A validated stable HPLC method for the simultaneous determination of rifampicin and 25-O-desacetyl rifampicin – evaluation of in vitro metabolism

• Autorzy: Kumar Saneesh , Bouic Patrick J. , Rosenkranz Bernd

Identyfikatory

DOI

10.1556/1326.2018.00361

• Języki publikacji: EN

Abstrakty

EN

A simple, efficient, and stable high-performance liquid chromatography (HPLC) separation method for a combination of rifampicin (RIF), its major metabolite 25-O-desacetyl rifampicin (25ODESRIF), and neostigmine (NEO) was developed and validated. The drugs individually, and in combination, were analyzed using a Waters Alliance 2695 HPLC coupled with 2996 photodiode array detector (PDA). Successful separation of combined drugs was achieved by gradient elution on a reverse-phase C-18 Phenomenex Luna column, using a mobile phase consisting of water and methanol at detection wavelength of 254 nm. The HPLC retention times were consistent at ±7.70 min, ±8.25 min, and ±10.70 min for RIF, 25ODESRIF, and NEO, respectively. The regression data for the calibration plots exhibited linear relationship (R² = 0.995) in the range of 0–200 μM for both RIF and 25ODESRIF, and the lower limit of detection (LLOD) and lower limit of quantification (LLOQ) were calculated at 5.86 μM and 17.75 μM for RIF and 7.78 μM and 23.57 μM for 25ODESRIF, respectively. The method was evaluated using in vitro human liver microsomes (HLMs) assays, and linearity was established for the 15, 30, 45, and 60 min incubations (R² = 0.99). The formation of 25ODESRIF was characterized by hyperbolic kinetics (Km 48.23 μM, Vmax 1.233 pmol/min/mg protein, and CLint 0.026 μl/min/mg protein). The method was applied in HLM assays to understand the herb–drug interaction (HDI) potential of Althaea officinalis, a popular African herb consumed by tuberculosis (TB) patients, with RIF. None of the extracts of A. officinalis inhibited the esterase-mediated metabolism pathway of RIF, compared to the positive control nelfinavir (IC50 = 9.59 μM). The method provides a tool for quantifying RIF and 25ODESRIF in in vitro drug metabolism assays as well as investigating herb– and drug–drug interactions (DDIs).

Słowa kluczowe

EN

HPLC; C-18; rifampicin; 25-O-desacetyl rifampicin; neostigmine; human liver microsomes; Michaelis–Menten kinetics; Althaea officinalis; herb–drug interaction

• Wydawca: University of Silesia in Katowice ; Akademiai Kiado
• Czasopismo: Acta Chromatographica
• Rocznik: 2019
• Tom: Vol. 31, no. 2
• Strony: 92--98
• Opis fizyczny: Bibliogr. 36 poz., rys., tab.

Twórcy

autor

Kumar Saneesh

• Division of Clinical Pharmacology, Department of Medicine, University of Stellenbosch, Tygerberg, Cape Town, South Africa

autor

Bouic Patrick J.

• Division of Medical Microbiology, Faculty of Health Sciences, University of Stellenbosch, Cape Town, RSA
• Synexa Life Sciences, Montague Gardens, Cape Town, RSA

autor

Rosenkranz Bernd

• Division of Clinical Pharmacology, Department of Medicine, University of Stellenbosch, Tygerberg, Cape Town, South Africa

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Uwagi

PL

Opracowanie rekordu w ramach umowy 509/P-DUN/2018 ze środków MNiSW przeznaczonych na działalność upowszechniającą naukę (2019).