Optimization of a HPLC-UV bioanalytical method using Box-Behnken design to determine the oral pharmacokinetics of neratinib maleate in Wistar rats
© 2023 John Wiley & Sons Ltd..
The current research work reports the development and validation of a sensitive, robust and reproducible bioanalytical method for quantifying neratinib maleate in rat plasma. More than 85% of the drug was extracted from the plasma samples by protein precipitation. The method was optimized using Box-Behnken design, a response surface method. The effect of three critical factors, viz., the pH of the buffer (X1 ), the aqueous phase proportion in the mobile phase (X2 ) and the mobile phase flow rate (X3 ), was studied on two response variables, retention time (Y1 ) and United States Pharmacopoeia (USP) width (Y2 ). With the highest overall desirability function value of 0.943, the obtained optimized method conditions were: X1 = 2.4 ± 0.1; X2 = 66.7 ml, and X3 = 0.85 ml/min. Under the optimized conditions, the values of Y1 and Y2 for a sample containing 1 ppm of the drug were found to be 14.1 min and 0.50 ± 0.003, respectively. Single-dose intravenous bolus (7.5 mg/kg) and oral (15 mg/kg) pharmacokinetic studies were performed to determine the absolute bioavailability of the drug. The optimized bioanalytical method was sensitive enough to capture 95% of the drug eliminated from the body. The absolute oral bioavailability of the drug was 49.30%.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2023 |
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| Erschienen: |
2023 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:37 |
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| Enthalten in: |
Biomedical chromatography : BMC - 37(2023), 11 vom: 18. Nov., Seite e5731 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Mahajan, Radhika [VerfasserIn] |
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| Links: |
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| Themen: |
Absolute oral bioavailability |
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| Anmerkungen: |
Date Revised 16.10.2023 published: Print-Electronic Citation Status Publisher |
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| doi: |
10.1002/bmc.5731 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM361498225 |
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| 520 | |a The current research work reports the development and validation of a sensitive, robust and reproducible bioanalytical method for quantifying neratinib maleate in rat plasma. More than 85% of the drug was extracted from the plasma samples by protein precipitation. The method was optimized using Box-Behnken design, a response surface method. The effect of three critical factors, viz., the pH of the buffer (X1 ), the aqueous phase proportion in the mobile phase (X2 ) and the mobile phase flow rate (X3 ), was studied on two response variables, retention time (Y1 ) and United States Pharmacopoeia (USP) width (Y2 ). With the highest overall desirability function value of 0.943, the obtained optimized method conditions were: X1 = 2.4 ± 0.1; X2 = 66.7 ml, and X3 = 0.85 ml/min. Under the optimized conditions, the values of Y1 and Y2 for a sample containing 1 ppm of the drug were found to be 14.1 min and 0.50 ± 0.003, respectively. Single-dose intravenous bolus (7.5 mg/kg) and oral (15 mg/kg) pharmacokinetic studies were performed to determine the absolute bioavailability of the drug. The optimized bioanalytical method was sensitive enough to capture 95% of the drug eliminated from the body. The absolute oral bioavailability of the drug was 49.30% | ||
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