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近年来临床治疗上已广泛运用黄连或小蘖硷(黄连素)治疗各种细菌感染的疾患。它们对溶血性链球菌、肺炎双球菌、金色葡萄球菌、(?)贺氏痢疾桿菌、福氏痢疾桿菌及大肠桿菌等均有强大的抗菌作用。但是,黄连及小蘖硷口服剂量大,味苦,收效较慢,对不能口服和需要急速治疗的患者感到不便。为此,作者等拟将盐酸小蘖硷精制成可供注射之用的注射剂。经过一段时间的摸索,已经试制成功盐酸小蘖硷纯品,其O.1%水溶液,用纸上色层分离法证明其纯度与进口的E.Merck 的纯品完全相同。该注射液曾先后数次进行动物实验,初步证实该注射液对动物静脉注射后无毒性反应。我院附属医院已试用于一例败血症患者(曾经口服黄连),从效果上观察盐酸小蘖硷静脉注射有一定疗效,在使用的适当剂量内无副作用,但因病例尚不多,有待继续试用总结。本文仅自精制盐酸小蘖硷的操作过程及动物实验治疗效果、毒性方面作出初步报导。制造过程制造原料系购自重庆中药科学研究所供口服用的盐酸小蘖硷,内合杂质(大多是粘液质)。我们以无醛醇为溶媒,通过活性氧化铝吸附柱以除去杂质,其步骤如下:
In recent years, clinical treatment has been widely used berberine or berberine (berberine) for the treatment of various bacterial infections. They have a strong antibacterial effect on hemolytic streptococcus, pneumococcus, Staphylococcus aureus, Shigella dysenteriae, Shigella flexneri and Escherichia coli. However, oral administration of berberine and berberine dose large, bitter, slow-acting, for those who can not be oral and need immediate treatment inconvenience. To this end, the authors intend to make small-berberine into refined for injectable injection. After a period of exploration, the trial has successfully produced pure berberine hydrochloride, its O.1% aqueous solution, using paper chromatography to prove its purity and imports of pure E. Merck exactly the same. The injection has been carried out several animal experiments, initially confirmed that the injection of non-toxic animals after intravenous injection. Affiliated Hospital of our hospital has been tested in a patient with sepsis (oral administration of berberine), observed from the efficacy of small berberine hydrochloride intravenous injection has a certain effect, the use of the appropriate dose without side effects, but not many cases yet to be continued trial Summary . This article only from the refined process of small berberine hydrochloride and animal experimental treatment, toxicity made a preliminary report. Manufacture of raw materials manufacturing process purchased from Chongqing Institute of Chinese Medicine for oral administration of berberine hydrochloride, combined with impurities (mostly mucinous). We use non-alcoholic alcohol as solvent to remove impurities through the activated alumina adsorption column. The steps are as follows: