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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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.
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.
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.
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.
KeywordsSuppository PEG Witepsol Acetamidophenol β-cyclodextrin Controlled release
- 1.David SJ. Pharmaceutics dosage form and design, 2nd edition, chapter 4; 2016:4–7.Google Scholar
- 2.Jahromi MM, Ghaemi H, Tafti MA, Arabzadeh A, Afsharypuor S. Vaginal and rectal dosage forms in Iranian traditional pharmacy. J Nat Pharm Prod. 2015;10:1–3.Google Scholar
- 3.Schrewsbury R. Applied pharmaceutics in contemporary compounding, 3rd edition, 2015.Google Scholar
- 4.Baviskara P, Bedsea A, Sadiqueb S, Kundea V, Jaiswal S. Drug delivery on rectal absorption: suppositories. Int J Pharm Sci Rev Res. 2013;13:70–6.Google Scholar
- 5.El-Majri MA, El-Basir MM. Formulation and evaluation of ibuprofen suppositories. J Res Pharm Pract. 2016;7:87–90.Google Scholar
- 8.Sinha VR, Nanda A, Kumria R. Cyclodextrins as sustained-release carriers. J Pharm Technol 2002:36–46.Google Scholar
- 9.Allen JR, Loyd V. Quality control of suppositories. Suppositories, 1st edition; 2007:139–158.Google Scholar
- 10.Yousfan A, Hasian J. Preparation and evaluation of levodropropizine suppositories. J Chem Pharm Res. 2015;7:274–82.Google Scholar
- 11.Ramadan AA. Formulation and evaluation of bioadhesive vaginal suppositories containing miconazole nitrate. J Pharm Bio Sci. 2013;4:455–72.Google Scholar
- 12.Pandey S, Varshney HM, Gupta MM. Effect of adjuvants on the release pattern of suppositories containing paracetamol. J Chem Environ Sci. 2013;1:19–25.Google Scholar
- 13.Amiri S, Rahimi A. Self-healing hybrid nanocomposite coatings containing encapsulated organic corrosion inhibitors nanocontainers. J Polym Res 2014, DOI: https://doi.org/10.1007/s10965-014-0624-z.
- 14.Amiri S, Rahimi A. Synthesis and characterization of supramolecular corrosion inhibitor nanocontainers for anticorrosion hybrid nanocomposite coatings. J Polym Res. 2015 DOI: https://doi.org/10.1007/s10965-015-0699-1
- 15.Amiri S, Rahimi A. Preparation of supramolecular corrosion inhibitor nanocontainers for self-protective hybrid nanocomposite coatings. J Polym Res 2014, DOI: https://doi.org/10.1007/s10965-014-0566-5
- 18.The United States Pharmacopeia, USP 38, Volume 1, 2015.Google Scholar
- 19.Cwiertnia B. Effect of water soluble carrier on dissolution profiles of diclofenac sodium. J Pharm Technol. 2013;70:721–6.Google Scholar
- 20.Gowthamarajan K, Kulkarni TG, Nenkateswaran G, Samanta MK, Suresh B. Formulation and dissolution properties of meloxicam solid dispersion incorporated suppositories. Indian J Pharm Sci. 2002;1:525–8.Google Scholar