11种盐酸小檗碱片剂在不同溶出度介质中溶出度曲线特征的比较

doi:10.5246/jcps.2020.02.008

中国药学(英文版) ›› 2020, Vol. 29 ›› Issue (2): 102-112.DOI: 10.5246/jcps.2020.02.008

11种盐酸小檗碱片剂在不同溶出度介质中溶出度曲线特征的比较

余飞^1,2,3,4, 周文莉^1,2,3,4, 阚家义^4*, 彭灿^1,2,3*

1. 安徽中医药大学, 安徽合肥 230012
2. 中药复方安徽省重点实验室, 安徽合肥 230012
3. 安徽省中医药科学院药物制剂研究所, 安徽合肥 230012
4. 安徽省食品药品检验研究所, 安徽合肥 230051

收稿日期:2019-10-25 修回日期:2019-11-24 出版日期:2020-02-29 发布日期:2019-12-24
通讯作者: Tel.: +86-13956024560; +86-13965046611, E-mail: Pengcan@ahtcm.edu.cn; 1487835386@qq.com
基金资助:
National Institutes for Food and Drug Control (Grant No. 017ZX09101001).

Comparison of dissolution profile characteristics of 11 berberine hydrochloride tablet brands in different dissolution media

Fei Yu^1,2,3,4, Wenli Zhou^1,2,3,4, Jiayi Kan^4*, Can Peng^1,2,3*

1. School of Pharmacy, Anhui University of Chinese Medicine, Hefei, Anhui 230012, China
2. Anhui Province Key Laboratory of Chinese Medicinal Formula, Hefei, Anhui 230012, China
3. Institute of Pharmaceutics, Anhui Academy of Chinese Medicine, Hefei, Anhui 230012, China
4. Anhui Institutes for Food and Drug Control, Hefei, Anhui 230051, China

Received:2019-10-25 Revised:2019-11-24 Online:2020-02-29 Published:2019-12-24
Contact: Tel.: +86-13956024560; +86-13965046611, E-mail: Pengcan@ahtcm.edu.cn; 1487835386@qq.com
Supported by:
National Institutes for Food and Drug Control (Grant No. 017ZX09101001).

摘要/Abstract

摘要：

盐酸小檗碱通常用于治疗细菌性痢疾、肠胃炎和其他疾病。当今市场上有许多生产厂家, 生产过程和配方却大不相同, 这可能直接影响药物的治疗效果。为此, 根据药典中盐酸小檗碱溶出法(篮法), 检测了11种不同生产厂家的盐酸小檗碱片剂。此外, 分别考察其在四种不同pH值的溶出介质中的溶出过程, 采用相似因子(f₂) 评估。通过高效液相色谱(HPLC) 对不同厂家的盐酸小檗碱片的体外溶出度进行测定。该方法具有线性好、精度高、稳定性好、重复性好等优点。基于f₂值, 大部分生产厂家的盐酸小檗碱片剂的溶解行为存在显着差异。该研究也为以后的进一步深入研究奠定了基础。尽管药物规格(0.1 g)相同, 但溶出曲线存在差异。这种现象可能是因为片剂的赋形剂和晶型影响片剂在体外的释放和溶解。

关键词: 盐酸小檗碱, 片剂, 溶出, 高效液相法, 方法学, 体外试验

Abstract:

Berberine hydrochloride is commonly used to treat bacterial dysentery, gastroenteritis and other diseases. Many manufacturers are available on the market today, while the production process and formulation are quite different, which may directly affect the therapeutic effect of the drug. To this end, 11 different production producers of berberine hydrochloride tablets were collected according to the pharmacopeia berberine hydrochloride dissolution method (basket method). In addition, the dissolution process was carried out in four elution media with different pH, and the difference was similar (f₂). Factors were calculated to evaluate in vitro dissolution requirements, and in vitro dissolution of different manufacturers of berberine hydrochloride tablets was determined by high performance liquid chromatography (HPLC). The method was verified by linearity, precision, stability and robustness. Based on the f₂ value, there was a significant difference in the dissolution behavior of the formulations of most berberine hydrochloride tablet brands. This research provided the basis for further in-depth research in the later period. Although the drug specifications (0.1 g) were the same, the dissolution curve was different. This phenomenon may be attributed to the fact that the excipients and crystal form of the tablets affected the release and dissolution of the tablets in vitro.

Key words: Berberine hydrochloride, Tablet, Dissolution, HPLC analysis, Method validation, In vitro test

中图分类号:

R944

Supporting:

余飞, 周文莉, 阚家义, 彭灿. 11种盐酸小檗碱片剂在不同溶出度介质中溶出度曲线特征的比较[J]. 中国药学(英文版), 2020, 29(2): 102-112.

Fei Yu, Wenli Zhou, Jiayi Kan, Can Peng. Comparison of dissolution profile characteristics of 11 berberine hydrochloride tablet brands in different dissolution media[J]. Journal of Chinese Pharmaceutical Sciences, 2020, 29(2): 102-112.

参考文献

[1] Jia, B.X.; Li, Y.Q.; Wang, D.C.; Duan, R. Study on the interaction of β-cyclodextrin and berberine hydrochloride and its analytical application. PLoS One. 2014, 9, e95498.

[2] Wen, A.L.; Peng, X.X.; Zhang, P.P.; Long, Y.F.; Gong, H.M.; Xie, Q.R.; Yue, M.; Chen, S. Spectrofluorometric determination of berberine using a novel Au nanocluster with large Stokes shift. Anal. Bioanal. Chem. 2018, 410, 6489-6495.

[3] Tan, W.; Li, Y.B.; Chen, M.W.; Wang, Y.T. Berberine hydrochloride: anticancer activity and nanoparticulate delivery system. Int. J. Nanomedicine. 2011, 6, 1773-1777.

[4] Zhu, T.Y.; Wang, Y.D.; Kong, H.W. Clinical study on Berberine Hydrochloride Tablets combined with mesalazine in treatment of distal ulcerative colitis. Drugs Clin. 2018, 33, 3183-3186.

[5] Guo, S.J.; Wang, Y.P.; Fu, S.J.; Zhang, Z.M.; Xu, Q.Q.; Determination of Berberine Hydrochloride Content in Qingwen Baidu Granule by HPLC. Anim. Husb. Feed Sci. 2014, 6, 27-30.

[6] Wang, D.; Xu, Q.L.; Zuo, D.; Xiong, H.L. Determination of berberine hydrochloride in Shihu yeguang pills by HPLC. Med. Plant. 2010, 1, 74-75, 78.

[7] Nie, L.R.; Song, H.; Yohannes, A.; Liang, S.W.; Yao, S. Extraction in cholinium-based magnetic ionic liquid aqueous two-phase system for the determination of berberine hydrochloride in Rhizoma coptidis. RSC Adv. 2018, 8, 25201-25209.

[8] Wagner, D.; Glube, N.; Berntsen, N.; Tremel, W.; Langguth, P. Different dissolution media lead to different crystal structures of talinolol with impact on its dissolution and solubility. Drug Dev. Ind. Pharm. 2003, 29, 891-902.

[9] Desai, D.; Wong, B.; Huang, Y.D.; Tang, D.; Hemenway, J.; Paruchuri, S.; Guo, H.; Hsieh, D.; Timmins, P. Influence of dissolution media pH and USP1 basket speed on erosion and disintegration characteristics of immediate release metformin hydrochloride tablets. Pharm. Dev. Technol. 2015, 20, 540-545.

[10] Kovačič, N.N.; Pišlar, M.; Ilić, I.; Mrhar, A.; Bogataj, M. Influence of the physiological variability of fasted gastric pH and tablet retention time on the variability of in vitro dissolution and simulated plasma profiles. Int. J. Pharm. 2014, 473, 552-559.

[11] Hoti, E.; Censi, R.; Ricciutelli, M.; Malaj, L.; Barboni, L.; Martelli, S.; Valleri, M.; Di Martino, P. Validation of an HPLC-MS method for rociverine tablet dissolution analysis. J. Pharm. Biomed. Anal. 2008, 47, 422-428.

[12] Ji, J.; He, X.; Yang, X.L.; Du, W.J.; Cui, C.L.; Wang, L.; Wang, X.; Zhang, C.F.; Guo, C.R. The in vitro/vivo evaluation of prepared gastric floating tablets of berberine hydrochloride. AAPS PharmSciTech. 2017, 18, 2149-2156.

[13] Paim, C.S.; Martins, M.T.; Malesuik, M.D.; Steppe, M. LC determination of entacapone in tablets: in vitro dissolution studies. J. Chromatogr. Sci. 2010, 48, 755-759.

[14] Huang, J.; Goolcharran, C.; Ghosh, K. A Quality by Design approach to investigate tablet dissolution shift upon accelerated stability by multivariate methods. Eur. J. Pharm. Biopharm. 2011, 78, 141-150.

[15] Box, K.J.; Comer, J.; Taylor, R.; Karki, S.; Ruiz, R.; Price, R.; Fotaki, N. Small-scale assays for studying dissolution of pharmaceutical cocrystals for oral administration. AAPS PharmSciTech. 2016, 17, 245-251.

[16] Rachid, O.; Rawas-Qalaji, M.; Simons, F.E.; Simons, K.J. Dissolution testing of sublingual tablets: a novel in vitro method. AAPS PharmSciTech. 2011, 12, 544-552.

[17] Kraemer, J.; Gajendran, J.; Guillot, A.; Schichtel, J.; Tuereli, A. Dissolution testing of orally disintegrating tablets. J. Pharm. Pharmacol. 2012, 64, 911-918.

[18] Ferrero, C.; Jiménez-Castellanos, M.R. In vitro release testing of matrices based on starch-methyl methacrylate copolymers: effect of tablet crushing force, dissolution medium pH and stirring rate. Int. J. Pharm. 2014, 461, 270-279.

[19] Maezawa, K.; Yajima, R.; Terajima, T.; Kizu, J.; Hori, S. Dissolution profile of 24 levofloxacin (100 mg) tablets. J. Infect. Chemother. 2013, 19, 996-998.

[20] Yuce, M.; Capan, Y. Development and validation of hplc analytical methods used-for determination of assay, content uniformity and dissolution of immediate release candesartan cilexetil 32 Mg tablets. Acta Pol. Pharm. 2017, 74, 357-367.

[21] Hussain, A.; Qureshi, F.; Abbas, N.; Arshad, M.S.; Ali, E. An evaluation of the binding strength of okra gum and the drug release characteristics of tablets prepared from it. Pharmaceutics. 2017, 9, E20.

[22] Simionato, L.D.; Petrone, L.; Baldut, M.; Bonafede, S.L.; Segall, A.I. Comparison between the dissolution profiles of nine meloxicam tablet brands commercially available in Buenos Aires, Argentina. Saudi Pharm. J. 2018, 26, 578-584.

[23] Gabbott, I.P.; Al Husban, F.; Reynolds, G.K. The combined effect of wet granulation process parameters and dried granule moisture content on tablet quality attributes. Eur. J. Pharm. Biopharm. 2016, 106, 70-78.

[24] Guo, H.; Zhang, Z.; Yao, Y.; Liu, J.L.; Chang, R.R.; Liu, Z.; Hao, H.Y.; Huang, T.H.; Wen, J.; Zhou, T.T. A new strategy for statistical analysis-based fingerprint establishment: Application to quality assessment of Semen sojae praeparatum. Food Chem. 2018, 258, 189-198.

[25] Kassahun, H.; Asres, K.; Ashenef, A. In vitro and in vivo quality evaluation of glibenclamide tablets marketed in Addis Ababa, Ethiopia. J. Pharm. (Cairo). 2018, 1-7.

[26] Grube, A.; Gerlitzki, C.; Brendel, M. Dissolution or disintegration - substitution of dissolution by disintegration testing for a fixed dose combination product. Drug Dev. Ind. Pharm. 2019, 45, 130-138.

[27] Nickerson, B.; Kong, A.; Gerst, P.; Kao, S.M. Correlation of dissolution and disintegration results for an immediate-release tablet. J. Pharm. Biomed. Anal. 2018, 150, 333-340.

[28] Stumpf, F.; Keck, C.M. Tablets made from paper. Int. J. Pharm. 2018, 548, 812-819.

[29] Mayock, S.P.; Saim, S.; Fleming, A.B. In vitro drug release after crushing: evaluation of xtampza® ER and other ER opioid formulations. Clin. Drug Investig. 2017, 37, 1117-1124.

[30] Franc, A.; Muselík, J.; Zeman, J.; Lukášová, I.; Kurhajec, S.; Bartoníčková, E.; Galvánková, L.; Mika, F.; Dominik, M.; Vetchý, D. The effect of amorphous and crystal sodium warfarin and its content uniformity on bioequivalence of tablets. Eur. J. Pharm. Sci. 2018, 125, 120-129.

[31] Braig, V.; Konnerth, C.; Peukert, W.; Lee, G. Enhanced dissolution of naproxen from pure-drug, crystalline nanoparticles: A case study formulated into spray-dried granules and compressed tablets. Int. J. Pharm. 2019, 554, 54-60.

11种盐酸小檗碱片剂在不同溶出度介质中溶出度曲线特征的比较

Comparison of dissolution profile characteristics of 11 berberine hydrochloride tablet brands in different dissolution media

RichHTML

PDF (PC)

可视化

摘要/Abstract

引用本文

使用本文

参考文献

相关文章 15

编辑推荐

Metrics

本文评价

[1]	陈谕园, 吴松, 陈丽青, 张媛媛, 高钟镐, 李天磊, 黄伟, 杨庆云. 激光衍射法测定地拉罗司的粒径分布及其与体外溶出度的相关性研究[J]. 中国药学(英文版), 2021, 30(11): 912-923.
[2]	沈新宇, 王星辰, 顾彩虹, 严峰, 潘博, 高利增, 颜丙春, 刘岐, 胡荣. 较人参皂苷Rg3生物高效的新型制剂-竹节参片研究[J]. 中国药学(英文版), 2019, 28(9): 650-664.
[3]	马维娜, 谷福根, 王毅, 孟根达来, 吴春芝. 羟丙基-β-环糊精对水难溶性药物利培酮的包合及促溶作用[J]. 中国药学(英文版), 2015, 24(1): 47-53.
[4]	宋文丁, 杜若, 宋平, 钟婷, 张卫强, 赵阳, 王超, 张烜, 张强. 非布索坦二氧化硅固体分散体的制备及表征[J]. 中国药学(英文版), 2014, 23(7): 463-470.
[5]	肖珑, 韩晋, 黄雪, 张媛媛, 袁海龙^*, 肖小河. 基于生物检测的双黄连片溶出度研究[J]. , 2011, 20(1): 77-82.
[6]	孙葭北, 刘祥瑞, 王坚成, 吕万良, 张烜*, 张强. 紫杉醇-PVP固体分散体的制备、物相鉴定及细胞药效 [J]. , 2008, 17(2): 113-117.
[7]	朱静, 杨照罡, 陈晓梅, 孙葭北, 古丽斯坦·阿吾提, 张烜^*, 张强. 槲皮素PVP固体分散体的制备及物相鉴定[J]. , 2007, 16(1): 51-56.
[8]	魏兰兰, 孙佩男, 田蕾, 唐歆, 姚婷婷, 潘卫三^*. 卡维地洛固体自微乳化药物传递系统的应用[J]. , 2006, 15(4): 223-227.
[9]	舒德忠, 万先惠, 刘华蓉, 杨俊卿, 周岐新^*. 盐酸小檗碱对葡聚糖硫酸钠所致小鼠结肠炎的作用研究[J]. , 2006, 15(3): 182-187.
[10]	全东琴^*, 徐贵霞. 维甲酸自乳化给药系统的体外溶出及比格犬药物动力学研究[J]. , 2005, 14(2): 105-109.
[11]	谷福根, 崔福德^*, 高永良. 羟丙基-β-环糊精的包合作用对前列腺素E₁溶解度、溶出速率及稳定性的影响[J]. , 2004, 13(3): 158-165.
[12]	李凤前^*, 胡晋红, 姜远英. 水飞蓟素-聚乙二醇6000固体分散体系的制备及其特征考察[J]. , 2003, 12(2): 76-81.
[13]	赵甘霖, 沈晓斌. 尼莫地平由溶胀性亲水性骨架中释放的动力学[J]. , 2000, 9(2): 104-107.
[14]	苏杰, 崔勇, 张钧寿. 评价固体制剂的体内外相关性的一种新方法[J]. , 1999, 8(4): 222-228.
[15]	赵甘霖, 沈晓斌. 尼莫地平固体分散体在速释制剂中的溶出性质[J]. , 1999, 8(2): 68-72.