Skip to main content
Log in

Preparation, Characterization, and Pharmaceutical Application of Linear Dextrins. II. Complexation and Dispersion of Drugs with Amylodextrin by Freeze-Drying and Kneading

  • Published:
Pharmaceutical Research Aims and scope Submit manuscript

Abstract

The ability of amylodextrin (a linear dextrin) to act as a complexing agent or as a carrier for solid dispersion was evaluated. Blends of amylodextrin with diazepam or prednisolone were freeze-dried and kneaded at elevated temperatures, respectively. The products were analyzed by DSC, X-ray diffractometry, and FTIR spectroscopy. Complex formation with amylodextrin by freeze-drying was found not to occur for diazepam but for prednisolone at a molar ratio of 1 to 1. The freeze-dried product of diazepam with amylodextrin proved to be a solid dispersion. Solid dispersions were formed by both wet (with ethanol) and dry kneading at elevated temperatures of low-melting drugs such as lidocain, diazepam, and methyl-PABA with amylodextrin. No solid dispersions were obtained for high-melting drugs such as prednisolone and salicylic acid. The results point to the formation of solid dispersions by a melting mechanism during the process of kneading at elevated temperatures of low-melting drugs with amylodextrin.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Similar content being viewed by others

REFERENCES

  1. C. F. Lerk. Improvements of dissolution rates for drugs in oral dosage forms. In D. D. Breimer, D. J. A. Crommelin, and K. K. Midha (eds.), Topics in Pharmaceutical Sciences, Federation Internationale Pharmaceutique (FIP), The Hague, 1989, pp. 195–209.

    Google Scholar 

  2. J. Szejtli. A review with 16 references on toxicity, enzymic degradation, absorption and metabolism of CDs. J. Drug Dev. Suppl. 4:3–11 (1991).

    Google Scholar 

  3. K. Uekama and M. Otagiri. Cyclodextrins in drug carrier systems. CRC Crit. Rev. Ther. Drug Carrier Syst. 3:1–40 (1986).

    Google Scholar 

  4. H. W. Frijlink. Biopharmaceutical Aspects of Cyclodextrins, Thesis, University of Groningen, Groningen, 1990.

  5. G. H. P. Te Wierik, A. C. Eissens, A. C. Besemer, and C. F. Lerk. Preparation, characterization, and pharmaceutical application of linear dextrins. I. Preparation and characterization of amylodextrin, metastable amylodextrins, and metastable amylose. Pharm. Res. 10:1274–1279 (1993).

    Google Scholar 

  6. H. W. Frijlink, A. J. M. Schoonen, and C. F. Lerk. The effects of cyclodextrins on drug absorption. I. In vitro observations. Int. J. Pharm. 49:91–102 (1989).

    Google Scholar 

  7. H. Vromans, A. C. Eissens, and C. F. Lerk. Mechanisms of dissolution of drug-cyclodextrin complexes: A pragmatic approach. Acta Pharm. Technol. 35:250–255 (1989).

    Google Scholar 

  8. J. Pitha, S. M. Harman, and M. E. Michel. Hydrophilic cyclodextrin derivatives enable effective oral administration of steroidal hormones. J. Pharm. Sci. 75:165–167 (1986).

    Google Scholar 

  9. M. Vikmon, A. Stadler-Szoke, G. Hortobagyi, I. Kolbe, and J. Szejtli. Stabilization of mydeton with β-cyclodextrin. Acta Pharm. Technol. 32:29–32 (1986).

    Google Scholar 

  10. Y. Nakai. Molecular behaviour of medicinals in ground mixtures with microcrystalline cellulose and cyclodextrins. Drug Dev. Ind. Pharm. 12:1017–1039 (1986).

    Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Rights and permissions

Reprints and permissions

About this article

Cite this article

Te Wierik, G.H.P., Eissens, A.C., Besemer, A.C. et al. Preparation, Characterization, and Pharmaceutical Application of Linear Dextrins. II. Complexation and Dispersion of Drugs with Amylodextrin by Freeze-Drying and Kneading. Pharm Res 10, 1280–1284 (1993). https://doi.org/10.1023/A:1018957410821

Download citation

  • Issue Date:

  • DOI: https://doi.org/10.1023/A:1018957410821

Navigation