目的 制备他达拉非片并考察其体内外释药特性。方法 以溶出度为评价指标，筛选他达拉非片各辅料用量及包衣增重。用相似因子（f₂）法比较自制制剂与参比制剂在0.5% SDS溶液、含0.5% SDS的0.1 mol/L的盐酸溶液、含0.5% SDS的pH 4.5醋酸钠缓冲液、含0.5% SDS的pH 6.8磷酸盐缓冲液中溶出曲线的相似性。比较二者在Beagle犬体内的药动学特征。结果 他达拉非片处方为他达拉非20 mg、乳糖50M 227.625 mg、羟丙基纤维素L 10.5 mg、交联羧甲基纤维素钠19.6 mg、SDS 0.525 mg、微晶纤维素M102 70 mg、硬脂酸镁1.75 mg，包衣增质量范围2%～4%。自制与参比制剂在4种溶出介质中的f₂均大于65，二者体外溶出行为相似。2种制剂在Beagle体内的药动学参数AUC_0~t、C_max、t_max均无显著性差异，自制他达拉非片的相对生物利用度为（101.67±8.99）%。结论 成功制备他达拉非片，其体外溶出和体内药动学行为与参比制剂相似。

Objective To prepare Tadalafil tablets and investigate its in vitro-in vivo release characteristics. Methods Using dissolution degree as index,to screen the amount of each excipient and the coating weight gain. f₂ similarity factor method was used to compare the similarity of dissolution curves between self-made preparation and reference preparation in 0.5%SDS solution, 0.1 mol/L hydrochloric acid solution containing 0.5% SDS, pH 4.5 sodium acetate buffer containing 0.5%SDS, and pH6.8 phosphate buffer containing 0.5% SDS.To compare the pharmacokinetic characteristics of the two preparations in beagle body. Results The formulation of tadalafil tablets was tadalafil 20 mg, 227.625 mg lactose 50M, 10.5 mg hydroxypropyl cellulose L, croscarmellose sodium 19.6 mg, SDS 0.525 mg, 70 mg microcrystalline cellulose M102, and magnesium stearate 1.75 mg, and the coating weight gain ranged from 2% to 4%.The similarity factor (f₂) of the self-made preparation and the reference preparation was greater than 65 in the four dissolution media, and the dissolution behavior of the two preparations was similar in vitro. There were no significant differences in pharmacokinetic parameters AUC_0-t, C_max and t_max. The relative bioavailability of self-made tadalafil tablets was (101.67 ±8.99)%. Conclusions Tadalafil tablets were successfully prepared, and its in vitro dissolution and in vivo pharmacokinetic behavior were similar to reference preparations.

R944.4

国家手性制药工程技术研究中心资助项目（2016GGH4528）