利伐沙班片的制备及处方优化

Preparation and formulation optimization of Rivaroxaban tablets

目的制备利伐沙班片剂,优选适合中试生产的最佳处方。方法通过设计不同处方,对增溶剂、崩解剂、黏合剂、填充剂的用量及工艺进行考察,并进行了中试三批放大,测定在四种溶出介质中的溶出曲线、含量均匀度和有关物质等指标。结果用利伐沙班为主药,以乳糖、微晶纤维素为填充剂,以十二烷基硫酸钠为增溶剂,以交联羧甲基纤维素钠为崩解剂,以羟丙基甲基纤维素为黏合剂、以硬脂酸镁为润滑剂,以胃溶型薄膜包衣预混剂为包衣材料,制得利伐沙班片。结论该制剂工艺稳定,制得利伐沙班片(10 mg)与原研市售品溶出行为相似,质量符合规定。

Objective To prepare Rivaroxaban tablets and choose the best prescription for pilot scale production.Methods Through the design of different prescriptions and the selection of the amount of solubilizers, disintegrants, fillers and formulation process, three bat-ches of test product in pilot scale were prepared according to the optimized formulation.The dissolution curve, content uniformity, related substances and other indicators tested in four kinds of dissolution media were determined correspondingly.Results Rivaroxaban tablets were formulated with Rivaroxaban as the main drug,lactose and microcrystallinecellulose as fillers, sodium lauryl sulfate as solubilizer, roscarmellose sodium as disintegrant, stearic magnesium as lubricant, film coating premixed adjuvant（gastric-dissolving type）as the coat-ing material.Conclusion The present formulation process of newly developed Rivaroxaban tablets（10 mg） was stable.The dissolution behavior of newly developed formulation was similar to that of the originally commercial product.The quality complies with the provisions.