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`Unieersiflr re! I-azlwa
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`LUPIN EX 1066
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`LUPIN EX 1066
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`Page 3 of 66
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`Fig. I
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`J.l:l'!lT|.'l-
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`iiua L-5-e am: being E’i.4.'.[i1.-'Ei'_u' uxplured. Iungiiig frum sulid.
`hyrimphuhic. ur inydrnphilic -:.i-i:-.-"mi.-:i. 1E1..'Jt urn:
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`ii1-L-ji- I'u-rmuiatiun
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`rnuriviediji
`ii‘L-.11‘-i:a:i::: Lhi: drug rI'_=:iiJI:ni:1:
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`lh-::r*::l':'_-.' pi:n1.'idi|:1g dnlg
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`Frequency 1l:.ii:
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`I‘.-n miriiiitt-n- are
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`J":-urn ]:ir_]1.Liv:J
`[LEI gI:I L.’Il' 5|.'.Ellifi'iJiilJ [1-7"]-
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`in thia
`chapter we tiiscuifi 1|'H: cntirc .=i:nnpi.: u:r|'i:uiI-i1.~i':n.ii:r-.itiiiii:'i
`ii1-.'nI~.i.-:J
`in the {lei-elnpsaiani
`-:11" -r_rph:J1.::iu:in: pram.-u:I_-a,
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`lhrnugh phyaiurrchcmical.
`rs-;4.l'L*tj.'.
`-.iri-cl
`i:Iiii.:aL'].-'
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`aidrraiiuiis. to ii
`i:|i.sv.:u:a~:.in::Ii n:>i'1g.'].'n:a5 of damage I'm-rru:
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`[1-r:-_ir.'Lil.ii::«ri.I:r_
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`unc.
`is !i't~E 4Zi13'Ei.Q.|1 and 4.":-.i|u.-iiimn +:i|'n:n.J:n1-.1-:1 lens are
`|'I-I'L‘-ii:;iL'l:_ wi'iin:J1 uri: Iuguiulud i:n_u-
`lhi: LLS.
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`|dl'j' 1:3.-ei. The ;i1h..-1:m-.meu:iu:.i[
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`‘.1.-iJ'-':lE1.-I:-I35 ii:i. pn.‘nl|gi'i11eL' and iJi|.'|'i'|‘1tI1.EI'!i{|i sciences as is
`|.:'|."i'|J.l.‘-I'll in Ilu: 1'-.1IIL‘Iwmg :.'-:.1:Ii.-::-I15.
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`II. FIISTUIIIC.-ill. HAFKIIRUIJNH
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`:'-i.:igninr':= I::.'e. L1»: shall
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`Hut
`ii" slit 11113.-s:u:::in
`in so doing "ii-an 1.:-.iu.~3v2:J Hm:
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`113:3.“ shall -2111 UIT hi‘: Fraud." Hi: fizr-rty.-iling Excerpts in‘:
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`plan: in human hii'.ii'iJ'_I,' Ihui [iI:ria.1-::i whcn ri:i"i'.:rr:ni::.' in
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`in 5.-nuiiiurii Mesaiiiiuniia.
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`Page 5 of 66
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`Page 5 of 66
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`egre nttilteup wttl-i. no rlotthi. some tieneFtcia;I effect
`against infection. owing to the antilzutctei-ial properties
`or’ copper [F-"E.
`'l'l'tc standard it-tiund stilt-e til’ the Smith
`Papyrus i_-‘.i'|'.!||3|I'C|JtlF|'|-i'.It~tI‘!li_'ti'
`lT-‘fill
`tt.t'.l—gi-ease.
`liutit:3.r
`and |iut—prut:ntit3.r served as one ot'
`l'.l'.||'_' earliest oint-
`ments or ointrrieitt bases lot the treatment til’ eye dis-
`ease or wtiunds. The Ciruelts e.-tpandert on this haste
`st-tlite to urriire at s tjrptcul eiiairnun teniterne]-. ti
`ILll'L|.E
`For fresh wouncls. whit.-h might i‘Ifil'i-‘E t'ontat';neo copper.
`lead. or itlum. in addition to ni;.'rrl':i and ttuuilrini.-ieiiste
`[lit] The use til’ the tirurniittc substance l1t't_'it'l'J'i'l in tlie
`form of stt-clts. I1-locl-ts. ur probes has hueo documented
`and attributed to the ltotiians iind Grec lts. Such sticlts
`were c.-tilled t.-.rti'l'_i'rri:
`itt't-t:l wert: dtssttlitod in 'tt".ttei'.
`tttill-:.
`or egg white for use as ei-udrups. The Latin word roi-
`i'_i-riiaii is it deriitratiite oi" the tfireelt wuni. .it'ttt'l'_t-i=r'r=.ri tin
`tum derived from iriii'.i_i-tit.
`it
`roll ot' course brea-til.
`l'|'i|:tiIllil'Ig El glutinous paste matte from 'ii.'hcel and water
`that was rolled into thin oortes. runs. or blocks. Dftett
`the 1:ih;t'sician‘s name was inscribed on these hotiics
`[i I]. Pl.iiie3.- the Elder tea. it rt. 23- -'.'-"ll tIi‘.l"i'Ut':tt’tt:d the. use
`ulcgijr whites to "cool" inllttirietl eyes. and lgrei urn. one
`til’ the most popular oi‘ the plant -it:-tIt't.tct:ti of India. was
`rccomnienderl especially for "eye trouiiles“ [12]
`ttilu.-r i‘t.'j1.'ittg placed the origin of at toast in-rt dosage
`l'o1'i1is isolation and ointment} For treating disorders or
`wounds of tJ'Ie e1.-ic between i'l.|2lI[!IrI.‘.I.'|:lt'I'.lJ.I|.t.'i_:i' the first and
`second milleiiiiitrrti
`e_t_‘_, we can reaitlilgi reflect on the
`progress thttt the designers cl’ dosage forms for egtie
`ruotlucts luiue nittrle iiown through the tiges—ttttti'l
`reltitii-iel;t recently.
`little or none. fleet
`the past
`two
`i:lt'.-e1tt.ies. lltowi:t-er. we have begun to see new concepts
`enieriong. sortie t'ee-eiiring the enthusiastic supririrt of
`the ophthalmologist and optometrist. whereas others.
`not so for-titnate- have been relegatietl to the status oi"
`little-usecl iiot-cities.
`
`III.
`
`.-*._?'iM'I"{}Il'i-'l't' HF THE lI't"E iltililfl t'tEl|i'-i EIA
`
`lit-tlepth tiisciissioiis ot the itllhltirlilj-' ut' the eye and
`iiclncitn have heart t|tT.lI2.'Il|Ui'tlIt.‘l_‘_r' ooireruri elsewhere in the
`[|Il'J...'IIl't'tl..tlittEtitliit::l.lIlllt:n1lLlrI:[I3---l'.7]EInl.'l
`in recent tettt.-ton
`ocular tt:t'.I:tt-t.t-rrt}' Here it lirieI'oi'ert-iei.i.- is presenietl or’
`the critical itntitui-uictit letituret that influence the not-
`are and etlmintsirstioii iii‘ uplithiilmie 11-l‘c]Jttn'tlli2ttlH- In
`this tlis_eitsstun. consitlertitiun will he gl't't:Il primarily to
`drugs itppliecl
`topically.
`that
`is. onto the comes or
`-i.=i:t-rL]|.it'It.‘1:li-‘H or into the rittltiettral Furnices.
`liicrcs.s-
`inglgr. drugs are heittg clei-'e|i:+_tt-eel Fi:u' administration b3.-
`|:I'etrI:t'lIt.'|'tIi-I1-'|‘|E! ilosiige l'oniis £l2|l.'tIi.7It.1'2|'lj|.||1t.‘U‘i"ttll]i-'. irtio
`Llie anterior and posterior chambers.
`the '|r'llf:l't.'_t‘l1J.‘§.
`chtiniber. Te-non‘s capsule. or by retrohultiiir iiiji.-ctiott.
`
`Page 6 of 66
`
`
`
`Table 1 fitttutrunieal Structures cut" the E_-toTh
`
`Lari-Eflltii.
`
`L‘-EIt1jI1ItI:iwa
`Jt1l'-trictr t:-oriiurii.-ti1.'ul sur
`5't.i1:Ieni:rt etinruneti-'.-il site
`
`Cornea
`Epithelium
`Be-u-t-iitin'e niemrzutine
`Sltornttt lstt hstuntitt pictorial
`Ilescerrit-t's trtenil-ii-tine
`E.:|'It2ltJlII1i:ll'IrrI'|i
`
`Iris
`[lt-i.-.tt
`Fusteri-zit cli.aml:te|'
`J!-:i-nttles. i1l' Ijrtti
`Lens
`‘iiitret;-us humor
`
`Terri.-iri.'s c.1ps.iile-
`lvl;et.in.tt
`tt-ocl1.- [e-uric]
`t‘i|ititi.'
`ii-icihrimittti flli'lF.ll:l:t
`
`Ft.n1-et'ii'Ir chtttuher
`rlinplc of atiteriut elitttrnlziet
`3t.'l'tlentt't'i‘i. lfillllll
`Spec-es u-I‘ Ilontanti
`Ft‘.-etina
` j
`
`i"tt-sterior i:|Itirn|!:-er
`"-"itrcn1.is cliitmtior
`
`Because some til’ the dosage Forms described mttj.-' he
`urinsidered its itdjunctiine to otiltthalnue it-Ltrgical pro-
`cedures. these procedures and the concomitant use tit’
`tl-ic drug are tie.-ierilicd in Sec. ‘i-'lll.D. For orientiitioii.
`readers are eiicounigod Lt.t familiarise tltttittseli-cs with
`the aruitomictil strttetures oi" the eye tTalile 1]. some or
`which are shown in Fig. 3-.
`the
`The e_'re is essentially a globe suspettded in
`oeulitr orhit. soucuilized for sight through an arrange-
`ment ulmultiple tissues that Funetiuii to t'oetts. trans-
`ntit. ancl detect iti.-coming light. Tltt:r-t: is ti centrttl pttih
`Lliat
`light
`traitcls to the retina. with all
`intervening
`tissues {corn-est. acriteuus hiu-itur. rittoil.
`lens. and intr-
`eous humor] |:t-eirtg transparent. .15. ll surrounding tissues
`serve to nourish. support. and protect these essential
`structures.
`
`The cornea critnuoses only one siiith nt‘ t_he outer
`surface oi‘ the eye. yet it is the tirst and one of the roost
`imp-ortiint httrtiers to ettternal mttteriiiis The cot-ttca is
`composed of three layers ul ‘t'l.lF'_It'lll_g structural and
`chemical properties that t'oi-in barriers tiasetl on solu-
`l:ii|itg.r. polanty tintl p-.trtiu'-nnittg properties- niolecuiiir
`wetiytt and geometry. and specific hiiitling '.‘l‘l.tI.l‘-1-l;'l:I2l'r
`istics. The presence and type ot' interceiliiitit functions
`regulate molecular rtitiusion around the cells. while the
`ii].-drorihilic or lip-otshiiic characteristic cit‘ each liiyet
`cuntrnls tiillusioii across and along the cell membrane.
`The cornea itself has no blood vessels so it relies on
`].'till55i‘t-‘I: dittiisiun cl" nutrients from sutruuritittig tissues
`and aqueous humor.
`'|'he uuten-nost In}-er. ll.'|.-l.' epithelium. is composed ot'
`five to seieti
`layers of tiratitied epithelial cells that
`multcuri only lll"!"o
`[fill pm] of the tutttl corneal
`
`Page 6 of 66
`
`

`
`
`
`l'.|phIl1:lrm'I: I-‘It-tttntti-tI.'I-tltti-I.'I-tl
`
`I'm-titi-t.'I:I-i
`
`-IHII
`
`I5I.|'t|E':rlt;tl thambarjha
`
`fiI".erit:Ir chamber angle
`
`F|.|"I-EHCIT If‘:|||F_|I':|t'
`'n'EIl'|
`
`I:-'_'l3'||I."lE||'.I'a.
`
`|:IZI"|"‘EEl
`
`Canal at flenlemm
`
`-— Drainage |1flI'fi'V.'.Ir'|Ic
`
`
`
`5uEtIIEII'I5Dr-.-' ||gtarI'tenI :tiIe='1a
`EEi:nn;.rI-ein
`
`F'I:I$.*.erit:-r eharrttaer
`
`F1], 3 .-"tn:3=.1:-n'it:e! er-.:-5.: 5.-eutit:-n til" the human eye.
`
`that.-.‘r.n-:s5.. Bueu] eell.~t m" the epttiteiiunt me I't'Iil|.II[i.|Z2'tI“_'.-'
`;ti;'tit':. 1':rn1.-‘filing at Ftg1.1J.'lF .=it.1]1]:i-lg.‘ c-I" t..'t:lE.-i
`It1- replenish
`[11-nee
`lei’-I
`threugh :nt1rn1'.I| sinughtng nr t:n_iur'_-'. Tllr:
`tight juttetitms ettci Iipephilie eemp-esitie-it -:11" the epi-
`thelium CII|]'.|'||'.|-'i1'.||i'_'
`tr: fti-mt i.11'l -:JTt:t:ti1.'t:
`|'.;Ii.'t]Ti.uEE ttt n1t_1|::-
`
`utile-_=. and Fnreign =.u!'Ist:J nL'-:.=. that £I.I'l: h}'dr-.1]'i-hili-:: nnr n|'
`high iue-teeul.-ti
`tueigltl The 11.'i|.F“."«. eempeeed el'i:ntaein.
`
`t]'tI: L‘|'.'|i.[|'|:'L"-
`:]t:I1JI:EI:|1l!i um] lipid [:II1t1.Iit:5_ serve to h.'_t.-dritlr:
`Iittrn, pri.--.--:t11 Ltt'.‘“'li'.!!-ii{tl1
`ttt' I:I:1-::tI:n'.'.t and other I"-:.1re.-i_t_m
`materi-u|.~t. JJTIL1 influenee the -I.'ii:=..lrihtll|IZ"|!'| :tnr:| tn:-:ieir1r el‘
`ftireigtt r.t1'.t[-:'J'ia1I:«t [IE]. F1'tt:tI|'_-..
`the epiti-ieijunt 'i'.-]]"Iv&1.i3t-
`hr-!Li:Lt||3.-' htghiy ar.'ti:1.-t: against nenubjutics; t-t-'h't!I:
`;:I:rt.1-
`ieetiwe ugztittst tmtie 5uh5t:Inr.tt. this uu:1i'-':1:.' 1'n.1_'g.'
`:L|=t:-:1
`tI:|'l|'Ii1i:.'l
`tl:n.u_: IJiU[11'Hilflhi|il} rt:n-..1 thetztru.-utie 1:1-flex 5:5-
`nti'Ir_':.tnt]}'. E-t.twrn.'t.n'e membrane -_-tt1':|:t.'tr.1|!t:t-.- the I:p'tItlLu'.'-
`lium {mm the air-nrnn. Ihi: I‘.-t i_-.'t:r that IL'EtTl1[i'rt!1'I:!i
`‘I-‘ii"r'1. nF
`the I.'L‘I|'|1r.':|
`
`In L't.'tIt'l[Et.I5-l tn the upitheiiuttt. lite it-lttmitt in TE: 3|}"»i-
`
`fiI'.|l'IiJfi. In L!
`[if cv:1]]::t[.=,i::t
`1'nt.r:tI|'_t.'
`r;-.'int't1]'i-ttzlt-H]
`water tanrl
`htgltl;-' ergenieed t'|-Tm].-' with i|1E|2i‘-"-|:1':'I:!fi iilleri with glu-
`C|I“|5Etl:II'Lil.'IC|g|.j-'|.'2i.1JJ gtuund tuhstuttee am-:] at eeettering ef
`]'tl:FLt|I'.‘]-IL'}'lt:'.'i. H-:t
`j=|'.[I'Il.‘lit.t-[l.fi are prrattftti. _Irt:t Litt: h.i_i.Idrtt—
`1'I1'it'1ie eenip-eecitiun rlreecnle It
`lctguifiettnt
`|'|-1-||!'i'i{!1' In |-i-
`pephilie muieettiett. Tilte
`stmma
`ie
`:'.u;e:ep-tihie
`tu
`swelling, and 1.'I.'aE‘-:r t‘:t1nD::nt rmist he HI..'1.i.'|.'I.'1]_|.-'I:."'lI|-l'Il:l'-l.'l-||.Il‘.'1iI|
`tLt
`|1rt:t-i:'n1 ttpaetfiutttinn. This: is-. cl ttrintury Functtr-:1 :'-I'
`the en-zjetlieitum,
`in single layer of heimgunttilyr ur-
`rttnged t.‘¢.‘|.|::
`fit'.'I.|r.t.I.':1lI2d I'rt.itu ttu: fi1I'C|I2l1£t
`lt_'.' E:et:r.-:nt:t'-_»;
`:n'It:mh1'.'mi;: Sine:
`the i:i.1rnt:.t|
`t:nr.i:1ti':I:titi| E-.-.|J.t
`|'lI'I"r'i,'.'
`
`tee-r.|i|3-' pest-ea
`_iLlI‘:I:'|ii42!|15. wttter
`ciiaeentitttieus tight
`the 5LH.'|-Et1.[. Tu
`|'tu:tIt‘.I1
`'.1t’.‘rI.155r
`[til
`ft-:'IJn the it-.itt:.'-'.1u~.-.
`I..'tIu:nrr:r tI11':..
`i:r.:iIt.t]'.tr
`in-n nurnpat
`rnJI:i:nt:-Jiit ]1rnpt:r |1;.'-
`dr:I1iett -::r|'
`tltn: 5-til’-t111'|Jl
`h-gr
`.I-:tI'-H: Iran.=pnrI inf tetra met
`mm the t'LIi.|I.t.1’.'L'-LIES |1Lt|'I'HII-i-' 1'-':i1|1.
`'wnte:- i'eJiett-iitg the ie-:t':L-
`
`"lee1:}"'
`::u:i~seitt: diifiteie-it. The.-te
`tittetigit
`gradient
`t11i.tj-' pr-.:3I:n't
`il
`I.2I.‘I:I1:.-l'.t:t[
`|'|.t'lnt'.'il1"|J bf titer-
`iIJl.'l1.'|.iiiJ11fi
`I1'_t.'I;!r.'t1'Lnn In the .*i|ITl.'l-Tl1tt and present Ittt]: UT nu |JHi]'l.'i.Er
`t-::r dttig pettetmtien. |::u.Lt ere eeeeltl i.1| In the tit1i'u5:en e|'
`nutrients from lhr: uqueuus imumer into the cut-it-eat. ‘fine
`t:ntJnnI:i1e|iLLn't hm‘. an t::'I.'-:r4|.|. lipr_tphEiiL' ttuture that limits
`eiifltisien el‘ hgrtlrerlhtite n'Ie|er.'u|e.<-.
`it
`is !I':i'iI]'.I-!'Irt-tlltl
`tn
`rte-te [hut the |tum:uI. etttinthelitittt has ti. titted nutuhet
`
`ittsl-eel] -:-:.1n1a
`I1-.:lt'1r't:.
`t11itt.rtt'I::Lti|1.'
`rte-I:
`Ur t.'t:Ji£. tlutt Ltrt:
`pensating far ::!1 inst: 011]}
`lhI'nt.tgl't mtgruttnn .'1nr.l
`|:t3.-pei'ti't.~ph'_v nI' incitt-ttitltti
`t.'e1]5 to err‘-'et garlic 1i1
`lite
`tug.-t.-r. In'etl:|i3iI._'g.' te etnttperieatte t'-:Ji' eeil tees ti-ilit result an
`LIZIHH. nf |'1.1netinn and t:I3mI::J| upaeifiuuljtin. 5-int:-e t:n-
`uiethettitl eel!-5 -ztte fiettstiltte le chemical and rneehnnieitl
`
`-i:tJU|::J eeittuet
`intuit. any uplttltitiittie piiepemtieri Hi-'.|.l
`I|'l‘.'.'i-‘I: 1.:-:H.~a must 1:: 1:.'t.:r::1'u1i:.-
`It:'."i.tJIJE|.|'.I::I:J 11::
`!'.Ii-:I-.:t:I:n1:.'tI-
`rhriity
`The eeittee is eenneeta:-:1 ill the Itmtltla re the epeqile
`.~ar.-icra,
`lht’: Laugh fihrue-Iaatir capsule than encloses: the
`t:_1.-t: ;tn:l
`rirn-'.'t't‘]r:.~i euppnrt stud rirttteutittn fltr lht: in-
`tet'in.i:' :=.tt'uettIIee. The weitaie .'m:.-I eI't1'I-: eelert-I
`"is gen-
`:ra|l;-.- n:I'ern:uJi
`to as llltl‘ enn_i1Jm'1'rt--.1. Tlte etr-a:u1t:t. has
`J:1n:t.-:|-_.' packed collagen |"Ii't-rtlsi with 5L'Hll1El.'IHJ. I'tI'Ir:J-:3.-‘I:-t.':~
`and |}_'1.I.-
`1:t-]-um-i:l
`t.'i:5:tr:1-5 -.:~;t;-t:T;-I
`tn the |it11|::ua=t|
`'.1.ft:.'I. Nn
`juncttnttal eetttplexee are present. so the seler-.t pteeettte
`:1nI_t-'
`:3
`|!l'|'lIt1'|1|'li|.'iIi.' harrie:
`t-.:I
`flsn:'ti__-n
`2l'.l.'lJ.|'.Cri.i|J1~. Tht:
`Itmhus. is nah in I3:-Iimud 'I.'t.'.fi5.I:'.‘|.'i.
`ttntfl 53r'Htt:n1ir nhfinrptitt-n
`-:-F
`Ie]t:e:tl|3.- applied -::|t'Ltg,e neeurs.
`h~e.t'e
`['I:|'|T2l'.It'].l'i|]r'.
`Wtthln the tntt:r.i-:.1r i.'-I" rJ1t: l!_'p'|:. tl't.t: Etntbul elm L'L1n'tLtint.
`[Inc Lr.tttct:t.th-tr mt::;]11.t.'nr|c rind. ca n:t| nI' Sichlrrnrn .-11 the
`
`i|."t5 and eel:-I'tt. These 5-l]'i|t'.!|Z'|li'I.:5 Iifilitt.
`junetien er‘ IJ!tt'.'
`.'t|.'[l.1t:t'l1J."t. E‘|'|.II'I'.lE1F l'rI:tm tilt: Etl.'lLt.'EiL'i'l.' -.:i:titttt:EII.:t.
`.1 Tuntlittn
`es,-3-t:nt;]'..'tI
`tn.
`|'tret.'i:n1 Httld |lI2I'_'1!lIl'.|1.1].1Ii{Il1.
`incrtntscd in-
`tmeueuiatr |we.=isu1e.
`:t.:ln.'d 3!.-ttite-mt'Ia
`'I'iie iris.
`.1 ring e’r'
`
`Page 7 of 66
`
`Page 7 of 66
`
`

`
`‘I’'I'I'II""IZit-
`
`-Ell
`
`rrtttseuiar tissttc that te_i_gul:ttcs Iteht entry into the haett
`oi" the eye through the pttptl. is located itt front ofthc
`lens and physically iorttts the diyision hetween the
`ttntrtiot chamber and the posterior chamber. This
`structure is
`rich in binnd vessels. which dilate when
`esprtsctl to seven‘ irritants resulting in it-iditrl hyper-
`erntrt and edema Tlte Lnnervtttic-tt of the ins prnyides
`the means lty wltich the pruct.iu'oner can control pir-
`[:tiiIur'y' dilation.
`The lens it-t essentially u flattened sphere that: ts held in
`place and connected to the ciiiary h-rt-t:ly It-y fiher-like
`slrttnds.
`the .i.'|.':IEI.Lth.'.fi
`i.'tl'
`.7-_"itttt_ Crtrrrposetd of totsneerttric
`layers o|'crystuJltne Iihers. the t-it-asrular lens has it single
`layer of epithelial cells on the ttrlleric-r' sut'I'tt».:e and is
`surrounded by a thin but t'o-cg: capsule that cornrerticcntiy
`p.rt'_'ts'IEE-I213 tlte suppt.'tIr|. for an intrstttcttlar lens tll.‘tI,J ortee a
`catttrttctcus lens has been tetnct.-"ed. The lens epithelial
`ceils hove snrtte rttirntic neu-city- and older cells prc-p.res-
`sit.-ely lose their celttttrtr contents and tntet-.tre tn form the
`crystatllittetihers. The tens is ileitible and changes shape in
`order to adjust
`focal
`length For near obj-tcts {accom-
`tttodatinnt. Ltlt ability that is lost with age it is intportant
`lit 11'EIl‘t:l]t'r1l there.‘ is Illlitttflttihttnge r-tI"r||i_i|,i::riaIItt:ir:1,||i_I.-lens.
`t-llltl.'l no loss oI'cel]s so tl'Lu1 rlrcyt accta-rtulztttttn should be
`investigated For
`tiphrhnltnic prep:-trtttinns that are oh-
`sorhorl
`lttt-::r Lire eye. The ciliary |::u:trd1.' ]tus in-ttt. m.1jor
`Functions. The ciltttry muscle connects to the eottules tot’
`Eitttt and controls lerct aectttttrnodution. The anterior
`pcirtit:-it oi‘ the ciliary hody l'at:ing the posterior ehttmhct'
`prnrluc-as the aqueous humor tltttr circulates across and
`lltrottgh the pupil to the antetittrt-Jssstnhcr and out of the
`iE:j-‘E for it n‘.-t't]'tI.i1tLt..'t|
`lLtt'rtt;t-oer t._tI' fluid.
`
`Behind the lens is the vitreous eh.-smher that con-
`tuins vitreous hllm-ill‘. a trtrn.-rp:-trettt gelatinou.-i ||_|_|]'lL'riE|.I.
`that has no turrtover and is in direct contact with the
`retina. The t-cljrtc is a ltilayered Ittgltly metabolically
`ue’r'rtrt.:
`tissue that trunsfitrtns light to an electrical sig-
`nal. which is processed and transmitted as electronic
`Images to the brain The tissue is composed oi" a
`complex atrunpcntent oi‘ pltotnreeeptor cells [rods and
`cones] ctrerlying the retittal piernenrcd epithelium
`[RPE} ttnd is
`isolated frtttu vtt.t_r.t'_t|I.'_rr fluids by the
`ttltsocl-telittui 1't.ttn'i-.‘.' r. u t..'-t.1n't|'tin.;||iit-rt i_'tI'1:|_1-d_i_'_t|h{'|iflJ .;y_-II
`tight jutteooos littittg the retirtttl blood vessels and tight
`junctions hctween the RPE cells that restricts dt'FFt.tsiott
`front the systemic circulation. The choroid is it highly
`yascttlstrnted eoltttgettous tissue lying I-tetweett the re-
`titttt ttntl the ttclent from the ciliary ho-dy to the optic
`tterve. The optic nerve connects to the retintt at the
`optic diitit. a highly vascular-ined area that is susceptihie
`to -t-cttlar hypertension and drop eti'ects. Finally. sev-
`eral t.tecr:ss-o-t'y tissues radtt».-_su:t are essential to proper
`
`Lllllfl ct IL
`
`Funetrontttg of the eye. Tenon's cap-suie- a thin tncrn-
`hrttnc surrourtritng the sclertt. separates the eye from
`the surrounding socket tlor Freedom of r[|I:'t'|rt."m-2-:1'tl- 'l'|te
`lac:-irnal and Mtih-Dmihit giunels provide tusentittl tear
`and lipid r_'ctn'tp-on-ettts while the eyeiids assist in rear
`distribution end protect ttgatllltil mechanical injury.
`From this t‘_l'rs'r.'tI.-it-'uit:tt't. the reader term up-p-rt.-at.-i.;tle the
`intncticy oi" the eye and the care required in devising
`c-[Ihthah-nic preparations in order to 1-trot-itie sure and
`eJTect-ice therapy.
`
`l"'tt'. FHA lili'lrl_dt.I‘.'_'|I'J LfltG't’ AND
`
`THERA. PEL'T[IE‘5i [IF EIPHTH.-it l.l'tTIC
`MEDICATIDN
`
`it is not the purpose of this tcttt to present an in-depth
`review of the phannocolc-yo-' ot' ophthalmic drttps. For
`this |:tt.tt'].'t-ose the l'|.’dti-El.’
`is referred Itt fl-Flt
`-t'tF Il'Itr itrt-
`thorittttiye treattnents of this subject | I 9-1:]- Howe-ten
`since this topic is not commonly coyered in pharmacy
`school curricula. it hr'teI'treatntco1 is presented here.
`For the tnost pert. drugs used itt the eye fall into one ni'
`.set'eta| categories, including mic-ties. mydriirtics {with
`or it-ithottt cyclcplegie .i°t.t3lJs'il.'_~':|. cycloplcgics, untt-ltt-
`llurnntarorics.
`ttnti-itttoctiyes
`tincluding antibiotics.
`lll1Tl'|r'l|'.il|!'i... and antihuetenalsjn.
`ut.'tt'.i,p',lt'tI.ltt:t-III-I1‘ttl
`tlnsgs,
`surgical .ttiyttttcts. diagnostics. and il category of drugs
`for rntsecliartcutts uses. The intended ophthaintic use
`will deftne more precisely what drug or cnrnhinatiort oi"
`drugs is to he used. the ttppitopriate dosage form. and
`route of adtttittzistrtttttttt. For example. the practitioner
`will. with knowledge of certain cortti-atntlieetione. us:
`rnydriatie drugs specifically for their papillary anrl
`acetmtrnodatit.-‘e eFFeci5., hcth in the pt'o-oess ol' refrac-
`tion unrl
`in die management of Itidouyelitis. tritis. ac-
`cottttttodutit-e
`esotrnpitt.
`uttd
`so
`on
`.'?tt=l.r-::I|1:i:t'.It'.'.
`hetuutrnpitte. scopohcntitte.
`trnpicantidc. and cycle-
`pentolttte are esst rtrples ct" porasyctttpathomtmetic drugs
`prtssessttte rtrydriatic and eycloplegic activity, whereas
`phenylephrtne and eprncphtitte ore e.-titntples of‘ sym-
`pulbotnimerie drugs pttssessing only tttydriatic activity.
`['JI"Ug5 |.J'tttl mt.'t}' ht.‘
`I:'IIn5t'.'t1 I't:!r use In the rtt.hnttge-
`ntent of yrlrtttconta may he topiealhr applied rnintics,
`such as pilocurpitte hydrochloride or nitrate, carbu-
`ehol. echothinphore iodide, or den-ieeariurn bromide;
`epinephrine prodruys lil-re dipivefrin hydrochloride,
`ttonseicctive .!'i—ut.lrenet']gic blocking agents such as ri-
`rnc-Iol
`tttuleute and hunolnl hyclrochlot-ide, end selec-
`tive fi-adrencrgte I-iioei-ting agents sttelt as raeernie- or
`the more |.'||:||.-|:nI
`it_-'tt-t-Itnettttrctlol hydr-o.r_-hlu-rn:le_ mm.
`pounds ctet-nit.-l nI' papillary erTect-. topitstlly tttltt:tinii.-
`tered
`curhontt:
`ttnhyrtrasc
`inhibitors.
`iuch
`as
`
`Page 8 of 66
`
`Page 8 of 66
`
`

`
`t:};lifliiiJrriii.' PHIl111IlI'1'.'IIiEIl
`
`I'HlI2It|l."I'h-
`
`-4-11
`
`dor:-ioliiinjde iinrl hniizolernide; rircstaglnndtn tinzilogs
`.-if the class PfiF_.,,. sueli its tstiiiiopiost uiid tnii-oiii-osi.
`
`irttrisclcuiar pressure {ll'l|F'] sig-
`[IF lfl-'i'|."I.'.Tl'|.'|g
`c::|p-.il;i|e
`Ttil'l.t2'i'tI'Ill.'_'-' wrtli
`little or no infinmrnntorgi or i'iisoi:li|.1~
`Ieiry respiiiise; or
`their
`J'I'Iil'_'.' he I:.'I|'lLii]i= odnttritsterod
`
`ll'Lu:l will luwcr in-
`drugs tn Tl-Fi'.2'5{.‘l'llZ an IZII1iJ'l1Ll-l!l|_' eJTei;[
`tiiioetiliir pressiirc. such li'lt'-
`‘iEJ'”ru glycerin or 41%-
`ltit!I5t1]'l.'ii-IJ.-E.
`'Cl|ll't-ET diugs administered ointlg to loiii.-r
`iiitriieieiilar pressure are the carbonic anhydrous iii-
`|i'itiiioi's iieetiieoiiiniirle F||'H'l mcthrieoliirmdc. 1-'i:rt1ier—
`
`n-ion.-_ Ihi: iiiiotie drugs iri.ig.- he ciioseii to rei-terse 1lie
`c‘Ft'ceI: riF n13.-'driaI:.i-L's after ri:.'I'r:-ictiou or cluri:1i_..-. surgical
`procedures such iis critriniet rcrniwiil. There is new
`in-u:i]al::|e uii
`:II.‘t[illI’I:i'|Z!|'i1'|.illI“ drug dei-'oii:E oI'
`|:-i.L[!-'ttl:ii'i.'
`-.icI,i-.'i1:.r,
`-i.l.ii]'ii]'i1'ttiI'.iilI: 1'i_-.-'dri.ichli.irii.’Ei.-,
`-.i-'E'iis:l'i
`is i._-.uinin_c
`importance in the 3l"C‘-'t'.?|.'.‘H1l or‘ the et-l'o»:t riI'1n}-'t-lntiiicii.
`Depeiidiiig on line location of ocultir inllriniiiiiitien.
`F.I. sjpiecilie ceirlioostertiiii in :1 specific dosage l'I.‘irn'i
`I1'!El_'p'
`he chosen.
`I-rir instance. rt corticosteroid or high Tin-
`l-:."t'It.'_|r'. such as prednisclone iieeitttc. fiimioniethnione.
`cieritrrieiliiisoiie. or
`ririieiiotoiie.
`rn.ii§.- be chosen for
`
`lruv;.'t_ Further
`i1'_iFltIi'nmiitiL-n of the uiecui
`ijccp-sen=|.e.icI
`treatment or‘ such infiemniritinli may title: the Font: of
`sulznenoii injections or oral tsirsteiiiiej adiitiiiistrelion
`i.'ii's.cleerei:I isrirticcisteroitls, depending on Use inrllculion
`:1|1d the dosage !'i.'inns n1.r;iilsLl'iLe. For influmm Lition oi' si
`more superficial iiiiuire.
`the lower strengths of tired-
`niscileine iiceiute or the II.‘-'-Ii-‘er-1:Ii.*-I-i:1'Ic_|..' c-'.'irtiI.'I.'Istit't'I.1i::ls-,
`such its. hydroenntsone or medrysnne. still usually l'i-e
`ehoseii. It is now also possible to trail inflnmnitition
`'|.|'Il.l.'l ni.i1'tsI.i:'t'Lii.iJ:i.il iigcills liltc diclofeiiuc iir ls-;-tli:-rcilltiis.
`drugs not eitrieclecl
`to raise ICIP.
`Drugs use-d l'or Ihe Ireiitrrieiil of oeiiinr infection will
`g'l.‘I'I1.‘t'il]lj-' he clioseti hiised on the presiiiiiiitiirie d't:ig~
`nticsis of the cuusutisc agent by the optithaleiologist.
`
`ci;iriIi1'|'i1it1irin h_}' micreiliiul cullurc tincl
`I_,_l|tIl:I]'fltl:If:|i'
`ideiittfieiitioii is t'ou1'iiieli.- conducted er-neiirreiililii with
`the initiation of [1'icrag:I'_i-'. This is geiieiitllg J1IE|2|.':3Fi.il.l"_'r
`
`li-cciiusi: i:;il' the s.e'i'ei:1tg.I iini:l sight-threatening nature t'ii'
`some types tiI'irifee1ioii For esnmple. il".i
`|;i:iIiI:nI l1l't.‘i-H
`1'r_ii-eign body lodged in the coiiiea oi-jgiiisijiig from 4
`[in-ten=tisiII}' etintsrnirtatcti environment.
`the ]:ih'_-rsician
`iiiiiir choose to begin treiirmeiit of the cg.-'i:. H-n£t.!T Foreign
`li-od'_».- ienioi-at. wi:i11 ti single or |Z2i_'illlIi.'Il|'Ifl.il.-|.'Itl oIiti"o:ioti'c.
`such as gentiimicin, ti.il'i-ram;-'cirt. chltirumplicnictil. and
`-‘L
`11eoiii,i'I:in—r:ii:i[:.'rn',-'=:in
`ecrniiiniiliiin
`Recent
`1T'|-
`tiioduetion or"-iiutttolurie antibiotics like ci|.iI'ofio:i:.'tc'iii.
`ofltiictcin. ancl
`EllIIIE2lit.'Htl'l.IL".l1'|
`ltuvc eiipaniittil the 1:il'i_-.-'si-
`-:i:in's choice of .'ii-iiiIi1|'i|e |'|Il'-|'H'l|.|-1.!l3-'i- for c-i:ul:Ii' Infec-
`tioiis. The iipplieutioii o1" tliese tigents "is eonstdeied
`anfiriipnste- since an infection with i"".'.'e'.i.'i'.i’t.Ii'rr.:-Iri.:.'.'-' E-l':"."-
`riefiiirisrr eitn -iiestrriy ii. co men in Es-l—-ll-H hours. cener:-.tll'_..'
`
`ielc1'|1tI';..' nn intectiiius iigent. Less.
`it Takes 1ri
`1hi: rimi:
`fuliiiiiiiiting.
`lint no less diingeimis.
`tire
`lr‘iIit‘€TiI:I11fi
`t-iiusud l:i-3.:
`‘.-'it!|'i-l.'tLl_‘i stuiilij.-iticoceai]
`iiiid streptococcal
`organisms.
`I-'oi' stiperliciiil
`l‘:-.'i.cI.e1'Liil
`inl'ei:ti-:ins ni' Ihe
`coiijtiiictii-ii iiiid eyelids. suifoiiainiiiles. such ll-5 sodniiii
`sult'.-ieetamiide an: usually rirescribed. as are _I,'e||u-i.
`mercuric i.‘-sicle and mild stiiler protein.
`l-"'ro|1h1-'l.ue1'ti:
`ther.ipj.-
`It-ii
`I.‘i]'r]'IlIi'Iii1l|'l1l-ll neoiirituriitini
`is neLti'|_i'
`imi-
`i-'ersall3.- requireiil
`in IJ'iie United States, with silver ni-
`trnle. penicillin G. or Ilrj-'lii'lTt'.Il.'I'Ij.'Ii."l11 heing the firimiirg.-'
`iiiiti.-int'ectii-es. ii-icd. F'ro- .intI postsiirgienl jirophgrliisis
`is becorntng irnire eoinirtoiiplnee with the popularity o:l'
`stirgtcniiy etirreeleizl 1.-isio-no uni.l combinations of unli-
`iiifeeiiires with :inii-in1'le.riiniaiior;.' ag