药学学报, 2021, 56(8): 2282-2288
引用本文:
张天翼, 杜若飞, 王优杰, 胡佳亮, 吴飞*, 冯怡*. 盐酸小檗碱树脂复合物的制备、表征及其体外释放[J]. 药学学报, 2021, 56(8): 2282-2288.
ZHANG Tian-yi, DU Ruo-fei, WANG You-jie, HU Jia-liang, WU Fei*, FENG Yi*. Preparation, characterization and in vitro release of berberine hydrochloride resin complex[J]. Acta Pharmaceutica Sinica, 2021, 56(8): 2282-2288.

盐酸小檗碱树脂复合物的制备、表征及其体外释放
张天翼, 杜若飞, 王优杰, 胡佳亮, 吴飞*, 冯怡*
上海中医药大学, 中药现代制剂技术教育部工程研究中心, 上海 201203
摘要:
制备具有掩味效果的盐酸小檗碱树脂复合物。以盐酸小檗碱为模型药物,Amberlite IRP69为载药树脂,通过阐明一定温度范围内盐酸小檗碱在潜溶剂中的溶解度与温度关系曲线,指导复合物制备过程中盐酸小檗碱的加入量及反应温度等参数的研究。对制得的复合物进行物性表征和体外释放研究,验证复合物的形成并预测复合物的体内释放行为。实验结果表明,用60%乙醇作为潜溶剂在50℃下恒温搅拌1 h,制得的复合物载药量和药物利用率分别为35%和64%,且具有较好的掩味效果。本研究提供了一种制备盐酸小檗碱掩味制剂的方法。
关键词:    盐酸小檗碱      离子交换树脂      掩味      药物树脂复合物      溶解度     
Preparation, characterization and in vitro release of berberine hydrochloride resin complex
ZHANG Tian-yi, DU Ruo-fei, WANG You-jie, HU Jia-liang, WU Fei*, FENG Yi*
Engineering Research Center of Modern Preparation Technology of TCM of Ministry of Education, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China
Abstract:
The object of this study is to preparate the berberine hydrochloride (BBH) resin compound with taste masking effect. We took the BBH as the model drug and Amberlite IRP69 as the drug carriers, uncovered the curve of solubility of BBH in different cosolvent with a certain range of temperature, and then used it to calculate the parameters during the preparation of the complex such as adding quantity of BBH and the reaction temperature. Afterwards, the characteristic and in vitro release experiments were studied to verify the formation and predict the in vivo release behavior of the complex. The results showed that in the condition of using 60% ethanol as a cosolvent and stirring at 50℃ for 1 h, the drug loading and drug availability of the complex are at about 35% and 64%, respectively, and has a better taste-masking effect. In this study, a method was provided for preparing a taste-masking preparation of BBH.
Key words:    berberine hydrochloride    ion exchange resin    taste masking    drug-resin complex    solubility   
收稿日期: 2021-03-09
DOI: 10.16438/j.0513-4870.2021-0347
通讯作者: 吴飞,Tel/Fax:86-21-51322431,E-mail:wufei_shutcm@126.com;冯怡,Tel/Fax:86-21-51322493,E-mail:fyi_shutcm@163.com
Email: wufei_shutcm@126.com;fyi_shutcm@163.com
相关功能
PDF(650KB) Free
打印本文
0
作者相关文章
张天翼  在本刊中的所有文章
杜若飞  在本刊中的所有文章
王优杰  在本刊中的所有文章
胡佳亮  在本刊中的所有文章
吴飞*  在本刊中的所有文章
冯怡*  在本刊中的所有文章

参考文献:
[1] Su F, Yan JL, Li Y, et al. Research progresses in ion exchange resin in extended/controlled-release and taste masking pharmaceutical preparations[J]. Cent South Pharm (中南药学), 2020, 18:1852-1857.
[2] Li WN, Nan Y, Yang DQ, et al. Application of ion exchange resins in preparation of traditional Chinese medicine[J]. Acta Chin Med Pharm (中医药学报), 2011, 39:101-102.
[3] Strickley RG, Iwata Q, Wu S, et al. Pediatric drugs——a review of commercially available oral formulations[J]. J Pharm Sci, 2008, 97:1731-1774.
[4] Aman RM, Meshali MM, Abdelghani GM. Ion-exchange complex of famotidine:sustained release and taste masking approach of stable liquid dosage form[J]. Drug Discov Ther, 2014, 8:268-275.
[5] Alayoubi A, Daihom B, Adhikari H, et al. Development of a tastemasked oral suspension of clindamycin HCl using ion exchange resin Amberlite IRP 69 for use in pediatrics[J]. Drug Dev Ind Pharm, 2016, 42:1579-1589.
[6] Kouchak M, Ramezani Z, Bagheri F. Preparation and evaluation of taste masking iron suspension:taking advantage of weak cationic exchange resin[J]. AAPS PharmSciTech, 2018, 19:719-729.
[7] Fan TY, Yang YS, Hu XX, et al. Anti-MRSA activities of cycloberberine derivatives with a novelchemical scaffold[J]. Acta Pharm Sin (药学学报), 2019, 54:1627-1635.
[8] Jiang LY, Wu RG. Research progress of berberrine[J]. Guangdong Chem Ind (广东化工), 2021, 48:274-275.
[9] Fu LN. Study In Vitro Dissolution and Establishment of the Dissolution Methods of Poorly Souble Drugs (难溶性药物体外溶出评价及溶出度方法的建立) [D]. Hangzhou:Zhejiang University of Technology, 2014.
[10] State Pharmacopoeia Commission. Pharmacopoeia of the People's Republic of China (中华人民共和国药典) [S]. 2020 Ed. Vol 4. Beijing:China Medical Science Press, 2020:132.
[11] Zeng HX. Studies on Drug Delivery System with Drug-Resinate Complex and Its Pharmacokinetics (离子交换树脂复合物的药物传递系统与药物动力学研究) [D]. Shenyang:Shenyang Pharmaceutical University, 2008.
[12] Zhang YE. Design and Preparation of Sustained Release Suspension of Ambroxol Hydrochloride Ion-Exchange Resin Complex (盐酸氨溴索-离子交换树脂缓释混悬液的研制) [D]. Suzhou:Soochow University, 2017.
[13] Lin X, Poudel AJ, Huang LX, et al. Nanocellulose hyperfine network achieves sustained release of berberine hydrochloride solubilized with β -cyclodextrin for potential anti-infection oral administration[J]. Int J Biol Macromol, 2020, 153:633-640.
[14] Tan DCT, Ong JJ, Gokhale R, et al. Hot melt extrusion of ionexchange resin for taste masking[J]. Int J Pharm, 2018, 547:385-394.
[15] Zhao MH, Wang SN, Li XH, et al. Preparation of sustained release berberine hydrochloride ion-exchange resin complex by one-step method in alcohol-water mixed solvent[J]. J Shenyang Pharm Univ (沈阳药科大学学报), 2019, 36:554-560.
[16] Zhang QM, Xie MF, Ning BM, et al. Evaluation of solid oral products by dissolution profiles in different mediums[J]. Chin J Pharm (中国医药工业杂志), 2009, 40:946-950, 955.
相关文献:
1.陈飞;张悦;刘强;庞茗之;杨星钢;潘卫三.星点设计法优化盐酸小檗碱树脂复合胃黏附给药系统的研究[J]. 药学学报, 2008,43(9): 963-968