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Subject :- biopharmaceutics and pharmacokinetics, b pharm 3rd year , Reference:- biopharmaceutics and pharmacokinetics - A Treatise Authors :- D.M. Brahmankar , Sunil.B.Jaiswal One compartment open model IV bolus administration Schematic representation of one compartment open model IV bolus administration, Estimation of pharmacokinetics parameters:- a) Elimination rate constant b) Elimination half life c) Apparent volume of distribution d) clearance
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ONE COMPARTMENT OPEN MODEL
TNTRAvENOUS BOLUS ADMI NIS TRATION.
(i-e v bolus or slug), ?t takes about one to three
The Model can be deprcted as fllows
Drug
Ka Input body tissues (Absovption)
to the body s dz dt
Bood othut
.The Generad Kapresson tor Rot o7 drug presentation
dt
be
output
be comnes;
-Rate ot
Metabolism Ecreton
-(2)
Tate of absor pion is negdeckd &n caleulations.
Sinst-orden
whene,
1
d
Ahe boduy.
climfnalion follo us hinefis, then i
Finst oydn^ elinfnaion^ rote^ Constont
umaning to^ be^ eltminated.
've' Sian ndicas^ tha^ the^ dYug^ é^ befng^ Aost^ trom
ESTIMAT 1ON OF PHARMPCOKINErLC PARAMETER
Elontn ation^ Rate^ Conatunt^ (KE^ )
4t clearane (ci).
Inteqrotion o Equation (3)yield. , H).
whne Co (^) plasma (^) drug (^) cone (^) fromediately affer
. Equaton(e) is that astathtShaight tne and
Gndtcates the Semi-loq dot ot loq C versus t will bt lineaY witth
. The eliifnaion Rate (onstant ds dintcdly obtahed
LoqConcertrotion-s
Log 1
y- (^) întercept log (^) Co
Time
2.303 (ty-t)
s the time taken oT the amOunt
to decdine by one - Half or 50% itt fnitia value
Halt,,l?e & aelated to eleination rate let Constont by tol louoing equalion;
ty, :^ 0.693.^ (9)
Seconday aromoter daperdert prfrnang poromakrs clearonce (cu) and aparent volume ok distrbution (vA)) O,693 Va (^) (to)
VA is (^) the (^) measure o (^) the (^) extnt ok (^) distibution ok drug and us enpressed fn I?tres.
on
X C.
b} Hepatie^ cleavan^ ce^ i
X (^) : Vd
Rate oh^ elinsnotion^ by^ 1fver (oncentation
ct Orqan cleaYance
C
whne
Rate o pesertation to orqan
Rate o^ elininatio^ n^ Cn^ Cout
Rat h exit
ER = (Ctn - Cautcn
drug that entess the orqan o elfnnation (c tn) yields an exorss ion for Cearane of drug by
Extacien Rato.
-(15)
& called as
orqan unds^ considaion.^ Thus,
Based on^ ER (^) values, (^) drugdrug
dru qs^ wi^ th^ Low
Can be (^) classtfied tnto (^3) qro (^) upsi
drens with^ ntermed+ate^ ER^ (betwten^ o,4^ -^ 0.3)
(above .4)
an fndux^ of^ houw^ Hienty^ the^ elminaing tt o drg
orqan clea1s the bloocd fluingyouwing tthroughit