Authors:Youjiu Zhang, Yujie Xu, Ran Zhu, Mingjiang Hu, Jianxiang Li, Yuejin Chen, Daojin Wang and Wo Fan
This study examined the tissues distribution and pharmacokinetics of rhTNT-IL2, a fusion protein, in rats and macaques after
iv. injection. The rhTNT-IL2 was labeled with 125I. The 125I-rhTNT-IL2 was administered into rats and macaques at a dose of 250 μg·kg−1 and 125 μg·kg−1, respectively. Upon administration, rhTNT-IL2 declined in tri-exponentially with the half-lives of 1.78 h (T1/2α), 25.06 h (T1/2β), 114.19 h (T1/2γ) for rats and 1.87 h (T1/2α), 9.82 h (T1/2β), 43.17 h (T1/2γ) for macaques. The fraction of 125I-rhTNT-IL2 excreted in feces was low (about 1%), while the majority of 125I-rhTN-IL2 was excreted in urine. The tissue distributions showed that the liver, spleen and heart were major organs for deposition
of the fusion protein in rats and macaques in 48-hour post-injection, and the fusion protein could not penetrate through blood
Palmatine is a compound with good water solubility extracted from Coptis chinensis, Fibraurea recisa Pierre, Cortex Phellodendri Chinensis. Palmatine has good antibacterial activity and mainly used for the treatment of bacterial dysentery, gynecological inflammation, surgical infection, and conjunctivitis. It has anti-diabetic, anti-oxidant, and cognitive-enhancing activities. In this study, we used UPLC-MS/MS to determinate palmatine in rat plasma, and investigated its pharmacokinetics. Coptisine was utilized as an internal standard (IS), and acetonitrile precipitation method was used to process the plasma samples. Chromatographic separation was achieved using a UPLC BEH C18 column using mobile phase of acetonitrile- 0.1% formic acid with gradient elution. Electrospray ionization (ESI) tandem mass spectrometry in multiple reaction monitoring (MRM) mode with positive ionization was applied. The results indicated that within the range of 1–500 ng/mL, linearity of palmatine in rat plasma was acceptable (r > 0.995), and the lower limit of quantification (LLOQ) was 1 ng/mL. Intra-day and inter-day precision RSD of palmatine in rat plasma were less than 14%. Accuracy range was between 93.7 and 107.1%, and matrix effect was between 101.6 and 109.4%. The method was successfully applied in the pharmacokinetics of palmatine in rats after oral and intravenous administration. The absolute bioavailability of the palmatine was 15.5% in rats.
Authors:Jianbo Li, Zheng Yu, Cheng Han, Zhening Wang, Yujie Hu, Congcong Wen and Chongliang Lin
In this study, we used UPLC–MS/MS to determine diosmetin-7-o-β-d-glucoside in rat plasma and investigated its pharmacokinetics in rats. Six rats were given diosmetin-7-o-β-d-glucoside (5 mg/kg) by intravenous (i.v.) administration. The blood (150 μL) was withdrawn from the caudal vein after administration. Diazepam was used as an internal standard (IS), and a one-step acetonitrile precipitation method was used to process the plasma samples. Chromatographic separation was achieved using a UPLC BEH C18 column using a mobile phase of acetonitrile–0.1% formic acid with gradient elution. Electrospray ionization (ESI) tandem mass spectrometry in multiple reaction monitoring (MRM) mode with positive ionization was applied, 463.1 → 301.0 for diosmetin-7-o-β-d-glucoside, m/z 285.1 → 193.0 for diazepam (IS). Intra-day and inter-day precision of diosmetin-7-o-β-d-glucoside in rat plasma were less than 14%. The method was successfully applied in the pharmacokinetics of diosmetin-7-o-β-d-glucoside in rats after intravenous administration. The t1/2 of diosmetin-7-o-β-d-glucoside is 1.4 ± 0.4 h, which indicates the quick elimination.