厚朴酚-交联羧甲基纤维素钠固体分散体的制备及体外溶出研究

Preparation and in vitro dissolution of magnolol solid dispersion

为提高厚朴酚的溶出度,以交联羧甲基纤维素钠为载体,采用溶剂蒸发法制备厚朴酚固体分散体,并对其溶出行为、稳定性、物相特征进行研究。厚朴酚和交联羧甲基纤维素钠按照1∶5制备的固体分散体,120 min时药物的体外累积溶出度达到80.66%,是原料药厚朴酚的6.9倍。经差示扫描量热、红外色谱、扫描电镜分析,固体分散体中药物以无定形态存在于载体中;经过6个月加速稳定性试验后,固体分散体中药物含量和溶出度均未发生明显变化。因此以交联羧甲基纤维素钠为载体制备的固体分散体能有效提高厚朴酚的溶出度和稳定性。

In this study,solid dispersion system of magnolol in croscarmellose sodium was prepared by using the solvent evaporation method,in order to increase the drug dissolution. And its dissolution behavior,stability and physical characteristics were studied. The solid dispersion was prepared with magnolol and croscarmellose sodium,with the proportion of 1∶ 5,the in vitro dissolution of magnolol solid dispersion was up to 80. 66% at 120 min,which was 6. 9 times of magnolol. The results of DSC（ differential scanning calorimetry）,IR（ infra-red） spectrum and SEM（ scanning electron microscopy） showed that magnolol existed in solid dispersion in an amorphous form. After an accelerated stability test for six months,the drug dissolution and content in magnolol solid dispersion showed no significant change. So the solid dispersion prepared with croscarmellose sodium as the carrier can remarkably improve the stability and dissolution of magnolol.