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黄连素一般是以盐酸盐的形式供药用,由于水中溶解度太小(1:500),欲制备浓度较大的注射液,最好将其转化为枸橼酸盐或重硫酸盐使用。文献上所报道的转化方法[药学学报(2):91,1963],操作繁琐,原材料耗损较大。如采用离子交换法进行盐酸黄连素的酸根转化,不仅操作简单易行,效果理想,而且可直接以盐酸盐为原料配制0.5%的构橼酸黄连素或1%的重硫酸黄连素注射液,使盐酸黄连素的利用率达99%以上。
Berberine is generally available in the form of hydrochloride for pharmaceutical use. Due to its low solubility in water (1: 500), it is best to convert it to citrate or bisulfate to prepare a more concentrated injection. The transformation methods reported in the literature [Acta J. Exp. (2): 91, 1963] are cumbersome to operate and consume more raw materials. Such as the use of ion exchange method of berberine hydrochloride acid radical conversion, not only easy to operate, the effect is ideal, and can be directly prepared hydrochloride hydrochloride citrate 0.5% citrate or citrate 1% bisulfate injection , So that berberine hydrochloride utilization rate of 99% or more.