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。
Objective To prepare the tablets containing telmisartan and mesoporous silica solid disperse sys-tem 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, to-gether 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 mag-nesium stearate 4 g were mixed and directly compressed to produce 1 000 tablets, content uniformity and dis-solution 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 sub-seauent oreoaration can exist as amorohous state at least 12 months.
出处
《沈阳药科大学学报》
CAS
CSCD
北大核心
2013年第1期8-12,共5页
Journal of Shenyang Pharmaceutical University
基金
辽宁省教育厅重点实验室基金资助项目(LS2010161)
关键词
难溶药物
替米沙坦
介孔硅
无定型
稳定性
poorly soluble drug
telmisartan
mesoporous silica
amorphous
stability
