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Effect of amoxicillin on the expression of PEPT1 and pharmacokinetics upon acute hypoxia at high altitude in rat
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Bing-feng LUO1, 3, Jun ZHANG1, Tao YANG2, Juan-hong ZHANG1, Wen-bin LI1, Chang WANG1, Ming-xia ZHANG1, 3, Rong WANG1, 3, *
Acta Pharmaceutica Sinica | 2017, 52(11) : 1715 - 1721
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Acta Pharmaceutica Sinica | 2017, 52(11): 1715-1721
• ORIGINAL ARTICLES •
Effect of amoxicillin on the expression of PEPT1 and pharmacokinetics upon acute hypoxia at high altitude in rat
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Bing-feng LUO1, 3, Jun ZHANG1, Tao YANG2, Juan-hong ZHANG1, Wen-bin LI1, Chang WANG1, Ming-xia ZHANG1, 3, Rong WANG1, 3, *
Affiliations
  • 1. PLA Key Laboratory of the Plateau of the Environmental Damage Control, Lanzhou General Hospital, Lanzhou Command, Lanzhou 730050, China
  • 2. Department of Pharmacy, Gansu Provincial Maternity and Child Care Hospital, Lanzhou 730050, China
  • 3. School of Pharmacy, Lanzhou University, Lanzhou 730000, China
Published: 2017-11-12 doi: 10.16438/j.0513-4870.2017-0562
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The relationship between PEPT1 (peptide transporter) and drug efficacy has drawn more and more attention in the treatment of disease. PEPT1 represents a promising strategy for improvement of drug bioavailability and an important starting point for clinical rationalization of drug selection. The effect of PEPT1 on transport and pharmacokinetics of amoxicillin was investigated under hypoxia condition at high altitude in rat. The mRNA and protein expressions of PEPT1 were increased by 36.87%, 216.21%, 577.8% and 535.9% respectively in the hypoxia group in the small intestine and kidney of rats. However, the mRNA and protein expressions of PEPT1 were reduced by 43.90% and 84.7% in the liver. Compared with the control group, the AUC, tmax, Cmax, MRT and t1/2 of amoxicillin were significantly enhanced by 312.17%, 63.04%, 110.93%, 67.11% and 16.96% respectively in the hypoxia group, while the CL was significantly decreased by 74.51%. After acute exposure to high altitude, the expressions of drug transporter PEPT1 were distinctly changed in rat tissues, which can affect the pharmacokinetics of amoxicillin.

acute hypoxia at high altitude  /  peptide transporter  /  expression change  /  amoxicillin  /  pharmacokinetics
Bing-feng LUO, Jun ZHANG, Tao YANG, Juan-hong ZHANG, Wen-bin LI, Chang WANG, Ming-xia ZHANG, Rong WANG. Effect of amoxicillin on the expression of PEPT1 and pharmacokinetics upon acute hypoxia at high altitude in rat[J]. Acta Pharmaceutica Sinica, 2017 , 52 (11) : 1715 -1721 . DOI: 10.16438/j.0513-4870.2017-0562
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Article Info
doi: 10.16438/j.0513-4870.2017-0562
  • Receive Date：2017-06-11
  • Online Date：2026-01-14
  • Published：2017-11-12
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History
  • Received：2017-06-11
  • Revised：2017-08-31
Funding
Affiliations
    1. PLA Key Laboratory of the Plateau of the Environmental Damage Control, Lanzhou General Hospital, Lanzhou Command, Lanzhou 730050, China
    2. Department of Pharmacy, Gansu Provincial Maternity and Child Care Hospital, Lanzhou 730050, China
    3. School of Pharmacy, Lanzhou University, Lanzhou 730000, 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
species (%)
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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