Moradiya Hiren G, Nokhodchi Ali, Bradley Michael S A, Farnish R, Douroumis Dennis
a Faculty of Engineering & Science , School of Sciences, University of Greenwich , Chatham , Kent , UK .
b School of Life Sciences, University of Sussex , Brighton , UK .
Pharm Dev Technol. 2016;21(4):445-52. doi: 10.3109/10837450.2015.1022783. Epub 2015 Mar 11.
Carbamazepine (CBZ) shows a poor dissolution, therefore, it is important to enhance its dissolution in GI tract to improve its bioavailability. In the present study, a new hydrophilic carrier, d-gluconolactone (GNL), was extruded with CBZ at various molar ratios to produce granules by using hot melt extrusion (HME) processing. The granular extrudates were characterised by X-ray powder diffraction, differential scanning calorimetry and hot stage microscopy to determine the solid state of CBZ. It was found that bulk CBZ (Form-III) transformed to the polymorphic Form-I during the HME processing. GNL was proved to be an efficient carrier for CBZ to enhance the dissolution rate. The increase in the dissolution rate was observed for both physical mixtures and the extrudates of CBZ-GNL. However, the extrudates showed faster dissolution rates compared to physical mixtures in an ascending order of 2:1 < 1:1 < 1.5:1 (CBZ:GNL). The increase in the dissolution rates was attributed to the transformation of CBZ III to Form-I and also to the increased drug wettability/solubilisation in the presence of the carrier.
卡马西平（CBZ）的溶出度较差，因此，提高其在胃肠道中的溶出度以改善其生物利用度非常重要。在本研究中，一种新型亲水性载体，D-葡萄糖酸内酯（GNL），与CBZ以不同的摩尔比通过热熔挤出（HME）工艺挤出以制备颗粒。通过X射线粉末衍射、差示扫描量热法和热台显微镜对颗粒挤出物进行表征，以确定CBZ的固态。结果发现，在HME过程中，块状CBZ（III型）转变为多晶型I型。GNL被证明是一种有效的CBZ载体，可提高溶出速率。在CBZ-GNL的物理混合物和挤出物中均观察到溶出速率的增加。然而，挤出物的溶出速率比物理混合物更快，顺序为2:1 < 1:1 < 1.5:1（CBZ:GNL）。溶出速率的增加归因于CBZ III型向I型的转变，也归因于在载体存在下药物润湿性/溶解度的增加。
