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


ABSTRACT: 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.

SUBMITTER: Kim TH 

PROVIDER: S-EPMC4229966 | biostudies-literature | 2014

REPOSITORIES: biostudies-literature

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

Kim Tae Hwan TH   Park Gi-Young GY   Shin Soyoung S   Kwon Dong Rak DR   Seo Won Sik WS   Shin Jeong Cheol JC   Choi Jin Ho JH   Joo Sang Hoon SH   Weon Kwon-Yeon KY   Min Byung Sun BS   Baek Kyung Min KM   Upadhyay Mahesh M   Zhao Bing Tian BT   Woo Mi Hee MH   Kwon So Hee SH   Shin Beom Soo BS  

Evidence-based complementary and alternative medicine : eCAM 20141029


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 det  ...[more]

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