盐酸司维拉姆的合成及其磷酸结合度研究

论文编号:CL114  论文字数:8836,页数:21

摘要：慢性肾功能衰竭患者磷代谢紊乱，血磷升高。高血磷可诱发严重的心血管疾病，是终末期肾病患者死亡率增高的重要因素。使用磷结合剂、应用活性维生素D控制继发性甲状旁腺功能亢进等方法降低血磷是治疗的关键。由于高血磷后果严重，传统的治疗药物和方法又有很多不足，人们试图寻找更加有效的新药物以达到治疗目的。本文介绍的是一种新药有盐酸司维拉姆，属于非铝非钙结合剂。盐酸司维拉姆是一种阳离子多聚体，主要成分是盐酸多聚丙烯酰胺，可与磷结合。生理pH下其氨基几乎完全质子化，通过离子交换结合磷，在胃肠道内水合膨胀成数倍于原体积的凝胶，且不被肠道吸收。临床试验表明盐酸司维拉姆能有效地降低血磷水平，其效果可与含钙磷结合剂媲美。盐酸司维拉姆不会引起高钙血症，可显著减少心血管病变的发病率。此外，应用盐酸司维拉姆降低血磷时，可以使用钙三醇控制继发性甲状旁腺功能亢进。目前盐酸司维拉姆被认为是一种较理想的磷结合剂。但有报道盐酸司维拉姆有轻度降低血液中碳酸氢盐的水平、减少脂溶性维生素A、D、E、K的吸收等副作用，使其临床应用受到一定限制。盐酸司维拉姆长期使用的安全性仍有待进一步验证。

关键词：高磷血症；磷结合剂；环氧氯丙烷；烯丙胺盐酸盐

Abstract: Phosphorus in patients with chronic renal failure metabolic disorders, elevated serum phosphate. Hyperphosphatemia can induce severe cardiovascular disease, end stage renal disease is an important factor in increased mortality. Use of phosphate binders, active vitamin D control of application of secondary hyperparathyroidism and other ways to reduce phosphorus is the key to treatment. Serious consequences due to high serum phosphorus, traditional medicines and methods of treatment there are a lot less people trying to find more effective new drugs for therapeutic purposes. This article is a new drug with the Secretary Villam hydrochloride, a non-aluminum non-calcium binders. Division Villam hydrochloride is a cationic polymer, the main components of polyacrylamide hydrochloride, combined with phosphorus. Physiological pH, the protonated-amino almost entirely through the combination of ion exchange of phosphorus in the gastrointestinal tract into a hydrated expanded several times the original volume of the gel, and not be absorbed in the intestine. Clinical trials show that the Secretary Villam hydrochloride can effectively reduce serum phosphorus levels, the effect can be comparable with the phosphate binder. Secretary Villam hydrochloride does not cause hypercalcemia, can significantly reduce the incidence of cardiovascular disease. In addition, the application of hydrochloric acid Division Villam reduce phosphorus, you can control the use of calcitriol secondary hyperparathyroidism. Currently the Division Villam hydrochloride is considered an ideal phosphate binder. But it was reported slightly lower hydrochloride Division Villam blood bicarbonate levels, reduce the fat-soluble vitamins A, D, E, K absorption and other side effects, its clinical application is limited. Long-term use hydrochloride Division Villam security is yet to be verified.

Keywords：Hyperphosphataemia; Phosphate binder; epichlorohydrin; ene hydrochloride
 
 
目  录
中文摘要 I
英文摘要 II
目录 Ⅳ
1. 绪论 1
 1.1 高血磷及对策 1
 1.1.1 磷结合剂 2
 1.1.2 充分透析 3
 1.2丝维拉姆的合成 3
      1.2.1相关知识--自由基聚合 3
      1.2.2合成步骤 6
2. 实验部分 8
 2.1 实验仪器和试剂 8
 2.1.1 实验仪器  8
 2.1.2 实验试剂  8
 2.2实验步骤 10
     2.2.1合成路线 10
     2.2.2丙烯胺盐酸盐的制备及聚合 10
     2.2.2聚丙烯胺的交联 10 
3. 结果与讨论 11
 3.1  磷酸结合度分析  11
 3.2  丙烯胺盐酸盐的制备及聚合过程中需要注意的问题 13
 3.3  聚丙烯胺的交联过程中需要注意的问题 13
4．总结与展望 14
致谢 15
参考文献 16

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