HPLC method with fluorescence detection for the determination of ligustilide in rat plasma and its pharmacokinetics

Abstract

Context: Few methods have been reported for the quantification of ligustilide (LIG) in biosamples: the pretreatment of the biological samples were laborious and time-consuming. Objective: A high-performance liquid chromatographic method with fluorescence detection (HPLC-FLD) for the determination of LIG in rat plasma was developed and validated. Pharmacokinetics and bioavailability of LIG were determined by systematic investigation in Sprague-Dawley rats. Materials and methods: LIG was isolated from the volatile oil of Radix Angelica sinensis and further purified by silica gel column chromatography. Podophyllotoxin was used as an internal standard. The analytes were detected by using fluorescence detection at an excitation and emission wavelength of 290 and 395 nm during 0-4 min, and 336 and 453 nm during 4-14 min, respectively. LIG pharmacokinetics was studied in rats after oral and intravenous administration of 12.5, 25 and 50 mg/kg doses. Results: Two calibration curves (Y ¼ 133.49 X À 14.27 (r ¼ 0.9995), Y ¼ 145.61 X þ 13.76 (r ¼ 0.9996)) were constructed in the range of 2.44-10 000 ng/mL for LIG with a lower limit of quantitation of 2.44 ng/mL. Both intra-day and inter-day precision were less than 6%. Accuracy ranged from 88.93 to 99.52%. The recovery ranged from 89.07 to 99.71%. The absolute bioavailability values were 71.36, 68.26 and 75.44% for oral doses of 12.5, 25 and 50 mg/kg, respectively. Conclusion: The present HPLC-FLD method was rapid, sensitive and reliable. LIG was absorbed and eliminated rapidly in rat.

Z-ligustilide and n-Butylidenephthalide Isolated from the Aerial Parts of Angelica tenuissima Inhibit Lipid Accumulation In Vitro and In Vivo

“…In this study, we found that the plasma concentrations of the active ingredients of the ATX extracts, namely Z-ligustilide, n-butylidenephthalide, chlorogenic acid, and ferulic acid, were below the detection limit after 24 h of the oral administration in mice. The low concentration of the ingredients may be attributed, at least in part, to their short biological half-lives (i.e., [the half-life determined in rats] Z-ligustilide, 3.02-6.90 h [33]; n-butylidenephthalide, 3.54 h [34]; chlorogenic acid, 1.70 h [35]; ferulic acid, 0.618-0.885 h [36]). In addition to the rapid disappearance, the lack of proper exposure (i.e., low oral bioavailability) may be contributed to the difficulty in the detection.…”

Pharmacokinetics of Anthraquinones from Medicinal Plants

“…Glucuronic acid and sulfuric acid conjugates of rhein are dominant in urine and fecal excreta. Only 20% of the prototype rhein is excreted in urine and feces (Wan et al, 2013).…”

Quality assessment and traceability study of Angelicae Sinensis Radix via binary chromatography, triple quadrupole tandem mass spectrometry, and multivariate statistical analysis

“…Traditionally, ASR can be distinguished by experienced Danggui farmers [12], but this method is obviously dependent on highly subjective judgments and lacks of universality. On the other hand, thin layer chromatography, HPLC, CE-DAD, GC-MS, LC-MS analytical methods are used to discriminate ASR [13][14][15][16][17]. Although these methods have made significant contributions to the progress of quality control of ASR, however, they cannot effectively distinguish the geographic origin of ASR due to insufficient compound information.…”