Disintegrants in tableting

Pharmaceutical Dosage Forms: Tablets, Third Edition: Volume 2: Rational Design and Formulation

Volumn , Issue , 2008, Pages 217-249

  Moreton, R Christian ^a  

^a FinnBrit Consulting   (United States)

Author keywords

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Indexed keywords

EID: 73749087795     PISSN: None     EISSN: None     Source Type: Book    
DOI: None     Document Type: Chapter

References (77)

1. Khan KA, Rhodes CT. Efficiency of disintegrants in tablet formulations. Manuf Chem Aerosol News 1973; 44(9):48, 51–4.
2. Lowenthal W. Disintegration of tablets. J Pharm Sci 1972; 61(11):1695–711.
3. Kanig JL, Rudnic EM. The mechanisms of disintegrant action. Pharm Technol 1984; 8(4): 50–64.
4. Guyot-Herman AM. Tablet disintegration and disintegrating agents. STP Pharma Sci 1992; 2(6):445–62.
5. Roche Johnson J, Wang L-H, Gordon MS, et al. Effect of formulation solubility and hygroscopicity on disintegration efficiency in tablets prepared by wet granulation, in terms of dissolution. J Pharm Sci 1991; 80(5):469–71.
6. Ferrari F, Bertoni M, Bonferoni MC, et al. Influence of porosity and formula solubility on disintegrant efficiency in tablets. STP Pharma Sci 1995; 5(2):116–21.
7. Caramella C, Colombo P, Conte U, et al. Water uptake and disintegrating force measurements: Towards a general understanding of disintegration mechanisms. Drug Dev Ind Pharm 1986; 12(11–13):1749–66.
8. Khan KA, Rhodes CT. Water-sorption properties of tablet disintegrants. J Pharm Sci 1974; 64 (3):447–51.
9. Lerk CF, Bolhuis GK, Smallenbroek AJ, et al. Interaction of tablet disintegrants with magnesium stearate during mixing II: Effect on dissolution rate. Pharm Acta Helv 1982; 57 (10,11):282–6.
10. Proost JH, Bolhuis GK and Lerk CF. The effect of the swelling capacity of disintegrants on the in vitro and in vivo availability of diazepam tablets, containing magnesium stearate as a lubricant. Int J Pharm 1983; 13:287–96.
11. Hess H. Tablets under the microscope. Pharm Technol 1978; 2(9):36–49.
12. Guyot-Herman A-M, Ringaard J. Disintegration mechanisms of tablets containing starches: Hypothesis about the particle-particle repulsive force. Drug Dev Ind Pharm 1981; 7(2):155–77.
13. Matsumara H. Mechanism of tablet compression and disintegration IV; Evolution of wetting heat and its relation to compression force. Yakugaku Zasshi 1959; 79:63–4.
14. Lowenthal W. Mechanism of action of tablet disintegrants. Pharm Acta Helv 1973; 48(11,12): 589–609.
15. List PH, Muazzam UA. Swelling, the force that disintegrates. Drugs Made in Germany 1979; 22(4):161–70.
16. Niazi SK. Handbook of Pharmaceutical Manufacturing Formulations: Volume 1—Compressed Solid Products. Boca Raton, FL: CRC Press, 2004.
17. Niazi SK. Handbook of Pharmaceutical Manufacturing Formulations: Volume 5—Over-the-Counter Products. Boca Raton, FL: CRC Press, 2004.
18. Nyström C, Karehill P-G. The importance of intermolecular bonding forces and the concept of bonding area. In Alderborn G, Nyström C, eds. Pharmaceutical Compaction Technology. New York: Marcel Dekker, 1996:17–53.
19. Eyjolfsson R. Crospovidone: position in granulate and disintegration. Pharmazie 1999; 54 (12):945.
20. Khattab I, Menon A, Sakr A. A study of the effect of disintegrant distribution ratio on tablet characteristics using a central composite design. Eur J Pharm Biopharm 1993; 39(6):260–3.
21. Gordon MS, Chowhan ZT. Effect of mode of croscarmellose sodium incorporation on tablet dissolution and friability. J Pharm Sci 1990; 79(1):43–7.
22. Shotton E, Leonard GS. The effect of intra-and extragranular maize starch on the disintegration of compressed tablets. J Pharm Pharmacol 1972; 24:798–803.
23. Rubinstein MH, Bodey DM. Disaggreagtion of compressed tablets. J Pharm Sci 1976; 65(12): 1749–53.
24. Gordon MS, Chatterjee B, Chowhan ZT. Effect of mode of croscarmellose sodium incorporation on tablet dissolution and friability. J Pharm Sci 1990; 79(1):43–7.
25. Gadalla MAF, Abdel-Hameed MH, Ismail AA. A comparative evaluation of some starches as disintegrants for double compressed tablets. Drug Dev Ind Pharm 1989; 15(3):427–46.
26. Gould PL, Tan SB. The effect of recompression on disintegrant efficiency in tablets prepared by wet granulation. Drug Dev Ind Pharm 1985; 11(2,3):441–60.
27. Gould PL, Tan SB. The effect of recompression on the swelling kinetics of wet massed tablets containing superdisintegrants. Drug Dev Ind Pharm 1985; 11(9,10):1819–36.
28. Gould PL, Tan SB. The effect of recompression on the dissolution of wet massed tablets containing superdisintegrants. Drug Dev Ind Pharm 1986; 12(11–13):1929–45.
29. Thibert R, Hancock BC. The effects of milling upon the physicochemical properties and functional behavior of some disintegrants. STP Pharma Sci 2001; 11(2):123–8.
30. Smallenbroek AJ, Bolhuis GK, Lerk CF. The effect of particle size of disintegrants on the disintegration of tablets. Pharm Weekbl Sci Ed 1981; 116:1048–51.
31. Lowenthal W. Mechanism of action of tablet disintegrants. Pharm Acta Helv 1973; 48(11,12): 589–609.
32. Bolhuis GK, Lerk CF, Zulstra HT, et al. Film formation by magnesium stearate during mixing and its effect on tableting. Pharm Weekbl Sci Ed 1975; 110(16):317–25.
33. Bolhuis GK, Smallenbroek AJ, Lerk CF. Interaction of tablet disintegrants and magnesium stearate during mixing I: Effect on tablet disintegration. J Pharm Sci 1981; 70(12):1328–30.
34. Mohamad H, Aiache JM, Remoux R. Intérêt de la mesure du temps de mouillage pour le contrôl des comprimés. Sci Tech Prat Pharm 1985; 1(7):638–45.
35. Bolhuis GK, van Kamp HV, Lerk CF, et al. On the mechanism of action of modern disintegrants. Acta Pharm Technol 1982; 28(2):111–4.
36. Rowe RC, Sheskey PJ Owen SC, eds. The Handbook of Pharmaceutical Excipients, 5th ed. Washington, DC: American Pharmaceutical Association, and London: Pharmaceutical Press, 2006.
37. French D. Organization of starch granules. In: Whistler RK, BeMiller JN, Pascall EF, eds. Starch: Chemistry and Technology, 2nd ed. Orlando: Academic Press, 1984:183–247.
38. Whistler RK, BeMiller JN, Pascall EF, eds. Starch: Chemistry and Technology, 2nd ed. Orlando: Academic Press, 1984.
39. United States Food and Drug Administration, Center for Drug Evaluation and Research, Inactive Ingredient Database, www.fda.gov/cder
40. Kottke MK, Chueh H-R, Rhodes CT. Comparison of disintegrant and binder activity of three corn starch products. Drug Dev Ind Pharm 1992; 18(20):2207–23.
41. Feinstein W, Bartilucci AJ. Comparative study of selected disintegrating agents. J Pharm Sci 1966; 55(3):332–4.
42. Ingram JT, Lowenthal W. Mechanism of action of starch as a tablet disintegrant I: Factors affecting the swelling of starch grains at 37˚. J Pharm Sci 1966; 55(6):614–7.
43. Nogami H, Nagai T, Fukuoka E, et al. Disintegration of the aspirin tablets containing potato starch and microcrystalline cellulose in various concentrations. Chem Pharm Bull 1969; 17(7):1450–5.
44. Fraser DR, Ganderton D. The effect of starch type, concentration and distribution on the penetration and disruption of tablets by water. J Pharm Pharmacol 1971; 23(Suppl):18S–24S.
45. Sakr AM, Kassem AA, Farrag NA. The effect of certain disintegrants on water soluble tablets. Manuf Chem Aerosol News 1973; January:37–41.
46. Smallenbroek AJ, Bolhuis GK, Lerk CF. The effect of particle size of disintegrants on the disintegration of tablets. Pharm Weekbl Sci Ed 1981; 3:172–5.
47. Gebre-Mariam T, Schmidt PC. Characterization of enset starch and its use as a binder and disintegrant for tablets. Pharmazie 1996; 51(5):303–11.
48. Holstius EA, DeKay HG, A statistical study of some disintegrating and binding agents in certain compressed tablets. J Am Pharm Assoc Sci Ed 1952; XLI(9):505–9.
49. Gebre-Mariam T, Schmidt PC. The use of starch obtained from Dioscorea abyssinica in tablet formulations. 1st communication: The native starch as a binder and disintegrant. Pharmazie 1996; 58(2):167–72.
50. Lowenthal W. Mechanism of starch as a tablet disintegrant V: Effect of starch grain deformation. J Pharm Sci 1972; 61(3):455–9.
51. Japanese Pharmaceutical Excipients. Tokyo: Yakugi Nippo, 2004.
52. International Conference on the Harmonization of Technical Requirements for Registration of Pharmaceuticals for Human Use. Harmonized Tripartite Guideline: Impurities: Residual Solvents Q3C, 1997.
53. Rudnic EM, Kanig JL, Rhodes CT. Effect of molecular structure variation on the disintegrant action of sodium starch glycolate. J Pharm Sci 1985; 74(6):647–50.
54. Bolhuis GK, van Kamp HV, Lerk CF, et al. Effect of variation of degree of substitution, crosslinking and purity on the disintegration efficiency of sodium starch glycolate. Acta Pharm Technol 1984; 30(1):24–32.
55. Miseta M, Pintye-Hódi K, Szabó-Révész P, et al. Investigation of new commercial sodium starch glycolate products. Pharm Ind 1993; 55(5):515–8.
56. Bolhuis GK, Arends-Scholte AW, Stuut GJ, et al. Disintegration efficiency of sodium starch glycolates prepared from different native starches. Eur J Pharm Biopharm 1994; 40(5): 317–20.
57. Gebre-Mariam T, Winnermöller M, Schmidt PC. The use of a starch obtained from Dioscorea abyssinica in tablet formulations. 2nd Communication: The sodium starch glycolate from Dioscorea abyssinica as a disintegrant. Pharm Ind 1996; 58(2):255–9.
58. Rudnic EM, Rhodes CT, Welch S, et al. Evaluations of the mechanism of disintegrant action. Drug Dev Ind Pharm 1982; 8(1):87–109.
59. Rudnic EM, Kanig JL, Rhodes CT. Effect of molecular structure on the function of sodium starch glycolate in wet granulated systems, Drug Dev Ind Pharm 1983; 9(3):303–20.
60. Zhao N, Augsburger LL. The influence of product brand-to-brand variability on superdisintegrant performance: A case study with croscarmellose sodium. Pharm Dev Technol 2006; 11:179–85.
61. Bertoni M, Ferrari F, Bonferoni MC, et al. Functionality tests for tablet disintegrants: The case of sodium carboxymethylcelluloses. Pharm Technol Eur 1995; 7(11):17–24.
62. Gordon MS, Rudraraju VS, Dani K, et al. Effect of the mode of superdisintegrant incorporation on dissolution in wet granulated tablets. J Pharm Sci 1993; 82(2):220–8.
63. Khattab I, Menon A, Sakr A. Effect of mode of incorporation of disintegrants on the characteristics of fluid-bed wet-granulated tablets. J Pharm Pharmacol 1992; 45:687–91.
64. Shah U, Augsburger L. Evaluation of the functional equivalence of Crospovidone NF from different sources. I. Physical characterization. Pharm Dev Technol 2001; 6(1):39–51.
65. Rudnic EM, Lausier JM, Chilamkurti PN, et al. Studies on the utility of cross linked polyvinylpyrrolidone as a tablet disintegrant. Drug Dev Ind Pharm 1980; 6(3):291–309.
66. Miller RA, Down GRB, Yate CH, et al. An evaluation of selected tablet disintegrants. Can J Pharm Sci 1985; 15(3):55–8.
67. Sallam E, Ibrahim I, Abu Dahab R, et al. Evaluation of fast disintegrants in terfenadine tablets containing a gas-evolving disintegrant. Drug Dev Ind Pharm 1998; 24(6):501–7.
68. Schmidt J, Zessin G. Investigation of different vegetable cell walls as disintegrants in direct compression tablets. Drug Dev Ind Pharm 1997; 23(6):527–32.
69. Juslin M, Paronen P. Xylan—a possible filler and disintegrant for tablets. J Pharm Pharmacol 1984; 36:256–7.
70. Duru C, Gaudy D, Neye H, et al. A new tablet disintegrating agent, Xanthan SM: Formulation and drug release studies. Pharmazie 1995; 50(4):272–5.
71. Rizk S, Barthélémy C, Duru C, et al. Investigation of a new modified USP xanthan with tablet disintegrating properties. Drug Dev Ind Pharm 1997; 23(1):19–26.
72. Bhargava HN, Shah D, Anaebonam A, et al. An evaluation of Smecta as a tablet disintegrant and dissolution aid. Drug Dev Ind Pharm 1991; 17(15):2093–102.
73. Khan KA, Rhodes CT. Effect of disintegrant concentration on disintegration and compression characteristics of two insoluble direct compression systems. Can J Pharm Sci 1973; 8(3): 77–80.
74. Colombo P, Caramella C, Conte U, et al. Disintegrating force and tablet properties. Drug Dev Ind Pharm 1981; 7(2):135–53.
75. Caramella C, Ferrari F, Gazzaniga A, et al. A new computer-aided apparatus for simultaneous measurements of water uptake and swelling force in tablets. Drug Dev Ind Pharm 1988; 14 (15–17):2167–77.
76. United States Pharmacopeia 30th Revision (2007). General Chapter < 701= Disintegration. Rockville, MD: United States Pharmacopeia Convention, 2006: 276–7.
77. Massimo G, Cantellani PL, Santi P, et al. Disintegrating propensity of tablets evaluated by means of disintegrating force kinetics. Pharm Dev Technol 2000; 5(2):163–9.