非布索坦二氧化硅固体分散体的制备及表征

doi:10.5246/jcps.2014.07.061

中国药学(英文版) ›› 2014, Vol. 23 ›› Issue (7): 463-470.DOI: 10.5246/jcps.2014.07.061

非布索坦二氧化硅固体分散体的制备及表征

宋文丁¹, 杜若¹, 宋平¹, 钟婷¹, 张卫强¹, 赵阳¹, 王超¹, 张烜^1,2*, 张强^1,2

1. 北京大学医学部药学院药剂学系, 北京 100191
2. 北京大学医学部药学院天然药物及仿生药物国家重点实验室, 北京 100191

收稿日期:2014-05-05 修回日期:2014-05-14 出版日期:2014-07-18 发布日期:2014-05-31
通讯作者: Tel.: +86-10-82805928, Fax: +86-10-82805928
基金资助:
National Natural Science Foundation of China (Grant No. 81172992) and the National Basic Research Program of China (Grant No. 973 Program 2009CB930300) and Innovation Team of Ministry of Education (Grant No. BMU20110263).

The preparation and characteristics of febuxostat SiO2 solid dispersions

Wending Song¹, Ruo Du¹, Ping Song¹, Ting Zhong¹, Weiqiang Zhang¹, Yang Zhao¹, Chao Wang¹, Xuan Zhang^1,2*, Qiang Zhang^1,2

1. Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University Health Sciences Center, Beijing 100191, China
2. State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University Health Sciences Center, Beijing 100191, China

Received:2014-05-05 Revised:2014-05-14 Online:2014-07-18 Published:2014-05-31
Contact: Tel.: +86-10-82805928, Fax: +86-10-82805928
Supported by:
National Natural Science Foundation of China (Grant No. 81172992) and the National Basic Research Program of China (Grant No. 973 Program 2009CB930300) and Innovation Team of Ministry of Education (Grant No. BMU20110263).

摘要/Abstract

摘要：

本文选择Sylysia (SiO₂)为多孔载体材料, 以非布索坦(febuxostat, FBT)为模型药物, 制备非布索坦二氧化硅固体分散体并进行表征。首先我们建立了非布索坦的HPLC测定方法, 对非布索坦固体分散体的DSC、PXRD、SEM和粒径进行表征, 对非布索坦固体分散体的溶解度和溶出度进行测定。DSC和PXRD数据结果表明, 非布索坦在固体分散体中以无定型存在。SEM和粒径结果表明, 非布索坦固体分散体的粒径和Sylysia相近。溶解度和溶出度结果显示, 非布索坦固体分散体的溶解度和溶出度相对于非布索坦而言显著提高。上述结果表明, 所制备的非布索坦固体分散体可增加难溶性药物非布索坦的溶解度和溶出度。

关键词: 非布索坦, Sylysia, 固体分散体, 溶解度和溶出度

Abstract:

In the present research, we selected Sylysia as a porous material and febuxostat (FBT) as model drug to prepare the FBT SiO₂ solid dispersions using a solvent evaporation method. We firstly established an HPLC method for determining FBT in our prepared FBT SiO₂ solid dispersions. And then, the characteristics of FBT SiO₂ solid dispersions were investigated, including differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), scanning electron microscope (SEM), particle size and distribution. The solubility and dissolution of FBT SiO₂ solid dispersion were also evaluated. The results of DSC and PXRD showed that the FBT existed in an amorphous state in FBT SiO₂ solid dispersions. The SEM and particle size results indicated that the shape and average particle size of FBT SiO₂ solid dispersions was similar to the Sylysia. The solubility and dissolution of FBT in FBT SiO₂ solid dispersions were significantly enhanced compared with the pure FBT. In conclusion, we successfully prepared FBT SiO₂ solid dispersions to increase the solubility and dissolution rate of the poorly water-soluble FBT.

Key words: Febuxostat, Sylysia, Solid dispersion, Solubility and dissolution

中图分类号:

R943

Supporting:

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.

Wending Song, Ruo Du, Ping Song, Ting Zhong, Weiqiang Zhang, Yang Zhao, Chao Wang, Xuan Zhang, Qiang Zhang. The preparation and characteristics of febuxostat SiO2 solid dispersions[J]. Journal of Chinese Pharmaceutical Sciences, 2014, 23(7): 463-470.

参考文献

[1] O’Driscoll, C.M.; Griffin, B.T. Adv. Drug Deliv. Rev. 2008, 60, 617-624.

[2] Gamsiz, E.D.; Thombre, A.G.; Ahmed, I. Ann. Biomed. Eng. 2011, 39, 455-468.

[3] Thakkar, H.P.; Patel, B.V.; Thakkar, S.P. J. Pharm. Bioallied. Sci. 2011, 3, 426-434.

[4] Shah, S.; Maddineni, S.; Lu, J.; Repka, M.A. Int. J. Pharm. 2013, 453, 233-252.

[5] Laza-Knoerr, A.L.; Gref, R.; Couvreur, P. J. Drug Target. 2010,18, 645-656.

[6] Miura, H.; Kanebako, M.; Shirai, H.; Nakao, H.; Inagi, T.; Terada, K. Eur. J. Pharm. Biopharm. 2010, 76, 215-221.

[7] Simovic, S.; Heard, P.; Hui, H.; Song, Y.; Peddie, F.; Davey, A.K.; Lewis, A.; Rades,T.; Prestidge, C.A. Mol. Pharm. 2009, 6, 861-872.

[8] Zhang, Y.; Wang, J.; Bai, X.; Jiang, T.; Zhang, Q.; Wang, S. Mol. Pharm. 2012, 9, 505-513.

[9] Ahuja, G.; Pathak, K. Indian J. Pharm. Sci. 2009, 71, 599-607.

[10] Wu, C.; Wang, Z.; Zhi, Z.; Jiang, T.; Zhang, J.; Wang, S. Int. J. Pharm. 2011, 403, 162-169.

[11] Sharma, S.; Sher, P.; Badve, S.; Pawar, A.P. AAPS. Pharm. Sci. Tech. 2005, 6, 618-625.

[12] Ito, Y.; Arai, H.; Uchino, K.; Iwasaki. K.; Shibata, N.; Takada, K. Int. J. Pharm. 2005, 289, 69-77.

[13] Miura, H.; Kanebako, M.; Shirai, H.; Nakao, H.; Inagi, T.; Terada, K. Chem. Pharm. Bull. 2011, 59, 686-691.

[14] Takeuchi, H.; Nagira, S.; Yamamoto, H.; Kawashima, Y. Int. J. Pharm. 2005, 293, 155-164.

[15] Wang, L.; Cui, F.D.; Sunada, H. Chem. Pharm. Bull. 2006, 54, 37-43.

[16] Uchino, T.; Yasuno, N.; Yanagihara, Y.; Suzuki, H. Pharmazie. 2007, 62, 599-603.

[17] Miura, H.; Kanebako, M.; Shirai, H.; Nakao, H.; Inagi, T.; Terada, K. Eur. J. Pharm. Biopharm. 2010, 76, 215-221.

[18] Planinšek, O.; Kovačič, B.; Vrečer, F. Int. J. Pharm. 2011, 406, 41-48.

[19] Kovačič, B.; Vrečer, F.; Planinšek, O. Chem. Pharm. Bull. 2011, 59, 427-433.

[20] Miura, H.; Kanebako, M.; Shirai, H.; Nakao, H.; Inagi, T.; Terada, K. Chem. Pharm. Bull. 2011, 59, 686-691.

[21] Jia, Z.; Lin, P.; Xiang, Y.; Wang, X.; Wang, J.; Zhang, X.; Zhang, Q. Eur. J. Pharm. Biopharm. 2011, 79, 126-134.

[22] Wang, X.Q.; Fan, J.M.; Liu, Y.O.; Zhao, B.; Jia, Z.R.; Zhang, Q. Int. J. Pharm. 2011, 419, 339-346.

[23] Jondhale, S.; Bhise, S.; Pore, Y. AAPS. Pharm. Sci. Tech. 2012, 13, 448-459.

[24] Ernst, M.E.; Fravel, M.A. Clin. Ther. 2009, 31, 2503-2518.A

[25] Tayar, J.H.; Lopez-Olivo, M.A.; Suarez-Almazor, M.E. Cochrane Database Syst. Rev. 2012, 11, CD008653.

[26] Hussar, D.A.; ABilbow, C. J. Am. Pharm.Assoc (2003). 2009, 49, 460-463.

[27] Tomillero, A.; Moral, M.A. Clin. Pharmacol. 2009, 31, 541-557.

[28] Kumar, S.; Gupta, S.K. Recent Pat. Drug Deliv. Formul. 2013, 7, 111-121.

[29] Alam, M.A.; Ali, R.; Al-Jenoobi, F.I.; Al-Mohizea, A.M. Expert Opin. Drug Deliv. 2012, 9, 1419-1440.

[30] Warren, D.B.; Benameur, H.; Porter, C.J.; Pouton, C.W. J. Drug Target. 2010, 18, 704-731.

[31] Tran, P.H.; Tran, T.T.; Lee, K.H.; Kim, D.J.; Lee, B.J. Expert Opin. Drug Deliv. 2010, 7,647-661.

非布索坦二氧化硅固体分散体的制备及表征

The preparation and characteristics of febuxostat SiO2 solid dispersions

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