对乙酰氨基酚栓剂的制备与质量控制.doc

对乙酰氨基酚栓剂的制备与质量控制

对乙酰氨基酚栓剂的制备与质量控制
摘    要 
本文主要研究对乙酰氨基酚栓剂的制备，以改变给药途径。通过考察剂型的含量、释放曲线确定栓剂的最佳处方，解决口服药长期服用时对肝脏、肾等器官的危害，此外栓剂还具有易于给药、避免肝脏首过效应、且作用恒定缓慢以提高药物的生物利用度。同时还进行了该剂型的质量检查。
结果表明，对乙酰氨基酚与辅料有良好的相容性，对乙酰氨基酚在6~14µg/mL的浓度范围内符合，吸光度与浓度呈良好的线性关系；建立了分光光度法测定对乙酰氨基酚栓中主药含量的方法，方法符合要求；制备了不同基质的栓剂，通过比较，以油溶性基质半合成脂肪酸甘油酯为最佳基质，APAP:半合成脂肪酸甘油酯=1:6.6时溶出度较好，稳定性高，对乙酰氨基酚在栓剂中含量为13.1%，干燥失重和融变时限均符合要求。
关键词  对乙酰氨基酚；栓剂；质量控制

Paracetamol suppository preparation and quality control

Abstract
     In this paper it was studied on the preparation of paracetamol suppositories to change the route of administration. By examining the determination of dosage forms, the release curve to determine the best prescription suppositories, oral solution when long-term used on liver, kidney and other organ damage, in addition to suppository administration also was easy to avoid the liver first pass effect, and the role of constant was slow to increase drug bioavailability. Also it was carried on the quality inspection of the formulations.
     The results were shown that acetaminophen and excipients have good compatibility, paracetamol concentrations in the range of 6-14μg/mL line, absorbance and concentration showed a good linear relationship between paracetamol in suppositories in content of 13.1%; prepared with different matrix suppository, by comparison, oil-soluble semi-synthetic fatty acid glyceride matrix for the matrix, APAP:semi-synthetic fatty acid glyceride = 1:6.6 when the dissolution good, high stability, loss on drying and financial variables were time to meet the requirements.  
Keywords: Paracetamol ; Suppository; Quality Control
 

目  录
摘    要 I
Abstract II
目  录 III
第1章 绪    论 5
1.1 研究背景 5
1.2 对乙酰氨基酚的概述 5
1.2.1 对乙酰氨基酚的基本性质 5
1.2.2 对乙酰氨基酚的研究进展 6
1.3 栓剂的概述 7
1.3.1 栓剂的剂型特点 7
1.3.2 栓剂的制法 8
1.3.3 栓剂基质与附加剂 8
1.3.4 栓剂的研究进展 9
1.4 课题研究的目的和内容 9
1.4.1 目的 9
1.4.2 内容 10
第2章 处方前研究 11
2.1 仪器与试药 11
2.1.1 仪器 11
2.1.2 试药 11
2.2 标准曲线的绘制 11
2.3 栓剂的制备 12
2.3.1 热熔法制备栓剂 12
2.3.2 热熔法制备空白栓 14
2.4 栓剂辅料的阴性对比 15
2.4.1 试验方法 15
2.4.2 结果 15
2.5 本章小结 15
第3章 对乙酰氨基酚栓剂的制备 16
3.1 仪器与试药 16
3.2 含量测定方法学考察 16
3.2.1 标准曲线的绘制 16
3.2.2 阴性对比实验 16
3.2.3 含量测定方法 16
3.2.4 加样回收率实验 17
3.2.5 精密度实验 17
3.2.6 重复性实验 17
3.3 剂型检查 18
3.3.1 溶出度测定方法 18
3.3.2 融变时限 20
3.3.3 干燥失重 21
3.3.4 稳定性考察 21
3.4 本章小结 21
结  论 23
致   谢 24
参考文献 25
附录A 26
附录B 32