Pharmacokinetic alteration of baclofen by multiple oral administration of herbal medicines in rats

Tae Hwan Kim, Gi Young Park, Soyoung Shin, Dong Rak Kwon, Won Sik Seo, Jeong Cheol Shin, Jin Ho Choi, Sang Hoon Joo, Kwon Yeon Weon, Byung Sun Min, Kyung Min Baek, Mahesh Upadhyay, Bing Tian Zhao, Mi Hee Woo, So Hee Kwon, Beom Soo Shin

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9 Citations (Scopus)


The potential pharmacokinetic (PK) interaction of conventional western drug, baclofen, and oriental medications Oyaksungisan (OY) and Achyranthes bidentata radix (AB) extract for the treatment of spasticity has been evaluated. Rats were pretreated with distilled water (DW), OY, or AB extract by oral administration every day for 7 days. After 10 min of the final dose of DW or each herbal medication, baclofen (1 mg/kg) was given by oral administration and plasma concentrations of baclofen were determined by LC/MS/MS. The plasma baclofen concentration-time profiles were then analyzed by noncompartmental analysis and a population PK model was developed. Baclofen was rapidly absorbed, showed biexponential decline with elimination half-life of 3.42-4.10 hr, and mostly excreted into urine. The PK of baclofen was not affected by AB extract pretreatment. However, significantly lower maximum plasma concentration (C max) and longer time to reach C max (T max) were observed in OY pretreated rats without changes in the area under the curve (AUC) and the fraction excreted into urine (F urine). The absorption rate (K a) of baclofen was significantly decreased in OY pretreated rats. These data suggested that repeated doses of OY might delay the absorption of baclofen without changes in extent of absorption, which needs further evaluation for clinical significance.

Original languageEnglish
Article number402126
JournalEvidence-based Complementary and Alternative Medicine
Publication statusPublished - 2014

Bibliographical note

Publisher Copyright:
© 2014 Tae Hwan Kim et al.

All Science Journal Classification (ASJC) codes

  • Complementary and alternative medicine


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