厄贝沙坦氢溴酸盐的毒理学和药效学研究

目的比较厄贝沙坦氢溴酸盐与厄贝沙坦的毒性和药效。方法采用无创血压测量比较了厄贝沙坦氢溴酸盐、厄贝沙坦对自发性高血压大鼠血压的影响。分别ip、ig给药,观察两种药物的半数致死量(LD50),对心率、呼吸以及动物自主活动的影响。结果自发性高血压大鼠的血压明显高于非自发性高血压大鼠,给予厄贝沙坦氢溴酸盐、厄贝沙坦后血压均降至正常水平,且两种药物的降压作用差异无显著性,但厄贝沙坦氢溴酸盐的药效持续时间更长。厄贝沙坦氢溴酸盐、厄贝沙坦对动物的呼吸、心率以及自主活动的影响无差异,但厄贝沙坦氢溴酸盐的LD50明显高于厄贝沙坦。结论厄贝沙坦氢溴酸盐具有和厄贝沙坦相同的降压作用,但是作用时间更长,安全性更高。     

Versapulse多波长激光治疗皮肤色素性病变的临床应用

目的探讨Ｖｅｒｓａｐｕｌｓｅ多波长激光治疗皮肤色素性病变的应用效果。方法选取４２例各类皮肤色素性病变病例，应用Ｖｅｒｓａｐｕｌｓｅ多波长激光治疗仪进行治疗，观查治疗前后的皮肤变化，分析其治疗效果。结果Ｖｅｒｓａｐｕｌｓｅ波长治疗机对皮肤色素性病变疗效显著，治疗后不留疤痕。结论该机利用“选择性光热作用”原理，将四种波长激光器集于一体，可以较好地完成对各种皮肤色素性疾患的治疗，既满足了治疗疾病的要求又达到了不损伤周围正常组织的目的。     

克拉维酸钾反应结晶研究

克拉维酸钾是重要的β-内酰胺酶抑制剂。本文考察了溶剂种类、晶种、搅拌速率、流加速率、溶液pH值、结晶温度等工艺条件对克拉维酸钾反应结晶过程的影响。在优化工艺条件下，制得粒度较为粗大的棒状克拉维酸钾结晶，平均粒度48．86μm，分散性和流动性良好，产品质量符合中国药典2000年版和美国药典USP24要求。     

固定化青霉素酰化酶反应器研究进展

介绍固定化青霉素酰化酶反应器的研究现状，将这类反应器分为搅拌釜反应器、柱式填充床反应器、中空纤维膜反应器以及电渗析耦合反应器，从工程角度分析了各类反应器的优缺点，并展望其今后的发展趋势。     

氨苄西林钠溶析结晶的工艺研究

氨苄西林钠是全世界第一个应用于临床的广谱半合成青霉素类药物,溶液结晶技术是决定氨苄西林钠产品质量的关键因素.为解决目前氨苄西林钠工业结晶产品聚结、粒度分布不均一等问题,本文提出了氨苄西林钠溶析结晶工艺,考察了晶种的加入量、结晶温度、溶析剂流加速度、表面活性剂对产品的主粒度和粒度分布的影响,实验结果表明晶种加入量为产品初始加入量的0.1%、结晶温度为288K、变速流加溶析剂以及加入十二烷基磺酸钠表面活性剂的条件下,可获得主粒度大、粒度分布均匀的晶体产品.     

小檗碱的药理活性以及提升其口服生物利用度的策略

小檗碱(berberine)是一种天然存在的苄基异喹啉类生物碱,具有抗菌、抗癌、降血脂、抗糖尿病和止泻等广泛药理活性,但因其极低的口服生物利用度(<1%),限制了其在临床上的应用,尚无纯小檗碱配方被批准用于任何特定疾病。小檗碱口服生物利用度低主要是由于其在酸性条件下自聚集导致的溶解度差、渗透性低、P-gp(P-glycoprotein)介导的外排和肝肠代谢。提高小檗碱的口服生物利用度可提高小檗碱的药理活性,降低给药剂量进而减少不良反应。本文综述了小檗碱的多种药理活性、代谢过程、药代动力学特征,重点介绍了通过提高溶解度和渗透性、抑制P-gp外排和结构修饰等途径提高小檗碱口服生物利用度的策略,并对小檗碱的研究进行了展望,为其深入研究提供指导。     

头孢羟氨苄单水合物反应结晶工艺优化

利用头孢羟氨苄N,N-二甲基甲酰胺(DMF)溶剂化物在水溶液中反应结晶得到头孢羟氨苄单水合物晶体,产品往往存在聚结、松紧密度小、粒度分布不均匀、晶习不稳定等问题。本文考察了结晶过程中温度、搅拌速率、溶剂配比、溶液pH值等因素对产品粒度分布、晶习及晶体聚结的影响。研究结果表明,结晶温度对产品粒度、晶习和晶体聚结都有影响,搅拌速率和溶剂配比主要影响产品的粒度分布。实验优化得到了头孢羟氨苄单水合物反应结晶的最佳操作工艺并为工业化生产提供了重要的参考价值,利用该工艺得到的头孢羟氨苄单水合物产品为四方片状晶体、晶习完整、粒度分布均匀、产品不聚结,松紧密度分别为0.37g/mL和0.57g/mL,产品质量达国际水平。     

头孢羟氨苄反应结晶过程的研究

头孢羟氨苄是重要的头孢类抗生素。为提高产品的质量和收率,本文对目前工业上采用的间接法反应结晶制备工艺进行了优化,得到了经验最佳操作时间表;同时,研究了有较大发展潜力的直接法结晶生产头孢羟氨苄工艺,解决了该工艺中严重的“结胨”问题．为后续相关研究提供了思路。     

在线过程分析技术在抗生素等药物结晶中的应用

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