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| 1 | Combination of a biopharmaceutic classification system and physiologically based pharmacokinetic models to predict absorption properties of baicalein in vitro and in vivo显示文摘Objective: To determine the in vitro and in vivo absorption properties of active ingredients of the Chinese medicine, baicalein, to enrich mechanistic understanding of oral drug absorption.Methods: The Biopharmaceutic Classification System(BCS) category was determined using equilibrium solubility, intrinsic dissolution rate, and intestinal permeability to evaluate intestinal absorption mechanisms of baicalein in rats in vitro. Physiologically based pharmacokinetic(PBPK) model commercial software GastroPlus~(TM) was used to predict oral absorption of baicalein in vivo.Results: Based on equilibrium solubility, intrinsic dissolution rate, and permeability values of main absorptive segments in the duodenum, jejunum, and ileum, baicalein was classified as a drug with low solubility and high permeability. Intestinal perfusion with venous sampling(IPVS) revealed that baicalein was extensively metabolized in the body, which corresponded to the low bioavailability predicted by the PBPK model. Further, the PBPK model predicted the key indicators of BCS, leading to reclassification as BCS-II. Predicted values of peak plasma concentration of the drug(C_(max)) and area under the curve(AUC)fell within two times of the error of the measured results, highlighting the superior prediction of absorption of baicalein in rats, beagles, and humans. The PBPK model supported in vitro and in vivo evidence and provided excellent prediction for this BCS class II drug.Conclusion: BCS and PBPK are complementary methods that enable comprehensive research of BCS parameters, intestinal absorption rate, metabolism, prediction of human absorption fraction and bioavailability, simulation of PK, and drug absorption in various intestinal segments across species. This combined approach may facilitate a more comprehensive and accurate analysis of the absorption characteristics of active ingredients of Chinese medicine from in vitro and in vivo perspectives. | Yang Liu Jing Sun Linying Zhong Yu Li A Na Er Tong Li Le Yang Ling Dong | 2021 | Journal of Traditional Chinese Medical Sciences2021，8，3： | 2 |
| 2 | Effects of metal oproteinase inhibition in a murine model of renal ischemia-reperfusion injury显示文摘 | Novak KB Le HD Christison-Lagay ER | | 0，，03： | 1 |
| 3 | Correlates and heritability of nonalcoholic fatty liver disease in a minority cohort 显示文摘 | Wagenknecht LE Scherzinger AL Stamm ER | 2009 | Obesity ( Silver Spring)2009，17，6： | 1 |
| 4 | The spectrum of metabolic bone disease in lymphoblastic leukemia 显示文摘 | Cohn SL Morgan ER Mallette LE | 1987 | Cancer1987，59，2： | 1 |
| 5 | Colon cancer survival is associated with increasing number of lymph nodes analyzed: a secondary survey of intergroup trial INT-0089显示文摘 | Le VTE Sigurdson ER Hanlon AL | 2003 | Journal of clinical oncology : official journal of the American Society of Clinical Oncology2003，21，： | 1 |
| 6 | Colon cancer survival is associated with increasing number of lymph nodes analyzed:a secondary survey of intergroup trail INT-0089显示文摘 | Le Voyer TE sigurdson ER Hanlon AL | 2003 | J Clin Oncol2003，21，15： | 1 |
| 7 | Role of amlodipine in the mechanism if action of amlodipine:the PRAISE heart failure trial显示文摘 | Mohler ER Sorensen LE Ghali JK | | 0，，01： | 1 |
| 8 | Effects of metallopro- teinase inhibition in a murine model of renal ischemia-reperfusion in- jury 显示文摘 | Novak KB Le HD Christison-Lagay ER | 2010 | Pediatr Res2010，67，3： | 1 |
| 9 | Colon cancer survival is associated with increasing number of lymph nodes ana- lyzed : a secondary survey of intergroup trial INT - 0089 显示文摘 | Le Voyer TE Sigurdson ER Hanlon AL | 2003 | J Clin Oncol2003，21，15： | 1 |
| 10 | Pericardial effusions in pul- monary arterial hypertension characteristics, prognosis, and role of drainage显示文摘 | Fenstad ER Le RJ Sinak LJ | 2013 | Chest2013，144，5： | 1 |
| 11 | CHEMICAL INCORPORATING INSECTICIDES 1.SYNTHESIS OF NEWPYRETHROIDS WITH ORGANOPHOSPHATE AS POTENTIAL INSECTICIDES显示文摘CHEMICAL INCORPORATING INSECTICIDES 1.SYNTHESIS OF NEWPYRETHROIDS WITH ORGANOPHOSPHATE AS POTENTIAL INSECTICIDESCHEMICALINCOR... | Er Le ZANG Shi Yang XU Ping LI(Department of Applied Chemistry, Beijing Agricultural University, Beijing 100094) | 1995 | Chinese Chemical Letters1995，6，9： | 1 |
| 12 | Colon cancer survival is associated with increasing number of lymph nodes analyzed:a secondary survey of intergroup trial INT-0089显示文摘 | Le Voyer TE Sigurdson ER Hanlon AL | | 0，，15： | 1 |
| 13 | The spectrum of metabolic bone disease in lymphoblastic leukemia 显示文摘 | Cohn SL Morgan ER Mallette LE | 1987 | Cancer1987，59，2： | 1 |
| 14 | Cryobiopsy:should this be used in place of endobronchial forceps biopsies?显示文摘 | Rubio ER le SR Whatley RE | 2013 | Bio Med Research International2013，2013，73： | 1 |
| 15 | Colon cancer survival is associated with increasing number of lymph nodes analyzed: a secondary survey of intergroup trial INT-0089 显示文摘 | Le Voyer TEl Sigurdson ER Hanlon AL | 2003 | J Clin Oneol2003，21，15： | 1 |
| 16 | Preconception mental health predicts pregnancy complications and adverse birth outcomes:A National Population-Based Study显示文摘 | Witt WP Wisk LE Cheng ER | 2012 | Matern Child Health J2012，16，7： | 1 |
| 17 | Poor prepregnancy and antepartum mental health predicts postpartum mental health problems among US women:A nationally representative population-based study显示文摘 | Witt WP Wisk LE Cheng ER | 2011 | Womens Health Issues2011，21，： | 1 |
| 18 | Colon cancer survival is associated with increasing number of lymph nodes analyzed: a secondary survey of intergroup trial INT -0089 显示文摘 | Le voyer TE Sigurdson ER Hanlon AL | 2003 | J Clin Oncol2003，21，15： | 1 |
| 19 | Minimal criteria for defining multipotent mesenchymal stromal cel s:the International Society for Cel ular Therapy position statement显示文摘 | Dominici M Le Blanc K Muel er I | | 0，，： | 1 |
| 20 | Colon cancer survival is associated with increasing number of lymph nodes analyzed:a secondary survey of intergroup trial INT-0089显示文摘 | Le Voyer TE Sigurdson ER Hanlon AL | 2003 | J Clin Oncol2003，21，15： | 1 |
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