Clw@terizclon of tL*Mi. ,1cid in Di&tu',t Pho@dicd Dotuge Fw.d tn ...

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4tihislamic. Cdirizi@ wa mong thoe dNg! $,hich w€E wid.ly pEsrib.d ir EmF for aldey befoF it B inrodlc.d in Am.rica. Cetirizine dihydrccl ond€ anlain noi les 1h.n 99plo ed not hor thcn 100.5% or (R5).2-[2-l+l(a{hbbphcnyltpborl tr|I)l)lpiF@iD-l-rllerhoxyl*ric &id dihrdMhbnd(. cdculaled qiih Ffe€nce lo dd€d subsl&ce [al. II G@mic compoud) is p'ineily mid nel..bolite of hydrexyzir€ tsulting Aom compl.t. on{btion of prib!ry alohol noiety ed is auilaue d a vhil€ crrslallin po*der dut is valr-eluble. This onpoud is zwin rionic ud elatilely pold &d Zyn* is the br&d nm. of€dnizire [I5]. Th€ drug is isolubl€ it eebn€ md in n€thylene chlo.ide, les soluble in lipid, bui soluble in meli'anol having mol4dtr s.i8hr of 461.89. Its m.lliog Doi b 218-220 0C &d pH in solnlio. fom is 1.2- L8.lt@nrains hslamelal nol moE tbtu l0 ppln, moistN con|c nor moE $d 0.5% w/w dd sulphated ah not norc rhd 0,2370 vlx. Cctirizire loss on dryirg is rol moE lhe 0.5% dw md 6$y is not l€ss thd 9% w [61. C€tiiizine partly ecouls for lhe i, viw eile.ts t Sttctaft..lttitrElorio6,b ce&izine hs dboxyl group which h3 reducc &@$ ro th€ e al neoous syst m (CNs) 6 conpred lo thc hydsxyzin.. \vhs daly3is ws condud€d on thc lipophilicity bchavior of cetnizine, pdial inta nol€cula chege naddiation *a obsned in the Gtanol/sater md .lode@e/wrd.y$etu. The ionic Fflirion dilgm i.dicaled lhat cdnizie &t 6 a pbid rasponer &o$ int rfaces wd.r c@in @ndilions oI pH Il?l ln coEbinaljon Nifi one of $e bsic nilroge.s of pipe@i.e ring, rcid fuction.lily tules ihis conpound a very uique n terion. Ceboxylic SDup of @tntirc inlttul with th. tsic nitroS.n via folded @.fotl'@, thqdolE, il Fsi.ss Elativ.ly hjgh lipopbilicity at physioloei.il pH (LogD- 1.5). Phmscotin€iics orcelidziDc sisnin@ y dif€$ fiom lho* ofthe baic ed lipophilic hydroxyzin . Duc to ryitterionic attuctE dd ils P-gly6prol.in etility. cetiiizin. h4 onch low CNS D.netrarion thq hydtuxyzin . Ccliddft display3 dinind a&mlae€s over the b6ic hydmrytre in sv.El c.r.gon6 sNh d slow E@ptor diswiaiion ntc, hieb sel€cliviq od ncgliSible liv€r enzyG inr.Erio. [r8]. Ih snall sE@tudl cheg6 in hydoxlzin l€d to th€ difd€nl phm@kinctb prcnle ed the phtuodr@ic sDectu M al$ ch&8.d. In ev€rl i, v,D i61 modcb, c.tirizire prorrd to be poLnl conDourd
wilh l@g le*iDg .ctivily. h I ob*o€d lltrl al dos tblr .lletirrl, bl@l tLe &don of httrnift in thc akin ed luB @tuizire ldninisr.tion clicir.d linle or no s€dation or el€ct@ocephalosrm {EEc)che8q [19]. 4 C.fuaru 6d.Nndo6 C€ririzl!. ii a chir.l dsg ed .Mtion6 @ pE$ot a .&rly l: r nixte. Snrdi.! 6i.d on th. n6d r€sist&e b @mwE the €freB of rdmic. R ad S edrizinc indioied thlt S €Mtion6 docs mt exl bir anihi$din cfretl N shou by botn @nic .nd R. e@tion6. IE emat€ dd R cMrioIM irldbicd histrsi!. ed induced e inclEe i. 6al rsisra&e, thw irdietilg the andhisi.nine Plopenies of R alirizine 1201. CdiriziF hav€ b..n sFtbesizd by vqiour ncihods in licBnre [21-2!], Detk et ar, dielo$d th€ p@tical laluolo8y ro. lh. pepetion of (,t)-cdir'ane 2Hcl v,a dis€It@letivc orsrnonelallic addilid to x4..r-bui.n6ulfDyl sldiniB [24]. r""r \4.^." tv ru o."- *S**
Page 1 and 2: DRUG.DRUG INTERACTION STUDIES OF CE
Page 3 and 4: llfris tfr-tis is &atcf to rtJ N6rr
Page 5 and 6: S.No Dadl3 B c D E B c D E Hisory H
Page 7 and 8: E F CairiziE witb NSA.ID'3 Sinuli'e
Page 9 and 10: l0 |l l2 RESEARCII PUBLICATIONS ANT
Page 11 and 12: ABERf,VIATIONS Alnl An odipine PMA
Page 13 and 14: d ephthyldin . Th. rca.tion mh&bm f
Page 15 and 16: INTRODUCTION
Page 17: €valutcd. The nosl aDnug smup is
Page 21 and 22: sllbiliad by inta holecurd hydrcgd
Page 23 and 24: iii High pre$we liquid chtohatogaph
Page 25 and 26: kela.@n@le withoul ihc incEbed nlk
Page 27 and 28: C Int nctilgdrug! Cetinzine is wide
Page 29 and 30: Resfuh on 4{uinolon.-3.carboxyhr€
Page 31 and 32: 3 Notst@idd .ttiJnfunmto,f dr.tt (N
Page 33 and 34: dslhma swh s coughinS, whezing, dd
Page 35 and 36: Hist.oc./melabolic s}t'dmne, which
Page 37 and 38: mirlende. rh. sErion of homones ed
Page 39 and 40: e$enrid fuciion ol cob.h is rs a co
Page 41 and 42: tdd hody kd.a d.r diliihdm ir tutld
Page 43 and 44: the h@d imw sysid pDi€ct lion dip
Page 45 and 46: u CwrhaealdttutirB Whia Dlood ard e
Page 47 and 48: Raw @&ituls a.d wft of Dtmr.uticd p
Page 49 and 50: AllD( 500 MHz spetron i.r sing IMS
Page 51 and 52: T.bl.2l LMit rdgd of@lra ob.yirls B
Page 53 and 54: solutiors. Con@.nadon tug€3 of al
Page 55 and 56: 3 Dmg- dru! i .ncriob srndi6 The D
Page 57 and 58: la* dd HBSS+ *s !dd.d to @h wll to
Page 59 and 60: RESULTS AND DISCUSSION The possibil
Page 61 and 62: s€@ we obs.led to b. 0.04 l!gn[ '
Page 63 and 64: povatul My of optinizing sel*dvny \
Page 65 and 66: m. xrcjD ., d. t{31 dd€lop.d d R!
Page 67 and 68: Ruggedrs ol ihc medod @ hld.!.d by
Page 69 and 70:
Hce, b = lldr logth of $e ell ( I c
Page 71 and 72:
nin'mM detectable linit of 5 lenl,
Page 73 and 74:
The develoted nelhod M lppli.d tor
Page 75 and 76:
Irr &nltri.al nsim for feotidirc .t
Page 77 and 78:
tbh aS9 Ituftti@ r.s,Ls otethxiE wi
Page 79 and 80:
et dt. [22E] q@rifi.d rhe sinvlsrlr
Page 81 and 82:
Intudide pr*iriN of the Ntho.l % RS
Page 83 and 84:
tbn ct .[dtttEadtu r=ll3!7i+0.0017
Page 85 and 86:
Tr! Mid risr.l ohriBt ftr l[. Fw.dr
Page 87 and 88:
l :l &rF1(,: Chudo'u.of iGdon .r Ct
Page 89 and 90:
3 C.dddr. rttt qrbolon6 I Shrtt@Bd.
Page 91 and 92:
Rerendon line obw.rl for ouinoton.s
Page 93 and 94:
LaLt al t*tdhl nattqedtur dh lo@t6
Page 95 and 96:
ft. r* ofofotuin .t pH I w fold ro
Page 97 and 98:
Rcg$sion sbdnics re sboh in tablc 3
Page 99 and 100:
T1E r'- of 3pd0oeir at pH I w'16I,
Page 101 and 102:
M .@onim @tate. aceroniuile and l'i
Page 103 and 104:
ihe ld.b of co@manon o. difrer d.F.
Page 105 and 106:
.5t lt9 Itur@tt@ wltt ofqd^nN db tn
Page 107 and 108:
.pfstd ttdiei3 ol c.tizitu dd z'tod
Page 109 and 110:
ft. n€thod for rh€ dcimination
Page 111 and 112:
mon dtd. pra*tu oftlz nhd %RSD 0.16
Page 113 and 114:
Epsilaau c wiw t'ft^ 15100 t29\7 t6
Page 115 and 116:
Ite ini.@rion reeultr of nubiprof
Page 117 and 118:
Th. % availability of ednzie ra4.d
Page 119 and 120:
* i t I o! I ',.! i; s is P E 3 I q
Page 121 and 122:
sym€F of p€ali. The reteition t
Page 123 and 124:
R.snt@ lotiurs ol.attN dA pnn4tmme
Page 125 and 126:
guinfenesir dd hont€lntal weE nos
Page 127 and 128:
IlF rhtive $andard &virtion of th
Page 129 and 130:
It beraato., e@.s dedtutu vih qd$tl
Page 131 and 132:
(ztxi@ twiiiu .lr.tiniw ad Dhpnv:|.
Page 133 and 134:
Lalence [29?] developed s HPLC tech
Page 135 and 136:
nbi..r.d to l! r!.llrir i! F@ (r.bt
Page 137 and 138:
Trbl.3.ll2 HPLC HPLC HPI' Hptc 97.t
Page 139 and 140:
I! th. deib.d pc.d!n, sp{rtio of il
Page 141 and 142:
23 m t0 l5 5 t01., 97.58 lfi 55 9t.
Page 143 and 144:
fi. l4itu of gliquido* d pH 9 a obs
Page 145 and 146:
inding. Cctirizire sinply dbpl.c.d
Page 147 and 148:
i t s .! € ! a 3 .E E E E E F g E
Page 149 and 150:
The !R spccta ol nubiprofd showed c
Page 151 and 152:
The deshi€ldin! efl*t ws .x.ned i
Page 153 and 154:
F Synrb6ir of d..lr.tivs ol.dirlrim
Page 155 and 156:
M6iqn dat updQn47U 'y1 .^"-"-r" * \
Page 157 and 158:
7,21-7.7 ppm, Pre1on for th€ CII,
Page 159 and 160:
k meh Fonin !t at 3145.9? di , dipb
Page 161 and 162:
Emrs ninnnbdiN .elalatiM oldtMtvt B
Page 163 and 164:
€stosiblc for prcd@i!8 sup@xidc a
Page 165 and 166:
T.U.3Jl *n6tttc of eniziu atd iE t
Page 167 and 168:
.50 u, / i[ a r2s l{/ irl o3.12|,gr
Page 169 and 170:
i o lne @F sh&te of eririziE with d
Page 171 and 172:
l0 ll t2 l3 I5 l6 REFERDNCES John C
Page 173 and 174:
l2 33. 34 l5 36 37 38 t9 4l 45 Bewi
Page 175 and 176:
67 63 69 70 7l 72 11 14 15 16 77 78
Page 177 and 178:
03 H.ltltm JO, Linbid LE ald CilrM
Page 179 and 180:
tl9 Anyn€ Ms ed Sdr@ N (19E0) C.l
Page 181 and 182:
175 t16 t77 t78 t19 180 t8l 182 l8l
Page 183 and 184:
211. wmg D, Clcoenr P ed Smirz J 09
Page 185 and 186:
240 Ters@ H, Aliomi M ard T.tmi y (
Page 187 and 188:
tumour dcs cel.coxib ohace the dti,
Page 189 and 190:
300 301 302 Shilde vM. d6ai BS .rd
Page 191 and 192:
330 Baltaba UA, MaklMov Ac, ZdkiFv
Page 193 and 194:
cdi;rrcdihyddhroid. (Ps)-2-12-l4l(4
Page 195 and 196:
uor fron I b 9, ud rd lk Fq dutb: c
Page 197 and 198:
l ni[ rh.n annilused fdr 10 nii n 1
Page 199 and 200:
i.!r.IFliEdMJennd'd,4 JLD$ ftt ' 'o
Page 201 and 202:
n.'tr'ddn.nq!t4-d.F ut rr!-orre@dma
Page 203 and 204:
wdEldaNPlh.iffu&!nd@ry Modv.., our
Page 206 and 207:
vi4l.slocl?@'fud!@e@dd'd,(D''ih)'dy
Page 208 and 209:
I 56,|J'ciri's.c'.'|',vo|I.No'4.!04
Page 210 and 211:
Y* ser r.cl..,f.*,r, v"r. ro uIr.,
Page 212 and 213:
Simultrnoous Dctermination of Cctir
Page 214 and 215:
P49 An RP-HPIC m.lhod tor tte slnul
Page 216 and 217:
Ilt 3'7i-- L:; -_I i' a \l
Page 218 and 219:
Intenational Clenistry Conference R
Page 220 and 221:
,/ :l i{ AB,S RACTS 7'I INTERIATIoN
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Clw@terizclon of tL*Mi. ,1cid in Di&tu',t Pho@dicd Dotuge Fw.d tn ...

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