摘要
本研究采用逆向工程技术对Doppelherz®Energy DIRECT产品进行处方及工艺剖析,为自研复方咖啡因无水吞服颗粒的开发提供指导。处方剖析部分以产品官网原辅料信息为基础,根据药典及文献方法建立各辅料的检测方法,结合重量分析法确定处方中各原辅料用量,最终确定上市制剂的原辅料组成为:咖啡因、牛磺酸、B族维生素、无水葡萄糖(71.4%)、柠檬酸(7.0%)、山梨醇、三氯蔗糖、硬脂酸镁(<5.8%)。根据专利查询及拉曼成像等技术,基本确定了上市制剂的制备工艺,并在其基础上完成了自研制剂的开发。研究获得了军事医学研究院审查委员会的伦理批准,结合口感评价实验及制剂在1 min内咖啡因溶出量实验的结果,筛选出了热熔挤出技术作为自研制剂的掩味技术,通过差示扫描量热分析对热熔挤出工艺参数完成了筛选,最终制得口感好且质量合格的产品,为相关制剂的研发提供了可参考的方法。
In this study,the reverse engineering technology was used to analyze the prescription and process of Doppelherz®Energy DIRECT,based on the composition of the prescription on the official website of the product,the detection method of composition is established according to the pharmacopoeia and literature information,combined with gravimetric analysis to complete prescription analysis.The prescription composition of the reference listed drug was determined to be composed of caffeine,taurine,vitamin B,anhydrous glucose,citric acid,sorbitol,sucralose,magnesium salts of fatty acids,in which the glucose content was 71.4%,the citric acid content was 7.0%and the magnesium salts of fatty acids content was<5.8%.According to patent inquiry,Raman imaging and other technologies,the preparation process of the marketed preparation has been basically obtained,and the development of the self-made preparation has been completed on this basis.The study was approved by the Ethics Committee of the Academy of Military Medical Sciences.Combined with the results of the taste evaluation experiment and the caffeine dissolution test of the preparation in 1 min,the hot-melt extrusion technology was screened out as the taste-masking technology of the self-made preparation,the parameters of the hot-melt extrusion process were screened by differential scanning calorimetry analysis,and finally a product with good taste and qualified quality was obtained,which provided a reference method for the research and development of related preparations.
作者
范坤
丁珮
韩晓璐
王增明
李蒙
于彦周
郑爱萍
FAN Kun;DING Pei;HAN Xiao-lu;WANG Zeng-ming;LI Meng;YU Yan-zhou;ZHENG Ai-ping(Institute of Toxicology and Pharmacology,Academy of Military Medical Sciences,Beijing 100850,China;Sports Medical Department of Military Sports Training Center,Beijing 100851,China)
出处
《药学学报》
CAS
CSCD
北大核心
2022年第8期2512-2519,共8页
Acta Pharmaceutica Sinica
基金
国家“重大新药创制”科技重大专项资助项目(2018ZX09721003-007).
关键词
逆向工程
咖啡因
疲劳
掩味技术
热熔挤出
reverse engineering
caffeine
fatigue
taste masking technology
hot-melt extrusion
