Development of effective nano-sizing method for dispersible additive-free poorly-water-soluble drugs and its application

• Project/Area Number: 24655113
• Research Category: Grant-in-Aid for Challenging Exploratory Research
• Allocation Type: Single-year Grants
• Research Field: Functional materials chemistry
• Research Institution: Tohoku University
• Principal Investigator: ARITA TOSHIHIKO 東北大学, 多元物質科学研究所, 助教 (50423033)
• Co-Investigator(Kenkyū-buntansha): YABU Hiroshi 東北大学, 多元物質科学研究所, 准教授 (40396255)
• Project Period (FY): 2012-04-01 – 2014-03-31
• Project Status: Completed (Fiscal Year 2013)
• Budget Amount: ¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000); Fiscal Year 2013: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000); Fiscal Year 2012: ¥2,470,000 (Direct Cost: ¥1,900,000、Indirect Cost: ¥570,000)
• Keywords: ナノ医薬品材料 / 超微粒子 / 有機ナノ結晶 / コロイド / 結晶成長 / 過飽和溶解 / 固体分散

Research Abstract

This study aimed to solve most of problems of poorly-water-soluble drugs (acceleration of dissolution, reduction of additives, suppression of aggregation and improvement of solid dispersion) by additive-free nano-sizing. By using esculent carbon dioxide as the solvent and applying triboelectric charge as the dispersion force, additive-free nano-sizing (less than 100nm diameter) of poorly-water soluble drugs was achieved. As the result, above mentioned problems have been solved, in addition, supersaturated dissolution (10% excess dissolution to the saturated concentration) of the nano-sized drugs has been found.

Research Products

• [Journal Article] Instant and supersaturated dissolution of naproxen and sesamin (poorly water-soluble drugs and supplements) nanoparticles prepared by continuous expansion of liquid carbon dioxide solution through long dielectric nozzle (2012)
  • Author(s): Toshihiko Arita, Noriyoshi Manabe, Koichi Nakahara
  • Journal Title: J. Nanopart. Res. Volume: 14巻, artNo.1251 Issue: 11
  • DOI: 10.1007/s11051-012-1251-4
  • Peer Reviewed
• [Presentation] 無添加ナノ化難水溶性薬剤を用いた過飽和溶解とオストワルド熟成に関する研究 (2014)
  • Author(s): 有田稔彦、岸上美季、中原光一
  • Organizer: 日本化学会第94春季年会
  • Place of Presentation: 名古屋大学
  • Year and Date: 2014-03-27
• [Presentation] Preparation of additive-free organic nanoparticles: a tool for studying the mechanism of supersaturated dissolution and Ostwald ripening (2014)
  • Author(s): Toshihiko Arita
  • Organizer: 2014 Energy Materials and Nanotechnology (EMN) Spring Meeting
  • Place of Presentation: Las Vegas, USA
  • Year and Date: 2014-02-27
  • Invited
• [Presentation] Accelerated and supersaturated dissolution of nano-sized poorly-water-soluble (BCS Class 2) drugs (2013)
  • Author(s): Toshihiko Arita, Mizue Kishigami, Noriyoshi Manabe, Koichi Nakahara
  • Organizer: 5th Asian Arden Conference
  • Place of Presentation: 愛知学院大学
  • Year and Date: 2013-08-05
• [Presentation] 難水溶性薬剤の薬効向上へ向けた無添加ナノ粒子化による過飽和溶解と固体分散 (2013)
  • Author(s): 岸上美季、有田稔彦、真鍋法義、中原光一
  • Organizer: 第2回JACI/GSCシンポジウム
  • Place of Presentation: メルパルク大阪
  • Year and Date: 2013-06-07
• [Presentation] 難水溶性薬剤の無添加ナノ粒子化による飛躍的溶解速度向上と過飽和溶解 (2013)
  • Author(s): 有田稔彦、真鍋法義、岸上美季、中原光一
  • Organizer: 日本化学会第93春季年会
  • Place of Presentation: 立命館大学びわこ草津キャンパス
  • Year and Date: 2013-03-23
• [Presentation] Accelerated and supersaturated dissolution of nano-sized poorly water-soluble (BCS Class 2) drugs (2013)
  • Author(s): Toshihiko Arita, Mizue Kishigami, Noriyoshi Manabe, Koichi Nakahara
  • Organizer: 5th Asian Arden Conference
  • Place of Presentation: Aichi Gakuin University Kusumoto Campus, Nagoya
• [Presentation] 液体二酸化炭素と静電反発力を利用した難溶性化合物の非晶質ナノサイズ化 (2012)
  • Author(s): 有田稔彦、真鍋法義、中原光一
  • Organizer: 日本薬剤学会第27年会
  • Place of Presentation: 神戸国際会議場
  • Year and Date: 2012-05-26
• [Presentation] Preparation of additive-free organic nanoparticles: a tool for studying the mechanism of supersaturated dissolution and Ostwald ripening
  • Author(s): Toshihiko Arita
  • Organizer: 2014 Energy Materials and Nanotechnology (EMN) Spring Meeting
  • Place of Presentation: Red Rock Casino Resort and Spa, LasVegas, USA
  • Invited
• [Book] "Supercritical Hydrothermal Synthesis." In: Handbook of Advanced Ceramics: Materials, Applications, Processing, and Properties (2013)
  • Author(s): T. Adschiri, S. Takami, T. Arita, D. Hojo, K. Minami, N. Aoki, T. Togashi
  • Publisher: Academic Press: Elsevier Inc.
• [Book] "Supercritical Hydrothermal Synthesis." In: Handbook of Advanced Ceramics: Materials, Applications, Processing, and Properties. (2013)
  • Author(s): T. Adschiri, S. Takami, T. Arita, D. Hojo, K. Minami, N. Aoki, T. Togashi
  • Total Pages: 29
  • Publisher: Academic Press: Elsevier Inc.
• [Book] 高圧力の科学と技術 特集:高圧力技術によるナノマテリアル創製研究の最前線 「超臨界水熱プロセスによるナノ粒子の合成とハイブリッド化―粒子表面改質による相反機能材料開発―」 (2012)
  • Author(s): 阿尻雅文, 新井智宏, 石川佳澄, 上野真孝, 上田正孝, 岡田拓也, 大島英紀, 中川孝行, 福島敬二, 前田重之, 宮田建治, 森下丈弘, 山縣利貴, 高見誠一, 青木宣明, 有田稔彦, 他
  • Publisher: 高圧学会
• [Book] 高圧力の科学と技術 特集：高圧力技術によるナノマテリアル創製研究の最前線 「超臨界水熱プロセスによるナノ粒子の合成とハイブリッド化―粒子表面改質による相反機能材料開発―」 (2012)
  • Author(s): 阿尻 雅文, 新井 智宏, 石川 佳澄, 上野 真孝, 上田 正孝, 岡田 拓也, 大島 英紀, 中川 孝行, 福島 敬二, 前田 重之, 宮田 建治, 森下 丈弘, 山縣 利貴, 高見 誠一, 青木 宣明, 有田 稔彦, 他
  • Publisher: 高圧学会
• [Patent(Industrial Property Rights)] 高結晶性微粒子の製造方法 (2014)
  • Inventor(s): 有田稔彦、中原光一、岸上美季
  • Industrial Property Rights Holder: 東北大学、サントリー(株)
  • Industrial Property Rights Type: 特許
  • Industrial Property Number: 2014-212399
  • Filing Date: 2014-10-17
• [Patent(Industrial Property Rights)] 微粒子作成装置 (2012)
  • Inventor(s): 有田稔彦、中原光一
  • Industrial Property Rights Holder: 東北大学、サントリー(株)
  • Industrial Property Rights Type: 特許
  • Filing Date: 2012-11-21
  • Overseas