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.
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.
Authors: N Kondo; T Iwao; H Masuda; K Yamanouchi; Y Ishihara; N Yamada; T Haga; Y Ogawa; K Yokoyama Journal: Chem Pharm Bull (Tokyo) Date: 1993-04 Impact factor: 1.645
Authors: Kyriaki Hatziagapiou; Kostas Bethanis; Eleni Koniari; Elias Christoforides; Olti Nikola; Athena Andreou; Aimilia Mantzou; George P Chrousos; Christina Kanaka-Gantenbein; George I Lambrou Journal: Pharmaceutics Date: 2022-03-26 Impact factor: 6.525