Simultaneous determination of terbinafine (Lamisil) and five metabolites in human plasma and urine by high-performance liquid chromatography using on-line solid-phase extraction

Zehender, H; Denouël, J.; Roy, Michael C.; Saux, L. Le; Schaub, Peter

doi:10.1016/0378-4347(94)00483-l

Cited by 44 publications

(24 citation statements)

References 6 publications

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“…The concentrations of terbinafine and its N-demethyl (SDZ 86-621), carboxybutyl (SDZ 280-027), and N-demethyl-carboxybutyl (SDZ 280-047) metabolites in plasma, urine, and tissue samples were determined by validated and sensitive high-performance liquid chromatography methods (3,14). Standard curves were constructed independently for each biological matrix and analyte.…”

Section: Methodsmentioning

confidence: 99%

Multiple-dose pharmacokinetics and distribution in tissue of terbinafine and metabolites

Kovarik

Mueller

Zehender

et al. 1995

Antimicrob Agents Chemother

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The pharmacokinetics of terbinafine and its inactive metabolites SDZ 86-621 (the N-demethyl form), SDZ 280-027 (the carboxybutyl form), and SDZ 280-047 (N-demethyl-carboxybutyl form) in plasma were characterized for 10 healthy male subjects receiving 250 mg of terbinafine orally once a day for 4 weeks and in the subsequent 8-week washout phase. Terbinafine concentrations were also measured in sebum, hair, nail, and stratum corneum samples. Concentrations of the parent compound and metabolites were determined by validated high-performance liquid chromatography methods. Terbinafine was rapidly absorbed, with peak concentrations in plasma of 1.70 ؎ 0.77 g/ml occurring 1.2 ؎ 0.3 h postdose. Concentrations subsequently exhibited a triphasic decline, with a terminal disposition half-life of 16.5 ؎ 2.8 days. Terbinafine accumulated approximately twofold over the 4-week dosing phase. The predominant metabolite in plasma samples was SDZ 280-027; specifically, the ratios of metabolite area under the curve to terbinafine area under the curve following the last dose were 1.25, 1.38, and 1.08 for metabolites SDZ 86-621, SDZ 280-027, and SDZ 280-047, respectively. Nonrenal elimination constituted the major route of clearance for terbinafine and all three metabolites, with renal elimination playing a minor additional role in the clearance of metabolite SDZ 280-047. Measurable concentrations of terbinafine were achieved in sebum and hair samples within the first week of administration and by week 3 in stratum corneum and nail samples. Fungicidal concentrations persisted in plasma and peripheral tissue samples for prolonged periods (weeks to months) after administration of the last dose. These pharmacokinetic properties are likely an underlying factor in the shorter treatment times and good clinical cure rates which have been reported for terbinafine in the therapy of onychomycoses and dermatomycoses.

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Section: Methodsmentioning

confidence: 99%

Multiple-dose pharmacokinetics and distribution in tissue of terbinafine and metabolites

Kovarik

Mueller

Zehender

et al. 1995

Antimicrob Agents Chemother

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“…The determination in urine for those two compounds was performed under the same conditions. Determination of the other metabolites before and after hydrolysis was performed by HPLC with column switching and UV detection [8]. Both method quantifications were based on the peak area-concentration response of the calibration standard.…”

Section: Methodsmentioning

confidence: 99%

Pharmacokinetics of terbinafine and five known metabolites in children, after oral administration

Humbert

Denouël

Cabiac

et al. 1998

Biopharm. Drug Dispos.

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“…The most widely used are HPLC and GC methods. Several HPLC and GC methods for the determination of terbHCl in human plasma (Schatz and Haberl, 1989;Faergemann et al, 1993, 1994, Zehender et al, 1995, urine (Faergemann et al, 1993, Schatz andHaberl, 1989), dermis-epidermis (Faergemann et al, 1993(Faergemann et al, , 1994, stratum corneum (Faergemann et al, 1993(Faergemann et al, , 1994, hair (Faergemann et al, 1993(Faergemann et al, , 1994, nails (Faergemann et al, 1993(Faergemann et al, , 1994Schatz et al, 1995) and milk (Schatz and Haberl, 1989) have been reported. A method for determination of terbHCl in various rat tissues has also been described (Yeganeh and McLachlan, 2000).…”

Section: Terbhclmentioning

confidence: 97%

Determination of terbinafine hydrochloride in cat hair by two chromatographic methods

Kuz̆ner

Eržen

Drobnič‐Košorok

2001

Biomedical Chromatography

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Terbinafine hydrochloride (terbHCl) concentration on the site of infection with Microsporum canis is a very important indicator of drug effectiveness. Several chromatographic methods exist that can be used for the determination of terbHCl concentration in biological samples. A high performance liquid chromatographic (HPLC) method and a gas chromatographic (GC) method have been compared and critically evaluated for the determination of a terbHCl levels in cat hair. The sensitivity and the linearity of the previously developed HPLC method were 0.25 ng/mL and 0.25-3000 ng/mL, respectively. The limit of quantification (LOQ) was 0.01 microg/g of terbHCl in cat hair, and reproducibility of 96.6% and recovery of 93.8% were achieved using appropriate sample pre-treatment and optimal chromatographic conditions. The sensitivity of the GC method, 25 ng/mL (LOQ 625 ppb), was much lower than that of the HPLC method. The GC method still enables determination of terbHCl in a range of concentrations in cat hair. The reproducibility of terbHCl for the cat hair samples was 95.3% and the recovery was only 70.0%. Both methods can be used for the evaluation of drug effectiveness in cats and both of them require only basic chromatographic equipment that can be found in most analytical laboratories.

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Simultaneous determination of terbinafine (Lamisil) and five metabolites in human plasma and urine by high-performance liquid chromatography using on-line solid-phase extraction

Cited by 44 publications

References 6 publications

Multiple-dose pharmacokinetics and distribution in tissue of terbinafine and metabolites

Multiple-dose pharmacokinetics and distribution in tissue of terbinafine and metabolites

Pharmacokinetics of terbinafine and five known metabolites in children, after oral administration

Determination of terbinafine hydrochloride in cat hair by two chromatographic methods

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