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Pharmacokinetics of baicalin nanosuspension in rats
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DOI   10.11656/j.issn.1672-1519.2018.07.16
Key Words   baicalin;nanoparticle;LC-MS/MS;rat;pharmacokinetics
Author NameAffiliationE-mail
LU Peng Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China
Tianjin State Key Laboratory of Modern Chinese Medicine-Province and Ministry Co-established State Key Laboratory Cultivation Base, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China 
 
MAIKHONE VILAKHAMXAY Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China
Tianjin State Key Laboratory of Modern Chinese Medicine-Province and Ministry Co-established State Key Laboratory Cultivation Base, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China 
 
REN Jing Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China
Tianjin State Key Laboratory of Modern Chinese Medicine-Province and Ministry Co-established State Key Laboratory Cultivation Base, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China 
 
XING Yue Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China
Tianjin State Key Laboratory of Modern Chinese Medicine-Province and Ministry Co-established State Key Laboratory Cultivation Base, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China 
 
WANG Shuya Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China
Tianjin State Key Laboratory of Modern Chinese Medicine-Province and Ministry Co-established State Key Laboratory Cultivation Base, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China 
 
XUE Zhifeng Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China
Tianjin State Key Laboratory of Modern Chinese Medicine-Province and Ministry Co-established State Key Laboratory Cultivation Base, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China 
 
LIU Zhidong Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China
Tianjin State Key Laboratory of Modern Chinese Medicine-Province and Ministry Co-established State Key Laboratory Cultivation Base, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China 
lonerliuzd@163.com 
Abstract
    [Objective] To establish a liquid chromatography-mass spectrometry (LC-MS/MS) method to evaluate its pharmacokinetics in rats.[Methods] ALC-MS/MS method that column of Waters ACQUITY UPLC-HSS C18(1.8 μm, 2.1 mm×50 mm)and a mixture of 0.1% formic acid water solution (A)-acetonitrile (B) as the mobile phase at the flow-rate of 0.3 mL/min, the column temperature was 30℃ and the injection volume was 5 μL. Carbamazepine was used as the internal standard, detection was by postive ion electrospray ionization (ESI) mass spectrometry with multiple-reaction monitoring (MRM). Detection of ion pairs respectively are m/z 447.09→270.80 for baicalin, m/z 237.10→193.80 for carbamazepine employed to determine the concentration of baicalin in plasma by oral administration in rats and the pharmacokinetics software of WinNonlin version 6.0 was used to calculate the pharmacokinetics parameters.[Results] The linear calibration curves were obtained over the concentration range 24.75~4 950.00 ng/mL. Endogenous substances in the plasma did not interfere with the determination, the recovery rate, matrix effect, precision, accuracy and stability of the method are in accordance with the requirements of biological samples. The Cmax of BL-NSPS and BL-Bulk were (3 329.10±499.10) ng/mL and (1 257.84 ±158.21) ng/mL, respectively. The Cmax of BL-NSPS was significantly higher than that of BL-Bulk (P<0.05), and the relative bioavailability of BL-NIPS was (160.97±47.78)%.[Conclusion] The LC-MS/MS method has high accuracy and specificity, and can be used to detect the pharmacokinetics of baicalin. What's more, the experimental results show that baicalin nanosuspensions can increase the absorption rate of drugs, shorten the onset time of the drugs, improve the bioavailability of the drug in vivo and lay a foundation for the further development of baicalin preparation.

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