Superdisintegrants in new solid dosage forms – a review

Łukasz Zimmer; Piotr Belniak; Aleksandra Szopa; Ewa Poleszak

Authors

Łukasz Zimmer Departament of Applied Pharmacy, Medical University of Lublin, Poland Author https://orcid.org/0000-0003-2315-2747
Piotr Belniak Departament of Applied Pharmacy, Medical University of Lublin, Poland Author https://orcid.org/0000-0002-1036-1884
Aleksandra Szopa Departament of Applied Pharmacy, Medical University of Lublin, Poland Author https://orcid.org/0000-0002-7756-2904
Ewa Poleszak Departament of Applied Pharmacy, Medical University of Lublin, Poland Author https://orcid.org/0000-0003-4359-3953

Keywords:

superdisintegrants, disintegration, dissolution, novel solid dosage forms

Abstract

Despite increasing interest in controlled-release drug delivery systems, the most common tablets are intended to be swallowed whole and to disintegrate and release their medicaments rapidly in the gastrointestinal tract. The therm superdesintegrant refers to a substance which achieves disintegration faster than the disintegrants conventionally used. Tablets or capsules content breakup or disintegrate into smaller particles that dissolve more rapidly than in the absence of disintegrant and increase the rate of drug dissolution. The present study describes mechanisms of disintegrants action, influence of pH, disintegration efficiency and application of commonly used superdisintegrant: crospovidone, croscarmellose sodium and sodium starch glycolate in novel solid dosage forms.

References

1. Abed K.K. et al.: Formulation and optimization of orodispersible tablets of diazepam. AAPS Pharm. Sci. Tech., 11, 1, 356, 2010.

2. Alam M.A. et al.: Development and evaluation of acid-buffering bioadhesive vaginal tablet for mixed vaginal infections. AAPS Pharm. Sci. Tech., 8, 2007.

3. Balasubramaniam J., Bee T.: Influence of superdisintegrants of the rate of drug dissolution from oral solid dosage forms. Pharm. Tech. Apr. 1, 2009.

4. Bhalekar M.R., Desale S.S., Magdulkar A.R.: Synthesis of MCC-PEG conjugate and its evaluation as a superdisintegrant. AAPS Pharm. Sci. Tech., 11, 3, 2010.

5. Dashevsky A., Mohamad A.: Development of pulsatile multiparticulate drug delivery system coated with aqueous dispersion Aquqcoat ECD. Int. J. Pharm., 318, 124, 2006.

6. Fini A. et al.: Fast dispersible-slow releasing ibuprofen tablets. Eur. J. Pharm and Biopharm., 69, 335, 2008.

7. Gohel M.C. et al.: Improving the tablet characteristics and dissolution profile of ibuprofen by using novel coprocessed superdisintegrant: A technical Note. AAPS Pharm. Sci. Tech., 8, 2007.

8. Gohel M.C. et al.: Preparation and assessment of novel coprocessed superdisintegrant consisting of crospovidone and sodium starch glycolate: A technical note. AAPS Pharm. Sci. Tech., 8, 2007.

9. Gordon M.S. et al.: Effect of the mode of super disintegrant incorporation on dissolution in wet granulated tablets. J.Pharm. Sci. 82, 220, 1993. Published online: 21 SEP 2006.

10. Late S.G., Banga A.K.: Response Surface Methodology to optimize novel fast disintegrating tablets using β cyclodextrin as diluents. AAPS Pharm. Sci. Tech., 11, 1627, 2010.

11. Late S.G., Tu Y., Banga A.K.: Effects of disintegration-promoting agent, lubricants and moisture treatment on optimized fast disintegrating tablets. Int. J. Pharm., 365, 4, 2009.

12. Madgulkar A.R., Bhalekar M.R., Padalkar R.R.: Formulation design and optimization of novel taste masked mouth-dissolving tablets of tramadol having adequate mechanical strength. AAPS Pharm. Sci. Tech., 10, 574, 2009.

13. Modi A., Tayade P.: Enhancement of dissolution profile by solid dispersion (kneading) technique. AAPS Pharm. Sci. Tech., 7, 2006.

14. Mohamad A., Dashevsky A.: pH-independent pulsatile drug delivery system based on hard gelatin capsules and coated with aqueous dispersion Aquacoat ECD. Eur. J. Pharm and Biopharm., 64, 173, 2006.

15. Mohanachandran P.S., Sindhumol P.G., Kiran T.S.: Superdedintegrant: an overview. Int. J. Pharm. Sci. Review and Research, 6, 105, 2011.

16. Nalluri B.N. et al.: Tablet formulation studies on nimesulide and meloxicam-cyclodextrin binary systems. AAPS Pharm. Sci. Tech., 8, 2007.

17. Rahman Z., Zidan A.S., Khan M.A.: Risperidone solid dispersion for orally disintegrating tablet: Its formulation design and non-destructive method of evaluation. Int. J. Pharm., 400, 49, 2010.

18. Singh J., Philip A.K., Pathak K.: Optimization studies on design and evaluation of orodispersible pediatric formulation of indomethacin. AAPS Pharm. Sci. Tech., 9, 1, 60, 2008.

19. Srinarong P. et al.: Strongly enhanced dissolution rate of fenobibrate solid dispersion tablets by incorporation of superdisintegrant. Eur. J. Pharm and Biopharm., 73, 154, 2009.

20. Sungthongjeen S. et al.: Development of pulsatile release tablets with swelling and rupturable layers. J. Controll. Release 95, 147, 2004.

21. Zhao N., Augsburger L.L.: Functionality comparison of 3 classes of superdisintegrants in promoting aspirin tablet disintegration and dissolution. AAPS Pharm. Sci. Tech., 6, 2005.

22. Zhao N., Augsburger L.L.: The influence of swelling capacity of superdisintegrants in different pH media on the dissolution of hydrochlorothiazide from directly compressed tablets. AAPS Pharm. Sci. Tech., 6, 2005.

23. http://www.carterpharmaceuticalconsulting.com/articles/The-role-of-disintergrants.html Carter J.C.: The role of disintegrants in solid dosage manufacturing.