Crystal form Analysis of Felodipine and Its Preparations / 中国药学杂志

ABSTRACT

OBJECTIVE: To clarify the crystal forms of the active pharmaceutical ingredient and preparations of felodipine from different sources, and explore the relationship between quality and efficacy of felodipine and its crystal form. METHODS: Crystal form characterization of the active pharmaceutical ingredient from different sources was carried out by powder X-ray diffraction (PXRD), infrared spectroscopy (IR) and differential scanning calorimetry (DSC). The Origin software was used to analyze the crystal forms of felodipine in the sample preparations from different sources. Biological evaluation in vivo was conducted by using whole animals. RESULTS: There were some differences in the crystal state of the active pharmaceutical ingredient from different sources, but the main components were basically the same, all of which were type I. Biological studies showed significant differences in the main pharmacokinetic parameters of felodipine sustained release tablets from different sources. Among them, the ρmax, tmax, t1/2, and AUC0-t had maximal 1.8, 1.4, 8.2 and 1.5 times of differences. CONCLUSION: Although the main crystal forms of felodipine bulk drug from different origins are consistent, the crystal state significantly changes after the preparation process. This finding is of important scientific significance to guide the improvement of process and product quality.