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Formulation of Controlled-Release Baclofen Matrix Tablets II: Influence of Some Hydrophobic Excipients on the Release Rate and In Vitro Evaluation

  • Research Article/Themed Issue: Oral/Guest Editors: Stephen A. Howard and Jian-Xin Li
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Abstract

The aim of this study was to investigate the influence of polymer level and type of some hydrophobic polymers, including hydrogenated castor oil (HCO); Eudragit RS100 (E-RS100); Eudragit L100 (E-L100), and some fillers namely mannitol [soluble filler], Dibasic calcium phosphate dihydrate (Emcompress) and anhydrous dibasic calcium phosphate [insoluble fillers] on the release rate and mechanism of baclofen from matrix tablets prepared by a hot-melt granulation process (wax tablets) and wet granulation process (E-RS100 and E-L100 tablets). Statistically significant differences were found among the drug release profile from different classes of polymeric matrices. Higher polymeric content (40%) in the matrix decreased the release rate of drug because of increased tortuosity and decreased porosity. At lower polymeric level (20%), the rate and extent of drug release was elevated. HCO was found to cause the strongest retardation of drug. On the other hand, replacement of Emcompress or anhydrous dibasic calcium phosphate for mannitol significantly retarded the release rate of baclofen, except for E-L100 (pH-dependent polymer). Emcompress surface alkalinity and in-situ increase in pH of the matrix microenvironment enhanced the dissolution and erosion of these matrix tablets. The release kinetics was found to be governed by the type and content of the excipients (polymer or filler). The prepared tablets showed no significant change in drug release rate when stored at ambient room conditions for 6 months.

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Reference

  1. H. Abdelkader, O. Y. Abdalla, and H. Salem. Formulation of controlled-release baclofen matrix tablets: influence of some hydrophilic polymers on the release rate and in vitro evaluation. AAPS Pharm. Sc. iTech. 8(4):E100 (2007).

    Article  Google Scholar 

  2. H. O. Ammar, and R. M. Khalil. Preparation and evaluation of sustained-release solid dispersions of drugs with Eudragit polymers. Drug Dev. Ind. Pharm. 23:1043–1054 (1997).

    Article  CAS  Google Scholar 

  3. M. S. Kislalioglu, M. A. Khan, C. Blount, R. W. Goettch, and S. Bolton. Physical characterization and dissolution properties of ibuprofen: Eudragit coprecipitates. J. Pharm. Sci. 80:799–804 (1991).

    Article  PubMed  CAS  Google Scholar 

  4. A. H. Kibbe, ed. Handbook of Pharmaceutical Excipients. London, UK: American Association and The Pharmaceutical Society of Great Britain; 2000:401–406.

  5. E. A. Michael, ed. Pharmaceutics: The Science of Dosage Form Design. London, UK: Churchill Livingstone; 2002:289–303.

  6. A. H. Kibbe, ed. Handbook of Pharmaceutical Excipients. London, UK: American Association and The Pharmaceutical Society of Great Britain; 2000:94–95.

  7. A. H. Kibbe, ed. Handbook of Pharmaceutical Excipients. London, UK: American Association and The Pharmaceutical Society of Great Britain; 2000:63–67.

  8. R. K. Raghuram, M. Srinivas, R. Srinivas. Once-daily sustained-release matrix tablets of nicorandil: formulation and in vitro evaluation. AAPS PharmSciTech. 2003; 4 (4) Article 61. Available at: http://www.pharmscitech.org.

  9. L. Lachman, H. A. Lieberman, eds. The Theory and Practice of Industrial Pharmacy. Philadelphia, PA: Leas and Febiger; 1987:317–318.

  10. R. W. Korsmeyer, R. Gurny, E. Doelker, P. Buri, and N. A. Peppas. Mechanisms of solute release from porous hydrophilic polymers. Int. J. Pharm. 15:25–35 (1983).

    Article  CAS  Google Scholar 

  11. N. A. Peppas. Analysis of Fickian and non-Fickian drug release from Polymers. Pharm. Acta. Helv. 60:110–112 (1985).

    PubMed  CAS  Google Scholar 

  12. N. A. Peppas, and J. J. Sahlin. A simple equation for the description of solute release III. coupling of diffusion and relaxation. Int. J. Pharm. 57:169–17 (1989).

    Article  CAS  Google Scholar 

  13. P. L. Riteger, and N. A. Peppas. A simple equation for description of solute release. I. Fickian and non-Fickian release from non-swellable devices in the form of slabs, spheres, cylinders or discs. J. Control Rel. 5:23–35 (1987).

    Article  Google Scholar 

  14. M. M. Talukdar, P. Rommbaut, and R. Kinget. Comparative study on xanthan gum and hydroxypropyl methylcellulose as matrices for controlled-release drug delivery. I. Int. J. Pharm. 129:231–241 (1996).

    Article  Google Scholar 

  15. M. S. Reza, M. Abdul Quadir, and S. S. Haider. Comparative evaluation of plastic, hydrophobic and hydrophilic polymers as matrices for controlled-release drug delivery. J. Pharm. Pharmaceut Sci. 6:282–291 (2003).

    CAS  Google Scholar 

  16. J. E. Mockel, and B. C. Lippold. Zero-order release from hydrocolloid matrices. Pharm. Res. 90:1066–1070 (1993).

    Article  Google Scholar 

  17. H. G. Schroeder, A. Dakkuri, and P. P. Deluca. Sustained release from inert wax matrices I: Drug-wax combinations. J. Pharm. Sci. 67:350–353 (1978).

    Article  PubMed  CAS  Google Scholar 

  18. M. J. O’Neil ed. The Merck Index: An Encyclopedia of Chemicals, Drugs and Biologicals. 13th ed. USA: Merck research Laboratories; 2001:164–165.

  19. E. A. Michael, ed. Pharmaceutics: The Science of Dosage Form Design. London, UK: Churchill Livingstone; 2002: 197–210.

  20. A. H. Kibbe, ed. Handbook of Pharmaceutical Excipients. London, UK: American Association and The Pharmaceutical Society of Great Britain; 2000:294–297.

  21. M. H. Amaral, J. M. Sousa, D. C. Ferreira. Effect of hydroxypropyl methylcellulose and hydrogenated castor oil on naproxen release from sustained-release tablets. AAPS PharmSciTech., 2001; 2(2) Article 6. Available at: http://www.pharmscitech.org.

  22. M. A. Quadir, M. S. Reza, and S. S. Haider. Effect of PEGs on release of diclofenac sodium from directly compressed carnauba wax matrix tablets. J. Bang. Acad. Sci. 26:1–12 (2002).

    CAS  Google Scholar 

  23. P. C. Schmidt, and R. Herzog. Calcium phosphates in Pharmaceutical tableting I: Physico-phatmaceutical properties. Pharm. Wld. Sci. 15:105–110 (1993).

    Article  CAS  Google Scholar 

  24. Y. E. Zhang, and J. B. Schwartz. Melting granulation and heat treatment for wax matrix-controlled release. Drug Dev. Ind. Pharm. 29:131–138 (2003).

    Article  PubMed  CAS  Google Scholar 

  25. B. Sandip, T. Tiwari, K. Murthy, P. M. Raveendra, P. R. Mehta, and P. B. Chowdary. Controlled release formulation of tramadol hydrochloride using hydrophilic and hydrophobic matrix system. AAPS PharmSciTech. 2003; 4(3) Article 31. Available at: http://www.pharmscitech.org.

  26. A. Dakkuri, H. G. Schroeder, and P. P. Deluca. Sustained release from inert wax matrices II: Effects of surfactants on tripellenamine hydrochloride release. J. Pharm. Sci. 67:354–358 (1978).

    Article  PubMed  CAS  Google Scholar 

  27. T. Higuchi. Mechanism of sustained-action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices. Ibid. 52:1145–1153 (1963).

    CAS  Google Scholar 

  28. F. W. Goodhart, R. H. McCoy, and F. C. Niger. Release of a water soluble drug from a wax matrix times release tablet. ibid. 63:1748–1755 (1974).

    CAS  Google Scholar 

  29. M. S. Reza, M. A. Quadir, and S. S. Haider. Development of theophylline sustained release dosage form based on kollidon SR. Pak J Pharm Sci. 15:63–73 (2002).

    PubMed  Google Scholar 

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Acknowledgements

The authors wish to thank Pharo Pharmaceutical Company, Alexandria; Egypt, for baclofen gift.

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Authors and Affiliations

  1. Department of pharmaceutics, Minia University, Minia, Egypt

    Hamdy Abdelkader

  2. Department of pharmaceutics, Alexandria University, Alexandria, Egypt

    Ossama Youssef Abdalla

  3. Department of analytical chemistry, Minia University, Minia, Egypt

    Hesham Salem

Authors
  1. Hamdy Abdelkader
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  2. Ossama Youssef Abdalla
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  3. Hesham Salem
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Correspondence to Hamdy Abdelkader.

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Abdelkader, H., Youssef Abdalla, O. & Salem, H. Formulation of Controlled-Release Baclofen Matrix Tablets II: Influence of Some Hydrophobic Excipients on the Release Rate and In Vitro Evaluation. AAPS PharmSciTech 9, 675–683 (2008). https://doi.org/10.1208/s12249-008-9094-0

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