Adiphenine

Molecular formula: C20H25NO2 Molecular weight: 311.4 CAS Registry No.: 64-95-9 (adiphenine), 50-42-0 (adiphenine hydrochloride)

SAMPLE Matrix: blood, tissue Sample preparation: Tissue. Homogenize brain with 4 volumes MeOH, stir for 15 min, centrifuge at 1300 g for 10 min, acidify supernatant with 300 |xL 1 M HCl, evaporate to dryness under reduced pressure, reconstitute with mobile phase, inject an aliquot. Plasma. Extract 1 mL plasma with 15 mL MeOH, stir for 15 min, centrifuge at 1300 g for 10 min, acidify supernatant with 300 \LL 1 M HCl, evaporate to dryness under reduced pressure, reconstitute with mobile phase, inject an aliquot. HPLCVARIABLES Column: 300 X 4 10 jxm Si 100 Lichrosorb Mobile phase: Gradient. A was dichloromethane: diethylamine 100:0.2. B was dichloromethane:EtOH:diethylamine 80:20:0.2. A:B 100:0 for 4 min, to 50:50 over 13 min, maintain at 50:50 for 13 min. Flow rate: 2 Detector: UV 254; Radioactivity CHROMATOGRAM Retention time: 3.7 KEYWORDS normal phase; tritium labeled; 14C labeled; plasma; brain; rat REFERENCE
Michelot, J.; Moreau, M.F.; Veyre, A.; Labarre, P.; Meyniel, G. Adiphenine plasma levels and blood-brain barrier crossing in the rat. Eur.J.Drug Metab.Pharmacokinet, 1985, 10, 273-278

SAMPLE Matrix: formulations Sample preparation: Tablets. Grind 5 tablets to a fine powder, dissolve in 100 mL MeOH: 0.5% acetic acid 1:1, filter (paper), inject an aliquot. Suppositories. Cut up 3 suppositories, add to 100 mL MeOH: 0.5% acetic acid 1:1, heat at 40 until all the fat melts, shake, filter (paper), inject a 25 JJLL aliquot. Liquid formulations. Dilute 10 mL formulation to 100 mL with MeOH: 0.5% acetic acid 1:1, inject a 25 |xL aliquot. HPLCVARIABLES Column: 300 X 4 jxBondapak phenyl Mobile phase: Gradient. A was 10 mM heptanesulfonic acid in 1 mM acetic acid. B was 10 mM heptanesulfonic acid and 1 mM acetic acid in MeOH. A:B from 60:40 to 25:75 over 30 min Column temperature: 35 Flow rate: 1.75 Injection volume: 25 Detector: UV 225 CHROMATOGRAM Retention time: 20

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OTHER SUBSTANCES

Simultaneous: dipyrone (metamizol), diphenhydramine, drofenine, ethyldiphenacetate Interfering: promazine

KEYWORDS

tablets; suppositories; liquid formulations

REFERENCE
Facchini, G.; Zaccheo, R; Nannetti, M. Simultaneous determination of hydrochloride salts of adiphenine, diphenhydramine, ethyldiphenacetate, drofenine and promazine by ion-pair HPLC. Boll.Chim.Farm., 1983, 122, 405-411

SAMPLE Matrix: solutions

HPLCVARIABLES

Column: 300 X 4 10 jjim LiChrosorb RP-18 Mobile phase: Gradient. A was 27 mM ammonia in water. B was 27 mM ammonia in MeOH. A:B from 100:0 to 70:30 over 6 min, maintain at 70:30 for 5 min, to 30:70 over 15 min, maintain at 30:70 for 15 min, to 0:100 over 2 min, maintain at 0:100 for 20 min. Flow rate: 2 Detector: UV 254; Radioactivity
CHROMATOGRAM

Retention time: 37.3 OTHER SUBSTANCES Extracted: metabolites

KEYWORDS

tritium labeled; 14C labeled

REFERENCE
Michelot, J.; Madelmont, J.C.; Rousset, B.; Labarre, P.; Mornex, R.; Meyniel, G. Metabolism of adiphenine. II. Identification of major excretion metabolites in rats. Xenobiotica, 1982, 12, 457-462

ANNOTATED BIBLIOGRAPHY

Michelot, J.; Moreau, M.R; Madelmont, J.C.; Labarre, P.; Meyniel, G. Determination of adiphenine, diphenylacetic acid and diethylamino-ethanol by high-performance liquid chromatography. J.Chromatogr., 1983, 257, 395-399 [same procedure as Xenobiotica 1982, 12, 457]