非那雄胺片制剂的处方及工艺研究

Study on Formulation and Preparation Process of Finasteride Tablets

目的:对非那雄胺片(1mg)的处方工艺进行研究。方法:参照国外英文说明书中制剂所用的辅料,通过测定在四种不同溶出介质中的溶出曲线,使之达到与原研市售品溶出曲线相似,判断增溶剂、崩解剂、填充剂的用量及工艺进行考察,并对确定处方及制备工艺中试三批,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:用非那雄胺为主药,以乳糖、微晶纤维素和预胶化淀粉为填充剂,以泊洛沙姆188为增溶剂,以羧甲淀粉钠为崩解剂,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,制得非那雄胺片。结论:本制剂工艺稳定,各种辅料均有合法来源,制得非那雄胺片(1mg)与原研市售品溶出行为相似。

Objective： To study the formulation and preparation process of Finasteride Tablets. Methods：Based on the excipients listed in the package insert of Finasteride Tat）lets （English version）, dissolution curves in four kinds of dissolution medium were measured and made to show similar dissolution behavior as compared with the original commercial product. Through the selection of the amount of solubilizers, disintegrants, fillers and formulation process, three batches of test product in pilot scale were prepared according to the opti- mized formulation. The dissolution curve, the content uniformity, related substances and other indicators tested in four kinds of dissolution medium were determined correspondingly. Results：Finasteride tablets were formulated with finasteride as the main drug, lactose, micro- crystalline cellulose and pregelatinized starch as fillers, poloxamer 188 as solubilizer, sodium carboxymethyl starch as disintegrant, stearic magnesium as lubricant, film coating premixed adjuvant（gastric-dissolving type ）as the coating material. Conclusion：The present formu- lation process of our developed finasteride tablets （ 1 rag）was stable, the excipients of which are all from legitimate sources. The dissolution behavior of our developed formulation was similar to that of the original commercial product.