Han Yu-Mei, Yan Dan, Yuan Hai-Long
School of Bioengineering, Chongqing Institute of Technology, Chongqing 400050, China.
Zhongguo Zhong Yao Za Zhi. 2007 Dec;32(23):2508-10.
To study the plasma concentration-time curve, pharmacokinetic parameters and bioavilability of oxymatrine-phospholipid complex and to compare with oxymatrine in rats.
Rats were given oxymatrine-phospholipid 100 mg x kg(-1). Blood samples were collected at different times after oral administration. The internal standard was cimetidine. Protein in plasma was precipitated with merhanol and centrifuged at high speed. The supernatant was directly injected and assayed by CE method. The running buffer was 0.04 mol x L(-1) Tris-10 mmol x L(-1) sodium phosphate monobasic-40% isopropanol pH to 7.6 with phosphoric acid. The wavelength of detection was 205 nm.
The AUC of oxymatrine and oxymatrine-phospholipid complex were 4.52 mg x mL(-1) x h(-1) and 6.21 mg x mL(-1) x h(-1), respectively. The oxymatrine-phospholipid bioavailability enhanced 1.4 times.
It is concluded that after oral administration of oxymatrine-phospholipid complex in rats the bioavailability of oxymatrine is increased greatly. This is mainly due to an obvious improvement of the lipophilic property of oxymatrine-phospholipid complex compared with oxymatrine material and an increase in gastrointestinal absorption.
研究氧化苦参碱磷脂复合物在大鼠体内的血药浓度-时间曲线、药代动力学参数及生物利用度，并与氧化苦参碱进行比较。
给大鼠灌胃氧化苦参碱磷脂复合物100 mg·kg⁻¹。口服给药后在不同时间点采集血样。内标为西咪替丁。血浆中的蛋白质用甲醇沉淀并高速离心。上清液直接进样，采用毛细管电泳法测定。运行缓冲液为0.04 mol·L⁻¹ Tris-10 mmol·L⁻¹磷酸二氢钠-40%异丙醇，用磷酸调pH至7.6。检测波长为205 nm。
氧化苦参碱和氧化苦参碱磷脂复合物的AUC分别为4.52 mg·mL⁻¹·h⁻¹和6.21 mg·mL⁻¹·h⁻¹。氧化苦参碱磷脂复合物的生物利用度提高了1.4倍。
大鼠口服氧化苦参碱磷脂复合物后，氧化苦参碱的生物利用度显著提高。这主要是由于氧化苦参碱磷脂复合物与氧化苦参碱原料药相比，脂溶性明显改善，胃肠道吸收增加。
