高载药量的恩曲他滨替诺福韦片处方优化研究

摘要

目的：研究一种高载药量的恩曲他滨替诺福韦复方片处方，优化其处方配伍方案。方法在对国外上市制剂的处方工艺进行分析的基础上，进行稳定剂、填充剂、崩解剂、黏合剂的筛选和最终处方的放大验证，确定合理可行的处方工艺。结果以处方解析确定的高风险因素为考察指标，确定了高载药量的恩曲他滨替诺福韦片的处方：每片含恩曲他滨200 mg，富马酸替诺福韦二吡呋酯300 mg，预胶化淀粉60 mg，微晶纤维素100 mg，交联羧甲基纤维素钠30 mg，硬脂酸镁5 mg，95％乙醇为黏合剂。自制片与对照片质量比对结果一致。结论筛选的恩曲他滨替诺福韦复方片处方工艺合理可行，产品重现性和稳定性好。%Objective To explore the formula of a high drug loading of emtricitabine tenofovir compound tablets,and to optimize its compatibility prescription program.Methods Based on the analysis of the formulation and process of foreign drug,some pharmaceutical accessories were screened including stabilizers,fillers,disintegrants and binders,and the verification of the final amplification prescrip-tion was carried out in order to determine the reasonable and feasible prescription process.Results Some high-risk factors identified by prescription analysis were used as indexes,and then the prescription of high drug loading of emtricitabine tenofovir tablets was obtained, which was 200 mg emtricitabine,300 mg tenofovir disoproxil fumarate,60 mg pre-gelatinized starch,100 mg microcrystalline cellulose, 30 mg cross-linked sodium carboxymethyl cellulose,5 mg magnesium stearate,and 95% ethanol as a binder in each tablet.The com-pared results between the tablets prepared by above-mentioned prescription and the reference sample were consistent.Conclusions The screened prescription process of emtricitabine tenofovir compound tablets was reasonable and feasible with high reproducibility and stability.