a School of Pharmacy , Anhui University of Chinese Medicine , Hefei , Anhui , China.
b Clinical Drug Trial Institution , The First Affiliated Hospital of Bengbu Medical College , Bengbu , Anhui , China.
Drug Dev Ind Pharm. 2019 Jul;45(7):1079-1088. doi: 10.1080/03639045.2019.1593441. Epub 2019 Mar 25.
The objective of this study was to design and evaluate azilsartan osmotic pump tablets. Preformulation properties of azilsartan were investigated for formulation design. Azilsartan osmotic pump tablets were prepared by incorporation of drug in the core and subsequent coating with cellulose acetate and polyethylene glycol 4000 as semi-permeable membrane, then drilled an orifice at the center of one side. The influence of different cores, compositions of semipermeable membrane and orifice diameter on azilsartan release were evaluated. The formulation of core tablet was optimized by orthogonal design and the release profiles of various formulations were evaluated by similarity factor (). The optimal formulation achieved to deliver azilsartan at an approximate zero-order up to 14 h. The pharmacokinetic study was performed in beagle dogs. The azilsartan osmotic pump tablets exhibited less fluctuation in blood concentration and higher bioavailability compared to immediate-release tablets. Moreover, there was a good correlation between the dissolution and absorption of the tablets. In summary, azilsartan osmotic pump tablets presented controlled release , high bioavailability and a good correlation.
本研究旨在设计和评估阿齐沙坦渗透泵片。对阿齐沙坦的预制剂性质进行了研究，为制剂设计提供了依据。将药物加入到片芯中，然后用醋酸纤维素和聚乙二醇 4000 作为半透膜进行包衣，在一侧的中心钻一个孔，制备阿齐沙坦渗透泵片。考察了不同片芯、半透膜组成和孔径对阿齐沙坦释放的影响。采用正交设计优化了片芯的处方，并通过相似因子（）评价了各种处方的释放曲线。优化处方的阿齐沙坦渗透泵片可在 14 小时内近似零级释放。在比格犬中进行了药代动力学研究。与普通片相比，阿齐沙坦渗透泵片的血药浓度波动较小，生物利用度较高。此外，片剂的溶出度与吸收度之间具有良好的相关性。综上所述，阿齐沙坦渗透泵片具有控制释放、高生物利用度和良好的相关性。
