對(duì)乙酰氨基酚栓劑的制備與質(zhì)量控制

對(duì)乙酰氨基酚栓劑的制備與質(zhì)量控制
摘    要 
本文主要研究對(duì)乙酰氨基酚栓劑的制備，以改變給藥途徑。通過考察劑型的含量、釋放曲線確定栓劑的最佳處方，解決口服藥長期服用時(shí)對(duì)肝臟、腎等器官的危害，此外栓劑還具有易于給藥、避免肝臟首過效應(yīng)、且作用恒定緩慢以提高藥物的生物利用度。同時(shí)還進(jìn)行了該劑型的質(zhì)量檢查。
結(jié)果表明，對(duì)乙酰氨基酚與輔料有良好的相容性，對(duì)乙酰氨基酚在6~14µg/mL的濃度范圍內(nèi)符合，吸光度與濃度呈良好的線性關(guān)系；建立了分光光度法測定對(duì)乙酰氨基酚栓中主藥含量的方法，方法符合要求；制備了不同基質(zhì)的栓劑，通過比較，以油溶性基質(zhì)半合成脂肪酸甘油酯為最佳基質(zhì)，APAP:半合成脂肪酸甘油酯=1:6.6時(shí)溶出度較好，穩(wěn)定性高，對(duì)乙酰氨基酚在栓劑中含量為13.1%，干燥失重和融變時(shí)限均符合要求。
關(guān)鍵詞  對(duì)乙酰氨基酚；栓劑；質(zhì)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  錄
摘    要 I
Abstract II
目  錄 III
第1章 緒    論 5
1.1 研究背景 5
1.2 對(duì)乙酰氨基酚的概述 5
1.2.1 對(duì)乙酰氨基酚的基本性質(zhì) 5
1.2.2 對(duì)乙酰氨基酚的研究進(jìn)展 6
1.3 栓劑的概述 7
1.3.1 栓劑的劑型特點(diǎn) 7
1.3.2 栓劑的制法 8
1.3.3 栓劑基質(zhì)與附加劑 8
1.3.4 栓劑的研究進(jìn)展 9
1.4 課題研究的目的和內(nèi)容 9
1.4.1 目的 9
1.4.2 內(nèi)容 10
第2章 處方前研究 11
2.1 儀器與試藥 11
2.1.1 儀器 11
2.1.2 試藥 11
2.2 標(biāo)準(zhǔn)曲線的繪制 11
2.3 栓劑的制備 12
2.3.1 熱熔法制備栓劑 12
2.3.2 熱熔法制備空白栓 14
2.4 栓劑輔料的陰性對(duì)比 15
2.4.1 試驗(yàn)方法 15
2.4.2 結(jié)果 15
2.5 本章小結(jié) 15
第3章 對(duì)乙酰氨基酚栓劑的制備 16
3.1 儀器與試藥 16
3.2 含量測定方法學(xué)考察 16
3.2.1 標(biāo)準(zhǔn)曲線的繪制 16
3.2.2 陰性對(duì)比實(shí)驗(yàn) 16
3.2.3 含量測定方法 16
3.2.4 加樣回收率實(shí)驗(yàn) 17
3.2.5 精密度實(shí)驗(yàn) 17
3.2.6 重復(fù)性實(shí)驗(yàn) 17
3.3 劑型檢查 18
3.3.1 溶出度測定方法 18
3.3.2 融變時(shí)限 20
3.3.3 干燥失重 21
3.3.4 穩(wěn)定性考察 21
3.4 本章小結(jié) 21
結(jié)  論 23
致   謝 24
參考文獻(xiàn) 25
附錄A 26
附錄B 32