|助成対象者||門田 和紀 講師（製剤設計学研究室）|
|論文名||Feasibility of highly branched cyclic dextrin as an excipient matrix
in dry powder inhalers.
|掲載雑誌||European Journal of Pharmaceutical Sciences.79 , 79-86 (2015)|
|概要||We investigated the feasibility of highly branched cyclic dextrin (HBCD) as an excipient matrix in dry powder inhalers (DPIs). The fine particles of HBCD and HBCD/active pharmaceutical ingredients (API) were prepared by spray-drying an ethanol-aqueous solution containing HBCD. The particle size of spray-dried HBCD itself was approximately 3.0 μm with a wrinkled shape. Solid-state fluorescence emission spectroscopy of 1-naphthoic acid (1-NPA) showed that it was dispersed in a molecular dispersion/solid solution, if the model compound of 1-NPA was spray-dried with HBCD. Powder X-ray diffraction and differential scanning calorimetry indicate that 1-NPA was in the amorphous state after spray-drying with HBCD, which is confirmed by the fluorescence measurements, 1-NPA could be incorporated into HBCD. When the antimycobacterial agent, rifampicin, was spray-dried with HBCD for the purpose of pulmonary administration, the emitted dose and fine-particle fraction of the spray-dried particles of rifampicin with HBCD were 95.7±1.7% and 39.5±5.7%, respectively. The results indicated that HBCD possessed a high potential as an excipient in DPIs, not only by molecular association of API molecules with HBCD, but also by that of API fine crystals.|
|助成対象者||菊地 崇 助手（医薬品化学研究室）|
8(14),22-diene-3β,7β-diol, an unusual ergostane sterol from the fruiting bodies of pleurotus eryngii.
|掲載雑誌||European Journal of Organic Chemistry . 2015 , 4645-4649 (2015)|
|概要||A novel rearranged ergostane-type steroid, named eringiacetal A (1), together with a known compound (2), were isolated from the fruiting bodies of Pleurotus eryngii (Pleurotaceae). Its structure was fully elucidated by NMR spectroscopy and X-ray crystallography. Eringiacetal A (1) featured an unprecedented 5,6-seco-(5S, 6R, 7R, 9S)-5,6: 5,7: 6,9-triepoxyergosta-8(14),22-diene-3・,7・-diol. This is the first report of 5,6-seco-ergostane-type steroid. A plausible biogenetic pathway of 1 from 2 was also described. Furthermore, isolated compounds were evaluated for inhibitory effects on nitric oxide (NO) production induced by LPS in macrophages. Compound 1 exhibited inhibitory activity on NO production (IC50 19.9 ・M) accompanied by modest cytotoxicity (IC50 25.6 ・M). Compound 2 did not have inhibitory effects on NO production or cytotoxicity (IC50 >100 ・M each).|