Page 35 - 《中国药房》2022年4期

盐酸益母草碱片的制备及质量评价 Δ

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何国毅 ，周东阳 ，周 凯 ，陈国广 ，任丽莉 （1.南京工业大学生物与制药工程学院，南京 211816；2.南京工
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业大学2011学院，南京 211816；3.南京工业大学药学院，南京 211816）
中图分类号 R944.4 文献标志码 A 文章编号 1001-0408（2022）04-0413-06
DOI 10.6039/j.issn.1001-0408.2022.04.06

摘 要 目的 制备盐酸益母草碱片，并进行质量评价。方法 采用湿法制粒技术，以盐酸益母草碱为原料药，采用单因素实验筛选
填充剂、崩解剂、黏合剂、润滑剂种类；结合正交实验，以15 min累积溶出度（以水为溶出介质）为指标，筛选崩解剂占比、黏合剂溶
液质量分数、润滑剂占比，并进行验证。按2020年版《中国药典》（四部）通则方法对所制盐酸益母草碱片的体外溶出行为（溶出介
质分别为pH1.2的盐酸溶液、pH4.5的醋酸-醋酸钠溶液、pH6.8的磷酸盐缓冲液、水）、片剂外观、硬度、脆碎度、含量均匀度进行检
测。结果 盐酸益母草碱片的最优处方为盐酸益母草碱原料药500 mg、糊精9 250 mg、交联聚维酮200 mg、硬脂酸镁50 mg、1％羟
丙甲纤维素溶液4 mL。所制3批片剂的平均15 min累积溶出度为81.25％（RSD＝1.12％，n＝3）。在上述4种溶出介质中，所制片
剂均能在30 min内达到溶出平衡，且累积溶出度均超过85％。所制片剂外观颜色均一，呈米黄色，表面光滑，边缘完整，无杂色、
斑点、异物等，硬度为57.3 N（n＝6），减重率为0.15％，含量均匀度符合2020年版《中国药典》（四部）相关规定。结论 成功制备了
盐酸益母草碱片，且质量符合相关规定。
关键词 盐酸益母草碱片；制备工艺；单因素实验；正交实验；体外溶出度；质量评价

Preparation and quality evaluation of Leonurine hydrochloride tablets
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HE Guoyi ，ZHOU Dongyang ，ZHOU Kai ，CHEN Guoguang ，REN Lili（1. College of Biotechnology and
Pharmaceutical Engineering，Nanjing Tech University，Nanjing 211816，China；2. 2011 College，Nanjing Tech
University，Nanjing 211816，China；3. School of Pharmaceutical Sciences，Nanjing Tech University，Nanjing
211816，China）
ABSTRACT OBJECTIVE To prepare Leonurine hydrochloride tablets and evaluate the quality. METHODS The wet granulation
technology was adopted；leonurine hydrochloride was used as the crude drug，and the types of fillers，disintegrants，binders and
lubricants were screened by single-factor experiments. Combined with orthogonal experiments，using the cumulative dissolution rate
within 15 minutes （using water as dissolution media） as index，the proportion of disintegrants，the mass fraction of binder
solution，and the proportion of lubricants were screened and verified. The in vitro dissolution behavior of the prepared Leonurine
hydrochloride tablets（dissolution media were hydrochloric acid solution of pH1.2，acetic acid-sodium acetate solution of pH4.5，
phosphate buffer solution of pH6.8，water），tablet appearance，hardness，friability and content uniformity were tested according to
the general principles in 2020 edition of Chinese Pharmacopoeia （part Ⅳ）. RESULTS The optimal formulation of Leonurine
hydrochloride tablets included leonurine hydrochloride crude drug of 500 mg，dextrin of 9 250 mg，crosslinking polyvingy-
pyrrolidone of 200 mg，magnesium stearate of 50 mg，1％ hydroxypropyl methyl cellulose solution of 4 mL. The average
15-minute cumulative dissolution rate of the three batches of tablets was 81.25％（RSD＝1.12％，n＝3）. In above 4 dissolution
media，the dissolution equilibrium of prepared tablets could be reached within 30 minutes，and the cumulative dissolution rates
exceeded 85％. The prepared tablets had uniform beige in color，smooth surface，complete edge，no mottle，spot，foreign matter，
etc.，hardness of 57.3 N（n＝6），weight loss rate of 0.15％. The content uniformity was in accordance with relevant provisions in
2020 edition of Chinese Pharmacopoeia（part Ⅳ）. CONCLUSIONS Leonurine hydrochloride tablets are successfully prepared，
and the quality comply with relevant regulations.
KEYWORDS Leonurine hydrochloride tablets；preparation technology；single factor experiment；orthogonal experiment；in vitro
dissolution；quality evaluation

Δ 基金项目：国家“重大新药创制”科技重大专项资助项目 更年期综合征是一种困扰中年女性的常见疾病，主
（No.2017ZX09301057）
要临床表现有月经紊乱、易怒、焦虑等，部分患者还会出
＊硕士研究生。研究方向：药物新剂型与新技术。E-mail：
现抑郁、更年期忧愁等症状 [1－2] 。该综合征多因女性体
hgy@njtech.edu.cn
[3]
# 通信作者：教授，硕士生导师，博士。研究方向：药物新剂型与 内雌激素分泌量降低所致 ，其临床治疗方法主要为激
新技术。E-mail：renlili@njtech.edu.cn 素替代疗法，或辅以孕激素、雄激素联合治疗 [4－5] 。但有

中国药房 2022年第33卷第4期 China Pharmacy 2022 Vol. 33 No. 4 ·413 ·