盐酸益母草碱片的制备及质量评价

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9250 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。

Preparation and quality evaluation of Leonurine hydrochloride tablets

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(partⅣ).RESULTS The optimal formulation of Leonurine hydrochloride tablets included leonurine hydrochloride crude drug of 500 mg,dextrin of 9250 mg,crosslinking polyvingypyrrolidone 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(partⅣ).CONCLUSIONS Leonurine hydrochloride tablets are successfully prepared,and the quality comply with relevant regulations.