Advertisement

Pharmaceutisch Weekblad

, Volume 5, Issue 4, pp 165–171 | Cite as

Improvement by super disintegrants of the properties of tablets containing lactose, prepared by wet granulation

  • H. V. van Kamp
  • G. K. Bolhuis
  • C. F. Lerk
Original Articles

Abstract

The crushing strength, disintegration and dissolution properties of tablets, made by wet granulation with lactose as filler, gelatin as binder, potato starch as disintegrant and magnesium stearate as lubricant can be markedly improved when the potato starch (20%) is replaced by a much lower concentration (4%) of an insoluble super disintegrant, such as sodium starch glycolate (Primojel®) or crospovidone (Polyplasdone®Xl). The incorporation of partially water soluble super disintegrants such as low-substituted sodium carboxymethylcellulose (Nymcel®,Zsd 16), causing a viscous barrier in the tablets when containing water, is shown to be deleterious for both tablet disintegration and drug release.

In contrast to potato starch, the position of the super disintegrants (intragranular, extragranular or equally distributed) had hardly any effect on the tablet properties. The improved properties of the tablets containing insoluble super disintegrants, when compared to tablets with potato starch, are the result of the use of a much lower concentration of disintegrant, but especially of the difference in effect of magnesium stearate on the disintegration capacity of the slightly swelling potato starch and the strongly swelling super disintegrants, respectively. The latter cause, even in the presence of the liquid penetration inhibiting hydrophobic magnesium stearate, a chain reaction of opening of the tablet, starting at the outside and resulting in a fast disintegration.

Keywords

Starch Lactose Gelatin Drug Release Stearate 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. Asker, A.F., M.M. Abdel-Khalek andI. Machloof (1981)Drug Dev. Ind. Pharm. 7, 79–111.Google Scholar
  2. Bhatia, R.P., K.J. Desai andB.B. Sheth (1978)Drug Cosmetic Ind. 122 (Apr.), 38–52, 171–175.Google Scholar
  3. Boer, A.H. de, G.K. Bolhuis andC.F. Lerk (1978)Powder Technol. 20, 75–82.CrossRefGoogle Scholar
  4. Bolhuis, G.K., C.F. Lerk, H.T. Zijlstra andA.H. de Boer (1975)Pharm. Weekbl. 110, 317–325.Google Scholar
  5. Bolhuis, G.K., A.J. Smallenbroek andC.F. Lerk (1981)J. Pharm. Sci. 70, 1328–1330.PubMedGoogle Scholar
  6. Bolhuis, G.K., H.V. van Kamp, C.F. Lerk andF.G.M. Sessink (1982)Acta Pharm. Technol. 28, 111–114.Google Scholar
  7. Boymond, C., D. Gissinger andA. Stamm (1982)Pharm. Acta Helv. 57, 131–135.PubMedGoogle Scholar
  8. Formulary of the Dutch Pharmacists,Knmp. The Hague, The Netherlands.Google Scholar
  9. Gissinger, D., andA. Stamm (1980)Pharm. lnd. 42, 189–192.Google Scholar
  10. Groenwold, H., C.F. Lerk andR.J. Mulder (1972)J. Pharm. Pharmacol. 24, 352–356.PubMedGoogle Scholar
  11. Jaminet, F., L. Delattre andJ.P. Delporte (1969)Pharm. Acta Helv. 44, 418–432.PubMedGoogle Scholar
  12. Kamp, H.V. Van, G.K.Bolhuis and C.F.Lerk (1983) 3th Int. Conf. on Pharmaceutical Technology, Paris, accepted for publication.Google Scholar
  13. Khan, K.A.,andC.T. Rhodes (1972)Pharm. Acta Helv. 47, 41–50;Ibidem (1973)Mfg. Chemist Aerosol News 44, (Sept.) 48–54.PubMedGoogle Scholar
  14. Khan, K.A., andD.J. Rooke (1976)Mfg. Chemist Aerosol News 47, (Jan.) 25–26.Google Scholar
  15. Kornblum, S.S., andS.B. Stoopak (1973)J. Pharm. Sci. 62, 43–49.PubMedGoogle Scholar
  16. Lang, S. (1982)Mfg. Chemist Aerosol News 53, (Mar.) 31–33.Google Scholar
  17. Lerk, C.F., G.K. Bolhuis, A.J. Smallenbroek andK. Zuurman (1982)Pharm. Acta Helv. 57, 282–286.PubMedGoogle Scholar
  18. Malý, J., M. Chalabala andM. Heliová (1968)Acta Facultalis Pharm. Univ. Comenianae 21, 113–146.Google Scholar
  19. Miller, R.A., G.R.B. Down, C.H. Yates andJ.F. Millar (1980)Can. J. Pharm. Sci. 15, 55–58.Google Scholar
  20. Proost, J.H., G.K. Bolhuis andC.F. Lerk (1983)Int. J. Pharm. 13, 287–296.CrossRefGoogle Scholar
  21. Sakr, A.M., and N.A.Farrag (1975)Arch. Pharm. Chemi Sei. Ed. 3, 25–33.Google Scholar
  22. Sakr, A.M., A.A. Kassem andN.A. Farrag (1975)Pharm. lnd. 37, 283–287.Google Scholar
  23. Shangraw, R., A. Mitrevej andM. Shah (1980)Pharm. Technol. 4, (Oct.) 49–57.Google Scholar
  24. Shotton, E. (1972)Pharm. lnd. 34, 256–272.Google Scholar
  25. Shotton, E., andG.S. Leonard (1976)J. Pharm. Sci. 65, 1170–1174.PubMedGoogle Scholar

Copyright information

© Royal Dutch Association for Advancement of Pharmacy 1983

Authors and Affiliations

  • H. V. van Kamp
    • 1
  • G. K. Bolhuis
    • 1
  • C. F. Lerk
    • 1
  1. 1.Laboratory for Pharmaceutical Technology and DispensingUniversity of GroningenAW GroningenThe Netherlands

Personalised recommendations