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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Influence of polyvinylpyrrolidone quantity on the solubility, crystallinity and oral bioavailability of fenofibrate in solvent-evaporated microspheres
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Influence of polyvinylpyrrolidone quantity on the solubility, crystallinity and oral bioavailability of fenofibrate in solvent-evaporated microspheres

机译：聚乙烯吡咯烷酮数量对非诺贝特在溶剂蒸发微球中的溶解度，结晶度和口服生物利用度的影响

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摘要

The objective of this study is to explore the influence of polyvinylpyrrolidone (PVP) quantity on the solubility, crystallinity and oral bioavailability of poorly water-soluble fenofibrate in solvent-evaporated microspheres. Numerous microspheres were prepared with fenofibrate, sodium lauryl sulphate (SLS) and PVP using the spray-drying technique. Their aqueous solubility, dissolution, physicochemical properties and pharmacokinetics in rats were assessed. The drug in the solvent-evaporated microspheres composed of fenofibrate, PVP and SLS at the weight ratio of 1:0.5:0.25 was not entirely changed to the amorphous form and partially in the microcrystalline state. However, the microspheres at the weight ratio of 1:4:0.25 provided the entire conversion to the amorphous form. The latter microspheres, with an improvement of about 115000-fold in aqueous solubility and 5.6-fold improvement in oral bioavailability compared with the drug powder, gave higher aqueous solubility and oral bioavailability compared with the former. Thus, PVP quantity played an important role in these properties of fenofibrate in the solvent-evaporated microspheres.
机译：这项研究的目的是探讨聚乙烯吡咯烷酮（PVP）量对水溶性差的非诺贝特在溶剂蒸发微球中的溶解度，结晶度和口服生物利用度的影响。使用喷雾干燥技术，用非诺贝特，月桂基硫酸钠（SLS）和PVP制备了许多微球。评估了它们在大鼠中的水溶性，溶解性，理化性质和药代动力学。由非诺贝特，PVP和SLS重量比为1：0.5：0.25组成的溶剂蒸发微球中的药物并未完全变为无定形形式，并且部分处于微晶态。然而，重量比为1：4：0.25的微球提供了全部转化为无定形形式。与药物粉末相比，后一种微球的水溶性提高约115000倍，口服生物利用度提高5.6倍，与前者相比，其水溶性和口服生物利用度更高。因此，PVP的量在溶剂蒸发微球中非诺贝特的这些特性中起着重要作用。

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