EVALUATION OF CALLINECTES CHITOSAN AS A SUPERDISINTEGRANT IN METRONIDAZOLE TABLET

  • Emmanuel O. Olorunsola Department of Pharmaceutics and Pharmaceutical Technology, University of Uyo, Uyo, Nigeria
  • Musiliu O. Adedokun Department of Pharmaceutics and Pharmaceutical Technology, University of Uyo, Uyo, Nigeria
  • Ekaete I. Akpabio Department of Pharmaceutics and Pharmaceutical Technology, University of Uyo, Uyo, Nigeria

Abstract

Objective: The objective of this study is to evaluate callinectes chitosan as a superdisintegrant in tablet formulation; superdisintegrants are incorporated into tablets at concentrations below 5% of tablet weight to effect prompt break-up of tablets after administration.

Methods: Chitosan was extracted from shells of Callinectes gladiator. The polymer was characterized and then used as a disintegrant (in comparison with Ac-Di-Sol® and corn starch) at concentrations of 2, 4 and 8% for the formulation of metronidazole tablets. The micromeritic properties of granules; and mechanical and release properties of the tablets were studied.

Results: A yield of 36.7% chitosan having degree of deacetylation of 62.7% was obtained from the crab shell. Fourier Transform Infrared absorption bands at 1495 and 3240 cm-1 typical of N-H bending and stretching respectively; and endothermic peak of 159 °C typical of melting of chitosan were obtained. No adverse interaction between the chitosan and metronidazole was observed. The disintegration times of tablets containing 2, 4 and 8% chitosan were 12.2, 10.4 and 9.3 min respectively.

Conclusion: Callinectes chitosan is suitable for use as a superdisintegrant in tablets. It appears to be superior to corn starch as disintegrant although less effective compared to Ac-Di-Sol®. However, the relative cheapness and ready availability of chitosan would make it to be preferred to Ac-Di-Sol®.

Keywords: Callinectes gladiator, Chitosan, Metronidazole, Superdisintegrant

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References

1. Moreton RC. Excipient functionality. Pharm Technol 2004;98:99-119.
2. Himanshu D, Chandrashekhara S, Nagesh C, Amol M, Shridhar U. Superdisintegrant: a recent investigation and current approach. Asia J Pharm Technol 2012;2:19-25.
3. Wang QZ, Chen XG, Liu N, Wang SX, Liu CS, Meng XH, et al. Protonation constant of chitosan with different molecular weight and degree of deacetylation. Carbohydr Polym 2006;65:194–201.
4. Sonia TA, Sharma CP. Chitosan and its derivatives for drug delivery. Adv Polym Sci 2011;243:23–54.
5. Ritthide GC, Chomto P, Pummangura S, Menasveta P. Chitin and chitosan as disintegrants in paracetamol tablets. Drug Dev Ind Pharm 1994;20:2109-34.
6. Jimoh AA, Ndimele PE, Lemomu IP, Shittu UA. The biology of gladiator swim crab (Callinectes Pallidus) from Ojo creek, Southern Nigeria. J Fish Aqua Sci 2014;9:157-69.
7. Akin-Oriola G, Anetekhai M, Olowonirejuaro K. Morphometric and meristic studies in two crabs: Cardiosoma armatum and Callinectes pallidus. Turk J Fish Aqua Sci 2005;5:85-9.
8. Okafor FC. The ecology of Sudanonautes africanus (Crustacea: Decapoda) in Southeastern Nigeria. Trop Ecol 1988;29:89-97.
9. Ejike C. Macrofibres in the cuticles of the crab Callinectes gladiator (Benedict). Zool J Linn Soc 1973;53:253-5.
10. Olorunsola EO, Uwah TO, Olayemi OJ, Etukudo UB. Ex-vivo evaluation of crab shell chitosan as absorption enhancer in ciprofloxacin tablet formulation. Afr J Biotehnol 2016;15:1930–5.
11. Onyishi IV, Chime SA, Ugwu JC. Evaluation of binder and disintegrant properties of starch derived from Xanthosoma sagittifolium in metronidazole tablets. Afr J Biotechnol 2013;12:3064-70.
12. Bi Y, Sunada H, Yonezawa Y. Preparation and evaluation of a compressed tablet rapidly disintegrating in the oral cavity. Chem Pharm Bull 1996;44:2121-7.
13. Borriand A, Rinaudo M. Preparation and characterization of fully deacetylated chitosan. Int J Biol Macromol 1983;2:100-51.
14. Damodar R, Movva B. Preparation and in vitro evaluation of Metformin HCl tablets containing sustained release beads for increasing therapeutic window. J Bioequivalence Bioavailability 2014;6:91-5.
15. No HK, Meyers SP. Preparation and characterization of chitin and chitosan-A review. J Aqua Food Prod Technol 1995;4:27-52.
16. Green JH, Kramer A. Food processing waste management. West Port: AVI publishing Co.; 1984.
17. Li Q, Dunn ET, Grandmaison EW, Grosen MFA. Applications and properties of chitosan. J Bioact Comp Polym 1992;7:370-97.
18. Martino D, Sittinger A, Risbud M. Chitosan: a versatile biopolymer for orthopaedic tissue engineering. Biomaterial 2005;26:5983-90.
19. Puvvada YH, Vankayalapati H, Sukhavasi S. Extraction of chitin and chitosan from exoskeleton of shrimp for application in the pharmaceutical industry. Int Curr Pharm J 2012;1:258-63.
20. Coutts RT. Infrared spectroscopy. In: Chatten LG. editor. Pharmaceutical chemistry–instrumental techniques. New Delhi India: CBS Publishers and Distributors PVT Ltd.; 2008. p. 59–125.
21. Limam Z, Selmi S, Sadok S, El-Abed A. Extraction and characterization of chitin and chitosan from crustacean by-products: Biological and physicochemical properties. Afr J Biotechnol 2011;10:640–7.
22. Chung H, Lee E, Lim S. Comparison in glass transition and enthalpy relaxation between native and gelatinized rice starches. Carbohydr Polym 2002;48:287-98.
23. Horvat M, Mestrovic E, Danilovski A, Craig DMQ. An investigation into the thermal behaviour of a model drug mixture with amorphous trehalose. Int J Pharm 2005;294:1-10.
24. Iqbal MS, Massey S, Akbar J, Ashraf CM. Thermal analysis of some natural polysaccharides by isoconversion method. Food Chem 2013;140:178-82.
25. Zhang CH, Zhao BH, Huang Y, Wang Y, Ke XY, Zhao BJ, et al. A novel domperidone hydrogel: Prepararation, characterization, pharmacokinetic and pharmacodynamics properties. J Drug Delivery 2011;841054:1-9.
26. Sahu VK, Sharma N, Sahu PK, Saraf SA. Formulation and evaluation of floating mucoadhesive microsphere of novel natural polysaccharide for site specific delivery of ranitidine hydrochloride. Int J Appl Pharm 2017;9:15-9.
27. Wells JI, Aulton ME. Pharmaceutical preformulation. In: Aulton ME. editor. The Design and Manufacture of Medicine. 3rd ed. Hungary: Churchill Livingstone Elsevier; 2007. p. 336-60.
28. Ramu B, Shanmunga PP. Formulation and evaluation of gastroretentive floating bioadhesive tablet of hydrochlorothiazide. Asian J Pharm Clin Res 2017;10:150-5.
29. Aucamp ME, Campus NWVP. Assessment of the tableting properties of chitosan through wet granulation and direct compression formulations. M. Sc. Thesis. Northwest University, Poichefstroom campus, South Africa; 2004.
30. Gupta GD, Raud RS. Formulation and evaluation of nimesulide dispersible tablets using natural disintegrants. Indian J Pharm Sci 2000;62:339-42.
31. Caramella C, Columbo P, Conte U, La Manna A. Tablet disintegration update: The dynamic approach. Drug Dev Ind Pharm 1987;13:2111-45.
32. Chaudhary KPR, Rao DS, Sujatha R. Formulation and evaluation of dispersible tablets of poorly soluble drugs. Indian J Pharm Sci 1992;2:31-2.
33. Guest RT. Croscarmellose sodium. In: Rowe RC, Sheskey PJ, Cook WG, Fenton ME. editors. Handbook of Pharmaceutical Excipients. 7th ed. London, UK: Pharmaceutical Press; 2012. p. 224-6.
34. Siddiqui MN, Garg G, Sharma PK. Fast dissolving tablets-preparation, characterization and evaluation: a review. Int J Pharm Sci Rev Res 2012;4:87-96.
35. Al-Nuss R, El-Zein H. Enhancement of candesartan cilexetil dissolution rate by using different methods. Asian J Pharm Clin Res 2015;8:320-6.
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How to Cite
Olorunsola, E. O., M. O. Adedokun, and E. I. Akpabio. “EVALUATION OF CALLINECTES CHITOSAN AS A SUPERDISINTEGRANT IN METRONIDAZOLE TABLET”. International Journal of Pharmacy and Pharmaceutical Sciences, Vol. 9, no. 10, Oct. 2017, pp. 111-8, doi:10.22159/ijpps.2017v9i10.20788.
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