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Cryptotanshinone (CTS), tanshinone IIA (Tan IIA), dihydrotanshinone I (diTan I), and tanshinone I (Tan I) are the main active compounds in the liposoluble extract of <jats:italic>Salvia miltiorrhiza.<\/jats:italic> The differences in the pharmacokinetic and tissue distribution behaviors of the four tanshinones after oral administration of the liposoluble extract of <jats:italic>Salvia miltiorrhiza<\/jats:italic> and pure compounds are not clear. This study aims to compare the pharmacokinetics and tissue distribution of the four tanshinones after oral administration of pure tanshinone monomers and the liposoluble extract of <jats:italic>Salvia miltiorrhiza.<\/jats:italic> An ultra\u2010performance liquid chromatography\u2013tandem mass spectrometry (UPLC\u2013MS\/MS) analysis method was developed for the determination of the four tanshinones. The results showed that the AUC and C<jats:sub>max<\/jats:sub> of tanshinones in rats receiving the extract of <jats:italic>Salvia miltiorrhiza<\/jats:italic> were significantly increased compared with those receiving the pure tanshinones. In the tissue distribution experiments, the AUC of the four tanshinones in the extract was much greater than the AUC of the monomers in the lung, heart, kidney, liver, and brain, and the coexisting constituents particularly promoted the distribution of tanshinones into tissues that the drug cannot sufficiently penetrate. These findings suggested that the coexisting constituents in the liposoluble extract of <jats:italic>Salvia miltiorrhiza<\/jats:italic> play an important role in the alteration of plasma concentration and tissue distribution of the four tanshinones. Understanding these differences could be of significance for the development and application of <jats:italic>Salvia miltiorrhiza<\/jats:italic> extract and tanshinone components.<\/jats:p>","DOI":"10.1002\/bdd.2213","type":"journal-article","created":{"date-parts":[[2020,1,15]],"date-time":"2020-01-15T12:38:19Z","timestamp":1579091899000},"page":"54-63","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":47,"title":["Comparative pharmacokinetics and tissue distribution of cryptotanshinone, tanshinone IIA, dihydrotanshinone I, and tanshinone I after oral administration of pure tanshinones and liposoluble extract of <i>Salvia miltiorrhiza<\/i> to rats"],"prefix":"10.1002","volume":"41","author":[{"given":"Daifei","family":"Wang","sequence":"first","affiliation":[{"name":"School of Pharmaceutical Sciences Sun Yat\u2010sen University  Guangzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Weibang","family":"Yu","sequence":"additional","affiliation":[{"name":"School of Pharmaceutical Sciences Sun Yat\u2010sen University  Guangzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lin","family":"Cao","sequence":"additional","affiliation":[{"name":"School of Pharmaceutical Sciences Sun Yat\u2010sen University  Guangzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Chuncao","family":"Xu","sequence":"additional","affiliation":[{"name":"School of Pharmaceutical Sciences Sun Yat\u2010sen University  Guangzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Guoyao","family":"Tan","sequence":"additional","affiliation":[{"name":"School of Pharmaceutical Sciences Sun Yat\u2010sen University  Guangzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Zhongxiang","family":"Zhao","sequence":"additional","affiliation":[{"name":"School of Chinese Materia Medica Guangzhou University of Chinese Medicine  Guangzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Min","family":"Huang","sequence":"additional","affiliation":[{"name":"School of Pharmaceutical Sciences Sun Yat\u2010sen University  Guangzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-7384-0092","authenticated-orcid":false,"given":"Jing","family":"Jin","sequence":"additional","affiliation":[{"name":"School of Pharmaceutical Sciences Sun Yat\u2010sen University  Guangzhou China"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2020,1,22]]},"reference":[{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.3390\/molecules21121630"},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.2174\/18715206113139990115"},{"key":"e_1_2_7_4_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ijcard.2007.01.004"},{"issue":"9","key":"e_1_2_7_5_1","first-page":"1531","article-title":"Systematic evaluation and analysis on Dao\u2010di Herbs Angelica Sinensis","volume":"20","author":"Liu F. 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