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Improve Solubility of Acetamidophenol from PEG and Witepsol Suppositories via Formation of Inclusion Complex by β-Cyclodextrin with a Controlled Release Profile

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Abstract

Purpose

Acetamidophenol (ACP) is used to treat mild to moderate pain and reduce fever, but low water solubility and poorly dissolution of this compound restricted its bioavailability.

Methods

To overcome these problems and enhance the solubility of ACP, inclusion complex between ACP and β-cyclodextrin (β-CD) is formed with various mass ratios of β-CD:ACP (1:1, 1:2, 1:4, 1:8), and the effect of complex formation on solubility and release of ACP from PEG and Witepsol-based suppositories through rectal route of administration is investigated.

Results

Inclusion complexes formed with various ratios of β-CD:ACP and loaded in the formulation of suppositories by fusion method utilizing different suppository bases, i.e., Witepsol H15 and polyethylene glycol (4000, 400). FTIR, SEM, and XRD results indicate formation of inclusion complex between β-CD and ACP. Physical characteristics and in vitro drug release of the obtained suppositories are determined by several tests such as weight variation, melting point, hardness, and release rate.

Conclusion

Results indicate that PEG-based suppositories containing β-CD:ACP 1:1 mass ratio show the best in vitro drug release characteristic which released 19.3% of ACP after 8 h.

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Authors and Affiliations

  1. Department of Polymer Engineering, Science and Research Branch, Islamic Azad University, Tehran, Iran

    Faezeh Asgari & Sahar Amiri

  2. Iran Polymer and Petrochemical Institute, IPPI, Department of Polymer Science, Faculty of Science, P.O. Box: 14965/115, Tehran, Iran

    Majid Ghiass

Authors
  1. Faezeh Asgari
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  2. Sahar Amiri
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  3. Majid Ghiass
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Correspondence to Sahar Amiri.

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Asgari, F., Amiri, S. & Ghiass, M. Improve Solubility of Acetamidophenol from PEG and Witepsol Suppositories via Formation of Inclusion Complex by β-Cyclodextrin with a Controlled Release Profile. J Pharm Innov 14, 57–65 (2019). https://doi.org/10.1007/s12247-018-9328-y

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  • DOI: https://doi.org/10.1007/s12247-018-9328-y

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