Abstract Poorly water soluble drugs often show low oral bioavailability due to their low dissolution rate. In the present study, cross-linked poly(vinyl alcohol) hydrogel microspheres were prepared. Nanocrystals of fenofibrate as a model of poorly water soluble drugs were dispersed within the poly(vinyl alcohol) hydrogel microspheres by swelling the microspheres with fenofibrate/methanol solution, followed by evaporation of the solvent methanol. The fenofibrate dissolution rate from the fenofibrate-loaded hydrogel microspheres in a medium simulating gastrointestinal tract conditions was much higher than the dissolution rate of free fenofibrate. And the dissolution assay also showed that fenofibrate released from the hydrogel in a sustained manner. In vivo pharmacokinetic study showed that the fenofibrate-loaded hydrogel microspheres showed much higher bioavailability compared with free fenofibrate, and similar bioavailability but longer half-lives and mean residence time and lower maximum plasma concentration compared with a marked fenofibrate formulation Lipanthyl® after oral administration in rats, indicating that the fenofibrate-loaded PVA hydrogel exhibited lower fluctuation in plasma drug concentration and more sustained release behavior.

中文翻译：

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含有分散的非诺贝特纳米晶体的交联聚乙烯醇水凝胶微球作为口服持续递送系统

摘要 水溶性差的药物由于溶出度低，口服生物利用度低。在本研究中，制备了交联聚乙烯醇水凝胶微球。通过用非诺贝特/甲醇溶液使微球溶胀，然后蒸发溶剂甲醇，将作为水溶性差的药物模型的非诺贝特纳米晶体分散在聚乙烯醇水凝胶微球中。在模拟胃肠道条件的介质中，负载非诺贝特的水凝胶微球的非诺贝特溶出率远高于游离非诺贝特的溶出率。溶出试验还表明非诺贝特以持续的方式从水凝胶中释放出来。