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Assessment strategies for drug permeability during drug discovery and development
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Wen-qian LI, Jing-jing HAN, Xian ZHANG, Run-ze XU, Jin YANG*
Acta Pharmaceutica Sinica | 2021, 56(5) : 1279 - 1285
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Acta Pharmaceutica Sinica | 2021, 56(5): 1279-1285
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Assessment strategies for drug permeability during drug discovery and development
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Wen-qian LI, Jing-jing HAN, Xian ZHANG, Run-ze XU, Jin YANG*
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  • Center of Drug Metabolism and Pharmacokinetics, School of Pharmaceutical Sciences, China Pharmaceutical University, Nanjing 210009, China
Published: 2021-05-12 doi: 10.16438/j.0513-4870.2021-0102
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Permeability is a key factor in the bioavailability of oral drugs. Therefore, in the early stage of drug discovery, accurate and efficient evaluation of drug permeability is essential. The parallel artificial membrane permeability assay (PAMPA) with Caco-2 cells model was used by the industry as early evaluation methods. At present, the Ussing chamber rat model is also widely used. This review summarizes the human data for the in vivo single-pass perfusion technique (Loc-I-Gut)-the gold standard, and then focuses on the basic principles, experimental operation, and efficiency of the three in vitro methods, with correlation to the effective permeability coefficient (Peff) and fractional absorbed (Fa) in man. We provide recommendations for the use of proper permeability methods at different stages in drug discovery and development.

oral drug  /  permeability  /  parallel artificial membrane permeability assay  /  Caco-2  /  Ussing chamber  /  effective permeability coefficient  /  fraction absorbed
Wen-qian LI, Jing-jing HAN, Xian ZHANG, Run-ze XU, Jin YANG. Assessment strategies for drug permeability during drug discovery and development[J]. Acta Pharmaceutica Sinica, 2021 , 56 (5) : 1279 -1285 . DOI: 10.16438/j.0513-4870.2021-0102
Year 2021 volume 56 Issue 5
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doi: 10.16438/j.0513-4870.2021-0102
  • Receive Date:2021-01-18
  • Online Date:2025-12-18
  • Published:2021-05-12
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  • Received:2021-01-18
  • Revised:2021-02-28
Affiliations
    Center of Drug Metabolism and Pharmacokinetics, School of Pharmaceutical Sciences, China Pharmaceutical University, Nanjing 210009, China
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表12种不同金属材料的力学参数

Family
属数
Number of
genus
种数
Number of
species
占总种数比例
Percentage of
total species (%)

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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