Feng Zilin, Li Mengting, Wang Wenxi
Pharmazie. 2019 Sep 1;74(9):523-528. doi: 10.1691/ph.2019.9008.
Solid dispersions (SDs) have made great progress in the improvement of dissolution for poorly soluble drugs, however the low drug loading still limits their wide application. In the present paper, high carbamazepine (CBZ) loaded SDs with excellent dissolution and tabletability were prepared and characterized. The CBZ SDs were prepared with Eudragit EPO as carrier by hot-melt extrusion (HME) in the drug: carrier ratio of 4:1. Powder X-ray diffraction, differential scanning calorimetry, fourier transform infrared spectroscopy and powder dissolution was carried out to characterize the SDs. The results showed that the crystalline form the polymorph of CBZ in SDs was transformed into form I from form III after extruded at 140 °C. Wettability and microstructure of CBZ SDs were improved by the HME process, which promoted the dissolution significantly. More than 85 % drug dissolved within 5 min from CBZ SDs with even only 20 % Eudragit EPO as carrier. CBZ SDs tablets were prepared by direct tableting with a universal material testing machine at various compaction pressures. Compactibility and tabletability were enhanced significantly by the HME process. All of these results showed the CBZ SDs prepared by HME with 80 % CBZ and 20 % Eudragit EPO could improve the dissolution and tabletability significantly.
固体分散体（SDs）在改善难溶性药物的溶出度方面取得了很大进展，然而低载药量仍然限制了它们的广泛应用。在本文中，制备并表征了具有优异溶出度和可压性的高卡马西平（CBZ）载量固体分散体。以Eudragit EPO为载体，通过热熔挤出（HME）以4:1的药物:载体比例制备了CBZ固体分散体。采用粉末X射线衍射、差示扫描量热法、傅里叶变换红外光谱法和粉末溶出度测定对固体分散体进行表征。结果表明，在140℃挤出后，固体分散体中CBZ的晶型多晶型从III型转变为I型。热熔挤出工艺改善了CBZ固体分散体的润湿性和微观结构，显著促进了溶出。以仅20%的Eudragit EPO为载体的CBZ固体分散体在5分钟内药物溶出超过85%。使用万能材料试验机在不同的压片压力下通过直接压片制备了CBZ固体分散体片剂。热熔挤出工艺显著提高了可压性和可压片性。所有这些结果表明，以80%的CBZ和20%的Eudragit EPO通过热熔挤出制备的CBZ固体分散体可以显著提高溶出度和可压片性。
