Li Yuenan, Pan Hao, Duan Hongliang, Chen Jianting, Zhu Zhihong, Fan Jingxin, Li Pingfei, Yang Xinggang, Pan Weisan
Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang City, Liaoning Province 110016, China.
Liao Ning University, No. 66, Chongshan Middle Road, Huanggu District, Shenyang City, Liaoning Province 110036, China.
Asian J Pharm Sci. 2019 May;14(3):340-348. doi: 10.1016/j.ajps.2018.05.009. Epub 2018 Aug 19.
The aim of the study was to develop actarit double-layered osmotic pump tablets to overcome the weak points of actarit common tablets, such as short half-life and large plasma concentration fluctuations. Single factor experiment and orthogonal test were applied to optimize the formulation; the pharmacokinetic study was performed in beagle dogs adopting actarit common tablets as reference tablets. The optimal formulation was as follows: drug layer: 150 mg actarit, 240 mg PEO-N80, 50 mg NaCl; push layer: 140 mg PEO-WSR303, 20 mg NaCl; coating solution: 30 g cellulose acetate and 6 g PEG 4000 in 1000 ml 94% acetone solution, 60 mg coating weight gain. The pharmacokinetic study showed that was prolonged by the contrast of commercial common tablets with constant drug release rate, but the bioavailability was equivalent. And a good - correlation of the actarit osmotic pump tablets was also established. The designed actarit osmotic pump tablets can be applied for rheumatoid arthritis, proposing a promising replacement for the marked common products.
本研究的目的是开发阿克他利双层渗透泵片,以克服阿克他利普通片的缺点,如半衰期短和血浆浓度波动大。采用单因素实验和正交试验优化处方;以阿克他利普通片为参比制剂,在比格犬体内进行药代动力学研究。优化后的处方如下:药物层:150mg阿克他利、240mg聚氧化乙烯-N80、50mg氯化钠;推动层:140mg聚氧化乙烯-WSR303、20mg氯化钠;包衣液:30g醋酸纤维素和6g聚乙二醇4000溶于1000ml 94%丙酮溶液中,包衣增重60mg。药代动力学研究表明,与市售普通片相比,阿克他利渗透泵片的药物释放速率恒定,半衰期延长,但生物利用度相当。同时,阿克他利渗透泵片也建立了良好的相关性。所设计的阿克他利渗透泵片可用于类风湿性关节炎,有望成为现有市售普通产品的理想替代剂型。