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International Journal of Advances in Pharmaceutics 1 (1) 2012

Research Article

Preformulation study of LevofloxacinVimal kumar Shahwal*, Dr. B.K. Dubey, , Mithun Bhoumick

TIT College of Pharmacy,Bhopal (M.P.). India

*Correspondence Info:

TIT College of Pharmacy,Bhopal (M.P.). India

Email : vimalpharmacist1987 !mail.com

Keywords:"evo#lo$acin ,o#lo$acin ,

preeclampsia,antibiotic ,

pre#ormulation

1. Introduction

"evo#lo$acin is the "%isomer o# the racemate o#lo$acin, a &uinolone antimicrobial a!ent. 'hemically levo#lo$acin,a chiral #luorinate( carbo$y&uinolone, is the pure )*+%enantiomer o# the racemic (ru! substance #lo$acin.

1.1 Chemical Name: 9%#luoro%-, %(ihy(ro% %methyl%1/%)0%methyl%1%pipera inyl+%7%o$o%72%pyri(o31,-, %(e4% ben o$a ine%5%carbo$ylic aci(, hemihy(rate.

1. Chemical !ormula : ' 182 -/ 6 0% 2 - 1

1." Chemical Structure:

1.# $olecular wei%ht: 51. 57 -

1.& $eltin% point: -- %--7 '1.' ()aila ility : 991.+ rotein indin%: -0 to 81.- alf/life: 5 to 8 hours1.0 (ppearance: ;ale yello< soli( crystalline po

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1.1 Solu ility: 6reely soluble in !lacial acetic aci(, chloro#orm? sparin!ly soluble in nchemical terms, levlevo#lo$acin, a chiral #luorinate( carbo$y&uinolone, is the pure )%+%)*+%enantiomer o# the racemic (ru!substance levo#lo$acin. =he chemical name is )%+%)*+%9#luoro%-, %(ihy(ro% %methyl%1/%)0%methyl%1%pipera inyl+%7%o$o%7

pyri(o31,-, %(e4%1,0 ben o$a ine%5%carbo$ylic aci( hemihy(rate.

=he empirical #ormula is ' 182 -/ 6 0 2- , an( the molecular H(osin! re!imens. "evlevo#lo$acin is rapi(ly an(, in essence, completely absorbe( a#ter oral a(ministration. ;eak plasmaconcentrations are usually attaine( one to tH a(ministration is similar an( comparable in e$tent o# e$posure )CI'+ to that observe( #or "EHCJI> =abletst #unctions by inhibitin! D C !yrase, a type >> topoisomerase, an( topoisomerase iv, 8

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not kno

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1. urity : ot less than 99 .

1. " Contraindication: =he use o# eye (rop "evo#lo$acin is contrain(icate( in patients t

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• artition coefficient determination :% =he partition coe##icient o# "evo#lo$acin ma5: =he Qma$

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3a le 1: I; interpretation of dru%:

Name of thecompound

Interpretation

%' 2 %'2 'P '% 6 )halo!en !roup

"evo#lo$acin )stan(ar(+ -5 -9 1 17-0 1-90 1/8

"evo#lo$acin (ru! -5 . 9 -9 1.9/ 17-0.0- 1-90.-5 1/8 .95

0.- Cali ration Cur)e: *tan(ar( curve o# levo#lo$acin in phosphate bu##er solution );2 7.0+

3a le : ( sor ance )alue of le)oflo5acin in S p +.# =>ma5 0 nm?.

S. No. 2ru% Conc. =B%@ml? ( sor ance

1 - /.11/5

- 0 /.1808

5 /.- 8

0 8 /. 8/9

1/ /.0 9/

!i% : Standard cur)e of le)oflo5acin in S p +.# =>ma5 0 nm?.

#." Solu ility properties: *olubility o# levo#lo$acin in (i##erent solvents is recor(e(.

3a le " : Solu ility of le)oflo5acin in different sol)ent.

Sol)ent Solu ility

Rater *li!htly solubleFlacial acetic aci( 6reely soluble

;B* )p2 7.0+ practically soluble

Ethanol *li!htly soluble

Methanol sparin!ly soluble

'hloro#orm 6reely soluble

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Shahwal et al / International Journal of Advances in Pharmaceutics 1 (1) 2012

#.# artition Coefficient: =he partition coe##icient o# "evo#lo$acin H, an( the 0%&uinolonesS. Microbiol Mol Biol ev. 51 ) + *eptember 1997 :77L9-.

8. 2ussy ;, Maass F, =Vmmler B, Frosse 6, *chombur! I. SE##ect o# 0%&uinolones an( novobiocin on cal# thymus D C polymerase alpha primase comple$, topoisomerases > an( >>, an( !ron#ect. 1 ) stor.or! 1988.+ 1/: 108L109.1/. 6ors!ren C, Bre(ber! C, ;ar(ee CB, *chlossman *6, =e((er =6. SE##ects o# ciprlevo#lo$acin on eucaryotic pyrimi(ine

nucleoti(e biosynthesis an( cell !ro> as

the primary cellular tar!et #or the &uinolone ';%11 ,9 in yeastS. =he ournal o# Biolo!ical 'hemistry -57 )19+ uly 199-:1 1 /L .

10. *uto M , Doma!ala M, olan( FE, Maillou$ FB, 'ohen MC. S6luoro&uinolones: relationships bet

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Shahwal et al / International Journal of Advances in Pharmaceutics 1 (1) 2012 !

-1. *issi ', ;alumbo M. S=he &uinolone #amily: #rom antibacterial to anticancer a!entsS. 'urrent Me(icinal 'hemistry. Cnti%cancer C!ents )5+ -// : 0 9L /.

--. 6ors!ren C, Bre(ber! C, ;ar(ee CB, *chlossman *6, =e((er =6, C. SE##ects o# ciprlevo#lo$acin on eucaryotic pyrimi(inenucleoti(e biosynthesis an( cell !ronhibitory e##ects o# &uinolone antibacterial a!ents on eucaryotic topoisomerases an(relate( test systemsS . Cntimicrob. C!ents 'hemother. 0 )1+199/: 8L1-.

-0. 'ohen *. S;eripheral europathy Cssociate( nt Dermatol 00 )9+ *eptember -// : 789L 9/.

. Fun(u , C.? =ure(i, *.? Kalkan, C.? uho!lu, >. S"evlevo#lo$acin in(uce( myasthenia crisis.S. Emer! Me( - )8+ Cu!ust-//5: 55-

5. "ui C.".*., Feor!e F. ., ;e(ro .;., ;eter '.*., ptimi ation o# tablets containin! a hi!h (ose o# spray%Drie( plant e$tract:C =echnical ote. CC;* ;harm *ci =ech -// ? 5 ) +: 57% 71.

7. 'heuh 2. ., Tia 2., ho(es '.=., ptimi ation o# sotatol #loatin! an( bioa(hesive e$ten(e( release tablet #ormulation. Dru!Dev >nt ;harm 199 ? -1) +:17- %1707.

8. 2o##man C., Davi( *., Eran "., *ara ., Eytan K., ichael 6., ;harmacokinetic an( pharmaco(ynamic aspects o# !astroretentive (osa!e #orms. >nt ;harm -//0? -77: 101%1 .

9. >brahim E.F., Development an( in vitro evaluation o# novel #loatin! chitosan microcapsules #or oral use: comparison nt ;harm -//-? -09: 7%-1.

0/. Kiran K.M., Manish 2.*., Cnant K., Maha(ik K. ., Cnant ;., E##ect o# (ru! solubility an( (i##erent e$cipients on #loatin! behavior an( release #rom !lyceryl monooleae matrices. >nt ;harm -//0? -7-: 1 1%15/.

01. Mi(hat H., *abira 2., 6atima *., Cmina 2., Elve(ina H., E(iba 2., *tability o# raniti(ine in in ect able solutions. >nt ;harm-// ? - 5: 1/9%11 .

0-. Burns *. ., 'orness D., 2ay F., 2i!!inbottom *., Rhelan >., Ctt

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