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Pharm Res. 2002 Dec;19(12):1867-72.

Formation of fine drug particles by cogrinding with cyclodextrins. I. The use of beta-cyclodextrin anhydrate and hydrate.

Author information

1
Graduate School of Pharmaceutical Sciences, Chiba University, 1-33 Yayoi-cho, Inage-ku, Chiba 263-8522, Japan.

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 beta-cyclodextrin (beta-CD) anhydrate or beta-CD hydrate crystals at a mixing molar ratio of 2:1 (beta-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 beta-CD hydrate/PRK GM was dispersed in water, 96% of PRK loaded in GM became fine particles smaller than 0.8 microm. In contrast, only 1.4% of PRK in GM transformed to fine particles in the case of beta-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 beta-CD of higher water content can be an effective method to prepare fine drug particles at the submicron level.

PMID:
12523667
[Indexed for MEDLINE]

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