富马酸替诺福韦二吡呋酯片处方开发研究

摘要

目的：对富马酸替诺福韦二吡呋酯片的处方进行筛选，提取出最佳的处方配伍方案。方法参照国外上市片“VIREAD®”的处方工艺，对其稀释剂、崩解剂、粘合剂、润滑剂以及包衣工艺进行实验，并将自制样品与参比制剂在高温、高湿及光照条件下进行稳定性考察，筛选出合理的处方工艺。结果最终确定处方工艺为：富马酸替诺福韦二吡呋酯300mg；乳糖60mg；微晶纤维素165mg；预胶化淀粉100mg；交联羧甲基纤维素钠35mg；硬脂酸镁5mg；欧巴代薄膜包衣预混剂20mg；以纯化水为粘合剂。结论确定的处方工艺稳定，生产过程不苛刻，适合放大生产，稳定性研究结果与市售品性质相似，体外溶出行为相近，处方设计合理。%Objective To extract the best prescription compatibility program, the prescription of tenofovir disoproxil fumarate tablets were screened.MethodsAccording to prescription technology of foreign sales "VIREAD®", carried out experiments on its diluents, disintegrating agents, binders, lubricants and coating process, and homemade samples and reference preparation were stability studied under the conditions of high temperature, high humidity and illumination, screening a reasonable prescription process.ResultsPrescription process was ultimately determined including: tenofovir disoproxil fumarate 300mg; lactose 60mg; microcrystalline cellulose 165mg; pre-gelatinized starch 100mg; cross-linked sodium carboxymethyl cellulose 35mg; magnesium stearate 5mg; Opadry film coating premixes 20mg; purified water as a binder.Conclusion Prescription process determined is stable, production process is not harsh, suit amplification production, similar to the stability of the results and the nature of commercial products, similar behavior in vitro dissolution,the design of prescription is reasonable.