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

الملخص EN

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 (r>0.9932) with lower limits of quantitation (LLOQs) < 12 ng/mL.

The mean recoveries of the three analytes were higher than 75%.

The pharmacokinetics study indicated that the reduced absorption of ephedrine hydrochloride (EH) and pseudoephedrine hydrochloride (PEH) in honey-fried ephedra group might be the main reason for the moderation of the diaphoretic property.