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Terfenadine
Molecular formula: C32H41NO2
Molecular weight: 471.7
CAS Registry No.: 50679-08-8

SAMPLE
Matrix: blood
Sample preparation: 2 mL Whole blood or plasma + 2 mL buffer + 5 mL chloroform:
isopropanol: n-heptane 60:14:26, shake gently horizontally for 10 min, centrifuge at 2800
g for 10 min. Remove the lower organic layer and evaporate it to dryness under vacuum
at 45, reconstitute the residue in 100 |xL mobile phase, centrifuge at 2800 g for 5 min,
inject a 50 JJLL aliquot of the supernatant. (Buffer was saturated ammonium chloride
solution 25% diluted with water, adjusted to pH 9.5 with 25% ammonia solution.)

HPLCVARIABLES
Column: 300 X 3.9 4 jxm NovaPack C18
Mobile phase: MeOH:THF:buffer 65:5:30 (Buffer was 0.68 g/L (10 mM (sic)) KH2PO4
adjusted to pH 2.6 with concentrated orthophosphoric acid.) (At the end of each session
wash the column with water for 1 h and MeOH for 1 h, re-equilibrate for 30 min.)
Column temperature: 30
Flow rate: 0.8
Injection volume: 50
Detector: UV 259

CHROMATOGRAM
Retention time: 18.33
Limit of detection: <120 ng/mL

OTHER SUBSTANCES
Extracted: acebutolol, acenocoumarol, acepromazine, aceprometazine, acetaminophen,
aconitine, ajmaline, albuterol, alimemazine, alminoprofen, alpidem, alprazolam, alpren-
olol, amisulpride, amitriptyline, amodiaquine, amoxapine, aspirin, astemizole, atenolol,
benazepril, benperidol, benzocaine, benzoylecgonine, betaxolol, bisoprolol, bromazepam,
brompheniramine, bumadizone, bupivacaine, buprenorphine, buspirone, caffeine, carba-
mazepine, carbinoxamine, carpipramine, carteolol, celiprolol, cetirizine, chlorambucil,
chlordiazepoxide, chlormezanone, chlorophenacinone, chloroquine, chlorpheniramine,
chlorpromazine, chlorpropamide, cibenzoline, cicletanine, clemastine, clobazam, clomipra-
mine, clonazepam, clonidine, clorazepate, clozapine, cocaine, codeine, colchicine, cyame-
mazine, cyclizine, cycloguanil, cyproheptadine, cytarabine, dacarbazine, daunorubicin,
debrisoquine, demexiptiline, desipramine, dextromethorphan, dextromoramide,
dextropropoxyphene, diazepam, diazoxide, diclofenac, dihydralazine, diltiazem, diphen-
hydramine, dipyridamole, disopyramide, dosulepine, doxepin, doxylamine, droperidol,
ephedrine, estazolam, etodolac, fenfluramine, fenoprofen, fentiazac, flecainide, floctafen-
ine, flumazenil, flunitrazepam, fluoxetine, fluphenazine, flurbiprofen, fluvoxamine, gliben-
 clamide, glibornuride, glipizide, glutethimide, haloperidol, histapyrrodine, hydroxychlor-
oquine, hydroxyzine, ibuprofen, imipramine, indomethacin, iproniazid, ketamine,
ketoprofen, labetalol, levomepromazine, lidocaine, lidoflazine, lisinopril, loperamide, lo-
prazolam, loratadine, lorazepam, loxapine, maprotiline, medazepam, medifoxamine,
mefenamic acid, mefenidramine, mefloquine, melphalan, meperidine, mephenesin, me-
phentermine, mepivacaine, metapramine, metformin, methadone, methaqualone, meth-
ocarbamol, methotrexate, metipranolol, metoclopramide, metoprolol, mexiletine, mian-
serine, midazolam, minoxidil, moclobemide, moperone, morphine, nadolol, nalbuphine,
nalorphine, naloxone, naltrexone, naproxen, nialamide, nicardipine, nifedipine, niflumic
acid, nimodipine, nitrazepam, nitrendipine, nizatidine, nomifensine, nortriptyline, ome-
prazole, opipramol, oxazepam, oxprenolol, penbutolol, pentazocine, phencyclidine, phen-
obarbital, phenol, phenylbutazone, pimozide, pindolol, pipamperone, piroxicam, praze-
pam, prazosin, prilocaine, procainamide, procarbazine, proguanil, promethazine,
propafenone, propranolol, protriptyline, pyrimethamine, quinidine, quinine, quinupra-
mine, ramipril, ranitidine, reserpine, ritodrine, secobarbital, sotalol, strychnine, sulfin-
pyrazole, sulindac, sulpride, sultopride, suriclone, temazepam, tenoxicam, terbutaline, te-
tracaine, tetrazepam, thiopental, thioproperazine, thioridazine, tianeptine, tiapride,
tiaprofenic acid, ticlopidine, timolol, tioclomarol, tofisopam, tolbutamide, toloxatone, tra-
zodone, triazolam, trifluoperazine, trifluperidol, trimipramine, triprolidine, tropatenine,
verapamil, viloxazine, vinblastine, vincristine, vindesine, warfarin, yohimbine, zolpidem,
zopiclone, zorubicine
Interfering: bepridil, penfluridol

KEYWORDS
whole blood; plasma

REFERENCE
Tracqui, A.; Kintz, P.; Mangin, P. Systematic toxicological analysis using HPLC/DAD. J.Forensic ScL,
1995, 40, 254-262

SAMPLE
Matrix: blood
Sample preparation: 1 mL Plasma + 500 JULL 100 mM HCl + 5 mL 50 ng/mL propranolol
in MTBE: isopropanol 95:5, vortex for 20 s, centrifuge at 3000 g for 15 min, repeat the
extraction. Combine the organic layers and evaporate them to dryness under a stream of
nitrogen at 40, dissolve the residue in 100 JULL MeOH, inject a 40 |xL aliquot.

HPLCVARIABLES
Column: 150 X 4.5 5 |xm Microsorb cyanopropylsilane
Mobile phase: MeCN:buffer 75:25 (Buffer was 1 mM sodium acetate adjusted to pH 4.0
with acetic acid.)
Injection volume: 40
Detector: F ex 230 em 300 (cut-off filter 270 nm)

CHROMATOGRAM
Retention time: 15.1
Internal standard: propranolol (12.2)
Limit of quantitation: 2 ng/mL

OTHER SUBSTANCES
Extracted: metabolites
Noninterfering: acetaminophen, aspirin, ibuprofen, pseudoephedrine, tricyclic antidepres-
sants

KEYWORDS
plasma
REFERENCE
Surapaneni, S.; Khalil, S.K.W. A sensitive HPLC method for the determination of terfenadine and its
metabolite in human plasma. J.Liq.Chromatogr., 1994, 17, 2419-2428

SAMPLE
Matrix: blood
Sample preparation: Condition a 3 mL 500 mg Analytichem SPE C18 cartridge with two
2 mL volumes of MeOH, 2 mL water, 1.5 mL 200 mM pH 4.0 acetate buffer. Add 1 mL
75 ng/mL IS in 200 mM pH 4.0 acetate buffer and 1 mL plasma to the SPE cartridge and
blow through with nitrogen. Wash with 2 mL water, two 1 mL portions of MeOH: water
50:50, and 1 mL MeOH. Dry column by blowing nitrogen through at 8 mL/min for 5 min.
Elute with two 500 |xL portions of 50 mM triethylamine in MeOH. Evaporate the eluate
to dryness at 55 under a stream of nitrogen and dissolve the residue in 200 |xL mobile
phase, inject a 150 |xL aliquot.

HPLCVARIABLES
Column: 250 X 4.6 5 |xm Spherisorb S5CN cyano
Mobile phase: MeCN: MeOH:buffer 19:29:52 (Buffer was 12 mM, prepared from 0.5 g
ammonium acetate and 5 mL acetic acid in 520 mL water.)
Column temperature: 35
Flow rate: 1.8
Injection volume: 150
Detector: F ex 230 em 280

CHROMATOGRAM
Retention time: 13.5
Internal standard: MDL 26,042 (9.3)
Limit of quantitation: 10 ng/mL

OTHER SUBSTANCES
Extracted: metabolites
Simultaneous: acetaminophen, ephedrine, ibufenac, ibuprofen, norpseudoephedrine,
pseudoephedrine

KEYWORDS
plasma; SPE

REFERENCE
Coutant, J.E.; Westmark, RA.; Nardella, RA.; Walter, S.M.; Okerholm, R.A. Determination of terfena-
dine and terfenadine acid metabolite in plasma using solid-phase extraction and high-performance
liquid chromatography with fluorescence detection. J.Chromatogr., 1991, 570, 139-148

SAMPLE
Matrix: blood
Sample preparation: Add 1 mL plasma to an Analytichem C18 SPE cartridge, elute with
MeOH: 200 mM pH 4 sodium acetate 95:5, evaporate eluate to dryness under reduced
pressure, reconstitute in 200 |xL mobile phase A, inject a 150 |xL aliquot onto column A
with mobile phase A, collect terfenadine fraction at 12 min, evaporate to dryness, dissolve
residue in 100 |xL mobile phase B, inject an 80 |xL aliquot onto column B with mobile
phase B, monitor effluent from column B.

HPLCVARIABLES
Column: A 150 X 4.6 Spherisorb CN; B 150 X 4.6 5 |xm Ultron ES-OVM ovomucoid (MAC-
MOD Analytical)
Mobile phase: A MeOH: MeCN: 12 mM pH 4.0 sodium acetate 35:13:52; B MeOH: 25 mM
pH 4.6 phosphate buffer 25:75
Flow rate: A 1.5; B 1
Injection volume: A 150; B 80
Detector: F ex 200 em 280

CHROMATOGRAM
Retention time: 7 (S), 9 (R) (measured after injection on column B)
OTHER SUBSTANCES
Also analyzed: metabolites

KEYWORDS
plasma; SPE; rat; chiral
REFERENCE
Zamani, K.; Conner, D.P.; Weems, H.B.; Yang, S.K.; Cantilena, L.R., Jr. Enantiomeric analysis of ter-
fenadine in rat plasma by HPLC. Chirality, 1991, 3, 467-470

SAMPLE
Matrix: microsomal incubations
Sample preparation: 2 mL Microsomal incubation +1.6 mL cold MeCN + 400 |xL 500
ng/mL IS in MeCN, centrifuge at 10000 g for 10 min. Add a 500 |xL aliquot of the super-
natant to 400 |xL acetate buffer, inject a 200 \xh aliquot.

HPLCVARIABLES
Column: 250 X 4.6 5 |xm Spherisorb CN
Mobile phase: MeCN: 100 mM ammonium acetate buffer 40:60
Column temperature: 35
Flow rate: 1.3
Injection volume: 200
Detector: F ex 230 em 280

CHROMATOGRAM
Retention time: 10
Internal standard: MDL 16,232 (Marion Merrell Dow) (11.5)

OTHER SUBSTANCES
Extracted: metabolites, azacyclonol

KEYWORDS
human; liver
REFERENCE
Ling, K.-H.J.; Leeson, G.A.; Burmaster, S.D.; Hook, R.H.; Reith, M.K.; Cheng, L.K. Metabolism of ter-
fenadine associated with CYP3A(4) activity in human hepatic microsomes. Drug Metab.Dispos., 1995,
23, 631-636

SAMPLE
Matrix: microsomal incubations
Sample preparation: Add an equal volume of chilled MeOH to 0.25-1 mL microsomal
incubation, let stand on ice for 5 min, centrifuge at 2000 g for 10 min, inject a 50 |xL
aliquot of the supernatant.

HPLCVARIABLES
Guard column: 5 [xm cyano guard column (YMC)
Column: 250 X 4.6 5 ynn YMC-Pack cyano (YMC)
Mobile phase: Gradient. MeCN: 10 mM pH 4.0 ammonium acetate 25:75 for 40 min, to
50:50 over 5 min
Column temperature: 35
Flow rate: 1
Injection volume: 50
Detector: UV 230; F ex 230 em 280; radioactivity
CHROMATOGRAM
Retention time: 55
OTHER SUBSTANCES
Extracted: metabolites

KEYWORDS
human; liver; tritium labeled
REFERENCE
Rodrigues, A.D.; Mulford, D.J.; Lee, R.D.; Surber, B.W.; Kukulka, M.J.; Ferrero, J.L.; Thomas, S.B.;
Shet, M.S.; Estabrook, R.W. In vitro metabolism of terfenadine by a purified recombinant fusion
protein containing cytochrome P4503A4 and NADPH-P450 reductase. Comparison to human liver
microsomes and precision-cut liver tissue slices. Drug Metab.Dispos., 1995, 23, 765-775

SAMPLE
Matrix: solutions
HPLCVARIABLES
Column: 250 X 4 5 jxm LiChrospher 100 RP-8
Mobile phase: MeCN: 0.025% phosphoric acid .buffer 60:25:15 (Buffer was 9 mL concen-
trated phosphoric acid and 10 mL triethylamine in 900 mL water, adjust pH to 3.4 with
dilute phosphoric acid, make up to 1 L.)
Flow rate: 0.6
Injection volume: 25
Detector: UV 229
CHROMATOGRAM
Retention time: 12.24
OTHER SUBSTANCES
Also analyzed: acebutolol, acepromazine, acetaminophen, acetazolamide, acetophenazine,
albuterol, alprazolam, amitriptyline, amobarbital, amoxapine, antipyrine, atenolol, atro-
pine, azatadine, baclofen, benzocaine, bromocriptine, brompheniramine, brotizolam,
bupivacaine, buspirone, butabarbital, butalbital, caffeine, carbamazepine, cetirizine,
chlorcyclizine, chlordiazepoxide, chlormezanone, chloroquine, chlorpheniramine,
chlorpromazine, chlorpropamide, chlorprothixene, chlorthalidone, chlorzoxazone, cimeti-
dine, cisapride, clomipramine, clonazepam, clonidine, clozapine, cocaine, codeine, colchi-
cine, cyclizine, cyclobenzaprine, dantrolene, desipramine, diazepam, diclofenac, diflunisal,
diltiazem, diphenhydramine, diphenidol, diphenoxylate, dipyridamole, disopyramide, do-
butamine, doxapram, doxepin, droperidol, encainide, ethidium bromide, ethopropazine,
fenoprofen, fentanyl, flavoxate, fluoxetine, fluphenazine, flurazepam, flurbiprofen, fluvox-
amine, furosemide, glutethimide, glyburide, guaifenesin, haloperidol, homatropine, hy-
dralazine, hydrochlorothiazide, hydrocodone, hydromorphone, hydroxychloroquine, hydro-
xyzine, ibuprofen, imipramine, indomethacin, ketoconazole, ketoprofen, ketorolac,
labetalol, levorphanol, lidocaine, loratadine, lorazepam, lovastatin, loxapine, mazindol,
mefenamic acid, meperidine, mephenytoin, mepivacaine, mesoridazine, metaproterenol,
metformin, methadone, methdilazine, methocarbamol, methotrexate, methotrimeprazine,
methoxamine, methyldopa, methylphenidate, metoclopramide, metolazone, metoprolol,
metronidazole, midazolam, moclobemide, morphine, nadolol, nalbuphine, naloxone, na-
 phazoline, naproxen, nifedipine, nizatidine, norepinephrine, nortriptyline, oxazepam, ox-
ycodone, oxymetazoline, paroxetine, pemoline, pentazocine, pentobarbital, pentoxifylline,
perphenazine, pheniramine, phenobarbital, phenol, phenolphthalein, phentolamine,
phenylbutazone, phenyltoloxamine, phenytoin, pimozide, pindolol, piroxicam, pramoxine,
prazepam, prazosin, probenecid, procainamide, procaine, prochlorperazine, procyclidine,
promazine, promethazine, propafenone, propantheline, propiomazine, propofol, propran-
olol, protriptyline, quazepam, quinidine, quinine, racemethorphan, ranitidine, remoxi-
pride, risperidone, salicylic acid, scopolamine, secobarbital, sertraline, sotalol, spironolac-
tone, sulfinpyrazone, sulindac, temazepam, terbutaline, tetracaine, theophylline,
thiethylperazine, thiopental, thioridazine, thiothixene, timolol, tocainide, tolbutamide,
tolmetin, trazodone, triamterene, triazolam, trifluoperazine, triflupromazine, trimepra-
zine, trimethoprim, trimipramine, verapamil, warfarin, xylometazoline, yohimbine,
zopiclone

KEYWORDS
some details of plasma extraction
REFERENCE
Koves, E.M. Use of high-performance liquid chromatography-diode array detection in forensic toxicology.
J.Chromatogr.A, 1995, 692, 103-119

SAMPLE
Matrix: solutions

HPLCVARIABLES
Column: 150 X 4.6 5 |xm Ultron ES-OVM (Grom)
Mobile phase: Gradient. Isopropanol: 100 mM pH 5.5 phosphate buffer 4:96 for 20 min, to
12:88 over 1 min, maintain at 12:88 for 19 min.
Flow rate: 1
Detector: UV 224; F ex 230 em 280

CHROMATOGRAM
Retention time: 28 (R-(+)), 34 (S-(-))
OTHER SUBSTANCES
Simultaneous: metabolites

KEYWORDS
chiral
REFERENCE
Terhechte, A.; Blaschke, G. Investigation of the stereoselective metabolism of the chiral H r antihista-
minic drug terfenadine by high-performance liquid chromatography. J.Chromatogr.A, 1995, 694,
219-225

SAMPLE
Matrix: solutions

HPLCVARIABLES
Column: 150 X 4.6 Supelcosil LC-ABZ
Mobile phase: MeCN: 25 mM pH 6.9 potassium phosphate buffer 35:65
Flow rate: 1.5
Injection volume: 25
Detector: UV 254
CHROMATOGRAM
Retention time: 1.384

OTHER SUBSTANCES
Also analyzed: 6-acetylmorphine, amiloride, amphetamine, benzocaine, benzoylecgonine,
caffeine, cocaine, codeine, doxylamine, fluoxetine, glutethimide, hexobarbital, hypoxan-
thine, levorphanol, LSD, meperidine, mephobarbital, methadone, methylphenidate, meth-
yprylon, N-norcodeine, oxazepam, oxycodone, phenylpropanolamine, prilocaine, procaine

REFERENCE
Ascah, T.L. Improved separations of alkaloid drugs and other substances of abuse using Supelcosil LC-
ABZ column. Supelco Reporter, 1993, 12(3), 18-21

SAMPLE
Matrix: solutions

HPLC VARIABLES
Column: 150 X 4.6 5 ^m MicroPak MCH-5
Mobile phase: MeCN: 30 mM pH 3.0 phosphate buffer 70:30
Flow rate: 1.7
Injection volume: 20
Detector: UV 230

REFERENCE
Fernandez Otero, G.C.; Lucangioli, S.E.; Carducci, CN. Adsorption of drugs in high-performance liquid
chromatography injector loops. J.Chromatogr.A, 1993, 654, 87-91

SAMPLE
Matrix: solutions

HPLCVARIABLES
Column: 250 X 4.6 5 |xm Cyclobond I p-cyclodextrin (Advanced Separations Technologies)
Mobile phase: Hexane: MeOH: EtOH 90:5:5
Flow rate: 2
Detector: UV 220

CHROMATOGRAM
Retention time: 10.6 (S), 11.7 (R)

KEYWORDS
chiral

REFERENCE
Weems, H.; Zamani, K. Resolution of terfenadine enantiomers by beta-cyclodextrin chiral stationary
phase high-performance liquid chromatography. Chirality, 1992, 4, 268-272

SAMPLE
Matrix: solutions
Sample preparation: Prepare a 10 |xg/mL solution in MeOH, inject a 20 |JLL aliquot.

HPLCVARIABLES
Column: 125 X 4.9 Spherisorb S5W silica
Mobile phase: MeOH containing 10 mM ammonium perchlorate and 1 mL/L 100 mM
NaOH in MeOH, pH 6.7
Flow rate: 2
Injection volume: 20
Detector: E, LeCarbone, V25 glassy carbon electrode, H- 1.2 V

CHROMATOGRAM
Retention time: 1.76

OTHER SUBSTANCES
Also analyzed: acebutolol, acepromazine, acetophenazine, N-acetylprocainamide, albu-
terol, alprenolol, amethocaine, amiodarone, amitriptyline, antazoline, atenolol, azacy-
clonal, bamethane, benactyzine, benperidol, benzethidine, benzocaine, benzoctamine,
benzphetamine, benzquinamide, bromhexine, bromodiphenhydramine, bromperidol,
brompheniramine, brompromazine, buclizine, bufotenine, bupivacaine, buprenorphine,
butacaine, butethamate, chlorcyclizine, chlorpheniramine, chlorphenoxamine, chlorpren-
aline, chlorpromazine, chlorprothixene, cimetidine, cinchonidine, cinnarizine, clemastine,
clomipramine, clonidine, cocaine, cyclazocine, cyclizine, cyclopentamine, cyproheptaddne,
deserpidine, desipramine, dextromoramide, dextropropoxyphene, dicyclomine, diethylcar-
bamazine, diethylpropion, diethylthiambutene, dihydroergotamine, dimethindene, di-
methothiazine, diphenhydramine, diphenoxylate, dipipanone, diprenorphine, dipyrida-
mole, disopyramide, dothiepin, doxapram, doxepin, doxylamine, droperidol, ephedrine,
ergocornine, ergocristine, ergocristinine, ergocryptine, ergometrine, ergosine, ergosinine,
ergotamine, ethopropazine, etorphine, etoxeridine, fenethazine, fenfluramine, fenoterol,
fentanyl, flavoxate, fluopromazine, flupenthixol, fluphenazine, flurazepam, haloperidol,
hydroxyzine, hyoscine, ibogaine, imipramine, indapamine, iprindole, isothipendyl, isox-
suprine, ketanserin, laudanosine, lidocaine, lofepramine, loxapine, maprotiline, mecamy-
lamine, meclophenoxate, meclozine, medazepam, mephentermine, mepivacaine, mep-
tazinol, mepyramine, mesoridazine, metaraminol, methadone, methamphetamine,
methapyrilene, methdilazene, methotrimeprazine, methoxamine, methoxyphenamine,
methoxypromazine, methylephedrine, methylergonovine, methysergide, metoclopramide,
metopimazine, metoprolol, mianserin, morazone, nadolol, nalorphine, naloxone, napha-
zoline, nicotine, nifedipine, nomifensine, nortriptyline, noscapine, orphenadrine, oxeladin,
oxprenolol, oxymetazolin, papaverine, pargyline, pecazine, penbutolol, pentazocine, pen-
thienate, pericyazine, perphenazine, phenadoxone, phenampromide, phenazocine, phen-
butrazate, phendimetrazine, phenelzine, phenglutarimide, phenindamine, pheniramine,
phenmetrazine, phenomorphan, phenoperidine, phenothiazine, phenoxybenzamine, phen-
tolamine, phenylephrine, phenyltoloxamine, physostigmine, piminodine, pimozide, pin-
dolol, pipamazine, pipazethate, piperacetazine, piperidolate, pipradol, pirenzepine, piri-
tramide, pizotifen, practolol, pramoxine, prazosin, prenylamine, prilocaine, primaquine,
proadifen, procainamide, procaine, prochlorperazine, procyclidine, proheptazine, prolin-
tane, promazine, promethazine, pronethalol, properidine, propiomazine, propranolol, pro-
thipendyl, protriptyline, proxymetacaine, pseudoephedrine, pyrimethamine, quinidine,
quinine, ranitidine, rescinnamine, sotalol, tacrine, terazosin, terbutaline, thenyldiamine,
theophylline, thiethylperazine, thiopropazate, thioproperazine, thioridazine, thiothixene,
thonzylamine, timolol, tocainide, tolpropamine, tolycaine, tranylcypromine, trazodone, tri-
fluoperazine, trifluperidol, trimeperidine, trimeprazine, trimethobenzamide, trimetho-
prim, trimipramine, tripelennamine, triprolidine, tryptamine, verapamil, xylometazoline

REFERENCE
Jane, L; McKinnon, A.; Flanagan, R. J. High-performance liquid chromatographic analysis of basic drugs
on silica columns using non-aqueous ionic eluents. IL Application of UV, fluorescence and electro-
chemical oxidation detection. J.Chromatogr., 1985, 323, 191-225

SAMPLE
Matrix: urine
Sample preparation: 3 mL Urine + 3 mL 100 mM sodium bicarbonate, extract twice with
5 mL ethyl acetate. Combine extracts and evaporate them to dryness at 55 under a
stream of nitrogen. Dissolve the residue in 100 |xL MeOH -.water 20:80, inject a 10-30 \xJL
aliquot.
HPLCVARIABLES
Column: 250 X 4.6 5 |xm Cyclobond I
Mobile phase: MeOH: 14 mM sodium perchlorate 75:25
Flow rate: 0.2
Injection volume: 10-30
Detector: UV 210; UV 254

CHROMATOGRAM
Retention time: 43 ((+)-R), 47 ((-)-S)
OTHER SUBSTANCES
Simultaneous: metabolites

KEYWORDS
chiral
REFERENCE
Chan, K.Y.; George, R.C.; Chen, T.-M.; Okerholm, R.A. Direct enantiomeric separation of terfenadine
and its major acid metabolite by high-performance liquid chromatography, and the lack of stereo-
selective terfenadine enantiomer biotransformation in man. J.Chromatogr., 1991, 571, 291-297

ANNOTATED BIBLIOGRAPHY
Jurima-Romet, M.; Crawford, K.; Cyr, T.; Inaba, T. Terfenadine metabolism in human liver. In vitro
inhibition by macrolide antibiotics and azole antifungals. Drug Metab.Dispos., 1994, 22, 849-857
[extracted metabolites; microsomal incubations; rat; column temp 35; LOQ 92 nM]
von Moltke, L.L.; Greenblatt, D.J.; Duan, S.X.; Harmatz, J.S.; Shader, R.I. In vitro prediction of the
terfenadine-ketoconazole pharmacokinetic interaction. J.CUn.Pharmacol., 1994, 34, 1222-1227
[clomipramine (IS); microsomal incubations]
Chen, T.M.; Chan, K.Y; Coutant, J.E.; Okerholm, R.A. Determination of the metabolites of terfenadine
in human urine by thermospray liquid chromatography-mass spectrometry. J.Pharm.Biomed.Anal.,
1991, 9, 929-933 [LC-MS; UV detection]
George, R.D.; Contario, J.J. Quantitation of terfenadine, pseudoephedrine hydrochloride, andibuprofen
in a liquid animal dosing formulation using high performance liquid chromatography.
J.Liq.Chromatogr., 1988, 11, 475-488 [stability-indicating]
Gupta, S.K.; Gwilt, RR.; Lim, J.K.; Waters, D.H. High-performance liquid chromatographic determi-
nation of terfenadine in commercial tablets. J.Chromatogr., 1986, 361, 403-406