明胶胶囊中伯胺基含量测定研究与应用  

Determination of primary amine groups in gelatin capsules:research and application

作　　者：崔迎 苏宇 凌宗涛 董华平[1] 寿建昕[1] 朱帅辉 徐慧婷 骆翔 CUI Ying;SU Yu;LING Zongtao;DONG Huaping;SHOU Jianxin;ZHU Shuaihui;XUHuiting;LUO Xiang(Shaoxing University,Shaoxing 312000,China;Zhejiang Huaguang Capsule Co.,Ltd.,Shaoxing 312500,China)

机构地区：[1]绍兴文理学院,浙江绍兴312000 [2]浙江华光胶囊股份有限公司,浙江绍兴312500

出　　处：《中国药剂学杂志（网络版）》2023年第4期198-204,共7页Chinese Journal of Pharmaceutics：Online Edition

基　　金：2020年新昌县科技攻关计划(20200008);2020年浙江省大学生科技创新活动计划暨新苗人才计划(2020R444007);绍兴文理学院校级重点科研项目(2019LG1002)。

摘　　要：目的胶囊剂系指将药物盛装于硬质空胶囊或具有弹性的软质胶囊中制成的固体制剂,明胶胶囊占胶囊总量的90%以上。明胶胶囊易发生明胶—明胶自身交联或明胶—药物分子间交联。明胶胶囊中伯胺基含量可作为评价明胶胶囊交联程度的指标,对胶囊壳的质量控制有重大意义。需要探究出一种快速、准确检测明胶胶囊中伯胺基含量的方法。方法该研究以明胶胶囊壳为材料,运用茚三酮法、2,4,6-三硝基苯磺酸法(TNBS)分别对明胶胶囊壳中伯胺基含量进行测定。结果运用TNBS法测得2017年与2020年所产胶囊壳的伯胺基含量分别为(6.62×10^(-3)±2.37×10^(-4))mmol·mg^(-1)、(1.32×10^(-2)±5.57×10^(-4))mmol·mg^(-1)。然而,采用茚三酮法测得2017年与2020年所产胶囊壳的伯胺基含量分别为(2.42×10^(-3)±5.57×10^(-5))mmol·mg^(-1)、(3.39×10^(-3)±3.02×10^(-5))mmol·mg^(-1)。结论本研究发现茚三酮法对伯胺基的检测灵敏度较差,而TNBS法可以较为有效和准确地测定明胶中的伯胺基。我们通过测定伯胺基含量,准确定量评估胶囊壳交联程度,不但为解决明胶胶囊交联问题提供了理论基础和技术指导,而且有助于提高明胶胶囊的质量控制水平和胶囊有效期的准确界定。Purpose Capsules are solid preparations of drugs in hard and empty capsules or flexible and soft capsules,with gelatin capsules accounting for more than 90%of the total number of capsules.Gelatin capsules are prone to gelatin-gelatin self-crosslinking or gelatin-drug intermolecular crosslinking.The content of primary amino groups in gelatin capsules can be used as an indicator to evaluate the degree of cross-linking of gelatin capsules,which is of great significance for gelatin capsules quality monitoring.It is necessary to explore a rapid and accurate method for the determination of primary amino groups content in gelatin capsules.Methods This study was performed using ninhydrin colorimetric method and 2,4,6-trinitrobenzene sulfonic acid(TNBS)method for the quantitative analysis of primary amino groups in gelatin capsule.Results The contents of primary amino groups in gelatin capsules produced in 2017 and 2020 were(6.62×10^(-3)±2.37×10^(-4))mmol·mg^(-1) and(1.32×10^(-2)±5.57×10^(-4))mmol·mg^(-1) with TNBS method,respectively.However,the data obtained by ninhydrin colorimetric method were(2.42×10^(-3)±5.57×10^(-5))mmol·mg^(-1) and(3.39×10^(-3)±3.02×10^(-5))mmol·mg^(-1),respectively.Conclusion The results reveal that the sensitivity of the ninhydrin colorimetric method is not sensitive enough for the determination of primary amino groups in gelatin capsules.Therefore,the TNBS method is the most effective and accurate method for primary amino groups assay in gelatin capsules.In summary,this study provides a suitable method to evaluate the cross-linking degree of gelatin capsules by primary amino groups assay.By measuring the content of primary amino group,we evaluate the quantitative crosslinkin g degree of gelatin capsules,which not only provides a theoretical basis and technical guidance for solving the crosslinking problem of gelatin capsules,but also improves the quality control of gelatin capsules and accurately defined the validity period of gelatin capsules.

关 键 词：明胶胶囊 伯胺基含量 明胶交联 2 4 6-三硝基苯磺酸法 茚三酮法 

分 类 号：R94[医药卫生—药剂学]