In the present study, corn Starch-Neusilin UFL2 conjugates were prepared by physical, chemical, and microwave methods with the aim of using the conjugates as tablet superdisintegrant. Various powder tests, namely, angle of repose, bulk density, tapped density, Hausner’s ratio, Carr’s index, swelling index, and powder porosity were conducted on the samples. The conjugates were characterized by ATR-FTIR, XRD, DSC, and SEM techniques. Heckel and Kawakita models were applied to carry out compression studies for the prepared conjugates. Fast disintegrating tablets of domperidone were prepared using corn starch and corn Starch-Neusilin UFL2 conjugates as tablet superdisintegrants in different concentrations. Conjugates were found to possess good powder flow and tabletting properties. Heckel analysis indicated that the conjugates prepared by microwave method showed the slowest onset of plastic deformation while Kawakita analysis indicated that the conjugates prepared by microwave method exhibited the highest amount of total plastic deformation. The study revealed that the corn Starch-Neusilin UFL2 conjugates possess improved powder flow properties and could be a promising superdisintegrant for preparing fast disintegrating tablet. Also, the results sugessted that the microwave method was found to be most effective for the preparation of corn Starch-Neusilin UFL2 conjugates. 1. Introduction Amongst innumerable applications, starch and its derivatives are one of the most widely used excipients in the pharmaceutical industry as they are incorporated in the manufacture of assorted dosage forms due to their biodegradability and biocompatibility. Starches have become a valuable ingredient because of their inertness, abundance, and cost effectiveness in the food industry, where they are used as thickeners, bulking, water retention, and gelling agents, in the pharmaceutical industry where they are used as fillers, binders, and disintegrants in tablet formulations. Commercially, starches are obtained from a variety of cereals (corn, waxy corn, high amylose corn, wheat, and various rice varieties) and from the tubers and roots (predominantly potato and cassava). In the pharmaceutical formulations, starch can be used both as a disintegrant and as a binder depending on the explicit attributes crucial for the formulation. As a disintegrant, the mechanism of action of starch includes wicking, the imbibitions of water into the tablet matrix via capillary action. The concentration of starch used is crucial; if it is below the optimum concentration then there are insufficient
References
[1]
I. Rashid, M. Al-Remawi, S. A. Leharne, B. Z. Chowdhry, and A. Badwan, “A novel multifunctional pharmaceutical excipient: modification of the permeability of starch by processing with magnesium silicate,” International Journal of Pharmaceutics, vol. 411, no. 1-2, pp. 18–26, 2011.
[2]
O. A. Odeku and K. M. Picker-Freyer, “Analysis of the material and tablet formation properties of four Dioscorea starches,” Starch/St?rke, vol. 59, no. 9, pp. 430–444, 2007.
[3]
N. Visavarungroj and J. P. Remon, “An evaluation of hydroxypropyl starch an disintegrant and binder in tablet formulation,” Drug Development and Industrial Pharmacy, vol. 17, no. 10, pp. 1389–1396, 1991.
[4]
M. Nakano, N. Nakazono, and N. Inotsume, “Preparation and evaluation of sustained release tablets prepared with α-starch,” Chemical and Pharmaceutical Bulletin, vol. 35, no. 10, pp. 4346–4350, 1987.
[5]
O. A. Odeku and K. M. Picker-Freyer, “Freeze-dried pregelatinized Dioscorea starches as tablet matrix for sustained release,” Journal of Excipients and Food Chemicals, vol. 1, no. 2, pp. 21–32, 2010.
[6]
H. Staroszczyk, “Microwave-assisted silication of potato starch,” Carbohydrate Polymers, vol. 77, no. 3, pp. 506–515, 2009.
[7]
J. Singh, L. Kaur, and O. J. McCarthy, “Factors influencing the physico-chemical, morphological, thermal and rheological properties of some chemically modified starches for food applications: a review,” Food Hydrocolloids, vol. 21, no. 1, pp. 1–22, 2007.
[8]
I. Rashid, N. Daraghmeh, M. Al-Remawi, S. A. Leharne, B. Z. Chowdhry, and A. Badwan, “Characterization of chitin-metal silicates as binding superdisintegrants,” Journal of Pharmaceutical Sciences, vol. 98, no. 12, pp. 4887–4901, 2009.
[9]
I. Rashid, N. Daraghmeh, M. Al-Remawi, S. A. Leharne, B. Z. Chowdhry, and A. Badwan, “Characterization of the impact of magnesium stearate lubrication on the tableting properties of chitin-Mg silicate as a superdisintegrating binder when compared to Avicel 200,” Powder Technology, vol. 203, no. 3, pp. 609–619, 2010.
[10]
Y. Asai, M. Nohara, S. Fujioka, K. Isaji, and S. Nagira, “Application of Neusilin UFL2 on manufacturing of tablets using direct compression method, Development of core tablets containing the function of small degree of decrease of hardness at the humid conditions,” Pharmaceutical Technical Newsletter, vol. 25, pp. 67–70, 2009.
[11]
B. G. Prajapati and D. V. Patel, “Formulation and optimization of domperidone fast dissolving tablet by wet granulation techniques using factorial design,” International Journal of PharmTech Research, vol. 2, no. 1, pp. 292–299, 2010.
[12]
J. Cooper and C. Gunn, “Powder flow and compaction,” in Tutorial Pharmacy, S. J. Carter, Ed., pp. 211–233, CBS Publishers and Distributors, New Delhi, India, 1986.
[13]
H. Goel, G. Kaur, A. K. Tiwary, and V. Rana, “Formulation development of stronger and quick disintegrating tablets: a crucial effect of chitin,” Yakugaku Zasshi, vol. 130, no. 5, pp. 729–735, 2010.
[14]
J. M. Sonnergaard, “Impact of particle density and initial volume on mathematical compression models,” European Journal of Pharmaceutical Sciences, vol. 11, no. 4, pp. 307–315, 2000.
[15]
O. A. Odeku, “Assessment of Albizia zygia gum as a binding agent in tablet formulations,” Acta Pharmaceutica, vol. 55, no. 3, pp. 263–276, 2005.
[16]
F. Kiekens, A. Debunne, C. Vervaet et al., “Influence of the punch diameter and curvature on the yield pressure of MCC-compacts during Heckel analysis,” European Journal of Pharmaceutical Sciences, vol. 22, no. 2-3, pp. 117–126, 2004.
[17]
“United States Pharmacopeia 24/NF19,” in The Official Compendia of Standards, M. D. Asian Rockville, Ed., pp. 1913–1914, U.S. Pharmacopeial Convention, 2000.
[18]
T. Y. Puttewar, M. D. Kshirsagar, A. V. Chandewar, and R. V. Chikhale, “Formulation and evaluation of orodispersible tablet of taste masked doxylamine succinate using ion exchange resin,” Journal of King Saud University—Science, vol. 22, no. 4, pp. 229–240, 2010.
[19]
A. Fini, V. Bergamante, G. C. Ceschel, C. Ronchi, and C. A. F. de Moraes, “Fast dispersible/slow releasing ibuprofen tablets,” European Journal of Pharmaceutics and Biopharmaceutics, vol. 69, no. 1, pp. 335–341, 2008.
[20]
M. U. Uhumwangho and R. S. Okor, “Effect of humidity on the disintegrant property of α-cellulose. Part II. A technical note,” AAPS PharmSciTech, vol. 6, no. 1, article no. 7, pp. E31–E34, 2005.
[21]
T. Sasaki and J. Matsuki, “Effect of wheat starch structure on swelling power,” Cereal Chemistry, vol. 75, no. 4, pp. 525–529, 1998.
[22]
O. A. Itiola and N. Pilpel, “Tableting characteristics of metronidazole formulations,” International Journal of Pharmaceutics, vol. 31, no. 1-2, pp. 99–105, 1986.
[23]
O. A. Odeku and O. A. Itiola, “Evaluation of khaya gum as a binder in a paracetamol tablet formulation,” Pharmacy and Pharmacology Communications, vol. 4, no. 4, pp. 183–188, 1998.
[24]
O. A. Odeku and J. T. Fell, “Effects of the method of preparation on the compression, mechanical, and release properties of khaya gum matrices,” Pharmaceutical Development and Technology, vol. 11, no. 4, pp. 435–441, 2006.
[25]
O. A. Odeku and B. L. Akinwande, “Effect of the mode of incorporation on the disintegrant properties of acid modified water and white yam starches,” Saudi Pharmaceutical Journal, vol. 20, no. 2, pp. 171–175, 2012.
[26]
R. Shangraw, A. Mitrevej, and M. Shah, “A new era of tablet disintegrants,” Pharmaceutical Technology, vol. 4, no. 10, pp. 49–57, 1980.