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延胡索乙素是中药元胡的有效成分之一,有良好的镇痛、镇静作用,副作用小,安全度大。由于延胡索乙素在元胡中含量甚少,通常从黄藤(Fibraurea recisa Pierre.)的根、茎中提取黄藤素(Palmatine),经氢化成延胡索乙素。我们在试制和生产延胡索乙素注射液的过程中,改进了兄弟厂的方法,现介绍如下。由于延胡索乙素的中性硫酸盐(G_(21)H_(25)ON_4·1/2 H_2SO_4)在水中溶解度不大(2ml:60mg,在15℃左右即可析出结晶),以及受光、受热作用易脱氢成黄藤素,使注射液变黄。因此,解决其溶解度及抗氧化,就成了两个关键问题。兄弟厂的方法中加入丙二醇、山梨醇、苯甲醇(兼作止痛剂)作助溶剂,加入蛋氨酸、烟酸为稳定剂,配液时通入二氧化碳,灌封时
Tetrahydropalmatine is one of the active ingredients of Yuanhu, which has good analgesic and sedative effects with little side effects and high safety. Due to the low content of tetrahydropalmatine in Yuanhu, palmatine is usually extracted from the roots and stems of Fibraurea recisa Pierre. Hydrogenated into tetrahydropalmatine. In the process of trial production and production of tetrahydropalmatine injection, we have improved our brother factory’s method. We now introduce it as follows. Since the neutral sulfate of tetrahydropalmatine (G_(21)H_(25)ON_4·1/2 H_2SO_4) has a low solubility in water (2 ml: 60 mg, crystals precipitate at about 15°C), as well as light and heat. Easy dehydrogenation to cresylstacin to yellow the injection. Therefore, solving its solubility and antioxidants have become two key issues. In the brother factory method, propylene glycol, sorbitol, and benzyl alcohol (also known as analgesics) were added as auxiliary solvents, methionine and niacin were added as stabilizers, and carbon dioxide was introduced into the solution when potting.