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Effect of molecular weight of polyethylene glycol on pharmacokinetics of baicalin
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Ming-hao ZHOU1, 3, Min ZHANG1, Shuo ZHANG2, Peng-jiao WANG1, Xiao-xia MENG1, 3, Si-yuan CAO1, 3, Qi-mei YANG1, 3, Xiu-li GAO1, 3, *
Acta Pharmaceutica Sinica | 2021, 56(5) : 1416 - 1423
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Acta Pharmaceutica Sinica | 2021, 56(5): 1416-1423
• Original Articles •
Effect of molecular weight of polyethylene glycol on pharmacokinetics of baicalin
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Ming-hao ZHOU1, 3, Min ZHANG1, Shuo ZHANG2, Peng-jiao WANG1, Xiao-xia MENG1, 3, Si-yuan CAO1, 3, Qi-mei YANG1, 3, Xiu-li GAO1, 3, *
Affiliations
  • 1. State Key Laboratory of Functions and Applications of Medicinal Plants and School of Pharmacy, Guizhou Medical University, Guiyang 550025, China
  • 2. Experimental Animal Center of Guizhou Medical University, Guiyang 550025, China
  • 3. Center of Microbiology and Biochemical Pharmaceutical Engineering, Guizhou Medical University, Guiyang 550025, China
Published: 2021-05-12 doi: 10.16438/j.0513-4870.2020-1688
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The aim of this study was to investigate the effects of polyethylene glycol (PEGs) with different molecular weights (MW: 400, 1 000, 4 000) on the pharmacokinetics of baicalin, and preliminarily analyze its mechanism. Rats were gavaged with baicalin (168 mg·kg-1) + aqueous solution or baicalin + PEGs solution and plasma samples were collected from 0 to 24 h after administration. The concentration of baicalin and its main metabolite baicalein 6-O-β-D-glucuronide (B6G) were determined at different time points by UPLC-MS/MS, and the pharmacokinetic parameters were calculated with DAS 3.0 software. The results showed that PEGs with different molecular weights could effectively increase the AUC0-t of baicalin and B6G, increase the Cmax, and prolong the t1/2, effectively increasing the concentration of baicalin and B6G in vivo. The mechanism may be by promoting the activity of uridine diphosphate glucuronosyl-transferases 1A8 (UGT1A8) and 1A9 (UGT1A9), thereby increasing the transformation rate of baicalin and B6G. The rate of metabolism of B6G was faster than that of baicalin, suggesting that PEGs had a higher affinity for UGT1A8, and PEG400 had the most significant effect. The purpose of this study was to provide a basis for the clinical safe use of baicalin and other flavonoids and the design of new dosage forms with the participation of PEGs. The animal experiment protocol in this study was approved by the Experimental Animal Ethics Committee of Guizhou Medical University.

polyethylene glycol  /  baicalin  /  baicalein 6-O-β-D-glucuronide  /  uridine diphosphate glucuronosyl-transferases 1A8  /  uridine diphosphate glucuronosyl-transferases 1A9  /  pharmacokinetics
Ming-hao ZHOU, Min ZHANG, Shuo ZHANG, Peng-jiao WANG, Xiao-xia MENG, Si-yuan CAO, Qi-mei YANG, Xiu-li GAO. Effect of molecular weight of polyethylene glycol on pharmacokinetics of baicalin[J]. Acta Pharmaceutica Sinica, 2021 , 56 (5) : 1416 -1423 . DOI: 10.16438/j.0513-4870.2020-1688
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Article Info
doi: 10.16438/j.0513-4870.2020-1688
  • Receive Date：2020-11-03
  • Online Date：2025-12-18
  • Published：2021-05-12
Article Data
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History
  • Received：2020-11-03
  • Revised：2021-02-03
Funding
Affiliations
    1. State Key Laboratory of Functions and Applications of Medicinal Plants and School of Pharmacy, Guizhou Medical University, Guiyang 550025, China
    2. Experimental Animal Center of Guizhou Medical University, Guiyang 550025, China
    3. Center of Microbiology and Biochemical Pharmaceutical Engineering, Guizhou Medical University, Guiyang 550025, China
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
Genus		 种数
Number of
species		 占总种数比例
Percentage of total
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鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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