刘巍 刘文 宋信莉 王冠华 汪云霞 李云凯

中圖分类号 R944.4;R927.11 文献标志码 A 文章编号 1001-0408（2020）14-1690-05

DOI 10.6039/j.issn.1001-0408.2020.14.05

摘 要 目的：制备灯盏花素胃黏附片，并进行处方优化和质量评价。方法：以羟丙甲纤维素K100M、卡波姆934P为生物黏附剂和骨架材料，以乳糖为填充剂，以硬脂酸镁为助流剂、润滑剂，采用粉末直接压片法制备灯盏花素胃黏附片。采用加权法对灯盏花素胃黏附片在pH 6.8磷酸盐缓冲液中第2、6、12 h的累积释放度（Q2 h、Q6 h、Q12 h，以灯盏乙素计，由高效液相色谱法测定）评分和体外胃组织黏附力进行综合评分;以此评分为指标，通过L9（34）正交试验设计优化灯盏花素胃黏附片中羟丙甲纤维素K100M、卡波姆934P及乳糖的用量并进行验证。对所制胃黏附片的性质、鉴别、重量差异、脆碎度、释放度、灯盏乙素含量进行考察。结果：灯盏花素胃黏附片的最优处方为42%灯盏花素提取物、10%羟丙甲纤维素K100M、3%卡波姆934P和45%乳糖;验证试验结果显示，所制3批灯盏花素胃黏附片的平均Q2 h、Q6 h、Q12 h分别为20.36%、48.55%、87.00%，平均体外胃组织黏附力为31.36 g/cm2，平均综合评分为70.23（RSD=1.84%，n=3）。所制胃黏附片为淡黄色，味淡或微咸;其出峰时间与灯盏乙素对照品一致;重量差异为±6%，脆碎度为0.54%，Q12 h为83.51%（RSD=2.14%，n=6）;灯盏乙素含量为288.47 mg/g（RSD=0.70%，n=3）。结论：成功制得灯盏花素胃黏附片，其质量评价符合2015年版《中国药典》要求。

关键词 灯盏花素;胃黏附片;处方优化;质量评价

Preparation and Quality Evaluation of Breviscapine Gastric Adhesive Tablets

LIU Wei1，LIU Wen2，SONG Xinli1，WANG Guanhua1，WANG Yunxia1，LI Yunkai1（1. School of Pharmacy， Guizhou University of TCM， Guiyang 550002， China; 2. Party Office， the Affiliated Hospital of Guizhou Medical University， Guiyang 550004， China）

ABSTRACT   OBJECTIVE： To prepare Breviscapine gastric adhesive tablets， to optimize the formulation and to evaluate the quality. METHODS： HPMC K100M and carbomer 934P were used as bioadhesives and skeleton materials， and lactose was used as filler， and magnesium stearate was used as glidant and lubricant to prepare Breviscapine gastric adhesive tablets by direct powder pressing method. The comprehensive scores of scores of accumulative release rate of Breviscapine gastric adhesive tablets in pH 6.8 PBS at 2， 6， 12 h （Q2 h， Q6 h， Q12 h，with scutellarin meter，by HPLC method） and in vitro adhesion force of gastric tissue were evaluated by weighting method. Taking this scores as indexes， L9（34） orthogonal test design was used to optimize the amount of HPMC K100M， carbomer 934P and lactose in Breviscapine gastric adhesive tablets and validation tests were conducted. The properties， identification， weight difference， fragility， release and the content of scutellarin of the gastric adhesive tablets were determined. RESULTS： The optimal prescription of Breviscapine gastric adhesive tablets were 42% breviscapine， 10% HPMC K100M， 3% carbomer 934P and 45% lactose. The verification test results show that the Q2 h， Q6 h， Q12 h of 3 batches of Breviscapine gastric adhesive tablets were 20.36%， 48.55%， and 87.00% ; the average in vitro adhesion force of gastric tissue was 31.36 g/cm2;the average comprehensive score was 70.23 （RSD=1.84%， n=3）. The gastric adhesive tablets were light yellow， tasteless or slightly salty; the peak time was consistent with that of scutellarin control; its weight difference were ±6%， the fragility was 0.54%， and the Q12 h was 83.51% （RSD=2.14%， n=6）. The content of scutellarin was 288.47 mg/g（RSD=0.70%，n=3）. CONCLUSIONS： Breviscapine gastric adhesive tablets is prepared successfully， and its quality evaluation conforms to the requirements of Chinese Pharmacopoeia （2015 edition）.

KEYWORDS   Breviscapine; Gastric adhesive tablets; Formulation optimization; Quality evaluation

灯盏花素（Breviscapine）是从菊科植物短葶飞蓬[Erigeron breviscapus （Vant.） Hand.-Mazz.]中提取出来的黄酮类有效成分，是以灯盏乙素为主、另含有少量灯盏甲素的混合物[1]。现代药理研究表明，灯盏花素具有改善血流量、抗血小板凝聚、抗氧自由基、抗血栓等作用[2]，临床上主要用于冠心病、脑血栓、脑出血和心绞痛等心脑血管疾病的治疗[3]。……