Author:
Rajput Ashish S.,Jha Durgesh K.,Gurram Sharda,Shah Devanshi S.,Amin Purnima D.
Abstract
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
Publisher
Springer Science and Business Media LLC
Reference21 articles.
1. National Center for Biotechnology Information. Efonidipine hydrochloride, CID-119170. In: PubChem Database. https://pubchem.ncbi.nlm.nih.gov/compound/Efonidipine-hydrochloride. Accessed 10 Apr 2020
2. Miyamoto M, Oda T, Bunrin T, Okabe T, Nishiyama T (2001) Process for producing efonidipine hydrochloride preparations. US Patent 6,171,599 (9 Jan 2001)
3. Otsuka M, Maeno Y, Fukami T, Inoue M, Tagami T, Ozeki T (2016) Solid dispersions of efonidipine hydrochloride ethanolate with improved physicochemical and pharmacokinetic properties prepared with microwave treatment. Eur J Pharm Biopharm 108(10):25–31
4. Huang S, Zhang Q, Li H, Sun Y, Cheng G, Zou M, Piao H (2018) Increased bioavailability of efonidipine hydrochloride nanosuspensions by the wet-milling method. Eur J Pharm Biopharm 130(9):108–114
5. Schilling SU, Shah NH, Malick AW, Infeld MH, McGinity JW (2007) Citric acid as a solid-state plasticizer for Eudragit RS PO. J Pharm Pharmacol 59(11):1493–1500
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