大川芎方多元释药系统的体外释药特征和大鼠体内药动学研究
Release characteristics in vitro and pharmacokinetics of Da Chuanxiong Fang multiunit drug delivery system in rats
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摘要:
本文评价了大川芎方多元释药系统 (Da Chuanxiong Fang multiunit drug delivery system, DCXFMDDS) 体内外释药特点。以已知的有效成分阿魏酸 (ferulic acid, FA) 与洋川芎内酯I (senkyunolide I, SI) 为指标成分, 采用HPLC法测定其含量, 比较了DCXFMDDS与大川芎片的体外释药特征, 以及与大川芎方效应组分 (Da Chuanxiong Fang active fraction, DCXFAF) 的大鼠体内药动学特征。结果表明, DCXFMDDS中FA在体内外具有明显的缓释作用, 而SI在体内外均能快速释药, 两种物质体外释药特征及其机制均不相同, 但体内吸收程度 (以AUC表征) 均好于DCXFAF组。DCXFMDDS改变了不同化学成分在体内外释药特征, 可能是其起效快、药效好、药效维持时间长的原因之一。
Abstract:The drug release characteristics of Da Chuanxiong Fang multiunit drug delivery system (DCXFMDDS) in vivo and in vitro were evaluated. Ferulic acid (FA) and senkyunolide I (SI) were used as marker components, which were two of the effective components of Da Chuanxiong Fang. And their contents were determined by HPLC. Drug release characteristics in vitro of DCXFMDDS and Da Chuanxiong pills and pharmacokinetics characteristics of DCXFMDDS and Da Chuanxiong Fang active fraction (DCXFAF) in rats were compared. It was obvious that FA released from the DCXFMDDS in a sustained fashion but SI in a fast fashion both in vitro and in vivo. The releasing process and the releasing mechanism of FA and SI from DCXFMDDS were different, but the AUC value indicated that compared with DCXFAF the extent of absorption of FA and SI from DCXFMDDS was increased. Though from the same multiunit drug delivery system, FA an SI had different drug release characteristics both in vitro and in vivo, and that may be one of the reason why DCXFMDDS has the good properties such as rapid and long-lasting effect and high efficiency.
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