Improved dissolution rate and bioavailability of fenofibrate pellets prepared by wet-milled-drug layering

Author： Wang Puxiu   Luo Qing   Miao Yuqiang   Ying Lin   He Haibing   Cai Cuifang   Tang Xing  

Publisher： Informa Healthcare

ISSN： 0363-9045

Source： Drug Development and Industrial Pharmacy, Vol.38, Iss.11, 2012-11, pp. : 1344-1353

Disclaimer: Any content in publications that violate the sovereignty, the constitution or regulations of the PRC is not accepted or approved by CNPIEC.

Previous Menu Next

Abstract

Objective: The objective of this study is to investigate the wet-milled-drug layering process which could significantly improve the dissolution rate and oral bioavailability of fenofibrate pellets.Methods: Fenofibrate was milled with HPMC-E5 to prepare a uniform suspension in the micrometer and nanometer range, and this suspension was then layered on to sugar spheres to form the pellets (F1, F2).Results: The particle size was significantly reduced (from 1000 µm to 1–10 µm and 400 nm) but the fenofibrate in suspension retained its crystallinity from the results of DSC and PXRD investigations. The dissolution rate of F1-F2 and Antara® capsules was 55.47 %, 61.27 % and 58.43 %, respectively, in 0.01 mol/L SDS solution over 60 min. In addition, F1, F2, and Antara® capsules were given orally to 6 beagle dogs to determine the bioavailability. The Cmax of F1, F2 (8.21 ± 2.55 and 9.33 ± 2.37 μg/mL)and the AUC(0−t) of F1, F2 (152.46 ± 78.89 and 172.17 ± 67.58 μg/mL·h)were higher than those of Antara® (6.02 ± 3.34 μg/mL and 89.82 ± 46.46 μg/mL·h) and, F1, F2 reached their Cmax earlier than Antara® (F1: 2.0 ± 1.1 h; F2: 1.8 ± 1.2 h; Antara®: 6.0 ± 8.9 h).Conclusion: These results show that the wet-milled-drug layering technique is a powerful method to improve the dissolution rate and the bioavailability of fenofibrate.

Related content

Preparation of fenofibrate immediate-release tablets involving wet grinding for improved bioavailability

By Zhang Lili   Chai Guihong   Zeng Xueping   He Haibing   Xu Hui   Tang Xing  

Drug Development and Industrial Pharmacy, Vol. 36, Iss. 9, 2010-09 ,pp. : 1054-1063 (10)

Informa Healthcare

Access to resources Recommend Favorite

Enhanced dissolution rate and oral bioavailability of simvastatin nanocrystal prepared by sonoprecipitation

By Jiang Tongying   Han Ning   Zhao Buwen   Xie Yuling   Wang Siling  

Drug Development and Industrial Pharmacy, Vol. 38, Iss. 10, 2012-10 ,pp. : 1230-1239 (10)

Informa Healthcare

Access to resources Recommend Favorite

Enhancement of oral bioavailability of fenofibrate by solid self-microemulsifying drug delivery systems

By Kim Gun Gook   Poudel Bijay K.   Marasini Nirmal   Lee Dong Won   Hiep Tran Tuan   Yang Kwan Yeol   Kim Jong Oh   Yong Chul Soon   Choi Han-Gon  

Drug Development and Industrial Pharmacy, Vol. 39, Iss. 9, 2013-09 ,pp. : 1431-1438 (8)

Informa Healthcare

Access to resources Recommend Favorite

Investigation into physical–chemical variables affecting the manufacture and dissolution of wet-milled clarithromycin nanoparticles

By Shahbazi Niaz Maliheh   Traini Daniela   Young Paul M.   Ghadiri Maliheh   Rohanizadeh Ramin  

Pharmaceutical Development and Technology, Vol. 19, Iss. 8, 2014-12 ,pp. : 911-921 (11)

Informa Healthcare

Access to resources Recommend Favorite

Dissolution rate limited bioavailability of flutamide, and in vitro - in vivo correlation

By Posti J.   Katila K.   Kostiainen T.  

European Journal of Pharmaceutics and Biopharmaceutics, Vol. 49, Iss. 1, 2000-01 ,pp. : 35-39 (5)

Elsevier

Access to resources Recommend Favorite