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Analysis of five active ingredients of Er‐Zhi‐Wan, a traditional Chinese medicine water‐honeyed pill, using the biopharmaceutics classification system
Author(s) -
Cao Xuexiao,
Li Huanhuan,
Wang Meng,
Ren Xiaoliang,
Deng Yanru
Publication year - 2020
Publication title -
biomedical chromatography
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.4
H-Index - 65
eISSN - 1099-0801
pISSN - 0269-3879
DOI - 10.1002/bmc.4757
Subject(s) - biopharmaceutics classification system , chemistry , biopharmaceutics , bioavailability , in vivo , drug , chromatography , active ingredient , pharmacology , oleanolic acid , traditional medicine , pharmacognosy , medicine , in vitro , biochemistry , biological activity , alternative medicine , microbiology and biotechnology , pathology , biology
Er‐Zhi‐Wan (EZW) is a traditional Chinese medicine with many clinical applications and used as a health product in East Asia. Five active ingredients (salidroside, specnuezhenide, nuezhenoside, luteolin, and oleanolic acid) were screened out from EZW to develop an in vitro rapid evaluation method for the classification of in vivo drug absorption behavior by biopharmaceutics classification system (BCS). Ultra‐performance liquid chromatography was used for quantitative analysis. Solubility and permeability were assayed by equilibrium solubility and multiple models: everted rat intestinal sac model, cultured Caco‐2 cells, octanol–water partition coefficient (Log P ) method. The BCS properties of drugs were predicted using software applications, and the correlations of measured and predicted values of factors affecting oral drug absorption were calculated. The results were verified by measuring the absolute bioavailability of the active ingredients. Salidroside, specnuezhenide, and nuezhenoside were classified as BCS class III drugs, and luteolin was classified as a BCS class III/I drug because of the difference in Log P and intestinal permeability. Oleanolic acid was classified as a BCS class II/IV drug in acidic media and BCS class I/III drug in other media. Overall, EZW may be classified as a BCS class III drug, and permeability was identified as the primary factor limiting absorption. The results provide a novel method for the evaluation of the in vivo absorption of oral traditional Chinese medicines.