Particle Design Using a 4-Fluid-Nozzle Spray-Drying Technique for Sustained Release of Acetaminophen
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概要
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We prepared matrix particles of acetaminophen (Act) with chitosan (Cht) as a carrier using a newly developed 4-fluid-nozzle spray dryer. Cht dissolves in acid solutions and forms a gel, but it does not dissolve in alkaline solutions. Therefore, we tested the preparation of controlled release matrix particles using the characteristics of this carrier. Act and Cht mixtures in prescribed ratios were dissolved in an acid solution. We evaluated the matrix particles by preparing a solid dispersion using a 4-fluid-nozzle spray dryer. Observation of the particle morphology by scanning electron microscopy (SEM) revealed that the particles from the spray drying process had atomized to several microns, and that they had become spherical. We investigated the physicochemical properties of the matrix particles by powder X-ray diffraction, differential scanning calorimetry, and dissolution rate analyses with a view to clarifying the effects of crystallinity on the dissolution rate. The powder X-ray diffraction peaks and the heat of the Act fusion in the spray-dried samples decreased with the increase of the carrier content, indicating that the drug was amorphous. These results indicate that the system formed a solid dispersion. Furthermore, we investigated the interaction between the drug and carrier using FT-IR analysis. The FT-IR spectroscopy for the Act solid dispersions suggested that the Act carboxyl group and the Cht amino group formed a hydrogen bond. In addition, the measurement results of the ^<13>C CP/MAS solid-state NMR, indicated that a hydrogen bond had been formed between the Act carbonyl group and the Cht amino group. In the Act-Cht system, the 4-fluid-nozzle spray-dried preparation with a mixing ratio of 1:5 obtained a sustained release preparation in all pH test solutions.
- 公益社団法人日本薬学会の論文
- 2006-07-01
著者
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岡本 博
神戸学院大学薬学部 生命薬学部門 循環器薬理学研究室
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壇上 和美
名城大学薬学部製剤学研究室
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檀上 和美
Faculty of Pharmacy, Meijo University
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Danjo K
名城大学 薬学部
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Danjo Kazumi
Faculty Of Pharmacy Meijo University
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壇上 和美
名城大学薬学部製剤学教室
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OKAMOTO Hirokazu
Faculty of Pharmaceutical Sciences, Kyoto University
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Danjo K
Fac. Of Pharmacy Meijo Univ.
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Okamoto H
Faculty Of Pharmacy Meijo University
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CHEN Richer
Mintai Chemical Co., Ltd.
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Chen Richer
Mintai Chemical Co. Ltd.
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Okamoto Hirokazu
Fac. Of Pharmacy Meijo Univ.
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