基于物料性质表征的小儿蒲地蓝消炎糖浆剂型优化评价研究  

Optimization and evaluation of Xiaoer Pudilan Xiaoyan Syrup based on characterization of material properties

作　　者：李萱 丁珂 杨挡 姜梦华 李超 朱法根 邵建国 孙娥[1] 封亮 贾晓斌 LI Xuan;DING Ke;YANG Dang;JIANG Meng-hua;LI Chao;ZHU Fa-gen;SHAO Jian-guo;SUN E;FENG Liang;JIA Xiao-bin(Affiliated Hospital of Integrated Traditional Chinese and Western Medicine,Nanjing University of Chinese Medicine,Nanjing 210028,China;Jiangsu Key Laboratory of Chinese Medicine and Characteristic Preparations for Pediatrics,Jumpcan Pharmaceutical Co.,Ltd.,Taixing 225400,China;School of Traditional Chinese Pharmacy,China Pharmaceutical University,Nanjing 211198,China)

机构地区：[1]南京中医药大学附属中西医结合医院,江苏南京210028 [2]济川药业集团有限公司江苏省儿科中药与特色制剂重点实验室,江苏泰兴225400 [3]中国药科大学中药学院,江苏南京211198

出　　处：《中国中药杂志》2022年第21期5746-5756,共11页China Journal of Chinese Materia Medica

基　　金：国家重点研发计划项目(2018YFC1706902);江苏省儿科中药与特色制剂重点实验室开放课题项目(BM2019011);江苏省科技成果转化专项(BA2020077);江苏省医学创新团队项目(CXTDB2017003);江苏省研究生实践与创新计划项目(SJCX21-0716);中国药科大学双一流创新团队项目(CPU2018GY11);江苏省卫生健康发展研究中心开放课题团队项目(JSHD2021040);天然药物活性组分与药效国家重点实验室自主项目(SKLNMZZ202025)。

摘　　要：通过对蒲地蓝消炎口服液的口感分析可知,口服液不良口感主要来源于中药本身所固有的不良口感和制剂过程中引入的不良口感,导致其口感很难受儿童欢迎。因此,针对儿童这一特殊患群,通过工艺优化和剂型改进技术,制成小儿蒲地蓝消炎糖浆剂来改善不良口感,从而提高儿童服药依从性。以蒲地蓝消炎口服液和小儿蒲地蓝消炎糖浆的流浸膏物料性质为基础,通过比较两者的制剂性质(pH、密度、浊度、黏度、色度、粒径)、口感、5种质量标志物含量以及体内的药动学特征,评价小儿蒲地蓝消炎糖浆剂型优化的适宜性。结果表明,与蒲地蓝消炎口服液相比,小儿蒲地蓝消炎糖浆的pH、密度、浊度、黏度和色度性质显著改变,不良口感降低26%,主要有效成分菊苣酸转移率升高,黄芩苷的转移率与口服液相差较小;同时通过药代动力学可知,黄芩苷体内吸收总量较高,糖浆中黄芩苷和汉黄芩素的达峰时间Tmax显著延长,紫堇灵的体内滞留时间MRTlast显著延长;小儿蒲地蓝消炎糖浆和蒲地蓝消炎口服液在体内的吸收程度相同:黄芩苷>汉黄芩素>紫堇灵。新剂型工艺较原剂型简单,符合大生产需求,安全环保,合理可行,为小儿蒲地蓝消炎糖浆剂型优化的适宜性和科学性提供了依据,同时也为小儿蒲地蓝消炎糖浆进一步安全、合理用药奠定基础,从而扩大儿童临床应用范围。According to the taste analysis of Pudilan Xiaoyan Oral Liquid, the unpleasant taste of the oral liquid is mainly caused by the inherent taste of Chinese medicine and the taste introduced in the preparation process, which leads to its unpopularity among children. Therefore, aiming at the special children patient group, Xiaoer Pudilan Xiaoyan Syrup was developed via technology optimization and dosage form improvement to improve the unpleasant taste and enhance the medication compliance among children. Based on the material properties of Pudilan Xiaoyan Oral Liquid and Xiaoer Pudilan Xiaoyan Syrup extracts, the authors compared the properties(pH, density, turbidity, viscosity, chromaticity, particle size), taste, content of five quality markers and in vivo pharmacokinetic characteristics of these two preparations, to evaluate the suitability of Xiaoer Pudilan Xiaoyan Syrup. The results showed that compared with those of Pudilan Xiaoyan Oral Liquid, the pH, density, turbidity, viscosity and chromaticity of Xiaoer Pudilan Xiaoyan Syrup were significantly changed, and the unpleasant taste was reduced by 26%;the transfer rate of the main active ingredients chicoric acid was increased, while the transfer rate of baicalin had small difference from that of the oral liquid. In addition, pharmacokinetics revealed that the total absorption amount of baicalin in vivo was higher, and the time to peak Tmaxof baicalin and oroxindin in the syrup and the mean residence time MRTlastof corynoline in vivo were significantly prolonged. The absorption degree of Xiaoer Pudilan Xiaoyan Syrup and Pudilan Xiaoyan Oral Liquid in the body was the same: baicalin>oroxindin>corynoline. The new dosage form process was simpler than that of the original dosage form, safe, environmentally friendly, reasonable and feasible, meeting the mass production demand. This provided a basis for the reasonable and scientific optimization of Xiaoer Pudilan Xiaoyan Syrup, and also laid a foundation for its further safe and rational use, so as to expand the clini

关 键 词：小儿蒲地蓝消炎糖浆 剂型优化 物料性质表征 口感 有效性 药动学 

分 类 号：R283.6[医药卫生—中药学]