RP-HPLC method development and validation for the quantification of Efonidipine hydrochloride in HME processed solid dis
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(2020) 6:70
Future Journal of Pharmaceutical Sciences
RESEARCH
Open Access
RP-HPLC method development and validation for the quantification of Efonidipine hydrochloride in HME processed solid dispersions Ashish S. Rajput, Durgesh K. Jha, Sharda Gurram, Devanshi S. Shah and Purnima D. Amin*
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. Keywords: Efonidipine hydrochloride, Hot-melt extrusion, RP-HPLC, Micro-environmental pH, Solid dispersion
Background Efonidipine hydrochloride (EFO) (Fig. 1) is a novel 1,4dihydropyridine derivative calcium channel antagonist. Chemically, it is 2-(phenyl-(phenylmethyl) amino) ethyl 5-(5,5-dimethyl-2-oxo-1,3-dioxa-2λ5-phosphacyclohex2-yl)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3 carboxylate with empirical formula of C34H38N3O7P and molecular weight of 631.65. It is a pale yellowish powder with a melting range of 154.7 to 172.0 °C and a very high boiling point of 746.9 °C. The * Correspondence: [email protected] Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Matunga 400019, India
drug has a log P value of 5.44, which confirms its lipophilic nature. EFO is insoluble in water (< 10 μg/ml) but soluble in DMSO (5 mg/ml), methanol, ethanol, and acetonitrile [1]. The poor aqueous solubility of the drug poses a challenge for the drug bioabsorption and hence bioavailability. A simple yet very promising approach to enhance the solubility of the drug is the preparation of
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