Pharmaceutical Research

, Volume 19, Issue 12, pp 1867–1872

Formation of Fine Drug Particles by Cogrinding with Cyclodextrins. I. The Use of β-Cyclodextrin Anhydrate and Hydrate

  • Arpansiree Wongmekiat
  • Yuichi Tozuka
  • Toshio Oguchi
  • Keiji Yamamoto
Article

DOI: 10.1023/A:1021401826554

Cite this article as:
Wongmekiat, A., Tozuka, Y., Oguchi, T. et al. Pharm Res (2002) 19: 1867. doi:10.1023/A:1021401826554
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Abstract

Purpose. To improve the micromeritical properties of pranlukast (PRK) hydrate, a cogrinding process with cyclodextrin was used, and the formation of fine drug particles was investigated.

Methods. PRK crystals were ground with either β-cyclodextrin (β-CD) anhydrate or β-CD hydrate crystals at a mixing molar ratio of 2:1 (β-CD:PRK) to prepare the ground mixtures (GMs). Powder X-ray diffraction measurement and particle size analysis were performed.

Results. The two GMs differed from one another in appearance, wettability, and fine particle production. Quantitative determination demonstrated that when the β-CD hydrate/PRK GM was dispersed in water, 96% of PRK loaded in GM became fine particles smaller than 0.8 μm. In contrast, only 1.4% of PRK in GM transformed to fine particles in the case of β-CD anhydrate/PRK GM. The PRK fine particles were considered to be dispersed as small crystals. The stability of PRK particles in the aqueous solution was improved by the addition of a water-soluble polymer.

Conclusion. Cogrinding with a β-CD of higher water content can be an effective method to prepare fine drug particles at the submicron level.

pranlukast cyclodextrin cogrinding micronization fine particle poorly water/soluble drugs 

Copyright information

© Plenum Publishing Corporation 2002

Authors and Affiliations

  • Arpansiree Wongmekiat
    • 1
  • Yuichi Tozuka
    • 1
  • Toshio Oguchi
    • 1
  • Keiji Yamamoto
    • 1
  1. 1.Graduate School of Pharmaceutical SciencesChiba UniversityChibaJapan
  2. 2.Department of Pharmacy, Faculty of MedicineUniversity of YamanashiNakakoma-gun, YamanashiJapan

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