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

Overview

Journal Pharm Res

Specialties Pharmacology
Pharmacy

Date 2003 Jan 14

PMID 12523667

Citations 9

Authors

Arpansiree Wongmekiat

Yuichi Tozuka

Toshio Oguchi

Keiji Yamamoto

Affiliations

Soon will be listed here.

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.

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