AAPS PharmSciTech

, Volume 9, Issue 3, pp 917–923 | Cite as

Formulation Study and Evaluation of Matrix and Three-layer Tablet Sustained Drug Delivery Systems Based on Carbopols with Isosorbite Mononitrate

Research Article/Theme: Oral Controlled Release Development and Technology/Guest Editors: Stephen Howard and Jian-Xin Li

Abstract

The purpose of this research was to develop and evaluate different preparations of sustained delivery systems, using Carbopols as carriers, in the form of matrices and three-layer tablets with isosorbite mononitrate. Matrix tablets were prepared by direct compression whereas three-layer tablets were prepared by compressing polymer barrier layers on both sides of the core containing the drug. The findings of the study indicated that all systems demonstrated sustained release. The properties of the polymer used and the structure of each formulation appear to considerably affect drug release and its release rate. The three-layer formulations exhibit lower drug release compared to the matrices. This was due to the fact that the barrier-layers hindered the penetration of liquid into the core and modified drug dissolution and release. The geometrical characteristics/structure of the tablets as well as the weight/thickness of the barriers-layers considerably influence the rate of drug release and the release mechanisms. Kinetic analysis of the data indicated that drug release from matrices was mainly attributed to Fickian diffusion while three-layer tablets exhibited either anomalous diffusion or erosion/relaxation mechanisms. The advantage of Carbopol formulations is that a range of release profiles can easily be obtained through variations in tablet structure and thus Carbopols are appropriate carriers of oral sustained drug delivery systems for soluble drugs such as the isosorbite mononitrate.

Key words

Carbopol isosorbide mononitrate release kinetics sustained release three-layer tablets 

References

  1. 1.
    H. Ho-Wah, J. Robinson, and V. Lee. Design and fabrication of oral controlled release drug delivery systems. In J. Robinson, and V. Lee (eds.), Controlled Drug Delivery, Marcell Dekker Inc, New York, 1987, p. 373.Google Scholar
  2. 2.
    U. Conte, and L. Maggi. Multi-layer tablets as drug delivery devices. Pharm. Techn. 2:18–25 (1998).Google Scholar
  3. 3.
    N. Chidambram, W. Porter, K. Flood, and Y. Qiu. Formulation and characterization of new layered diffusional matrices for zero-order sustained release. J. Control. Release. 52:149–158 (1998).CrossRefGoogle Scholar
  4. 4.
    M. Efentakis, and S. Politis. Comparative evaluation of various structures in polymer controlled drug delivery systems and the effect of their morphology and characteristics on drug release. Eur. Polym. J. 42:1183–1195 (2006).CrossRefGoogle Scholar
  5. 5.
    L. Yang, and R. Fassihi. Accessibility of solid core tablet for dissolution in a asymmetric triple-layer matrix system. J. Pharm. Pharmcol. 55:1331–1337 (2003).CrossRefGoogle Scholar
  6. 6.
    A. Shajahan, and S. Pondar. A flexible technology for modified release of drugs: multilayer tablets. J. Control. Release. 97:393–405 (2004).Google Scholar
  7. 7.
    D. Alderman. A review of cellulose ethers in hydrophilic matrices for oral controlled release dosage forms. Int. J. Tech. Prod. Mfr. 5:1–9 (1984).Google Scholar
  8. 8.
    P. Katikanemi, S. Upadrashta, S. Neau, and A. Mitra. Ethylcellulose matrix controlled release tablets of a water-soluble drug. Int. J. Pharm. 123:119–125 (1995).CrossRefGoogle Scholar
  9. 9.
    B. F. Goodrich Bulletin. “Carbopol water soluble resins-controlled release tablets and capsules”. No 17 (1994).Google Scholar
  10. 10.
    M. Meshali, G. El-Sayed, Y. El-Said, and H. Abd El-Aleem. Preparation and evaluation of theophylline sustained release tablets. Drug Dev. Ind. Pharm. 22:373–376 (1996).CrossRefGoogle Scholar
  11. 11.
    A. Singla, M. Chawla, and A. Sigh. Potential applications of Carbomer in oral mucoadhesive controlled drug delivery systems: A review. Drug Dev. Ind. Pharm. 26:913–924 (2000).PubMedCrossRefGoogle Scholar
  12. 12.
    M. Efentakis, A. Koutlis, and M. Vlachou. Development and evaluation of oral multiple unit and single unit hydrophilic controlled release systems. aapspharmscitech.org. 1(4) article 34 (2000).Google Scholar
  13. 13.
    J. Waller. Optimal nitrate therapy with a once-daily sustained-release formulation of isosorbide mononitrate. J. Cardiovasc. Pharm. 34Suppl 2:S1–S7 (1999).Google Scholar
  14. 14.
    D. Franz. Cardiovascular drugs. In A. Gennaro (ed.), Remington: The Science and Practice of Pharmacy, Mack, Pennsylvania, 1995, p. 954.Google Scholar
  15. 15.
    K. Khan. The concept of dissolution efficiency. J. Pharm. Pharmacol. 27:48–49 (1975).PubMedGoogle Scholar
  16. 16.
    R. Korsmeyer, R. Gurny, E. Doelker, P. Buri, and N. Peppas. Mechanisms of solute release from porous hydrophilic polymers. Int. J. Pharm. 15:25–359 (1983).CrossRefGoogle Scholar

Copyright information

© American Association of Pharmaceutical Scientists 2008

Authors and Affiliations

  1. 1.Department of Pharmaceutical Technology, Faculty of PharmacyUniversity of AthensAthensGreece

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