邹芳　张志华　王布

摘      要：以对乙酰氨基酚为主药，稀释剂淀粉、稀释剂糊精、崩解剂羟丙甲纤维素等为辅料，通过湿法制粒压片法制备对乙酰氨基酚片剂。以外观、硬度、脆碎度、片重差异和崩解时限为考察指标，筛选出最优处方辅料种类，并通过正交实验筛选出对乙酰氨基酚片最优处方工艺。通过研究最佳处方工艺所制备的片剂在室温下放置的稳定性实验，用以评价片剂的质量是否达到片剂标准。结果表明：对乙酰氨基酚片最优处方辅料种类为淀粉浆作为黏合剂、羟丙甲纤维素作为崩解剂、硬脂酸镁作为润滑剂。最佳的制备工艺为：对乙酰氨基酚3 g、羟丙甲纤维素2 g、硬脂酸镁0.75 g、淀粉浆的浓度10% 。该片剂在 37 ℃保存 3个月后无异常变化，表明该片剂质量稳定，制备工艺可靠。

关  键  词：对乙酰氨基酚;片剂;正交实验;处方优化

中图分类号：R944.4           文献标识码： A       文章编号： 1671-0460（2020）07-1305-04

Preparation of Paracetamol Tablets and In Vitro Evaluation

ZOU FANG， ZHANG Zhing-hua， WANG BU

（The First Affiliated Hospital of Hebei North University， Zhangjiakou Hebei 075000， China）

Abstract： Paracetamol tablets were prepared by wet granulation and compression method with paracetamol as the main drug， starch， dextrin，hydroxypropylmethylcellulose as auxiliary materials.Taking appearance， hardness， brittleness， tablet weight difference and disintegration time limit as inspection indexes， the optimal prescription of paracetamol tablet was selected.Whether the quality of the tablets can meet the standard was evaluated by the stability experiment of the tablets prepared by the best prescription technology at room temperature. The results showed that the optimal formulation of paracetamol tablets was as follows： binder starch paste， disintegrator hydroxypropylmethyl- cellulose， lubricant magnesium stearate.The best preparation process was as follows： paracetamol 3 g， hydroxyl- propylmethylcellulose 2 g， magnesium stearate 0.75 g， and the concentration of starch slurry 10%. The results showed that the quality of the tablet was stable and the preparation process was reliable.

Key words： Paracetamol; Paracetamol; Orthogonal experiment; Prescription optimization

對乙酰氨基酚（Paracetamol），又名扑热息痛，属于非甾体抗炎药中的一种，它的药理作用与阿司匹林类似^[1-2]，在临床中应用广泛。对乙酰氨基酚能够通过抑制环氧酶的活性从而抑制前列腺素的生成，起到解热镇痛作用^[3-5]。研究表明，对乙酰氨基酚与布洛芬两药物合用对小儿呼吸系统感染性发热具有良好的治疗效果，能够缓解患者的临床病症^[6-7]。此外，对乙酰氨基酚具有中枢抗氧化应激损伤和抑制炎症反应的作用，而神经炎症反应和氧化应激损伤在许多神经退行性疾病的发病过程中起到关键作用，研究表明，对乙酰氨基酚能够降低细胞内氧化水平、稳定线粒体功能、通过抑制NF-κB信号通路而抑制细胞凋亡，起到中枢神经保护作用^[8-10]。……