盐酸西那卡塞固体分散体片的制备及溶出度评价

Preparation of cinacalcet hydrochloride solid dispersion tablets and evaluation of the dissolution

目的采用溶剂法制备盐酸西那卡塞固体分散体片并对其溶出度进行测定。方法以PVP K30作为载体,选用微晶纤维素(MCC)进行流化床制粒,将制得的固体分散体进行压片;采用差示扫描量热法(DSC)、X-射线衍射(XRD)、红外光谱法(FTIR)以及扫描电镜(SEM)对固体分散体进行表征,并对所制备的片剂进行溶出度测定。结果盐酸西那卡塞与PVP K30以氢键结合,药物以无定形状态高度分散于MCC表面;固体分散体片4种溶出介质中的溶出速度明显高于普通片;与市售制剂比较,相似因子f2值均大于50。结论盐酸西那卡塞与PVP K30、MCC制备的固体分散体片有效地提高了药物的溶出速度,且方法简单,易于实现产业化。

Objective To prepare cinacalcet hydrochloride solid dispersion tablets by solvent method and evaluate the dissolution behaviors of the tablets. Method PVP K30 was used as the carrier of solid dispersion. The solution containing cinacalcet hydrochloride and PVP K30 was sprayed to the surface of MCC using fluid bed granulation method, and then this preformed solid dispersion was used to prepare cinacalcet hydrochloride tablets. Fourier transform infrared spectroscopy(FTIR), X-ray diffraction(XRD), differential scanning calorimetry(DSC) and scanning electron microscopy(SEM) were employed to characterize solid dispersion. The dissolution behavior in vitro of cinacalcet hydrochloride solid dispersion tablets was also studied. Results Cinacalcet hydrochloride interacted with PVP K30 through hydrogen bonds and cinacalcet hydrochloride was highly dispersed on the surface of MCC in the form of amorphous. Cinacalcet hydrochloride solid dispersion tablets exhibited better dissolution which was similar with that of commercial tablets. Conclusion The solid dispersion tablets of cinacalcet hydrochloride based on PVP K30 and MCC effectively improved the dissolution of cinacalcet hydrochloride and this simple method is easy to realize industrial production.