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Preparation and Evaluation of Novel Supersaturated Solid Dispersion of Magnolol

Theme: Advancements in Amorphous Solid Dispersions to Improve Bioavailability

  • Research Article
  • Theme: Advancements in Amorphous Solid Dispersions to Improve Bioavailability
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Abstract

This article aimed to design a new type of supersaturated solid dispersion (NS-SD) loaded with Magnolol (Mag) to raise the oral bioavailability in rats. In the light of the solubility parameters, phase solubility experiments, inhibition precipitation experiment, and in vitro release experiment, Plasdone-630 (PS-630) was selected as the optimum carrier. In addition, Mag-NS-SD was prepared by adding Monoglyceride (MG) and Lecithin High Potency (LHP) into the Mag-S-SD (Mag:PS-630 = 1:3), so as to reduce the dosage of carrier and improve the release rate. Using central composite design of response surface method, the prescription was further optimized. As the optimized condition was Mag:PS-630: MG: LHP = 1:3:0.8:0.266, the drug release rate was the fastest. Besides, after 45 min, the release rate was nearly 100%. The constructed Mag-S-SD and Mag-NS-SD were characterized by powder X-ray diffraction and infrared absorption spectrum. The XRD patterns of Mag-S-SD and Mag-NS-SD indicated that all APIs were amorphous. The IR spectra of Mag-S-SD and Mag-NS-SD demonstrated the existence of hydrogen bonding in the systems. Furthermore, in vivo pharmacokinetic study in rats revealed that compared with Mag and Mag-S-SD, Mag-NS-SD significantly increased the bioavailability (the relative bioavailability was 213.69% and 142.37%, separately). In this study, Mag-NS-SD was successfully prepared, which could improve the oral bioavailability and may increase the clinical application.

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Acknowledgements

We are grateful that this work was supported by grants from 2020 Liaoning Provincial Department of Education Scientific Research Funding Project—Key Research Project (NO. 2020LZD02) and Open Fund of the State Key Laboratory of New Technology of Chinese Medicine Pharmaceutical Process (No. SKL2020Z0206).

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Authors and Affiliations

  1. School of Traditional Chinese Medicine, Shenyang Pharmaceutical University, No.103, Wenhua Road, Shenyang, 110016, China

    Jing Zhao, Pan Gao, Wenbin Deng & Dongxu Ji

  2. School of Pharmacy, Shenyang Pharmaceutical University, No.103, Wenhua Road, Shenyang, 110016, China

    Chengqiao Mu, Haowei Sun & Xinggang Yang

  3. Wuya College of Innovation, Shenyang Pharmaceutical University, No.103, Wenhua Road, Shenyang, 110016, China

    Jingqi Ning

  4. Faculty of Functional Food and Wine, Shenyang Pharmaceutical University, No.103, Wenhua Road, Shenyang, 110016, China

    Xiangrong Zhang

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  1. Jing Zhao
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Contributions

Jing Zhao: conceptualization, methodology, formal analysis, investigation, resources, data curation, writing—review and editing, visualization, supervision, project administration; Pan Gao: conceptualization, methodology, formal analysis, investigation, resources, data curation, writing—original draft, visualization, supervision, project administration; Chengqiao Mu: conceptualization, formal analysis, investigation, data curation; Jingqi Ning: conceptualization, methodology, data acquisition, formal analysis; Wenbin Deng: conceptualization, methodology, formal analysis, data curation; Dongxu Ji: literature review, writing—original draft, data curation; Haowei Sun: writing—original draft, visualization, supervision; Xiangrong Zhang: conceptualization, methodology, formal analysis, writing—review and editing, project administration; Xinggang Yang: conceptualization, methodology, formal analysis, writing—review and editing, project administration, funding acquisition.

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Correspondence to Xiangrong Zhang or Xinggang Yang.

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Jing Zhao and Pan Gao have contributed equally to this work and share first authorship.

Theme: Advancements in Amorphous Solid Dispersions to Improve Bioavailability

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Zhao, J., Gao, P., Mu, C. et al. Preparation and Evaluation of Novel Supersaturated Solid Dispersion of Magnolol. AAPS PharmSciTech 23, 97 (2022). https://doi.org/10.1208/s12249-022-02251-7

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