氢溴酸高乌甲素价格97792-45-5 植物提取物【医药级】

        氢溴酸高乌甲素    

                                                                                                                                                                                                                                            中文名称                                                                                                氢溴酸高乌甲素                                                                                                中文同义词                                                                                                氢溴酸高乌甲素 氢溴酸高乌甲素, 氢溴酸刺乌头碱 氢溴酸乌高素 氢溴酸高乌甲                                                                                                                                                                                                                结构式                                                                                                                                                                                                                                                                氢溴酸高乌甲素 用途与合成方法                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                                    生物碱                                            氢溴酸高乌甲素（Lappaconitine）是从毛茛科植物高乌头中分离得到的一种二萜类生物碱—拉巴乌头碱，其化学名称为(1α,14α,16β)-20-乙基-1,14,16-三甲氧乌头烷-4，8，9-三醇4-[2-（乙酰氨基）苯甲酸酯氢溴酸盐一水化合物。是国内首创的非成瘾性镇痛新药。具有镇痛、解热、消肿和局部麻醉等作用，且无成瘾性和积蓄作用，其镇痛作用比吲哚美辛强，比吗啡弱。
本信息由ChemicalBook的香云编辑整理。                                            来源植物                                            从毛茛科植物高乌头根中提取的一种生物碱（拉巴乌头碱）。
 
图1为高乌头                                            提取方法                                            将高乌头块根粉碎→加入到提取罐中加乙醇浸泡1h，加热回流3h 3次→浓缩，用2%的盐酸酸化，抽滤→加氨水碱化至PH 9-10，搅拌沉淀，过滤→沉淀用三氯甲烷溶解→加工艺用水，静置分层→加入无水碳酸钾搅拌脱水，减压抽虑至膏状→用乙醇溶解，回收乙醇至结晶析出→得到高乌甲素。                                            药理作用                                            1、镇痛作用 腹腔注射氢溴酸高乌甲素可以明显缓解慢性缩窄性损伤(CCL)大鼠的热痛觉,达到镇痛治疗效果,并且没有明显的毒性反应。
2、消炎作用 高乌甲素对于二甲苯引起的小鼠耳壳肿胀、大鼠关节炎性足肿胀及大鼠琼脂肉芽肿增生等均有明显的抑制作用。表明高乌甲素具有抗急、慢性炎症作用,此作用为高乌甲素用于临床治疗风湿性、类风湿性关节炎引起的疼痛、红肿提供了理论依据。
3、抗肿瘤作用 高乌甲素对小鼠肝癌的抑瘤率为11.20%一53.08%,对小鼠S180抑瘤率为29.81%-53.%。说明氢澳酸高乌甲素具有一定的抗小鼠肝癌S180作用,而且对小鼠体质量没有明显的影响。
4、抗心律失常作用 高乌甲素可以提高乌头碱诱发大鼠心律失常的常阈值,并能显著改善犬的心肌缺血性心律失常,从而降低心律失常得发生率，其作用机理可能是阻断钠离子通道。                                            药代动力学                                            【药物动力学】 氢溴酸高乌甲素的血浆消除半衰期(tl/2)、清除速率CL和表观分布容积V在高、中、低三种剂量下无明显差异,即该药物的药物动力学参数基本上不随剂量的改变而发生变化,表现为线性动力学行为。在体内的药-时过程符合二室开放模型,吸收较快,消除速度适中。
【分布】 在小鼠组织中广泛分布,且与组织蛋白结合,致使其在血浆中的药物浓度较低。
【代谢】 高乌甲素在大鼠中的代谢共有10种代谢物。代谢物包括羟基化代谢产物,O-去甲基代谢产物,N-去乙酰化代谢产物,O-去甲基N-去乙酞化代谢产物,双O-去甲基N-去乙酞化代谢产物,酯水解代谢产物。高乌甲素在大鼠体内的主要代谢途径有羟基化、O-去甲基化、N-去乙酰化和酯水解。这些代谢途径还可能发生交叉,生成次级代谢产物。                                            适应症                                            用于癌痛、手术疼痛、牙痛、痛经等中度以上疼痛。                                            毒理学                                            本品动物试验无致畸胎作用。急性毒性试验结果：大鼠经口LD50为20mg/Kg；小鼠腹腔注射LD50为9.1mg/Kg，静脉注射LD50为6.9mg/Kg。                                            不良反应                                            个别患者出现荨麻疹、心慌、胸闷、头晕等，停药后很快消失。                                            贮藏                                            避光，密封保存。                                            用途                                             适用于胃肠溃疡、胃炎、肝炎、胆囊炎、风湿病、坐骨神经痛、牙痛、术后疼痛、癌痛等症。