RP-HPLC method development and validation for the quantification of Efonidipine hydrochloride in HME processed solid dispersions

Abstract

Background Efonidipine hydrochloride (EFO) is a poorly water-soluble drug and, hence, has poor bioavailability. Solid dispersions (SDs) of EFO using Eudragit EPO were prepared using hot-melt extrusion (HME) for the first time. The current study aims at developing a simple RP-HPLC method to quantify EFO in the developed SDs. Results The chromatographic separation was carried out on an Agilent Eclipsed XDB-C18 column (4.6 × 250 mm), packed with 5 μm particles. The optimized mobile phase consisted of HPLC grade acetonitrile and 0.020 mol/L KH2PO4 (pH 2.5) buffer in the ratio of 85:15 v/v with a flow rate optimized at 1.2 ml/min. The developed method was validated for system suitability, linearity, accuracy, precision, and robustness. The linearity results showed an excellent linear relationship between the drug concentration and peak area, indicating the peak area is directly proportional to the analyte concentration within a specific range and an excellent correlation coefficient of 0.9998. Intermediate precision and repeatability confirmed that the method provides precise results with %RSD value less than 2% for EFO. The assay results of the developed formulations were in the acceptable range with RSD less than 2%. The enhanced drug dissolution from the Eudragit EPO carrier with 10% Citric Acid (CA) is attributed to the conversion of the drug from crystalline to amorphous form, and microenvironmental acidic pH provided by CA. Conclusion In a nutshell, the developed RP-HPLC method showed excellent ability to differentiate the formulations and highlights the role of the polymer and the plasticizer. Graphical abstract

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“…The DSC thermogram is shown in Figures 1-4 which correspond to the functional groups present in the structure of the drug and there was no change in the endothermic peaks of physical mixtures indicating no interaction. [10]…”

Development of ZnO-adorned glassy carbon electrode for voltammetric sensing and electro-kinetic investigations of antihypertensive drug efonidipine

“…Efonidipine also has a potent vasodilatory effect on cardiac smooth muscle and a prolonged hypotensive effect with a slow onset [20][21]. Several analytical methods such as LC-MS [22][23], RP-HPLC [24][25], rst-order derivative UV-Visible spectroscopy [26], differential thermal analysis (DTA) [27] and uorescence spectroscopy techniques [28] have been reported in the literature for the quanti cation of efonidipine in plasma and tablet form.…”