absorb by active diffusion
2] facilitated transport
 In this transport drug molecules move across the
concentration gradient ,but with the help of any carrier
bodies.
 Some large molecules or poorly diffusible substance
does not pass through passive transport , so they
required help of any carrier body to cross the
membrane
 Carrier such as SLS[solute carrier transporter]
3] active transport
 In this transport , drug molecules move against the
concentration gradient[low to high]
 It required energy due to movement of drugs against
the concentration gradient
 ATP is used.
4] Endocytosis
 In this transport , drugs of very large size get transport
via engulfment by cell membrane
 Due to large size ,they do not cross membrane and also
not fit in any channel
Factors affecting absorption
Physiochemical properties
1] ParticleSize [Drug Molecules]
2] Formulation[dosageForm]
3] ionisation
4] Ph
5] Lipid SolubilityAnd Concentration
biologicalfactor
1]surface Area
2]membrane Transport
3]gastric Emptying Time
4]blood Flow[circulation]
5]food
Routeof administration [ bioavailabilityand first pass metabolism]
1]physiochemical Properties
 1] particle size: it is inverslly proportional tothe absorption.
 particlesize
 Thesmallerthe particlesize ,thegreaterwill be itsabsorptionbecause
small size drug particles dissolveeasily.
 2] formulation: in solid,liquid,parental[injection]
 Parental.>liquiddosageform ……..>solid
 3] ionisation : we all know that ,both form [ionised+unionised]are
importantfor pharmacological responseof drugs ,but for absorption
drug must be in unionizedform.
 4] ph: it tell about natureof drug[acidic/basic]
 Acidic drug must absorbed in stomach EG.ASPIRIN
 Basic drug must absorbed in intestineEG. MORPHINE
 5] lipid solubility : lipophilicnature’sdrug has slightlyhigher
absorptionthan hydrophilic, because in membrane transportlipid
solubledrug cross membraneeasily
 6] concentration : we know thatpassivediffusion follow concentration
gradient,so highertheconcentrationof drugs thegreaterwill its
absorption.
3] Route Of Administration
 This affect drug absorption,because each route has its own
characteristics.
 Route of absorption affect bioavailibility of drug
 Bioavailibility:it is the actual amount of drug ,which
reach into the systematic circulation.
 Parental route has max.bioavaibility [drug absorb maximum]
 In intravenous ,drug directly release into blood ,so their absorption
and bioavalibily is 100 %.
 in subcutaneous /intramuscular ,drug injected near the capillaries
also have great absorption and bioavailibility.
 Enternal [oral] has less bioavailibility and absorption ,because it
follow first past metabolism drug passes through liver which
decrease the absorotion
2] BIOLOGICAL FACTORS
 1] surface area : area of absorbing surface .itsis directlyproportional
to the absorption.so, thelargerthe surface area for absorbing drug,the
greaterwill be itsabsorption.
 2]membrane transport:mostof thedrug absorb throughpassive
diffusion because it does not requireenergyor anything .and also
followconcentrationgradient.
 3]Gastric emtying time : thosedrug whosegastricemptying time is
more[fast] theirrateof absorptionis high .but time is nottoo fast
,otherwisedrug is excrete withoutabsorption . So it isat optimum time.
 4] blood flow circulation: directlyproportional the more blood flow
in body ,thegreaterwill be absorptionof drug.
 5]food : it will also affect theabsorptionof drug . If the food is present
insidethestomach ,then it dilutethedrug and absorption will be
decreases .so, take medicineaftersome timeof meal.
Absorption and Factors Affecting Absorption (1).pdf
Absorption and Factors Affecting Absorption (1).pdf

Absorption and Factors Affecting Absorption (1).pdf

  • 2.
    Pharmacokinetics  Pharmaco-drug  Kinetics-movement It is the branch of pharmacologyconcerned with the movement of drug in the bodyor study about [ADME]  Basicallyit is what drug does to the body.  It involve four process; a] Absorption b] Distribution c] Metabolism d] Excretion
  • 3.
    Absorption ❑ It isdefined as the movement of drug molecules from its site of administration to the systematic circulation . ❑ it is first and important step of pharmacokinetics ❑ When we take any drug through oral route, it goes into stomach in which it get disintegrate and dissolution take place then drug reach into intestine. ❑Now , after dissolution drug absorb into blood from intestine /stomach through membrane.
  • 4.
    Membrane ❖ It isa biological membrane which is made up with phospholipids and cholesterol and other groups ❖ It act as a semi permeable membrane.. ❑Now, drug reaches into systematic circulation through membrane transport Which are following 1] Passive Transport 2] Active Transport 3] Facilitated Transport 4] Endocytosis  Concentration gradient: when any drug/substance move from high concentration to lower concentration.
  • 5.
    1] passive transport Also known as passive diffusion  In this transport ,drug/substance move across the cocentration [high to low]  Most of the drug are absorb by active diffusion
  • 6.
    2] facilitated transport In this transport drug molecules move across the concentration gradient ,but with the help of any carrier bodies.  Some large molecules or poorly diffusible substance does not pass through passive transport , so they required help of any carrier body to cross the membrane  Carrier such as SLS[solute carrier transporter]
  • 7.
    3] active transport In this transport , drug molecules move against the concentration gradient[low to high]  It required energy due to movement of drugs against the concentration gradient  ATP is used.
  • 8.
    4] Endocytosis  Inthis transport , drugs of very large size get transport via engulfment by cell membrane  Due to large size ,they do not cross membrane and also not fit in any channel
  • 9.
    Factors affecting absorption Physiochemicalproperties 1] ParticleSize [Drug Molecules] 2] Formulation[dosageForm] 3] ionisation 4] Ph 5] Lipid SolubilityAnd Concentration biologicalfactor 1]surface Area 2]membrane Transport 3]gastric Emptying Time 4]blood Flow[circulation] 5]food Routeof administration [ bioavailabilityand first pass metabolism]
  • 10.
    1]physiochemical Properties  1]particle size: it is inverslly proportional tothe absorption.  particlesize  Thesmallerthe particlesize ,thegreaterwill be itsabsorptionbecause small size drug particles dissolveeasily.  2] formulation: in solid,liquid,parental[injection]  Parental.>liquiddosageform ……..>solid  3] ionisation : we all know that ,both form [ionised+unionised]are importantfor pharmacological responseof drugs ,but for absorption drug must be in unionizedform.  4] ph: it tell about natureof drug[acidic/basic]  Acidic drug must absorbed in stomach EG.ASPIRIN  Basic drug must absorbed in intestineEG. MORPHINE  5] lipid solubility : lipophilicnature’sdrug has slightlyhigher absorptionthan hydrophilic, because in membrane transportlipid solubledrug cross membraneeasily  6] concentration : we know thatpassivediffusion follow concentration gradient,so highertheconcentrationof drugs thegreaterwill its absorption.
  • 11.
    3] Route OfAdministration  This affect drug absorption,because each route has its own characteristics.  Route of absorption affect bioavailibility of drug  Bioavailibility:it is the actual amount of drug ,which reach into the systematic circulation.  Parental route has max.bioavaibility [drug absorb maximum]  In intravenous ,drug directly release into blood ,so their absorption and bioavalibily is 100 %.  in subcutaneous /intramuscular ,drug injected near the capillaries also have great absorption and bioavailibility.  Enternal [oral] has less bioavailibility and absorption ,because it follow first past metabolism drug passes through liver which decrease the absorotion
  • 13.
    2] BIOLOGICAL FACTORS 1] surface area : area of absorbing surface .itsis directlyproportional to the absorption.so, thelargerthe surface area for absorbing drug,the greaterwill be itsabsorption.  2]membrane transport:mostof thedrug absorb throughpassive diffusion because it does not requireenergyor anything .and also followconcentrationgradient.  3]Gastric emtying time : thosedrug whosegastricemptying time is more[fast] theirrateof absorptionis high .but time is nottoo fast ,otherwisedrug is excrete withoutabsorption . So it isat optimum time.  4] blood flow circulation: directlyproportional the more blood flow in body ,thegreaterwill be absorptionof drug.  5]food : it will also affect theabsorptionof drug . If the food is present insidethestomach ,then it dilutethedrug and absorption will be decreases .so, take medicineaftersome timeof meal.