Yoshioka M, Hancock B C, Zografi G
School of Pharmacy, University of Wisconsin-Madison 53706, USA.
J Pharm Sci. 1995 Aug;84(8):983-6. doi: 10.1002/jps.2600840814.
Differential scanning calorimetry and powder X-ray diffraction studies have been carried out with amorphous coprecipitates of indomethacin and poly(vinylpyrrolidone), PVP, to measure the glass transition temperature, Tg, as a function of mixture composition and the nonisothermal and isothermal crystallization of the indomethacin. Values of Tg as a function of mixture composition followed the ideal Gordon-Taylor equation up to about 50% w/w PVP. Inhibition of crystallization occurred at levels as low as 5% PVP and very significant inhibition was observed at and above 20% PVP. Inhibition of crystallization of indomethacin in the absence of PVP required a storage temperature 40-50 degrees C below Tg, whereas comparable inhibition with PVP was observed at storage temperatures 5 degrees C above Tg. This suggests that the inhibition of indomethacin crystallization by PVP may involve mechanisms other than just the general antiplasticizing effect (raising Tg) by PVP.
已采用吲哚美辛与聚维酮(PVP)的无定形共沉淀物进行差示扫描量热法和粉末X射线衍射研究,以测量玻璃化转变温度(Tg)作为混合物组成的函数以及吲哚美辛的非等温结晶和等温结晶情况。作为混合物组成函数的Tg值在PVP含量高达约50% w/w时遵循理想的戈登-泰勒方程。在PVP含量低至5%时就出现了结晶抑制现象,而在PVP含量达到20%及以上时观察到了非常显著的抑制作用。在不存在PVP的情况下,吲哚美辛结晶的抑制需要储存温度比Tg低40 - 50摄氏度,而在比Tg高5摄氏度的储存温度下就观察到了PVP具有类似的抑制作用。这表明PVP对吲哚美辛结晶的抑制可能涉及除了PVP一般的抗增塑作用(提高Tg)之外的其他机制。