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Dissolution and oral bioavailability enhancement of praziquantel by solid dispersions

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Abstract

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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Funding

This research was supported by the Key Laboratory of Animal Disease Control and Prevention ordinary (120105) operated by Northeast Agricultural University and also supported by the Supporting Program for Sci & Tech Research of China (2015BAD11B03-07) and by the earmarked fund for China Agriculture Research System (CARS-35).

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Author notes

  1. Yanyan Liu and Tianzi Wang are contributed equally to this work and should be considered co-first authors.

Authors and Affiliations

  1. College of Veterinary Medicine, Northeast Agricultural University, Harbin, 150030, People’s Republic of China

    Yanyan Liu, Tianzi Wang, Wenya Ding, Chunliu Dong, Xiaoting Wang, Jianqing Chen & Yanhua Li

  2. Heilongjiang Key Laboratory for Animal Disease Control and Pharmaceutical Development, Harbin, 150086, China

    Yanyan Liu, Wenya Ding, Chunliu Dong, Xiaoting Wang, Jianqing Chen & Yanhua Li

  3. Daxing District Center of Animal Disease Control, Beijing, 102600, China

    Tianzi Wang

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  1. Yanyan Liu
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Correspondence to Yanhua Li.

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The study was performed according to the Guiding Principles in the Use of Animals in Toxicology, as amended in 2008 by the Society of Toxicology.

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The authors declare that they have no conflicts of interest.

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All applicable international, national, and/or institutional guidelines for the care and use of animals were followed.

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Liu, Y., Wang, T., Ding, W. et al. Dissolution and oral bioavailability enhancement of praziquantel by solid dispersions. Drug Deliv. and Transl. Res. 8, 580–590 (2018). https://doi.org/10.1007/s13346-018-0487-7

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