Development of an analytical methodology from toxicokinetic to clinical studies for the anti-migraine drug frovatriptan

Laugher, L.; Briggs, Ray J.; Doughty, John; Noctor, T. A. G.

doi:10.1007/bf02493141

Cited by 9 publications

(6 citation statements)

References 5 publications

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“…Frovatriptan concentrations were determined by a liquid chromatographic/tandem mass‐spectroscopic (LC‐MS/MS) method with lower limits of quantification of 200 pg/mL for blood and 50 ng/mL for urine 19 . Absolute and dose‐ and body weight‐normalized pharmacokinetic parameters were estimated by standard noncompartmental analysis.…”

Section: Methodsmentioning

confidence: 99%

“…Frovatriptan concentrations were determined by a liquid chromatographic/tandem mass-spectroscopic (LC-MS/MS) method with lower limits of quantification of 200 pg/mL for blood and 50 ng/mL for urine. 19 Absolute and dose-and body weight-normalized pharmacokinetic parameters were estimated by standard noncompartmental analysis. Least square mean ratios were calculated between frovatriptan pharmacokinetic parameters in the presence and absence of propranolol, moclobemide, ergotamine, or fluvoxamine.…”

Section: In Vitro Studies-effects On Cytochrome P-450-mentioning

confidence: 99%

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Frovatriptan: A Review of Drug‐Drug Interactions

Buchan¹,

Wade²,

Ward

et al. 2002

Headache

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Section: Methodsmentioning

confidence: 99%

Section: In Vitro Studies-effects On Cytochrome P-450-mentioning

confidence: 99%

Frovatriptan: A Review of Drug‐Drug Interactions

Buchan¹,

Wade²,

Ward

et al. 2002

Headache

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“…In pharmacokinetic studies, frovatriptan was measured in whole blood, 14 plasma, and urine by similar liquid chromatographic/tandem mass‐spectroscopic (LC‐MS/MS) methods, with limits of quantification (LOQ) of 200 pg/mL in whole blood, 500 pg/mL in plasma, and 50 ng/mL in urine. A separate LC‐MS/MS method for determining the enantiomeric ratio of (+)‐frovatriptan to (−)‐frovatriptan in plasma had an LOQ for (+)‐frovatriptan (the major enantiomer) of 200 pg/mL.…”

Section: Bioanalysis Of Frovatriptan and Metabolitesmentioning

confidence: 99%

Clinical Pharmacokinetics of Frovatriptan

Buchan¹,

Keywood²,

Wade³

et al. 2002

Headache

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Frovatriptan can be taken without regard for food intake, and because of the large therapeutic margin and shallow dose-response curve, there is no need for dosage adjustment in the elderly, in women taking a combined oral contraceptive, in patients with mild-to-severe renal impairment, mild-to-moderate hepatic impairment, or according to gender. The long duration of exposure may reduce the likelihood of early migraine recurrence.

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“…The flow rate was 1.0 ml/min at ambient temperature. Detection was performed using an API-4000 QTRAP instrument (Applied Biosciences AB Sciex) [25].…”

Section: Analytical Proceduresmentioning

confidence: 99%

Development of Frovatriptan Succinate Microemulsion for Nasal Delivery: Optimization, in Vitro and in Vivo Evaluation

Galgatte¹,

Chaudhari

2019

Asian J Pharm Clin Res

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Objective: The main objective of the present research work was to develop, optimize, and characterize microemulsion (ME) of frovatriptan succinate to improve brain transport. Methods: The pseudoternary phase diagrams were constructed for ME formulations composed of Capmul MCM, Cremophor EL, and propylene glycol. Frovatriptan succinate-loaded ME was optimized by simplex lattice design having the concentration of oil, surfactant, and cosurfactant representing three apex points on the triangle. These were taken as independent variables and percentage drug release as a response variable. All developed batches of ME were characterized for in vitro tests, histopathology study, and pharmacokinetics in Swiss albino rats. Results: Clear MEs were obtained. F5 having particle size – 142.0 nm, zeta potential – 17.7–−7.8 mv, refractive index – 1.38±0.20, drug content – 98.24±0.20%, and drug diffused through dialysis membrane – 85% was the optimized batch. Drug permeation through the nasal mucosa of F5 in the ex vivo study was found to be 82.32%. Histopathology microscopic study has shown that F5 does not cause any irritation and structural changes in sheep nasal mucosa. The pharmacokinetic parameters were determined after nasal and oral administration of F5. For brain tissue, after nasal administration were Cmax181±1.51 ng/ml, Tmax – 2±1.01, area under curve (AUC)0−6 – 390.0±2.08 ng.h/ml. The AUC0−6 attained by nasal ME was 3.29 times greater than oral solution. Drug targeting index of frovatriptan succinate was 2.06. This was found satisfactory. Conclusion: Microemulsion of said composition was found to be enhancing delivery of frovatriptan succinate to brain tissues through nasal route.

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Development of an analytical methodology from toxicokinetic to clinical studies for the anti-migraine drug frovatriptan

Cited by 9 publications

References 5 publications

Frovatriptan: A Review of Drug‐Drug Interactions

Frovatriptan: A Review of Drug‐Drug Interactions

Clinical Pharmacokinetics of Frovatriptan

Development of Frovatriptan Succinate Microemulsion for Nasal Delivery: Optimization, in Vitro and in Vivo Evaluation

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