Jin Ping, Madieh Shadi, Augsburger Larry L
University of Maryland, Baltimore, School of Pharmacy, 20 N. Pine Street, Baltimore, MD 21201, USA.
AAPS PharmSciTech. 2007 Dec 14;8(4):E105. doi: 10.1208/pt0804105.
The objectives of this research were to evaluate the stability of parthenolide in feverfew solution state and powdered feverfew (solid state), and explore the compatibility between commonly used excipients and parthenolide in feverfew. Feverfew extract solution was diluted with different pH buffers to study the solution stability of parthenolide in feverfew. Powdered feverfew extract was stored under 40 degrees C/0% approximately 75% relative humidities (RH) or 31% RH/5~50 degrees C to study the influence of temperature and relative humidity on the stability of parthenolide in feverfew solid state. Binary mixtures of feverfew powered extract and different excipients were stored at 50 degrees C/ 75% RH for excipient compatibility evaluation. The degradation of parthenolide in feverfew solution appears to fit a typical first-order reaction. Parthenolide is comparatively stable when the environmental pH is in the range of 5 to 7, becoming unstable when pH is less than 3 or more than 7. Parthenolide degradation in feverfew in the solid state does not fit any obvious reaction model. Moisture content and temperature both play important roles affecting the degradation rate. After 6 months of storage, parthenolide in feverfew remains constant at 5 degrees C/31% RH. However, approximately 40% parthenolide in feverfew can be degraded if stored at 50 degrees C/31% RH. When the moisture changed from 0% to 75% RH, the degradation of parthenolide in feverfew increased from 18% to 32% after 6-month storage under 40 degrees C. Parthenolide in feverfew exhibits good compatibility with commonly used excipients under stressed conditions in a 3-week screening study.
本研究的目的是评估小白菊内酯在小白菊溶液状态和小白菊粉末（固态）中的稳定性，并探索常用辅料与小白菊内酯在小白菊中的相容性。用不同pH缓冲液稀释小白菊提取物溶液，以研究小白菊内酯在小白菊中的溶液稳定性。将小白菊提取物粉末储存在40℃/0%至约75%相对湿度（RH）或31%RH/5至50℃条件下，以研究温度和相对湿度对小白菊内酯在小白菊固态稳定性的影响。将小白菊提取物粉末与不同辅料的二元混合物储存在50℃/75%RH条件下进行辅料相容性评估。小白菊内酯在小白菊溶液中的降解似乎符合典型的一级反应。当环境pH在5至7范围内时小白菊内酯相对稳定，当pH小于3或大于7时变得不稳定。小白菊内酯在小白菊固态中的降解不符合任何明显的反应模型。水分含量和温度都对降解速率起着重要作用。储存6个月后，小白菊内酯在5℃/31%RH条件下含量保持不变。然而，如果储存在50℃/31%RH条件下，小白菊中约40%的小白菊内酯会降解。当水分从0%变为75%RH时，在40℃下储存6个月后小白菊中小白菊内酯的降解率从18%增加到32%。在为期3周的筛选研究的强化条件下，小白菊内酯在小白菊中与常用辅料表现出良好的相容性。
