solubility profile pka, pH
Dcorite about
Partition coeffient Substan ces
soldbility Anatysis of duy
Ans xPretomylation olobility GAudies focus on
(ould during
the detivery
Solven Systems that and
Profile
Solubility
a drug candidate.
of the drugs Provde
* Under st anding mechanisms
Solvbilts ation
Possible 0ork.
for fo moloti or DneSude s:
basis Anay sis
Solubility
)Pka determina tion
Pprokle
PH
3) P
SOlubi6ty
arition coefAcien
deteminationt introdu e d via a
Pka chugn e e l s to be dosage orn shoud
As -the adninistration , a
9Oute of
s e l e c t e .
are a bs o r b e r ever before
be
Most of the
effect takes place.
acid H4', DA Can
-the theropeutic
example of an acsdl
conjugate base of an
iote nto A fon-thet .
dísso called
a hydroge
* where ka is
and H+4 issoci ation tonstant
HA
(s the negative
ka [AJ Cut] pka
Jogavithm of Ka
CH4)
that
pka - og ka amount o f
function ot the orm:
ka Uni onise o
exis t
in he rDonised form
ypH = Pkat form
of ionise an d
concentrai on
ohen t e egual, PH: plea.
unionised formi becomes
of 8 s tomatch- |-3
6T has en ive sange PH
ntes tine- S-8
Profle ons.
pH solubiity
Dogavithm of *
diflference
in
in he
the negative make a
PH is can
Chan9éngthe PH, basic
acidic Cov]
-the dro9
Solubilit y of pla s PH on
Jnluence of crug
Pka
PH/Se of Absorption
abso"pion
very oeale acid >80 Unionised at a PH/
throughout GT
-[Link] sed in gas tric
PR, ionised
Moderately useat g.5 |in intestinb pH/absorption
acid
acil
Sonise at al pH/ POor
|strog oabsorption
at al pH
/absorpton
aseak
nionised
very he GlT
base
-lt:o [Donised in gastic pH,
|Moderately weak s. o PH/
unt onised in Dntestinal
base absorpti on site
Dntestine
Donisedl at ase pH/Poor absorpio
strono bas
Parttion coeffdent
Conc of cug in organic phase
Crug in
in Qgueous pase
ne- of drug
Conc-
istributon ot drygs in the body body
e tstimation -the
distribute in the hydropho bic
Hydrophobic drugs biDayers of the cels .
Such as pid
areas
Hydrophiíc drugs are founol in the hydrophilic
Such as Lloo Sesun
area
experimentay by shake flask
Determine
neth od, higk per form ance Sipuid chromato graply
)iscss the in
poly movphism of
formuation development
Dolymevpkism more -han
One
Substance exists in designated
are
orms
Crysta line form -he diffevent morphism"
phenomeon - poly
Polymorphs and te fnaniotrop ic
Polym orphs are of too ty pes -
P* polymorphs o h í c h
Polymorphs and Mon otrop hic - iS the one
Car
* Enontiotropic polymorphs onother torm by altering
into
reverstbly hanpec Pre ssure .
be bo wh ich is
he temperature the one
polymbrphs - is and pressures
Monotropic a l l to
PfUn stable temperatures
other respect
at each
differ trom Solubili
Dolymorphs ike
* properties
density ete.
physica
tueir
Point, metastable
ors oth
meltng cated
forms are
other torms
the opposite Properties calorimetry,
Determined by differen tal Seannin9
Diffraction method.
X- RaY cevtical
detail n
Bio- pharma
corite in menton it 'S
3) CBPC) and
classi fcati on
iffer en tiate
Sgnificance
is System to
Bes of gs
basis of -
-the
)solubi íty
Permeabi i ty
, )Dissolu tion
Solubility dissolved in a
ot Solute
Maximum
amount
Under standaro Conditions
Solvent
Given temperature, Dressure, pH
of
to
* solobi lity is -the abiity of the
be in Solution after dissolUton
Penmeability:
Abiity of dry to pass -he
membrane cohich is ipophiicindirectly basel on
Dermeobili ty of a drug Substane.
the extent of abSorp tion
absorption f
Jissduion Solid Substance
Ds a Process in ohich
Solvent.
Solubi ises in Ups Apparatus I 00rpm
> Detey mìned using Sorpm
Or Apparatus D 00ml-o"Hc0, PH- us
S issolutton media :- 9
OY 68 buffer, Simulate Tntestinal Auid.
class Solubility
Permeabilt txamples
lass-T
Metaprolo
PropranoloL
lass-i
low Nifedipine
Naproxen
elass-n Cimetidline
Metformin
loo Taxol
Chlorthiazol
class-+
and ab%orbs ropidy
r gssolves apaiy Droperty.
shews eycellent
Gfves therape utic action, shows
miristra ion.
Tdeal or Oral ou te Of o
<lass-T op idly
and abSorb
sloly Via
>e Orgs dissolve
controlel grelease dryg ss t r a t i o n
op im um for 9OUte of
admini
Or ab Cor] intravenbus
contolledd.
issolu ion is
ate Jimitedl.
lass-im sorpton is
gapidly
but ah
cissoves
Incomplete
BioayaiLabis
t y is 9Ate Controlled
P Dermeability is p e r m e a b i l i t y
class iy Dous
te and
sote and
dissolution
loo
therapeutic
action not Prefemed.
acdninistratton
S
Ooal admini stration
and other 0utes
af
and othe
Dhtraven ous
is Preferrel
scientst or
Synifcance'
omglatton
tool or
bt Valuab
le dosage form
f upP and
desgn tine for Scase-
Selection of
and
Reduce cost
[Link] Qnd Pre- cDinical
post approvau
kApplcable in subje c t s
human
testng. -the neel of
exposure.
Public stand@rd
to Unnecessary
maintainipg agh
t of in
Helpstherapevtic eguivalence.
size and
partc le stodie,
f formylati or
4)explain he role
Pre
Paytcle hape n the
Potic De Sizelr foms
9elease fom drge phýsical
-tlexopeutc
action, suspenion s
dhyg ab Yorms
ike pourlers
Stability of dosgefloo properties
of
and emulsion S, flowabiitty of
fevence
nter fevente
Inter
in te
Oike micrometers
-the Paode denotel in
* PBoder Par-ticle Size methods:
di/fevent
Determinel by four ti bution
Dis
* microsCopy
Gives nu mber
Ancdreasen
*opical
methods - using
sediment a t i n
principle of
pipette method.
based on the
method - meth ods ike -
intensity using
Conductivity
method.
of ight scatteing
method, sght
coulter
Counter
Dartcle shape: SuYfae area,
the
influence
shape has
ond conpaci on
flou propertbes, packing
Surface are
of the partices.
mintmum
partcles
hove
Spherical properties.
better flocw
Oissolotion
and Dnfluences
a t e of
shape also
k
of regs of Pariele
Size - nieroscop
Seterminattor
metho d.
method and ight
ght scattevi
9iscuss the application tion tal
Dre tomlaDaren
of
consideation n the development f stabiliHes.
dosage forms and ts tmpact
on
bulk
* physio chemi col proper-ties ike analy sis .
and
characteris atton Qnd sol ubiity St u d i e s
- Spectro scopical
s p e c t r o s c o p i c a l .
Problems
|*chemtcal due t
chromato raphic studies ColDuration
b i e r . s O i s
Dresence
|*Chemical
Dro Yeaction 9c o o u d s due
hotochemícal of catlec
xidatior ond formation cystals
of Precip; tate Presence
of
Chemicad eactons , the Contai ne
to
at
ue tip
whiskers