金石利咽口崩片的制备及药效学研究

Study on Preparation and Efficacy of Jin Shi Li Yan Orally Disintegrating Tablets

目的:优化金石利咽口崩片处方和制备工艺,并考察其对急性咽炎的药效。方法:以片剂外观、硬度、脆碎度、口感和崩解时间为指标优化处方和制备工艺;采用超高效液相色谱法(UPLC)对有效成分绿原酸进行含量测定;以氨水咽部喷雾方法建立急性咽炎动物模型,比较金石利咽口崩片及原制剂金石利咽颗粒的药效。结果:优化处方为羧甲基淀粉钠55%、微粉硅胶9%、滑石粉0. 5%、硬脂酸镁0. 5%。以此处方制备金石利咽口崩片的硬度为4～6 kg,崩解时间为56 s,脆碎度在4. 8%左右;片剂中绿原酸含量为0. 033%。大鼠日常表现、血常规和炎症介质PGE2含量结果均表明,金石利咽口崩片治疗急性咽炎效果优于阳性药草珊瑚含片。结论:该口崩片处方工艺可行、操作简便,含量测定方法灵敏度高、重复性好,对急性咽炎有效,与金石利咽颗粒剂药效相当,将金石利咽颗粒剂改变剂型为金石利咽口崩片合理、可行。

Objective: To optimize the formulation and preparation process of Jin Shi Li Yan orally disintegrating tablets,and investigate its efficacy in treating acute pharyngitis. Methods: The prescription and preparation process were optimized with the appearance of tablets,hardness,fragility,taste and disintegration time. The content of chlorogenic acid was determined by UPLC,and the acute pharyngitis model of Wistar rats was established by the method of ammonia water pharynx spray to compare the efficacy of Jin Shi Li Yan orally disintegrating tablet and the original preparation Jin Shi Li Yan granule. Results: The optimized prescription was sodium carboxymethyl starch( 55 %), silicon dioxide( 9 %),talcum powder( 0. 5 %) and magnesium stearate( 0. 5 %). While Jin Shi Li Yan orally disintegrating tablets were prepared by using this prescription and process. The hardness was 4-6 kg,the disintegration time was 56 s and the friability was about 4. 8 %. The content of chlorogenic acid in the tablets was 0. 033 %. The results of daily performance,blood routine test and PGE2 content in rats showed that the effect of Jin Shi Li Yan orally disintegrating tablets on acute pharyngitis was better than that of positive herb. Conclusion: The prescription technology of orally disintegrating tablet is feasible and easy to operate, and the content determination method has high sensitivity and good reproducibility. Pharmacodynamic studies have proved it is effective for acute pharyngitis. That provided the basis for transforming Chinese patent medicinesJin Shi Li Yan granules into orally disintegrating tablets.