Structure and hydration properties of hydroxypropyl methylcellulose matrices containing naproxen and naproxen sodium

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  • Additional Information
    • Affiliation:
      a Department of Pharmaceutics, School of Pharmacy, The Hebrew University of Jerusalem, PO Box 12065, Jerusalem 91120, Israel
      b Department of Pharmaceutics, Free University, Kelchstrasse 31, 12169 Berlin, Germany
    • Keywords:
      Hydroxypropyl methylcellulose
      Naproxen
      Hydration
      Electron paramagnetic resonance
      Nuclear magnetic resonance
      Differential scanning calorimetry
    • Abstract:
      The present study was conducted to obtain a deeper insight into the mechanism of drug release from HPMC matrices. The microstructure, mobility, internal pH and the state of water within the gel layer of hydrated HPMC matrices (having different molecular weights) containing naproxen sodium (NS) and naproxen (N) were studied using Electron Paramagnetic Resonance (EPR), Nuclear Magnetic Resonance (NMR) and Differential Scanning Calorimetry (DSC) techniques. The study show that matrices composed of various viscosity grades of HPMC are characterized by similar microviscosity values in spite of the difference in their molecular weight. The NMR and DSC results led to the conclusion that higher molecular weights of HPMC are characterized by higher water absorption capacity and higher swelling. Analysis of non-freezable water in HPMC(K4M)–NS system revealed that addition of NS to solution increased the fraction of water bound to K4M+NS compared with the equivalent solutions without NS. The results suggest that the drug is participating in the crystallization of water and leads to the formation of a three dimensional network structure that decreases the freedom of water in K4M+NS samples. Calculation of the number of hydration shells showed that up to 2.2 layers are involved in HPMC-NS hydration compared to 1.5 layers for HPMC gel without NS. This was explained based on the different water ordering in the gel induced by NS as results of its absorption to polymer surface. Microviscosity values measured by EPR for K4M/N and K4M/NS hydrated matrices were found to be higher for K4M/N matrices, especially at initial stage of hydration. Mobile compartment calculations showed lower values for K4M/N compared with K4M/NS matrices. pH measurements by EPR revealed that incorporation of N to HPMC matrix led to lower internal pH value inside the hydrated tablet compared with NS. This behavior led to lower solubility of N which dictates its surface erosion mechanism, compared with NS matrix that was characterized by higher internal pH value and higher drug solubility. These properties of HPMC/NS increased chain hydration and stability, and led to drug release by the diffusion mechanism.
    • ISSN:
      0378-5173
    • Accession Number:
      10.1016/S0378-5173(00)00360-4
    • Accession Number:
      S0378517300003604
    • Copyright:
      Copyright @ 2000 Elsevier Science B.V. All rights reserved.
  • Citations
    • ABNT:
      KATZHENDLER, I.; MÄDER, K.; FRIEDMAN, M. Structure and hydration properties of hydroxypropyl methylcellulose matrices containing naproxen and naproxen sodium. International Journal of Pharmaceutics, [s. l.], v. 200, n. 2, p. 161–179, 2000. DOI 10.1016/S0378-5173(00)00360-4. Disponível em: http://search.ebscohost.com/login.aspx?direct=true&site=eds-live&db=edselp&AN=S0378517300003604&custid=s8280428. Acesso em: 18 jan. 2020.
    • AMA:
      Katzhendler I, Mäder K, Friedman M. Structure and hydration properties of hydroxypropyl methylcellulose matrices containing naproxen and naproxen sodium. International Journal of Pharmaceutics. 2000;200(2):161-179. doi:10.1016/S0378-5173(00)00360-4.
    • APA:
      Katzhendler, I., Mäder, K., & Friedman, M. (2000). Structure and hydration properties of hydroxypropyl methylcellulose matrices containing naproxen and naproxen sodium. International Journal of Pharmaceutics, 200(2), 161–179. https://doi.org/10.1016/S0378-5173(00)00360-4
    • Chicago/Turabian: Author-Date:
      Katzhendler, Ifat, Karsten Mäder, and Michael Friedman. 2000. “Structure and Hydration Properties of Hydroxypropyl Methylcellulose Matrices Containing Naproxen and Naproxen Sodium.” International Journal of Pharmaceutics 200 (2): 161–79. doi:10.1016/S0378-5173(00)00360-4.
    • Harvard:
      Katzhendler, I., Mäder, K. and Friedman, M. (2000) ‘Structure and hydration properties of hydroxypropyl methylcellulose matrices containing naproxen and naproxen sodium’, International Journal of Pharmaceutics, 200(2), pp. 161–179. doi: 10.1016/S0378-5173(00)00360-4.
    • Harvard: Australian:
      Katzhendler, I, Mäder, K & Friedman, M 2000, ‘Structure and hydration properties of hydroxypropyl methylcellulose matrices containing naproxen and naproxen sodium’, International Journal of Pharmaceutics, vol. 200, no. 2, pp. 161–179, viewed 18 January 2020, .
    • MLA:
      Katzhendler, Ifat, et al. “Structure and Hydration Properties of Hydroxypropyl Methylcellulose Matrices Containing Naproxen and Naproxen Sodium.” International Journal of Pharmaceutics, vol. 200, no. 2, Jan. 2000, pp. 161–179. EBSCOhost, doi:10.1016/S0378-5173(00)00360-4.
    • Chicago/Turabian: Humanities:
      Katzhendler, Ifat, Karsten Mäder, and Michael Friedman. “Structure and Hydration Properties of Hydroxypropyl Methylcellulose Matrices Containing Naproxen and Naproxen Sodium.” International Journal of Pharmaceutics 200, no. 2 (January 1, 2000): 161–79. doi:10.1016/S0378-5173(00)00360-4.
    • Vancouver/ICMJE:
      Katzhendler I, Mäder K, Friedman M. Structure and hydration properties of hydroxypropyl methylcellulose matrices containing naproxen and naproxen sodium. International Journal of Pharmaceutics [Internet]. 2000 Jan 1 [cited 2020 Jan 18];200(2):161–79. Available from: http://search.ebscohost.com/login.aspx?direct=true&site=eds-live&db=edselp&AN=S0378517300003604&custid=s8280428