Effects of particle size on the pharmacokinetics of puerarin nanocrystals and microcrystals after oral administration to rat |
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Authors: | Liangxing Tu Yueneng Yi Wei Wu Fuqiang Hu Kaili Hu Jianfang Feng |
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Institution: | 1. Murad Research Center for Modernized Chinese Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, People''s Republic of China;2. School of Pharmacy, Fudan University, Shanghai 201203, People''s Republic of China;3. School of Pharmacy, Zhejiang University, 388 Yu Hangtang Road, Hangzhou 310058, People''s Republic of China |
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Abstract: | Puerarin, which is extracted from traditional Chinese medicine, is widely used in clinic in China and mainly used as a therapeutic agent to cardiovascular diseases. Owing to its poor water solubility and adverse drug reactions caused by cosolvents after intravenous administration, the development of oral formulation is urgently needed. Nowadays, nanocrystals technique has become a preferred way to develop oral dosage form. In this study, we used high pressure homogenization (HPH) to prepare puerarin nanocrystals and microcrystals with different sizes ranged from 525.8 nm to 1875.6 nm and investigated the influence of particle size on pharmacokinetics. The nanocrystals and microcrystals prepared were characterized using DLS, DSC, XRD and SEM, and we found that the crystalline state of puerarin was changed during the preparation process and the drug was dispersed into HPMC. In the pharmacokinetic study, we observed an increasing of Cmax and AUC and a decreasing of CL/F with the decreasing of particle size. The AUC of the puerarin nanocrystals (525.8 nm) was 7.6-fold of that of raw puerarin suspension, with an absolute bioavailability of 21.44%. From the above results, we can conclude that nanocrystal technique is an efficient technology to improve the oral bioavailability of puerarin. |
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Keywords: | Puerarin Nanocrystals Microcrystals Bioavailability Particle size |
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