Wiranidchapong Chutima, Ruangpayungsak Nuchnan, Suwattanasuk Pattaraporn, Shuwisitkul Duangratana, Tanvichien Sujimon
Faculty of Pharmacy, Srinakharinwirot University , Nakhon-Nayok , Thailand and.
Drug Dev Ind Pharm. 2015 Jun;41(6):1037-46. doi: 10.3109/03639045.2014.925917. Epub 2014 Jun 11.
The objectives of this study were to investigate the effect of storage temperature on drug release from matrices containing 10, 40 and 70% w/w ibuprofen in Kollidon® SR (KSR). The matrix tablets were produced by direct compression and then kept at 30 and 45 °C for 3 months. Drug release from the matrix tablets was examined after storage for 0, 1, 4 and 12 weeks. Scanning electron microscope was used to reveal physical appearance of the tablet surface at the respective time intervals. In addition, differential scanning calorimeter was used to investigate glass transition temperature (Tg) of ibuprofen in KSR at 0-100% w/w based on the principle of Gordon-Taylor equation. At 45 °C, the dissolution of ibuprofen in KSR as well as the coalescence of polymer particles were observed to be higher than those of storage at 30 °C. The physical state of ibuprofen dispersed in the polymeric matrix and degree of polymer coalescence led to the variation of drug release. The coalescence of polymer particles was a result of the polymer transition from glassy to rubbery state according to water absorption of KSR and plasticizing effect of ibuprofen. The reduction of the Tg of ibuprofen blended with KSR could be better described by the Kwei equation, a modified version of Gordon-Taylor equation.
本研究的目的是考察储存温度对含10%、40%和70%(w/w)布洛芬的聚乙烯吡咯烷酮缓释剂(KSR)基质药物释放的影响。基质片剂通过直接压片法制备,然后在30℃和45℃下保存3个月。在储存0、1、4和12周后检测基质片剂的药物释放情况。使用扫描电子显微镜揭示各时间间隔下表片表面的物理外观。此外,基于戈登-泰勒方程原理,使用差示扫描量热仪研究0-100%(w/w)KSR中布洛芬的玻璃化转变温度(Tg)。在45℃下,观察到布洛芬在KSR中的溶出以及聚合物颗粒的聚结高于在30℃下储存的情况。布洛芬分散在聚合物基质中的物理状态和聚合物聚结程度导致了药物释放的变化。聚合物颗粒的聚结是聚合物根据KSR的吸水性和布洛芬的增塑作用从玻璃态转变为橡胶态的结果。与KSR混合的布洛芬Tg的降低可以用Kwei方程(戈登-泰勒方程的修正版)更好地描述。