2013 Fiscal Year Final Research Report
Preparation and formulation of pharmaceutical nano-cocrystals by using mechanochemical reaction
| Project/Area Number |
23790056
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Physical pharmacy
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| Research Institution | Nihon University |
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Principal Investigator |
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| Research Collaborator |
OZEKI Tetsuya 名古屋市立大学, 大学院薬学研究科, 教授 (60277259)
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| Project Period (FY) |
2011 – 2013
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| Keywords | コクリスタル / メカノケミカル / アセトアミノフェン / ベタイン / 製剤学的応用 |
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| Research Abstract |
Cocrystallization is a pharmaceutical technology which provides an improvement on solid properties of active pharmaceutical ingredients without modification of its chemical structure. In this study, paracetamol (acetaminophen) was used as model drug substance and to clarify the formation mechanism of cocrystal in molecular level. As a result of exploring screening study in solid state using mechanochemical reaction, novel three cocrystals were discovered. In particular, the pharmaceutical cocrystal consisting of paracetamol and trimethylglycine (betaine) at molar ration of 1:1 indicated improved pharmaceutical properties such as compact moldability and dissolution behavior. In addition, preparing cocrystal in nanogram scale and evaluating by using microscopic Raman spectroscopy were achieved.
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