Comparative Pharmacokinetics and Bioavailability of Three Ephedrines in Rat after Oral Administration of Unprocessed and Honey-Fried Ephedra Extract by Response Surface Experimental Design

Ephedra have been used as a common traditional Chinese medicine for thousands of years. However, the perspiration effect of the unprocessed ephedra was too strong. Clinical trials have shown that processing methods play a critical role in moderating the perspiration property of ephedra according to the needs. A LC-MS/MS method was developed and validated to compare the pharmacokinetic properties of the three ephedrines after oral administration of unprocessed and honey-fried ephedra extract. The contents of honey, frying temperature, and frying time were set at 20%, 116°C, and 7 min by the Box-Behnken response surface method, respectively. In the pharmacokinetics study, the biosamples were pretreated and extracted by protein precipitation method with acetonitrile and separated on an Agilent TC-C18 column (250 mm × 4.6 mm, 5 μm) using a mobile phase consisting of 0.1% formic acid methanol and 5 mM ammonium acetate aqueous solution (5 : 95, v/v). All calibration curves were linear () with lower limits of quantitation (LLOQs)

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