摘要
目的优化川乌-花椒挥发油凝胶贴膏成型工艺,探究花椒挥发油配伍川乌凝胶贴膏增效机制。方法以皮肤追随性、揭帖性、初黏力、剥离度为指标,对9种市售贴膏基质性能进行评价,并以量化的综合感官评价、初黏力、持黏力以及剥离度为指标,采用单因素试验与混料设计试验对凝胶贴膏基质辅料配比进行筛选,并采用在体动物评价法,以小鼠醋酸扭体次数为指标,筛选凝胶贴膏的载药量;另外采用甲醛致痛小鼠模型与代谢组学探究花椒挥发油对川乌凝胶贴膏药效的影响。结果不同品牌凝胶贴膏其追随性、揭帖性、初黏力、剥离度差别较大,且凝胶贴膏的初黏力与剥离度对其揭贴性影响较大,初黏力与剥离度越大,凝胶贴膏揭帖性越差;川乌凝胶贴膏的基质处方为3%聚丙烯酸钠NP700、1.5%羧甲基纤维素钠、0.25%卡波姆、0.06%结晶氯化铝、0.1%乙二胺四乙酸二钠、26%甘油、61.5%水、4%硅藻土、0.15%酒石酸;每贴川乌凝胶贴膏载药量为560 mg川乌提取物。花椒挥发油能够增强川乌凝胶贴膏的镇痛疗效,可能主要通过甘油磷脂代谢、亚油酸代谢等发挥疗效。结论为保证凝胶贴膏具有较好的追随性与揭帖性,所制备的凝胶贴膏的初黏力应控制在7~18号小球之间,剥离度应控制在0.03~0.97kN/m;所制备的川乌凝胶贴膏剂外观、黏附力、赋形性良好,镇痛效果明确,且花椒挥发油能够增强川乌凝胶贴膏的疗效,为川乌外用新制剂的开发与应用提供基础。
Objective To optimize the forming process of gel patch and explore the compatibility-synergistic mechanism of Aconiti Radix-Zanthoxyli Pericarpium volatile oil gel patch. Methods According to the indexes of skin followability, disclosing ability, initial adhesion and peeling degree, the substrate-property of eight commercially gel patches was evaluated. Then, with the comprehensive sensory evaluation, initial adhesion, stickiness and peeling degree as the index, single factor experiment and mixture design experiment were used to screen the proportion of matrix excipients of gel patch. Taking the number of acetic acid-induced writhing in mice as the index, the drug loading of gel paste was screened by in vivo animal evaluation. In addition, the compatibility effect of Aconiti Radix-Zanthoxyli Pericarpium volatile oil gel patch was studied by using formaldehyde-induced pain model and metabolomics. Results Different brands of gel plaster had great difference in their skin followability, disclosing ability, initial adhesion and peeling degree. The initial adhesion and peel degree of gel patch had great influence on its disclosing ability and the greater the initial adhesion and peel degree were, the worse disclosing ability was. The matrix of the Aconiti Radix gel patch was 3% polyacrylic acid sodium NP700, 1.5% carboxymethyl cellulose sodium, 0.25% Carbomer, 0.06% crystalline aluminum chloride, 0.1% ethylenediamine tetra acetic acid two sodium, 26% glycerol, 61.5% water, 4% diatomaceous earth, 0.15% tartaric acid;Drug dosage of each gel patch was 560 mg extracts of Aconiti Radix. Zanthoxyli Pericarpium olatile oil could enhance the analgesic effect of Aconiti Radix gel patch, which might be mainly through glycerol phospholipid metabolism and linoleic acid metabolism. Conclusion To ensure better adherence and disclosure of gel patch, the initial adhesive force of gel patch should be controlled between 7-18 balls and the peel degree should be controlled between 0.03-0.97 kN/m. The Prepared Aconiti Radix gel patch has a good appearance, adhesion and shape with a clear analgesic effect, and Zanthoxyli Pericarpium olatile oil can enhance analgesic effect of Aconiti Radix gel patch. This study provides a basis for the development and application of new preparations for the external use in Aconiti Radix.
作者
许润春
贺亚男
裴瑾
耿福能
杨明
张定堃
XU Run-chun;HE Ya-nan;PEI Jin;GENG Fu-neng;YANG Ming;ZHANG Ding-kun(State Key Laboratory Breeding Base of Systematic Research of Development and Utilization of Chinese Medicine Resources,Chengdu University of Traditional Chinese Medicine,Chengdu 611137,China;Sichuan Good Doctor Panxi Pharmaceutical Co.,Ltd.,Xichang 615000,China;Jiangxi University of Traditional Chinese Medicine,Nanchang 330004,China)
出处
《中草药》
CAS
CSCD
北大核心
2020年第6期1517-1529,共13页
Chinese Traditional and Herbal Drugs
基金
四川省中医药管理局中医药科研专项(2018QN008)
四川省中医药管理局花椒专项(2018HJZX008)
江西省重大科技研发专项(20194ABC28009)。
关键词
川乌
凝胶贴膏
成型工艺
花椒挥发油
配伍增效
皮肤追随性
揭帖性
初黏力
持黏力
剥离度
混料设计
代谢组学
镇痛
甘油磷脂代谢
亚油酸代谢
Aconiti Radix
gel patch
molding process
Zanthoxyli Pericarpium volatile oil
compatibility-synergistic mechanism
skin followability
disclosing property
initial adhesion
holding power
peeling strength
mixture design
metabolomics
analgesia
glycerophospholipid metabolism
linoleic acid metabolism
