2022 Fiscal Year Final Research Report
Physico-chemical stabilization of surfactant-free solid dispersion and improvement of aqueous dissolution of water-insoluble drugs
| Project/Area Number |
19H02499
|
|---|
| Research Category |
Grant-in-Aid for Scientific Research (B)
|
| Allocation Type | Single-year Grants |
|---|
| Section | 一般 |
|---|
| Review Section |
Basic Section 27010:Transport phenomena and unit operations-related
|
|---|
| Research Institution | Okayama University |
|---|
Principal Investigator |
|
|---|
| Project Period (FY) |
2019-04-01 – 2023-03-31
|
| Keywords | solid dispersion / spray drying / amorphous sugar / glass transition / over-dissolution / vacuum foam drying / nanoparticle / water sorption |
|---|
| Outline of Final Research Achievements |
We have developed a novel technique to prepare the molecular-level mixture of sugar and hydrophobic drug, without any surfactant (surfactant-free Amorphous Solid Dispersion). The aqueous dissolution of hydrophobic drugs could be significantly increased by the surfactant-free ASD technique, and the thermal annealing under appropriate conditions resulted in further improvement of the drug dissolution as well as the physicochemical stabilization of the ASD sample (increase in the glass transition temperature). In this study, we comprehensively investigated on how the “heat” could improve the aqueous dissolution of drugs from the surfactant-free ASD as well as the physicochemical stability of the ASD. Furthermore, amorphous sugar matrix dried from alcohols were characterized, and the ASD technique was applied to drying and powdering the suspension of easy-to-aggregate nanoparticle, without the particle aggregation.
|
| Free Research Field |
化学工学
|
| Academic Significance and Societal Importance of the Research Achievements |
現在，医薬品の候補物質として見出されたものの70％以上は難水溶性であると言われており，難水溶性薬剤の水系（生体内）溶解性の改善は医薬品業界において最重要課題となっている．本研究で提案する新規固体分散技術およびその熱処理による高度化は「難水溶性薬剤の溶解性の改善」そのものであり，製薬産業に対するインパクトは大きい．また，「水（に良く溶ける物質）と油（に良く溶ける物質）」を界面活性剤を用いずに均一混合する技術は広い産業分野で少なからぬ意義を持つと考えられる．さらに本来，糖のアモルファスマトリクスの物理化学的特性が溶媒の種類によって劇的に異なると言う知見は，特に食品分野で注目すべきものである．
|
