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PIIR 3.{2Clr42P- EsE L. Fall 2000 2. Comid< thc prc by which r oon-iooicdrug fqKulatc! fc ropical , Sk,n
sdminist-ation p{titions frcm air aquru vchiclf-mto thc (lipoidal) tltfd-L
Qu<iommarkcd.wirhe'x'@ntoalyfo.l42P l42p: xloo
"' @nt ooly for 342C lo{
Qrutions markcd with s (3) 8'. Iodi€rc { cothalpieuy favonblc $p€r of fiis pG. U* l0 wordsor lqs!
342C:- xloo
c(o o..
L"-+-.1+t"t - 6 ;\-o"{.-.
&*q ;tK "a
I
l. Abbott distributcsCrCtr for injctioo in l0ml vials ontaining a l0% rclution of
j CaCh. 2Hr0 (MW = 147.03gtmolc)
w , (3) b'. Indi€rc u cnrhalpielly unfavoBble sp€r of this prrcss. Ur l0 wordsor
ifi)N <ll
\=__:__<
"'{Ho*.-y *.q} Ca- rc ontaincd pcr ml of the l0% botutios?
lss!'
ft*,f__C.V
=
V*"sWrY+ffiYW\!*l
b*t k^;'\ wt-.4

extra credit
vn G#
1.36 (3) c'. AS'for tlreovaall partitioning prrcs is pmbably quite small. What is
primuily mponsible for whatcvq small AS'there might be? Use l0 wordsor
less!

fio\{ rsrb'. Hou, mmy meq of Cl- ue conrainedpcr ml of &i-i6zo lolution- l;lT-^"" ,^ av{e^*4 s-u}- t4v'.h"^'Ly
So.-.c c,a c"Lt* !
(3) d'. If (hedrug is quitetipophilic,AG'will be (circleon"Jn - n

#;;H A&"-- RT [tl[c5


-r.rr;a-v*" l' - I
v&b/ |
d. @\reu

(3) c'. Assuming AS' = 0 and if th€ drug is lipophilic, thcn the partitioningprcess is
(circlc onc)
(4)c. l2 meq of Ca* trc to b€ administcredby i.v. injcctionfor thc mpid (cmcgcncy) aa:-A6Ge-ffiia>
-
ACN clevation of scrumcalcium. How many ml of thc l0% CaClr. Zi{r0 should bc D, C0qonmrc
injected? c. can"ttell
tu'! = -Y- :) v--[8.8r u-/ \
l . Y*t ' r w'f 3(2-
147- 3(L l4-
l^\ / \/.\
o qBi tl*% = Q.zu,^"X/.{)(vJ-)
v--s,s>,*0 o.
0 - o
t o o lL

You havc 275 ml of-8.0.3%stck solutioo of drug A, u ugthctic with Mw


(6) 4a. Ust thc mods of intcrmolcular intcmction which must bc considcrcd in ords
316.2glmola
to cxplain ditTmnc iu thc physical prcpcaics of orgaic ompounds igl for

nuN '
ech modc of intcnctioq list thc molcrulsr 46qipto(s) which dcJc$in{s) thc
Afrl | (3) a'. What is thc mold @n€ntratioa of drug A in this so
srcngth of that intemction. ( uu rrd U , u.fi- S<f4 rtl )

lo.s+\(try!yt*. \ = e?x,oa
- ?.,( $
t ror\,fAr\-T7-,\=r a.r#7 t Mods-
a!'oh' sLA &;p& u^x-c*
f.sx ro--M @^
Yo* m4a,;t"L)!'t{l
lJr LrO'a< G+^a-Aa*-Aq
-ac''p+a-
Ol b'. nowmuYtl of mlof waterwouldvouncd to
t l
) l1l- t* tl d;t:+
ftCN prepm l5Ornl of :*;*f:"r|$"":"rrur
a 0.2% rclution-6-f drug A?

(0.'Z)(t' *() = lo.rZ)(vr5,2


)4 VrJ."[=toov'( (3) b. Which mode.(s)of itrtenctior iVm epable of orienting ooc molculc with
r{sp€t to ilothcr?

e!""hl!+A'' + (l'V*l^ao
/so - Vrl,4 -- V*^4,,4, Vu*^= $9 t-'-( (3) c. Which modc of intcnction scts ovc{ thc loogest distatre?

elu*'oalAL
(3) d. which node of interaction rcquiG thc shortdt distane for signifient
inierction?
Rn\\\ (4) C. 50ml of the above0.2% slutioo rc rra$fered ro a vial for steriliation. what
I lwl\ isthcmn€ntntionofdrugAinthcrcmainingl00ml? H-b*a1
9{W o-r02. (3) c- which modc(s) of intcmctioo iVac pr&ot bdw€n dl mol6ul6?

d^ip".tvir- (^-A a1-fs^'*)


(3) d'. t{ow muchdrugA is contaiog!-,irtrq 100m1?
lgmaining
fiO\{
=
4*=(#t)a.'or,c)
_ 6
(4> ?(>- ,(cL 3 cL
o
-
t t o {8 (s
'\d"""\d*, o[d="",,I (6) 8a Skctcl a gnph whict bst illusmre
how cquilibrium ostanrs dcmd oo
tcmpccm. I:bct ue ud ottrq
fqtus r wu donc on the boud in clus\i
D\

5) I Rank th: aPv: onpounds with


es3ggo thcir mcldng points
"t
p ut . > L
(5) b. Ranl the abovc mmpounds
-rr\ with sp€t
> JL

\k
to thcir rquous mlubilitis.
->E.
0r.)
j - /

(4) b. Writc m cquation which,consponds to your


VT cu- tr"rro B-f a"fa* lo/o', taur+<4; u.l.L 'ae;
gmph.
. -^ l- /l ,. -.r u{r,If
vr
0 v -=- a-*-'T
H " I * -E-
:.. e@_ctt{t*
tlly all "ral world" enrran,,.^cri.-^
(4) 6. Essenrially
*-?,i'ffi:";*:1, -,-@'.r.on.)
-__,
>E>f
G) &Ya
deviatioa ;lflr"*JffiH"":
fromRaout u"-"* _.1::i,'.tffi;il!i: \:i/
K / = -__4fl.1
&o,\ t=\_ - [ \ 7 . -_Tr\)
9. Drug _X is a oon clrcrrchte. Dng-Xis
orally adminisrcred4 a suspcsion (small
bits of solid drug-X suspendedi" i *r"tj""
"'ra.gi;j.'fr"?"or'""r,* *"igt,,
solubility, ad atanoUwater
ordrus-x ue473.2
g/mor!,
7.29x l'rN{,ed 2.. - ,", ,i#i1ll"iftrficieot
(4) 7. Auromorivcanrifea
is cscnLiallya aqueousmludon of ethylcne
v rY
ff\ I

$TT:il"."jtr'#o-"jl:l':lI'*o:-*"r-prviva.p.*rr'e-rr,"r.L.ingpoinr
glycol. Ir
(4) a Wlrrt is the concentrado ""1:-q:}:frY|**K:
"-_r"ting "[rr"-,l"Tl:'il"ff;:f ;.ff;TT:li#*j]if ,,,
Jffi,"-, exc.,.1^
;C; 'J z*^
;:#il:ffJn:.J,:Tff*""::Ti1ffi
:HlI_!*:":**l*J"'
soturion prorecs asainsl fr111c down _iirc
\aerqe g-4ln* t-l^J<f -> C.o.c=.,
protet agai6t overhuting? That
boil? r
," i".*t i, "mpemturc d6 it
is, at *to, ,"rf*t* *outd rhe solurion
(5) ,'
H = lTrt--tl
LtLxfu^.t SL^tA U tJW ^ v:--v+{aklt l1;l*::,T*:y
panidonintomd pcmate l:1i*,i,T,in".in,o,r," ur*hffiElliil
nc lnto the blood strum
dn,d. -,,.'
rhrough
ripoia"r*rr r"*i*.Ji:*" rii..l",,,, "
u&"A
e.&-k ll'' w-$-L---
theint*rinalwall. phmaceuriil sclenrisrs
decmine;;;;:;;;;;;'
4=f :i::.5::::: ili.r j".1.:.":"id"rry
"qu"ou,,orutioi
"ljl;;;".;"
A-r^-^r-
^,+= /:
ro ert=\ztw)lt.Kbdftl^):) \/tnt r'' z \
(lr^)=l6.tg_ iHJIj ll,l:i;?,L',?
i**"airiii:*ithin
jY^iY:: g:lip'd"i'''..on."n'i;il;ril;'"*
7t ^*0 . oe ripoiaal
nembriner
--->
:)- 3(L 41 = 6*!o .sr[LTt4 = (u.n*)(o,rr&7t): u ar\-*^( Ko, l.bxto\ X.'
.= )'oxto\
074= /., Kg,
?. {.c1
lh- 3{L
v
' f'l) 4{/" |

,,9,p,0/rs= 1 . 6 x l r 3= l Jh'{= -\
:(1
- T u = T o o+ A 7 o = / f o + ( - 7 > Nr. a
'rtl /-
b ' 1 ' tt o
o
I
T t = l o & ' > >c t4 (1
h.
ltlor,r" 0 . 1 8p r

tt"*
ffi,f;,'#*
*FgT+gstsq'" *,"n,'."smotic
with
t,
I I l. Drug-Y is a tron<l€rrolytc with lvfW,
K,* md aquou rlubility of 5?f .2 g/mole,
lI l l - =I 6 - sT : - [ \ I4 0 ^ . K i 27.4, and 3lm8*, GDectivcrv.
y_* ,1 ;i5J .--rp"ij
250m1of drug-y fomulutcd al a l5mg%
"*pilip,io" r",
T l solution in a io,ii-JIiT",*.*urrioo.
I
(4) b. Givq thc dara bclop, what is thc cooccotration (5) a.. What would bc the oaenrration
{ of r dqtIos etution which is of drug-y in thc aquaus phcc of thc
r\ i*cmotic with cp*t !o pl6ma? dqiad cmulsios-

crmod 4&,* E Mw t* At"= 4.4 * 4*+, j Kz,=rr.,(=


?")(u=p7.1
NaCl.
ddrwusP
0J8
o.o9
t.00
0.16
58.45
198.17
339
1.86
(r*6401) = (c,Xo.'
vtA * k,\g-evr$1
morphincsulfatc 0.09 0.14 7s8.82 610
/rr^^6%=
(>7.{crXo.t) + (c")(o-r) = 6.apcu
.l%
" =O*un :) x= s.7g%&x.tt(P 1.39 r"-6?o
_o.e1k
1e"
N"t\
=1ffiP\ (Hfr-*.J
=E,\r25%
d{xl
i2 6ug:4mY+-- | tm) (1,?r,
&blm)= D,L1qwl 4l o.)t rn
(4) c. Is a 59o Dcxkm USp (DsW) solurionhypenonic/iro,ooia6*i#ri.-)*
"% ( 3.ru.7? $>
lur r-^-r*L
rcspcct !o the @nr.ro of rcd blood ells? (circlc one)
q

--) LiPo{-'; 'l


(% < c'-78Y0
v

afP ,' Crll,,?r'Hro; nu: lf&'t1


Do-r{ra<.. YourMck IndcxtellvouthatrhcMW.ot dng_Z.u
5273glwlc, rhcsolubilityof
)a.fr.ore ia (OU,r0,j ne - Ro.t7 drug-Zis 0.37mg/ml
ai25.Cand.rhc
mctting$int of aruj.Z i. iott. v* "n;oy.l
PHR342Csomuchrharvoudecidero gt"."y*r
fri_A, i,iJi?* *io*
thoughL
3(> 5% UxJra{, r,5 wa,v*v*4.,;,^,rf p?c5
(?] .
/i.<-. nr-rf U*+.* ^-- n \ ' |\ - Y.".*.nil@rrolyrc,Atfd=Arf,-* Allj.a
\r-,
q r{
= O-Sl6k6) S(! Gi[ i! 6c blank)

(o
It
(cxm c.edit
l' (5) d. Given rharrhe value of AH'6" is 14.875kqVmolc, wtrut is rf,c rcluUititdj
drug-Zinarcfrigeratorat4"C?
(2) b. AH 6 can bc estimatedbased
oq rhe meldtrgpoint bccause,ar rhe m€ldng ' .._4---
period,
Ib L€"@-'_ \__|{.n(L"U* l)_ _ |
\o.ztnr--t ,flet
I o.o.nr7f"U4.",f,re6

#
Ail"= O
ASi-is fu,o4 o fu* @ x t3.te.u. = - l.?048
@,ii"r. ;,7; o,6i,"c,t;z' \ - t.qog
c. In order to helpjourI friend,
urcus, you
Jvu will necd-thevalue
rdrs! v r 4AH
of r -..
d.. EstimatingaH'r*
tr suggsted in part (b) would oot help bccaus the other tcm from pan (a)
)= e = o.t./91
cant be ecily estimated.However,bsau* you understoodPHR 342C
matcrial,you rcalirc thar you cm estimatcthe cntire Arra. basedonjusl the
informarionyou found in the Merck Index. DO NOT DO ANY MATH!!
SimPly cxplain the two major stepsyou would ned to perfom.

( e) Step I is simply a concentrationunit convcnioo. Write the starting


conentration (oumberud units) in the left blank. Write the desiredunits in
the right blank. = 5,Sl r"^C%
n
0.i7
(4) e. Given thc concentnrion of drug-Z in the parient,sfomulation, would drug.Z
"plugging" numbersinto m equationud solving for AH'&r". precipitateif storedin a refrigerator? Justify your yeVno mswer uslng
(: ) step 2 involvs numbcrs.
Write the equationtwice: once usingsymbolsand once using the numerical
valuesfor thosesymbols. Obviously,you will not write a numericalvalue for
AH'd". For the numericalvalue of the concentrationfrom step I, just write
'
"stcp 1". @l^-t
^//^/l4)
\ T ? =-3-t4(+-+\
" / V'QT-\ ,t, rt" / |

x l -e ( a , , t loora'*e

147- 3 4-L
l,(L 3(Z

s- . O

i 1 (

c {5e,
\ nXaQ
-g'lt,!-
\$ $s"i P.

'lt^
)
{

t
T

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