目的 考察黄连水煎液中不同固体微粒组分对有效成分小檗碱在体肠吸收的影响。方法 以高速离心法去除黄连水煎液中较大粒径固体微粒;以大孔弱碱性阴离子交换树脂对上清液中固体微粒进一步分离;以大鼠在体肠吸收模型评价黄连水煎液中固体微粒对小檗碱肠吸收特性的影响。结果 小檗碱在小肠各肠段均有吸收,空肠段吸收最好,吸收速率常数(K_a)和有效渗透系数(P_eff)分别为(3.587 9±0.005 2)×10^-4/s和(4.529 4±0.009 7)×10^-5 cm/s;黄连水煎液经高速离心分离和离子交换色谱柱分离后,得到粒径相近、电位差异较大的微粒P₁[粒径(272.7±25.2)nm,电位(-6.85±0.16)mV]和P₂[粒径(264.8±21.4)nm,电位(-18.20±0.71)mV];在体肠循环灌注实验表明,微粒P₁可显著提高小檗碱的在体肠吸收[K_a为(5.853 6±0.970 1)×10^-4/s、P_eff为(8.082 4±1.004 2)×10^-5 cm/s]。结论 黄连水煎液中固体微粒可以显著增加小檗碱的肠吸收,其中微粒表面电位可能是微粒影响小檗碱肠吸收的因素之一。

Objective To investigate the effects of particles in coptis (Coptidis Rhizoma)-decoction on the berberine absorption in intestine. Methods The particles in copitis-decotion were separated by the high-speed centrifugation and weak-base anion-exchange resin. The characteristics of berberine absorption in intestine were evaluated by the in situ intestinal perfusion in rats. Results Although each segment of small intestine exhibited obvious berberine absorption, the jejunum exhibited the highest absorption rate constant (K_a) of (3.587 9 ± 0.005 2) × 10^-4/s and effective permeability coefficient (P_eff) of (4.529 4 ± 0.009 7) × 10^-5 cm/s. Particles P₁ and P₂, with similar size of (272.7 ± 25.2) and (264.8 ± 21.4) nm and different surface potential of (-6.85 ± 0.16) and (-18.20 ± 0.71) mV, were obtained from the copitis-decotion. Particle P₁ could significantly improve the berberine absorption in intestine, with K_a of (5.853 6 ± 0.970 1) × 10^-4/s and P_eff of (8.082 4 ± 1.004 2) × 10^-5 cm/s. Conclusion Particles in coptis-decotion can improve the berberine absorption in intestine. The surface potential of the particles may be responsible for the improvement of berberine absorption.

国家自然科学基金资助项目(81303239)