• 主题
高级搜索  >
历史搜索 清空历史
首页> 美国卫生研究院文献>Marine Drugs >Lyophilization Serves as an Effective Strategy for Drug Development of the α9α10 Nicotinic Acetylcholine Receptor Antagonist α-Conotoxin GeXIVA12
【2h】

Lyophilization Serves as an Effective Strategy for Drug Development of the α9α10 Nicotinic Acetylcholine Receptor Antagonist α-Conotoxin GeXIVA12

机译：冻干剂是α9α10烟碱乙酰胆碱受体拮抗剂α-芋螺蓟啶gexiva的有效策略12

代理获取
本网站仅为用户提供外文OA文献查询和代理获取服务，本网站没有原文。下单后我们将采用程序或人工为您竭诚获取高质量的原文，但由于OA文献来源多样且变更频繁，仍可能出现获取不到、文献不完整或与标题不符等情况，如果获取不到我们将提供退款服务。请知悉。
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

α-Conotoxin GeXIVA[1,2] is a highly potent and selective antagonist of the α9α10 nicotinic acetylcholine receptor (nAChR) subtype. It has the advantages of strong efficacy, no tolerance, and no effect on motor function, which has been expected help patients with neuropathic pain. However, drug development for clinical use is severely limited owing to its instability. Lyophilization is applied as the most preferred method to solve this problem. The prepared lyophilized powder is characterized by differential scanning calorimetry (DSC), powder X-ray diffractometry (PXRD), and Fourier transform infrared spectroscopy (FTIR). Molecular simulation is also used to explore the internal distribution and forces formed in the system. The analgesic effect on paclitaxel-induced neuropathic pain following single and 14-day repeated administrations are evaluated by the von Frey test and the tail-flick test. Trehalose combined with mannitol in a ratio of 1:1 is employed as the excipients in the determined formulation, where trehalose acts as the stabilizer and mannitol acts as the bulking agent, according to the results of DSC, PXRD, and FTIR. Both GeXIVA[1,2] (API) and GeXIVA[1,2] lyophilized powder (formulation) could produce stable analgesic effect. These results indicated that GeXIVA[1,2] lyophilized powder could improve the stability and provide an effective strategy to push it into clinical use as a new analgesic drug.
机译：α-芋螺毒素Gexiva [1,2]是α9α10烟碱乙酰胆碱受体（NACHR）亚型的高效和选择性拮抗剂。它具有强效力，无耐受性和对电机功能的影响的优点，这是预期的有助于神经病疼痛的患者。然而，由于其不稳定，临床使用的药物开发严重限制。冻干作为解决这个问题的最优选方法。制备的冻干粉末的特征在于差扫描量热法（DSC），粉末X射线衍射法（PXRD）和傅里叶变换红外光谱（FTIR）。分子仿真还用于探索系统中形成的内部分布和力。通过von Frey试验和尾部轻型试验评估单一和14天重复施用后紫杉醇诱导的神经病疼痛的镇痛作用。根据DSC，PXRD和FTIR的结果，使用以1：1的比例为1：1的甘露醇作为所固体制剂中的赋形剂，其作为稳定剂和甘露醇作为膨胀剂。 Gexiva [1,2]（API）和GEXIVA [1,2]冻干粉末（配方）可以产生稳定的镇痛作用。这些结果表明，Gexiva [1,2]冻干粉可以提高稳定性，并提供一种有效的策略，以将其推入临床用途作为新的镇痛药。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
代理获取

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号