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One compartment open model i.v bolus administration - handwritten study notes (BKBP), Study notes of Biopharmaceutics and Pharmacokinetics

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

Typology: Study notes

2023/2024

Available from 07/05/2024

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bg1
ONE
COMPARTMENT
OPEN
MODEL
TNTRAvENOUS
BOLUS
ADMI
NIS
TRATION.
"
when
a
drug
that
distibues
raptdly
n
the
body
ts
qiven
n
the
qonm
o7
a
raptd
mtraeno
us
hection
(i-e
v
bolus
or
slug),
?t
takes
about
one
to
three
mfhutes
tor
complete
Crulation
and
theekore
te
the
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
present
ation
equation
dt
be
output
(eltrrtnation).
Snce,
RaBe
in
oY
absorption
o
absent,
the
be
comnes;
-
Rate
(tn)-
Rate
(out)
)
-Rate
ot
Metabolism
Ecreton
-(2)
Tate
of
absor
pion
is
negdeckd
&n
caleulations
.
pf3
pf4
pf5
pf8

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ONE COMPARTMENT OPEN MODEL

TNTRAvENOUS BOLUS ADMI NIS TRATION.

" when a drug that distibues raptdly nthe body

ts qiven n the qonm o7 a raptd mtraeno us hection

(i-e v bolus or slug), ?t takes about one to three

mfhutes tor complete Crulation and theekore te the

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

equation

dt

be

output

(eltrrtnation).

Snce, RaBe in oY absorption o absent, the

be comnes;

  • Rate^ (tn)-^ Rate^ (out)^ )

-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

X =^ Amount^ ob^ druq^ tn^ body^ at^ any^ time^ t

umaning to^ be^ eltminated.

've' Sian ndicas^ tha^ the^ dYug^ é^ befng^ Aost^ trom

ESTIMAT 1ON OF PHARMPCOKINErLC PARAMETER

Elontn ation^ Rate^ Conatunt^ (KE^ )

2 Elenfnaton^ Half^ 137e^ (ty).

3 Appar^ ent^ rolure^ o^ distrtbution^

(va)

4t clearane (ci).

1. Elfninate^ Rate^ Constant^ (Ke)

Inteqrotion o Equation (3)yield. , H).

whne Co (^) plasma (^) drug (^) cone (^) fromediately affer

I.V ?nieion

. 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

1Om he^ slope^ of^ the^ g^ line

LoqConcertrotion-s

d

" 14 hus units o min

Log 1

y- (^) întercept log (^) Co

Slope

Time

  • Ke

2.303 (ty-t)

EL?nfnation Halk Lefe (ty)

Also (aled os Biologit al Haly Lite

s the time taken oT the amOunt

oh druq in the body cs well as plasma Con entaian

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)

  1. (^) Appayent (^) volume of (^) Distribuon (va).

VA is (^) the (^) measure o (^) the (^) extnt ok (^) distibution ok drug and us enpressed fn I?tres.

on

Anount o drug n body

plagma dry concentecton

X C.

b} Hepatie^ cleavan^ ce^ i

X (^) : Vd

Rate oh^ elinsnotion^ by^ 1fver (oncentation

kmX

ct Orqan cleaYance

C

Rate o elinnation by orqan =

Clerqan

whne

Rate o pesertation to orqan

Rate o^ elininatio^ n^ Cn^ Cout

  • (Cn - Cout)

Rat h exit

trom the oggan.

ER = (Ctn - Cautcn

-(a4)

Eivsion of above equaton by concentraton of

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

  • drugs with^ High^ ER

dru qs^ wi^ th^ Low

Can be (^) classtfied tnto (^3) qro (^) upsi

drens with^ ntermed+ate^ ER^ (betwten^ o,4^ -^ 0.3)

ER (below a3)

an todx

(above .4)

an fndux^ of^ houw^ Hienty^ the^ elminaing tt o drg

ER.

orqan clea1s the bloocd fluingyouwing tthroughit