Construction of Coamorphous Technology Aimed at Improving Membrane Permeability and Application to Emulsion

  • Uchiyama Hiromasa
    Laboratory of Formulation Design and Pharmaceutical Technology, Department of Pharmacy, Osaka University of Pharmaceutical Sciences

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Other Title
  • 膜透過性改善を指向したコアモルファス技術の構築とエマルションへの応用
  • マク トウカセイ カイゼン オ シコウ シタ コアモルファス ギジュツ ノ コウチク ト エマルション エ ノ オウヨウ

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Abstract

<p>The coamorphous formation between naringenin (NRG) and hesperetin (HPT) was investigated with the aim of enhancing their solubility and membrane permeability. In addition, application to emulsion of coamorphous was investigated. The melt-quenched particles (MQPs) of NRG and HPT were prepared in a range of molar ratios of NRG/HPT (3/1 to 1/3). All MQPs showed the amorphous state and single glass transition temperature. MQPs of NRG/HPT (1/1) could kept the amorphous state under storage. On the other hand, other MQPs recrystallized from the compound with a higher molar ratio. These results indicated that NRG and HPT formed the coamorphous at a molar ratio of 1 to 1. The coamorphous formation enhanced the apparent solubilities of NRG and HPT in aqueous media. Furthermore, MQPs of NRG/HPT (1/1) increased a permeated amount of NRG and HPT via the synthetic membrane in Franz Cell. When the solubility of NRG and HPT in oil components were investigated, the MQPs of NRG/HPT (1/1) enhanced the solubility of both compounds. This study highlighted the importance of coamorphous formation as a formulation to enhance solubility in oil components and aqueous media, and membrane permeability of both NRG and HPT.</p>

Journal

  • YAKUGAKU ZASSHI

    YAKUGAKU ZASSHI 141 (11), 1223-1228, 2021-11-01

    The Pharmaceutical Society of Japan

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