Preparation and Quality Evaluation of Breviscapine Gastric Adhesive Tablets / 中国药房

ABSTRACT

OBJECTIVE：To prepar e Breviscapine gastric adhesive tablets ，to optimize the formulation and to evaluate the quality. METHODS ：HPMC K 100M 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 K 100M，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）.