Plasma and urinary tanshinol from Salvia miltiorrhiza (Danshen) can be used as pharmacokinetic markers for cardiotonic pills, a cardiovascular herbal medicine
文献类型：期刊论文
| 作者 | Lu, Tong2; Yang, Junling ; Gao, Xiumei4; Chen, Ping; Du, Feifei; Sun, Yan; Wang, Fengqing; Xu, Fang; Shang, Hongcai4; Huang, Yuhong4
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| 刊名 | DRUG METABOLISM AND DISPOSITION
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| 出版日期 | 2008-08 |
| 卷号 | 36期号:8页码:1578-1586 |
| ISSN号 | 0090-9556 |
| DOI | 10.1124/dmd.108.021592 |
| 文献子类 | Article |
| 英文摘要 | Cardiotonic pills are a type of cardiovascular herbal medicine. To identify suitable pharmacokinetic (PK) marker(s) for indicating systemic exposure to cardiotonic pills, we examined the in vivo PK properties of putatively active phenolic acids from the component herb Danshen (Radix Salviae miltiorrhizae). We also performed in vitro and in silico assessments of permeability and solubility. Several phenolic acids were investigated, including tanshinol (TSL); protocatechuic aldehyde (PCA); salvianolic acids A, B, and D; rosmarinic acid; and lithospermic acid. Plasma TSL exhibited the appropriate PK properties in dogs, including dose-dependent systemic exposure in area under concentration-time curve (AUC) and a 0.5-h elimination half-life. In rats, more than 60% of i.v. TSL was excreted intact into the urine. In humans, we found a significant correlation between the urinary recovery of TSL and its plasma AUC. The absorption rate and bioavailability of TSL were not significantly different whether cardiotonic pills were given p.o. or sublingually. The gender specificity in plasma AUC disappeared after body-weight normalization, but the renal excretion of TSL was significantly greater in women than in men. PCA was predicted to be highly permeable according to in vitro and in silico studies; however, extensive presystemic hepatic elimination and degradation in the erythrocytes led to extremely low plasma levels and poor dose proportionality. Integrated in vivo, in vitro, and in silico studies on the other phenolic acids showed poor gut permeability and nearly undetectable levels in plasma and urine. In conclusion, plasma and urinary TSL are promising PK markers for cardiotonic pills at the tested dose levels. |
| WOS关键词 | ROSMARINIC ACID ; PROTOCATECHUIC ALDEHYDE ; MASS-SPECTROMETRY ; AQUEOUS EXTRACT ; RAT ; METABOLISM ; BIOAVAILABILITY ; PERMEABILITY ; ABSORPTION ; HUMANS |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000257829900018 |
| 出版者 | AMER SOC PHARMACOLOGY EXPERIMENTAL THERAPEUTICS |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/272849]  |
| 专题 | 上海药物代谢研究中心 科研与新药推进处 |
| 通讯作者 | Li, Chuan |
| 作者单位 | 1.Tianjin Inst Pharmaceut Res, Tianjin State Key Lab Pharmacodynam & Pharmacokin, Tianjin, Peoples R China 2.Chinese Acad Sci, Grad Sch, Shanghai 201203, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Ctr DMPK Res, SIBS, Shanghai 201203, Peoples R China; 4.Tianjin Univ Tradit Chinese Med, Tianjin, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Lu, Tong,Yang, Junling,Gao, Xiumei,et al. Plasma and urinary tanshinol from Salvia miltiorrhiza (Danshen) can be used as pharmacokinetic markers for cardiotonic pills, a cardiovascular herbal medicine[J]. DRUG METABOLISM AND DISPOSITION,2008,36(8):1578-1586. |
| APA | Lu, Tong.,Yang, Junling.,Gao, Xiumei.,Chen, Ping.,Du, Feifei.,...&Li, Chuan.(2008).Plasma and urinary tanshinol from Salvia miltiorrhiza (Danshen) can be used as pharmacokinetic markers for cardiotonic pills, a cardiovascular herbal medicine.DRUG METABOLISM AND DISPOSITION,36(8),1578-1586. |
| MLA | Lu, Tong,et al."Plasma and urinary tanshinol from Salvia miltiorrhiza (Danshen) can be used as pharmacokinetic markers for cardiotonic pills, a cardiovascular herbal medicine".DRUG METABOLISM AND DISPOSITION 36.8(2008):1578-1586. |
入库方式： OAI收割
来源：上海药物研究所
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