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黄连素(小檗碱,Berberine)用于治疗慢性、迁延性肝炎,有一定疗效,但需做成含量较高的注射液,而盐酸盐水中溶解度很小(1: 500)。目前在临床应用较多的是枸橼酸黄连素。后者溶解度较盐酸黄连素大,在治疗中易达到有效剂量,且毒性、副作用较小,对神经、循环,消化系统均无明显毒性,用药安全。下面根据国内文献报道和我们自己的实践,对该药制备作一初步探讨。一、制备的原理黄连素是一种异喹啉生物碱,结构中的氮原子以季铵形式存在,能离子化,呈一定程度的亲水性,因此游离的黄连素在水中的溶解度较大(1:20)。但它与酸结合时,失去一分子水,酸根离子直接与氮结合成铵盐,分子中失
Berberine, used in the treatment of chronic, persistent hepatitis, has been shown to be effective but requires a high level of injection, whereas hydrochloric acid has a very low solubility (1: 500). At present, more clinical application of berberine citrate. The solubility of the latter than berberine hydrochloride in the treatment of easy to reach an effective dose, and toxicity, less side effects on the nerves, circulation, digestive system were no significant toxicity, drug safety. The following based on domestic literature and our own practice, the preparation of the drug for a preliminary discussion. First, the principle of preparation Berberine is a kind of isoquinoline alkaloids, the structure of the nitrogen atoms in the form of quaternary ammonium ionization, showing a certain degree of hydrophilicity, the solubility of free berberine in water larger (1:20). However, when it is combined with acid, it loses a molecule of water, and the acid ions directly combine with nitrogen to form ammonium salts.