他达拉非为生物药剂学分类系统(BCS)Ⅱ类药物，溶解性差、起效缓慢，生物利用度低。本研究将他达拉非包合于β-环糊精中，以增加药物的溶解度、掩盖不良气味。结果表明，当15 g/L的他达拉非丙酮溶液与80 g/L β-环糊精按1∶2体积比包合时，包合物收率和包封率均较高，且能掩盖他达拉非的不良气味。随后，以环糊精包合物替代原料药投料，制备他达拉非口腔崩解片，并采用Box-Behnken设计，以崩解时间和硬度为指标优化处方。优化的他达拉非口腔崩解片崩解时间和硬度为47.19 s与52.07 N，达到预期目标，且片重、厚度、含量和脆碎度符合要求。在不同pH介质中，3批自制口腔崩解片30 min溶出率均大于85％。Beagle犬体内的药动学试验结果表明，相较于参比制剂(Cialis)，自制片的tmax由2.08 h提前至1.16 h，cmax由15.66 ng/ml增至20.67 ng/ml，相对生物利用度为112.8％。

Tadalafil is a biopharmaceutical classification system(BCS) class Ⅱ drug with poor solubility, slow onset of action, and low bioavailability. In this study, the inclusion complexes of tadalafil and β-cyclodextrin were firstly prepared to increase the solubility of tadalafil and obtain the taste-masking ability. The results showed that when 15 g/L tadalafil acetone solution mixed with 80 g/L β-cyclodextrin in a volume ratio of 1∶2, both yield and encapsulation efficiency of the inclusion complexes were satisfactory and achieved an effective taste-masking ability. Then, the cyclodextrin inclusion complexes instead of the bulk drug were used to prepare tadalafil orally disintegrating tablets. The formulation was optimized by Box-Behnken design with disintegration time and hardness as the main indicators. The disintegration time and hardness of the optimal tablets were respectively 47.19 s and 52.07 N, which reached the expected standard. And all of the tablet weight, thickness, drug content, and friability met the requirements. The dissolution rates of three batches of self-made tablets were above 85％ in various pH media. The results of the pharmacokinetic test in Beagle dogs showed that tmax of the self-made tablets was shortened from 2.08 h to 1.16 h, and the cmax was increased from 15.66 ng/ml to 20.67 ng/ml compared with the reference preparation(Cialis). The relative bioavailability of the title tablets was 112.8％.