Bioavailability and pharmacokinetic comparison of tanshinones between two formulations of Salvia miltiorrhiza in healthy volunteers

Abstract Salvia miltiorrhiza (SM) is widely used to treat microcirculatory disturbance-related diseases; its lipophilic components play important roles in this application. Cryptotanshinone (CTS), tanshinone I (TSI) and tanshinone IIA (TSA) are the most widely-studied lipophilic ingredients, but low...

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Autores principales: Lu Xing, Zhi-Rong Tan, Jin-Le Cheng, Wei-Hua Huang, Wei Zhang, Wen Deng, Chun-Su Yuan, Hong-Hao Zhou
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Publicado: Nature Portfolio 2017
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spelling oai:doaj.org-article:88153701f68a45cf93eef459b149d1792021-12-02T15:06:16ZBioavailability and pharmacokinetic comparison of tanshinones between two formulations of Salvia miltiorrhiza in healthy volunteers10.1038/s41598-017-02747-42045-2322https://doaj.org/article/88153701f68a45cf93eef459b149d1792017-07-01T00:00:00Zhttps://doi.org/10.1038/s41598-017-02747-4https://doaj.org/toc/2045-2322Abstract Salvia miltiorrhiza (SM) is widely used to treat microcirculatory disturbance-related diseases; its lipophilic components play important roles in this application. Cryptotanshinone (CTS), tanshinone I (TSI) and tanshinone IIA (TSA) are the most widely-studied lipophilic ingredients, but low oral bioavailability limits their clinical application. It has been proven that micronization could improve the bioavailability of some drugs, so we’ve conducted this randomized study to investigate whether micronized granular powder (GP) of SM could improve the bioavailability of tanshinones compared with traditional decoction (TD). An oral dose of TD or GP of SM was administrated to subjects and blood samples were collected at predetermined time points. The plasma concentrations of tanshinones were detected by a validated method and pharmacokinetic parameters were calculated using a non-compartmental model. GP of SM resulted in a significant increase in mean maximum plasma concentration (C max ), elimination half-life and area under concentration-time curve (AUC) of tanshinones, with the plasma AUC of CTS, TSI and TSA in GP 5–184, 4–619 and 5–130 times higher than TD. In addition, the individual variances of C max and AUC were much lower after GP administration. Summarily, tanshinones in micronized GP of SM had higher oral bioavailability and lower individual variances, thus we speculate that it may indicate a better clinical efficacy and be a better choice than current treatments.Lu XingZhi-Rong TanJin-Le ChengWei-Hua HuangWei ZhangWen DengChun-Su YuanHong-Hao ZhouNature PortfolioarticleMedicineRScienceQENScientific Reports, Vol 7, Iss 1, Pp 1-10 (2017)
institution DOAJ
collection DOAJ
language EN
topic Medicine
R
Science
Q
spellingShingle Medicine
R
Science
Q
Lu Xing
Zhi-Rong Tan
Jin-Le Cheng
Wei-Hua Huang
Wei Zhang
Wen Deng
Chun-Su Yuan
Hong-Hao Zhou
Bioavailability and pharmacokinetic comparison of tanshinones between two formulations of Salvia miltiorrhiza in healthy volunteers
description Abstract Salvia miltiorrhiza (SM) is widely used to treat microcirculatory disturbance-related diseases; its lipophilic components play important roles in this application. Cryptotanshinone (CTS), tanshinone I (TSI) and tanshinone IIA (TSA) are the most widely-studied lipophilic ingredients, but low oral bioavailability limits their clinical application. It has been proven that micronization could improve the bioavailability of some drugs, so we’ve conducted this randomized study to investigate whether micronized granular powder (GP) of SM could improve the bioavailability of tanshinones compared with traditional decoction (TD). An oral dose of TD or GP of SM was administrated to subjects and blood samples were collected at predetermined time points. The plasma concentrations of tanshinones were detected by a validated method and pharmacokinetic parameters were calculated using a non-compartmental model. GP of SM resulted in a significant increase in mean maximum plasma concentration (C max ), elimination half-life and area under concentration-time curve (AUC) of tanshinones, with the plasma AUC of CTS, TSI and TSA in GP 5–184, 4–619 and 5–130 times higher than TD. In addition, the individual variances of C max and AUC were much lower after GP administration. Summarily, tanshinones in micronized GP of SM had higher oral bioavailability and lower individual variances, thus we speculate that it may indicate a better clinical efficacy and be a better choice than current treatments.
format article
author Lu Xing
Zhi-Rong Tan
Jin-Le Cheng
Wei-Hua Huang
Wei Zhang
Wen Deng
Chun-Su Yuan
Hong-Hao Zhou
author_facet Lu Xing
Zhi-Rong Tan
Jin-Le Cheng
Wei-Hua Huang
Wei Zhang
Wen Deng
Chun-Su Yuan
Hong-Hao Zhou
author_sort Lu Xing
title Bioavailability and pharmacokinetic comparison of tanshinones between two formulations of Salvia miltiorrhiza in healthy volunteers
title_short Bioavailability and pharmacokinetic comparison of tanshinones between two formulations of Salvia miltiorrhiza in healthy volunteers
title_full Bioavailability and pharmacokinetic comparison of tanshinones between two formulations of Salvia miltiorrhiza in healthy volunteers
title_fullStr Bioavailability and pharmacokinetic comparison of tanshinones between two formulations of Salvia miltiorrhiza in healthy volunteers
title_full_unstemmed Bioavailability and pharmacokinetic comparison of tanshinones between two formulations of Salvia miltiorrhiza in healthy volunteers
title_sort bioavailability and pharmacokinetic comparison of tanshinones between two formulations of salvia miltiorrhiza in healthy volunteers
publisher Nature Portfolio
publishDate 2017
url https://doaj.org/article/88153701f68a45cf93eef459b149d179
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