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European Journal of Drug Metabolism and Pharmacokinetics

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01-08-2016 | Original Paper

A study on the PK and BA profiles in the mouse body for leonurine O/O microemulsion with determination by the LC-MS/MS method

Authors: Yanan Sun, Xiang Zhang, Tao Lu, Yuan Yuan, Qi Ding, Chuanhua Lu

Published in: European Journal of Drug Metabolism and Pharmacokinetics | Issue 4/2016

Abstract

Leonurine (LE) has been found to have therapeutic efficacy in cerebral thrombosis, but its poor solubility in water leads to very low bioavailability. In this article, a leonurine O/O microemulsion (LE-ME) was prepared and investigated for its in vivo pharmacokinetic behavior and bioavailability in the mouse body using an aqueous suspension of leonurine (LE-SWW) for the control group. A simple, sensitive and specific method, HPLC-MS/MS, was developed for detection of the LE content in mouse plasma using n-benzoyl-l-arginine ethyl ester as an internal standard. The results demonstrated that the C _max of LE-ME was 2.46-fold higher than that of the suspension following oral administration. The absolute bioavailability was 10.95 %, while that of the suspension was only 1.78 %. The T _1/2β and MRT of LE-ME were 3.04- and 4.19-fold those of the suspension, respectively. In addition, following intramuscular administration of LE-ME, the absolute bioavailability was 37.45 %. The results indicated that LE-ME is a promising drug-delivery system to enhance the absorption and bioavailability of LE.

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Title: A study on the PK and BA profiles in the mouse body for leonurine O/O microemulsion with determination by the LC-MS/MS method
Authors: Yanan Sun
Xiang Zhang
Tao Lu
Yuan Yuan
Qi Ding
Chuanhua Lu
Publication date: 01-08-2016
Publisher: Springer International Publishing
Published in: European Journal of Drug Metabolism and Pharmacokinetics / Issue 4/2016
Print ISSN: 0378-7966
Electronic ISSN: 2107-0180
DOI: https://doi.org/10.1007/s13318-015-0268-3

At a glance: The STEP trials

Springer Medicine

A study on the PK and BA profiles in the mouse body for leonurine O/O microemulsion with determination by the LC-MS/MS method

Abstract

At a glance: The STEP trials

Springer Medicine

Abstract

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