槲皮素固体分散体单层渗透泵片的研制

doi:10.5246/jcps.2015.06.049

中国药学(英文版) ›› 2015, Vol. 24 ›› Issue (6): 383-392.DOI: 10.5246/jcps.2015.06.049

槲皮素固体分散体单层渗透泵片的研制

郝海军^1,2*, 贾幼智¹, 张红芹³, 韩茹¹, 王雪萍¹, 韩丽妹², 王建新²

1. 上海医药工业研究院分析测试中心, 上海 200437
2. 复旦大学药学院, 上海 201203
3. 国家中药制药工程技术研究中心, 上海 201203

收稿日期:2015-01-14 修回日期:2015-02-27 出版日期:2015-06-26 发布日期:2015-03-29
通讯作者: Tel.: 86-21-55514600-222
基金资助:
National Science & Technology Pillar Program during the 12th Five-year Plan Period (Grant No. 2012BAI29B08).

Preparation of monolithic osmotic tablet of quercetin loaded by solid dispersion

Haijun Hao^1,2*, Youzhi Jia¹, Hongqin Zhang³, Ru Han¹, Xueping Wang¹, Limei Han², Jianxin Wang²

1. Instrumental Analysis & Research Center, Shanghai Institute of Pharmaceutical Industry, Shanghai 200437, China
2. School of Pharmacy, Fudan University, Shanghai 201203, China
3. National Engineering Research Center for Traditional Chinese Medicine, Shanghai 201203, China

Received:2015-01-14 Revised:2015-02-27 Online:2015-06-26 Published:2015-03-29
Contact: Tel.: 86-21-55514600-222
Supported by:
National Science & Technology Pillar Program during the 12th Five-year Plan Period (Grant No. 2012BAI29B08).

摘要/Abstract

摘要：

本文主要介绍槲皮素单层渗透泵控释片的制备方法, 采用固体分散体技术提高槲皮素的溶解度和溶出速率。采用槲皮素固体分散体、助悬剂、渗透活性物质和其他辅料作为渗透泵片片芯, 以添加增塑剂的醋酸纤维素作为渗透泵片的控释膜; 通过优化处方中PEO用量、NaCl用量、增塑剂用量和包衣增重得到最优处方, 并探讨药物从单层渗透泵片中的释放机理。优化后的槲皮素固体分散体单层渗透泵片处方, 药物释放呈零级释药特征, 且12小时内释放度达到90.74%。本方法为制备其他难溶性药物控释片提供了新的策略。

关键词: 槲皮素, 固体分散体, 单层渗透泵, 控释制剂

Abstract:

The objective of this study was to prepare monolithic osmotic tablet of quercetin for controlled drug release. Quercetin-PVP solid dispersion was prepared to enhance its solubility and dissolution rate. Solid dispersion, suspending agents, osmotic agents and other conventional excipients were used as tablet core composition and cellulose acetate (CA) with plasticizer as release controlling membrane. Different formulation variables, the amounts of PEO (polyethylene oxide), NaCl, plasticizer, and coating weight gain were optimized to gain the optimum formulation. The mechanism of drug release from monolithic osmotic tablet was also discussed. The optimal monolithic osmotic pump tablet could deliver quercetin at the rate of approximate zero-order up to 12 h, and the cumulative release was 90.74%. The developed monolithic osmotic system for quercetin loaded by solid dispersion was found to be a promising approach for controlled release of poorly-water soluble drug candidates.

Key words: Quercetin, Solid dispersion, Monolithic osmotic tablet, Controlled drug delivery system

中图分类号:

R944

Supporting:

郝海军, 贾幼智, 张红芹, 韩茹, 王雪萍, 韩丽妹, 王建新. 槲皮素固体分散体单层渗透泵片的研制[J]. 中国药学(英文版), 2015, 24(6): 383-392.

Haijun Hao, Youzhi Jia, Hongqin Zhang, Ru Han, Xueping Wang, Limei Han, Jianxin Wang. Preparation of monolithic osmotic tablet of quercetin loaded by solid dispersion[J]. Journal of Chinese Pharmaceutical Sciences, 2015, 24(6): 383-392.

参考文献

[1] Siew, A. Pharm. Tech. 2013, 7, 40-44.

[2] Singhal, A.; Jain, H.; Singhal, V.; Elias, E.J.; Showkat, A. Pharmacognosy Res. 2011, 3, 35-39.

[3] Pang, X.; Lu, Z.; Du, H.; Yang, X.; Zhai, G. Colloids Surf. B Biointerfaces. 2014, 123, 778-786.

[4] Conley, R.; Gupta, S.K.; Sathyan, G. Curr. Med. Res. Opin. 2006, 22, 1879-1892.

[5] Liu, L.X.; Khang, G.; Rhee, J.M.; Lee, H.B. J. Control. Release. 2000, 67, 309-322.

[6] Hao, H.J.; Jia, Y.Z.; Han, R. J. Chin. Pharm.Sci. 2013, 22, 385-392.

[7] Lu, E.X.; Jiang, Z.Q.; Zhang, Q.Z.; Jiang, X.G. Chin. Pharm. J. 2002, 37, 841-844.

[8] Alexandra, H.; Simon, G.; Markus, W.; Karsten, M. J. Control. Release. 2012, 158, 403-412.

[9] Han, X.; Ghoroi, C.; To, D.; Chen, Y.; Dave, R. Int. J. Pharm. 2011, 415, 185-195.

[10] Surendra, S.; Kunal, P.; Mayur, S.; Pradeep, V. Int. J. Pharm. Tech. Res. 2013, 5, 730-745.

[11] Zhang, X.; Yi, Y.N.; Qi, J.P.; Lu, Y.; Tian, Z.Q.; Xie, Y.C.; Yuan, H.L.; Wu, W. Int. J. Pharm. 2013, 452, 233-240.

[12] Huang, Y.B.; Dai, W.G. Acta Pharm. Sinica. B. 2014, 4, 18-25.

[13] Xie, Y.C.; Lu, Y.; Qi, J.P.; Li, X.Y.; Zhang, X.; Han, J.; Jin, S.X.; Yuan, H.L.; Wu, W. Inter. J. Pharm. 2013, 441, 111-120.

[14] Zhu, J.; Yang, Z.G.; Chen, X.M.; Sun, J. B.; Awuti, G.; Zhang, X.; Zhang, Q. J. Chin. Pharm. Sci. 2007, 16, 51-56.

[15] Yang, Z.G.; Gulisitan, A.; Cao. Y.; Zhu, J.; Wu, B.S.; Wang, J.C.; Lu, W.L.; Zhang, Q. J. Chin. Pharm. Sci. 2006, 15, 69-75.

[16] Shokri, J.; Ahmadi, P.; Rashidi, P.; Shahsavari, M.; Rajabi-Siahboomi, A.; Nokhodchi, A. Eur. J. Pharm. Biopharm. 2008, 68, 289-297.

[17] Lu, E.X.; Jiang, Z.Q.; Zhang, Q.Z.; Jiang, X.G. J. Control. Release. 2003, 92, 375-382.

[18] Liu, L.; Xu, X. Int. J. Pharm. 2008, 352, 225-230.

[19] Zhang, Y.; Xin, T.G.; Ye, T.T.; Yang, X.G.; Pan, W.S. Asian. J. Pharm. Sci. 2014, 9, 35-41.

[20] Chen, H.H.; Jiang, G.Q.; Ding, F.X. Drug Dev. Ind. Pharm. 2009, 35, 131-137,

[21] Kumaravelraian, R.; Narayanan, N.; Suba, V. Lipids Health Dis. 2011, 10, 51-63.

槲皮素固体分散体单层渗透泵片的研制

Preparation of monolithic osmotic tablet of quercetin loaded by solid dispersion

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