坎地沙坦酯聚乙烯吡咯烷酮K30共沉淀物分散片的制备与质量评价  

Preparation and quality evaluation of Candesartan Cilexetil PVP-K30 Co-precipitate Dispersible Tablets

作　　者：徐丽清 张丽妍[1] XU Liqing;ZHANG Liyan(Department of Pharmacy,the Third People′s Hospital of Dalian,Dalian 116033,China)

机构地区：[1]大连市第三人民医院药剂科,大连116033

出　　处：《西北药学杂志》2021年第1期81-86,共6页Northwest Pharmaceutical Journal

摘　　要：目的制备坎地沙坦酯聚乙烯吡咯烷酮K30(PVP-K30)共沉淀物,并进一步制备成分散片,提高坎地沙坦酯的溶出度。方法以微粉硅胶作为载体,采用共沉淀技术制备坎地沙坦酯PVP-K30共沉淀物,利用差示热分析(DTA)、X射线粉末衍射分析(XRD)以及傅里叶红外光谱分析(FTIR)对坎地沙坦酯PVP-K30共沉淀物进行表征;经单因素实验筛选得到坎地沙坦酯PVP-K30共沉淀物分散片的最优处方;比较了坎地沙坦酯PVP-K30共沉淀物分散片与市售坎地沙坦酯分散片的体外溶出速率;并通过初步稳定性实验考察了坎地沙坦酯PVP-K30共沉淀物分散片的稳定性。结果XRD显示,坎地沙坦酯PVP-K30共沉淀物中药物以无定形存在;经优化得到坎地沙坦酯PVP-K30共沉淀物分散片的最佳处方用量为:微晶纤维素175 mg,乳糖175 mg,交联聚维酮26 mg,硬脂酸镁4 mg,与市售坎地沙坦酯分散片相比,坎地沙坦酯PVP-K30共沉淀物分散片可显著提高药物溶出速率;稳定性实验结果显示,坎地沙坦酯PVP-K30共沉淀物分散片加速6个月内稳定性良好。结论制备的坎地沙坦酯PVP-K30共沉淀物分散片可显著提高坎地沙坦酯的溶出速率,有望显著提高药物的生物利用度。Objective To prepare candesartan cilexetil PVP-K30 co-precipitate,and further prepared into dispersible tablets to improve the dissolution of candesartan cilexetil.Methods The candesartan cilexetil PVP-K30 co-precipitate was prepared by using co-precipitation technology with colloidal silicon dioxide as the carrier.candesartan cilexetil PVP-K30 co-precipitate was characterized by differential thermal analysis(DTA),X-ray powder diffraction analysis(XRD)and Fourier infrared spectrometry(FTIR).The formulation of Candesartan Cilexetil PVP-K30 Co-precipitate Dispersible Tablets was optimized by single factor experiments.In vitro dissolution rates of Candesartan Cilexetil PVP-K30 Co-precipitate Dispersible Tablets and Candesartan Cilexetil Dispersible Tablets were compared.The stability of the tablets was investigated through preliminary stability experiments.Results XRD showed that candesartan cilexetil existed in an amorphous state.The optimal formulation compositions of Candesartan Cilexetil PVP-K30 Co-precipitate Dispersible Tablets were as follows:the amount of microcrystalline cellulose 175 mg,the amount of lactose 175 mg,the amount of PVPP 26 mg,and the amount of magnesium stearate 4 mg.The prepared tablets could significantly increase drug dissolution rate compared with Candesartan Medoxomil Dispersing tablets.The stability experiment showed Candesartan Cilexetil PVP-K30 Co-precipitate Dispersible Tablets had good stability within 6 months.Conclusion Candesartan cilexetil was prepared into PVP-K30 Co-precipitate Dispersible Tablets,which can significantly increase the dissolution rate,and are expected to significantly improve the bioavailability of candesartan cilexetil.

关 键 词：坎地沙坦酯 聚乙烯吡咯烷酮K30 共沉淀物 分散片 溶出度 生物利用度 

分 类 号：R94[医药卫生—药剂学]