论文总字数：15992字

摘 要

近年来，随着社会科技的快速发展变迁，人们的饮食习惯生活方式都发生了很大变化，尤其是为了适应快节奏的工作需要，人们忽略了自身的健康需要，常吃快餐又疏于运动，这使我国越来越多的人患上以高血压为代表的心脑血管疾病。因此治疗心脑血管系统疾病的重要部分就是降压治疗。

本实验的讨论对象是硝苯地平缓释片，实验内容是在处方前研究的基础上建立硝苯地平的体外分析方法，为后期的处方筛选和工艺研究做铺垫。硝苯地平是常用来治疗高血压的钙离子拮抗剂中的1,4-二氢吡啶衍生物类。硝苯地平缓释片最早由德国拜尔公司研发生产，随后还有软胶囊和缓释片在欧美和日本地区上市，后来随着工艺技术的改进，日本又上市了普通片和颗粒剂，中国也仿制了滴丸剂和注射剂。它的常用规格也非常灵活，有5，10，20，30，60和90毫克不等。

体外分析方法的建立：本实验建立了HPLC法测定硝苯地平的含量分析方法，实验排除了空白辅料对测定的影响，实验结果表明,该方法线性度好,精密度好,回收率好，在室温遮光情况下24h内溶液稳定性良好，结果准确可靠。本试验建立了HPLC法测硝苯地平的体外释放度的方法，参照日本药典在JP16的质量标准下测定释放度，结果同样显示空白辅料不影响，在线性范围内线性关系良好，精密度、回收率良好，结果准确可靠。

关键词 硝苯地平 缓释片 钙离子拮抗剂 释放度 HPLC

Establishment of in vitro analysis method for nifedipine sustained release tablets

ABSTRACT

In recent years, with the rapid development of social science and technology, people's eating habits and lifestyles have undergone great changes, especially in order to meet the needs of fast-paced work, people neglect their own health needs, eat fast food and neglect sports. This makes more and more people in China suffer from cardiovascular and cerebrovascular diseases represented by high blood pressure. Therefore, a significant part of the treatment is antihypertensive therapy.

The subject of this experiment was the nifedipine sustained-release tablet. The experimental content was based on the pre-prescription study to establish an in-vitro analysis method of nifedipine, which will pave the way for the subsequent prescription screening and process research. Nifedipine is a 1,4-dihydropyridine derivative of the class of calcium antagonists commonly used to treat hypertension. The nifedipine sustained-release tablets were first developed by German Bayer Corporation, followed by soft capsules and sustained-release tablets in the US, Europe, and Japan. Later, with the improvement of process technology, Japan launched regular tablets and granules. Also imitation of pills and injections. Its common specifications are also very flexible, ranging from 5, 10, 20, 30, 60 and 90 mg.

  Establishment of in vitro analysis method: In this experiment, an analytical method for the determination of nifedipine by HPLC method was established. The effect of blank excipients on the determination was eliminated in the experiment, and good recovery rate. The stability of the solution was good in 24 h at room temperature, and the result was accurate and reliable. This test established a method for the determination of nifedipine in vitro release rate by HPLC method. The release degree was determined according to the Japanese Pharmacopoeia under the quality standard of JP16. The results also showed that the blank excipients did not affect the linear relationship within the linear range, precision, recovery The rate is good and the result is accurate and reliable.

Key words nifedipine sustained-release tablets calcium antagonist release degree HPLC

目 录

摘要 I

ABSTRACT I

目 录 II

第一章文献综述 1

1.1 硝苯地平研究背景 1

1.1.1 高血压研究背景 1

1.1.2 治疗高血压药物分类 1

1.1.4 硝苯地平剂型情况 7

1.1.5 硝苯地平国内上市情况 7

1.2 口服缓控释制剂研究进展 8

1.2.1 口服缓控释制剂概况 8

1.2.2 口服缓控释制剂研究进展 9

1.3 立题依据和主要研究内容 9

1.3.1 立题依据 9

1.3.2 主要研究内容 10

第二章 硝苯地平缓释片体外分析方法的建立 11

2.1 试验部分 11

2.1.1 试验材料 11

2.1.2 试验仪器 11

2.1.3 含量测定方法的建立 12

2.1.4 释放度测定方法的建立 18

2.2 本章小结 22

2.2.1 硝苯地平含量测定方法的建立 22

2.2.2 硝苯地平释放度测定方法的建立 22

参考文献 23

致谢 25

第一章 文献综述

1.1 硝苯地平研究背景

1.1.1 高血压研究背景

心脑血管疾病是心脏和血管的病变异常的循环系统类疾病，也是目前对人类健康影响最大的疾病，据不完全统计我国目前大概有近三亿人患有该类疾病，而且其中有一半以上的疾病是和高血压相关。

高血压是一种心血管疾病的进展性疾病,其主要临床表现是动脉血压升高,可引起心脏、脑、血管和肾脏的病理变化和死亡。高血压是一种常见的慢性疾病,是由一些先天性遗传因素、致病性增压因子和生理性减压因素相互作用引起的。[1]。

1.1.2 治疗高血压药物分类

当前高血压的治疗药物主要有利尿剂、α受体阻滞剂、β受体阻滞剂、钙离子拮抗剂、血管紧张素转换酶抑制剂（ACEI）、血管紧张素Ⅱ受体拮抗剂（ARB），还有复方制剂和中成药也可用于高血压的治疗。[6]

1.1.2.1 利尿药

利尿药的药理作用是通过舒张血管、降低外周阻力从而达到治疗目的。患者长期口服用此类降压药时能达到温和降压的效果而且很少出现耐受现象，此外，利尿药可以通过机制互补的作用达到更好的降压效果并抵消利尿剂的一些副作用，所以也是常用的联合抗高血压药物。

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