青黛表面改性对口腔溃疡双层膜质量与药效的影响  

Effects of surface modification of IndigoNaturalison quality and drug efficacy of oral ulcer bilayer film

作　　者：黄胜杰 钟婧娉 谢锦 贺亚男 郭治平 刘雪梅[1] 杨明 张定堃[1] 韩丽[1] HUANG Sheng-jie;ZHONG Jing-ping;XIE Jin;HE Ya-nan;GUO Zhi-ping;LIU Xue-mei;YANG Ming;ZHANG Ding-kun;HAN Li(State Key Laboratory of Southwestern Chinese Medicine Resources,Chengdu University of Traditional Chinese Medicine,Chengdu 611137,China;Sichuan Houde Pharmaceutical Technology Co.,Ltd.,Chengdu 610041,China;State Key Laboratory of Modern Chinese Medicine Preparations,Ministry of Education,Jiangxi University of Chinese Medicine,Nanchang 330004,China)

机构地区：[1]成都中医药大学西南特色中药资源省部共建国家重点实验室,四川成都611137 [2]四川厚德医药科技有限公司,四川成都610041 [3]江西中医药大学现代中药制剂教育部重点实验室,江西南昌330004

出　　处：《中草药》2023年第13期4118-4127,共10页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金面上项目(82173976);国家自然科学基金面上项目(81773918)。

摘　　要：目的采用溶剂浇铸法制备口腔溃疡双层膜剂,研究青黛表面改性前后对膜剂质量与药效的影响。方法通过单因素实验设计和响应面优化法优选膜剂最佳处方,并对膜剂表面形貌、黏附时间、抗拉强度、含量测定以及体外药物释放等性能进行评估。进一步采用化学灼烧法建立大鼠口腔溃疡模型,考察膜剂对溃疡组织肿瘤坏死因子-α(tumor necrosis factor-α,TNF-α)、白细胞介素-1β(interleukin-1β,IL-1β)、IL-6以及口腔溃疡组织形态的影响。结果空白隔离层确定为25 mg/mL的乙基纤维素乙醇溶液,载药膜最佳处方为63 mg/mL PVA17-88、55 mg/mL PVP K30、3.0 mg/mL明胶与0.047 mL/mL甘油。青黛表面改性后,双层膜剂比未改性双层膜剂具有更加光滑均一的外观、更高的含量均匀性和有效成分靛蓝释放率。药效学结果表明,与模型组相比,阳性组与青黛改性膜剂组显著降低了溃疡组织TNF-α、IL-1β、IL-6的含量(P<0.05),并减少了炎症细胞的浸润,溃疡组织愈合程度较高。结论青黛改性之后的口腔溃疡双层膜剂具有更好的质量与更佳的疗效,具有较好的应用前景。Objective To preparethebilayer film for oral ulcer by solventcasting method,and study the effect of surface modification on film quality and efficacy of Qingdai(IndigoNaturalis).Methods The optimal formulation of the film was optimized by single-factor experimental design and response surface optimization method,and the properties of the film such as surface morphology,adhesion time,tensile strength,content determination and drug release in vitrowere evaluated.A rat oral ulcer model was further established by the chemical burning method,and the effects of film preparations on tumor necrosis factor-α(TNF-α),interleukin-1β(IL-1β),IL-6 and oral ulcer tissue morphology were investigated.Results The blank isolation layer was determined to be 25mg/mLethyl cellulose ethanol solution,and the best formulation of the drug-loaded film wasas follow:63 mg/mLPVA17-88,55mg/mLPVP K30,3.0 mg/mLgelatin and 0.047mL/mL glycerin.After the surface modification of IndigoNaturalis,the double-layer film preparation hada smoother and more uniform appearance,higher content uniformity and release rate of active ingredient indigo than the unmodified Indigo Naturalis double-layer film preparation.The pharmacodynamic results showed that compared with the model group,the contents of TNF-α,IL-1β,and IL-6(P<0.05)were significantly reduced in the positive group and the modified film group and the infiltration of inflammatory cellswas reduced,and the healing degree of ulcer tissue was higher.Conclusion The double-layer film for oral ulcers of modified Indigo Naturalis has better quality and curative effect,and has a better application prospect.

关 键 词：青黛 粉体表面改性 口腔溃疡散 双层膜剂 药效评价 靛蓝 靛玉红 

分 类 号：R283.6[医药卫生—中药学]