title: Pharmacokinetic comparisons of Paeoniflorin and Paeoniflorin-6'O-benzene sulfonate in rats via different routes of administration.
abstract: 1. The pharmacokinetics study of Paeoniflorin (Pae) and its acylated derivative (CP-25) was performed. 2. The structure of CP-25 was identified by mass spectrometry (MS) and nuclear magnetic resonance spectroscopy (NMR). The rats were injected with CP-25(6, 12, 24 mg/kg) and orally treated with CP-25 (32, 64, 128 mg/kg), respectively. An high-performance liquid chromatography (HPLC) assay was developed to determine the plasma concentrations of Pae and CP-25. 3. The results of MS and NMR showed that the acylated product was Pae-6'O-benzene sulfonate (CP-25). The plasma levels in oral CP-25 groups were detectable, whereas those of Pae in the oral groups (25 and 50 mg/kg) were undetectable. More specifically, the Cmaxvalues of oral CP-25 were 0.12, 0.19 and 0.44 μg/ml, and the corresponding t1/2βof CP-25 were 1.44, 2.12 and 2.11 h, respectively. In addition, the t1/2βvalues of intravenous CP-25 were 161.99, 152.81 and 153.76 min, respectively. 4. Compared with the venous pharmacokinetics parameters of Pae, those of the t1/2β, MRT, Vd and CL/F in the CP-25 groups increased noticeably. As expected, compared with oral parameters of Pae, those of t1/2a, t1/2β, AUC, MRT and Vd in the CP-25 group increased obviously. Finally, the absolute bioavailability of Pae and CP-25 were 3.6 and 10.6%, respectively. 5. Our results indicate that CP-25 is characterized by improved absorption, well distribution, lower clearance, long mean residence time, and moderate bioavailability in rats.
authors.affiliation: a Institute of Clinical Pharmacology, Anhui Medical University, Key Laboratory of anti-Inflammatory and Immune Medicine of the Education Ministry of China, Anhui Collaborative Innovation Center of anti-Inflammatory and Immune Medicine , Hefei , PR China.
authors.forename: Chun
authors.initials: C
authors.lastname: Wang
authors.affiliation: a Institute of Clinical Pharmacology, Anhui Medical University, Key Laboratory of anti-Inflammatory and Immune Medicine of the Education Ministry of China, Anhui Collaborative Innovation Center of anti-Inflammatory and Immune Medicine , Hefei , PR China.
authors.forename: Jun
authors.initials: J
authors.lastname: Yuan
authors.affiliation: a Institute of Clinical Pharmacology, Anhui Medical University, Key Laboratory of anti-Inflammatory and Immune Medicine of the Education Ministry of China, Anhui Collaborative Innovation Center of anti-Inflammatory and Immune Medicine , Hefei , PR China.
authors.forename: Ling Ling
authors.initials: LL
authors.lastname: Zhang
authors.affiliation: a Institute of Clinical Pharmacology, Anhui Medical University, Key Laboratory of anti-Inflammatory and Immune Medicine of the Education Ministry of China, Anhui Collaborative Innovation Center of anti-Inflammatory and Immune Medicine , Hefei , PR China.
authors.forename: Wei
authors.initials: W
authors.lastname: Wei
mesh_terms: D000818:Animals; D005960:Glucosides / Q000008:administration & dosage / Q000493:pharmacokinetics*; D039821:Monoterpenes / Q000008:administration & dosage / Q000493:pharmacokinetics*; D051381:Rats; D006027:Glycosides
chemical_list: D005960:Glucosides; D039821:Monoterpenes; C000610980:paeoniflorin-6'-O-benzenesulfonate; C015423:peoniflorin; D006027:Glycosides
keywords: Absorption; bioavailability; paeoniflorin; paeoniflorin-6'O-benzene sulfonate; pharmacokinetics