【摘要】 目的将替米沙坦与介孔硅制备成片剂,并考察片剂的稳定性。方法在处方筛选的基础上,采用粉末直接压片法压制替米沙坦-介孔硅片剂;采用高效液相色谱法测定药物含量;采用示差扫描量热、X-射线衍射和溶出法考察制剂的晶型稳定性。结果替米沙坦-介孔硅分散体66 g、交联聚乙烯吡咯烷酮30 g、微晶纤维素50 g、甘露醇50 g、硬脂酸镁4 g,混合均匀,压制成1 000片,含量均匀度和溶出度符合要求,在12个月内替米沙坦稳定性良好,且一直以无定型状态存在。结论利用自制介孔硅制备固体分散体,介孔硅的孔道使难溶性药物长期以无定型状态存在,故制剂稳定性良好。更多还原

【Abstract】 Objective To prepare the tablets containing telmisartan and mesoporous silica solid disperse system and investigate its stability.Methods Based on the screening formulation,the tablets were produced with direct compression method.XRD and DSC were used for the identification of the crystal transformation,together with HPLC methods to quantify the drug.Results Telmisartan and mesoporous silica solid disperse system 66 g,crosslinked polyvinylpyrrolidone 30 g,microcrystalline cellulose 50 g,mannitol 50 g and magnesium stearate 4 g were mixed and directly compressed to produce 1 000 tablets,content uniformity and dissolution met the requirement,and stability was well and telmisartan in tablets maintained amorphous state during 12 months storage.Conclusions For poorly soluble crystalline drugs,short mesoporous pore channels of MSN self-made can be used to prepare the amorphous state solid disperse system,and the drug in its subsequent preparation can exist as amorphous state at least 12 months.更多还原