论文总字数：19443字

摘 要

盐酸齐拉西酮（Ziprasidone）为辉瑞公司开发的最新非典型广谱抗精神病药，用于治疗精神分裂症。本品属5-羟色胺和多巴胺受体拮抗剂，特别是对5-HT A2/DA D2受体亲合力强。该药口服剂型和肌注剂型分别于1998年和2000年9月在瑞典上市。对急性或慢性、初发或复发精神分裂症均有很好疗效；对精神分裂症相关症状（包括视听幻觉、妄想、动机缺乏和逃避社会）有效。与传统抗精神病药相比，该药除可改善阳性症状外，还可改善阴性症状，提高认知功能，不良反应特别是锥体外系症状大大减轻，耐受性明显提高；与已广泛使用的奥氮平、喹地平、利培酮等相比，本品对阴性症状疗效更好或相当，不引起体重增加和血清泌乳素水平升高，副作用小于现有的所有不典型抗精神病药。本品现有注射剂和胶囊两种剂型，可分别用于急性/短期和长期治疗。本文主要对盐酸齐拉西酮的药理药动，溶出度以及含量和有关物质进行讲解和研究。

关键字：盐酸齐拉西酮，药理学，药物动力学，溶出度，安全性

The Synthesis and Characterization of PLGA-PLL-PEG

Abstract

Ziprasidone Hydrochloride (Ziprasidone) for the development of the latest Pfizer broad spectrum of atypical antipsychotics for the treatment of schizophrenia. This product is a 5 - serotonin and dopamine receptor antagonists, especially 5-HT A2/DA D2 receptor affinity is strong. And intramuscular formulations of oral formulations of the drug were in 1998 and in September 2000 listed in Sweden. Acute or chronic , or recurrent onset schizophrenia have a good effect ; schizophrenia -related symptoms ( including visual hallucinations, delusions, lack of motivation and social withdrawal ) is valid. Compared with conventional antipsychotic drug in addition to improving positive symptoms , but also improve the negative symptoms, improve cognitive function, adverse reactions especially extrapyramidal symptoms greatly reduced tolerance improved significantly ; and has been widely used compared to olanzapine, quinoline horizon , such as risperidone , the efficacy of the product for better or fairly negative symptoms , do not cause weight gain and elevated serum prolactin levels , side effects, less than all existing atypical antipsychotics. This product is available in two formulations injections and capsules , respectively, for acute / short-term and long-term treatment . This paper focuses on the pharmacology of ziprasidone hydrochloride pharmacokinetics , and safety of dissolution to explain and research.

Keywords: Ziprasidone，Hydrochloride，Pharmacology，Pharmacokinetics， Dissolution，Security

目 录

摘要

Abstract

第一章 研究背景

1 概念

2 药理作用 1

3 药代动力学 2

4 药效学及临床应用研究 3

4.1 短期治疗 3

4.1.1控制阳性症状、阴性症状的疗效

4.1.2 治疗情感症状的疗效 4

4.1.3 治疗急性躁狂发作

4.1.4认知功能的改善

4.1.5 社交障碍 4

4.2 长期治疗

4.3 合并治疗

5 药物的注意事项 5

6 药物的不良反应 6

6.1 一般不良反应 6

6.2 QT间隔延长 6

6.3 体重增加 6

第二章 盐酸齐拉西酮的溶出度，含量和有关物质的测定 8

2.1 引言 8

2.2 实验部分 8

2.2.1 实验材料与仪器 8

2.2.2 实验方法和结果 9

1）盐酸齐拉西酮的体外溶出研究 9

1 色谱条件 9

2 标准曲线的制备 9

3 进样精密度实验

4 溶液稳定性实验

5 回收率实验

6 体外溶出度测定

2）盐酸齐拉西酮的含量测定 11

1 系统适用性试验 11

2 选择性试验 12

3 标准曲线的制备···································12

4 定量限···········································12

5 精密度实验·······································12

6 稳定性实验·······································13

7 含量测定·········································13

3）盐酸齐拉西酮的有关物质测定··························13

1 波长的选择·······································13

2 流动相和溶剂的确定·······························13

3 专属性实验·······································14

4 稳定性试验·······································16

5 检出限···········································16

6 有关物质的测定···································16

2.3 结果与讨论·············································17

2.4 本章小结···············································18

参考文献 19

致谢

第一章 研究背景

1 概念

齐拉西酮(ziprasidon ZIP)是一种新型的非典型广谱抗精神病药，化学名为5-[2-[4-(1, 2-苯并异噻唑- 3基）哌嗪-1基]乙基]-6氯吲哚-2-酮盐酸盐，物品性状为类白色至微粉色粉末。由美国Pfize r公司开发研制，该药的口服制剂和肌内注射剂，分别于1998年和2000年9月在瑞典上市;2001年2月FDA批准其胶囊剂在美国上市，推荐为一线抗精神病药物。

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