Dissolution and oral bioavailability enhancement of praziquantel by solid dispersions

被引:0
作者
Yanyan Liu
Tianzi Wang
Wenya Ding
Chunliu Dong
Xiaoting Wang
Jianqing Chen
Yanhua Li
机构
[1] Northeast Agricultural University,College of Veterinary Medicine
[2] Heilongjiang Key Laboratory for Animal Disease Control and Pharmaceutical Development,undefined
[3] Daxing District Center of Animal Disease Control,undefined
来源
Drug Delivery and Translational Research | 2018年 / 8卷
关键词
Praziquantel; Solid dispersion; Dissolution; Bioavailability; Solubility;
D O I
暂无
中图分类号
学科分类号
摘要
The aim of the present investigation was to enhance the solubility, dissolution, and oral bioavailability of praziquantel (PZQ), a poorly water-soluble BCS II drug (Biopharmaceutical Classification System), using a solid dispersion (SD) technique involving hydrophilic copolymers. The SD formulations were prepared by a solvent evaporation method with PZQ and PEG 4000 (polyethylene glycol 4000), PEG 6000, or P 188 polymers at various weight ratios or a combination of PEG 4000/P 188. The optimized SD formulation, which had the highest solubility in distilled water, was further characterized by its surface morphology, crystallinity, and dissolution in 0.1 M HCl with 0.2% w/v of sodium dodecyl sulfate (SDS). X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR) revealed the amorphous form of PZQ in the SDs. Moreover, at an oral dosage of 5 mg/kg PZQ, the SDs had higher Cmax values and areas under the curve (AUCs) compared to those of commercial PZQ tablets. Preparation of PZQ-loaded SDs using PEG 4000/P 188 is a promising strategy to improve the oral bioavailability of PZQ.
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页码:580 / 590
页数:10
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