Kibria Golam, Ul-Jalil Reza
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Dhaka, Dhaka-1000, Bangladesh.
Pak J Pharm Sci. 2008 Apr;21(2):92-7.
The aim of this study was to investigate the effect of physico-chemical properties of the polymers on the release profile of ketoprofen from the pellets dosage form. Ammonio Methacrylate Copolymer Type A (Eudragit RL 30 D) & Ammonio Methacrylate Copolymer Type B (Eudragit RS 30 D) were used as release rate retarding polymers. The drug containing core pellets were prepared by extrusion spheronisation technique and subsequently coated with 15% (w/w) polymer load of the combination of Eudragit RL 30 D & Eudragit RS 30 D having ratio 1:0, 4:1, 3:2, 1:1, 2:3, 1:4, 0:1 respectively. Significant differences were found among the drug release profile from different formulations. It was revealed that Eudragit RL 30 D has the effect to increase the initial drug release more significantly where as Eudragit RS 30 D has the effect to minimize the initial drug release but increase the terminal drug release more significantly. In acid media about 50% drug was released from pellets coated only with Eudragit RL 30 D where as only 5% drug was released in case of Eudragit RS 30 D but maximum 10% drug was released from pellets when coated with the combination of Eudragit RL 30 D & Eudragit RS 30 D. In buffer media, evidence of burst release was observed for the pellets coated with Eudragit RL 30 D & Eudragit RS 30 D having ratio of 1:0, 4:1, 3:2 respectively. It was also observed that drug release increases sharply as well as the release best fit to the zero order release kinetics when pellets coated with 1:1 ratio of Eudragit RL 30 D & Eudragit RS and follows Higuchi's release kinetics when ratio was 1:0 & 3:2. The results generated in this study showed that proper selection of polymeric materials based on their physico-chemical properties is important in designing sustained release pellets dosage form with suitable dissolution profile.
本研究的目的是考察聚合物的物理化学性质对酮洛芬从微丸剂型中释放曲线的影响。A型甲基丙烯酸铵共聚物(尤特奇RL 30 D)和B型甲基丙烯酸铵共聚物(尤特奇RS 30 D)用作缓释聚合物。含药的核心微丸通过挤出滚圆技术制备,随后分别用比例为1:0、4:1、3:2、1:1、2:3、1:4、0:1的尤特奇RL 30 D和尤特奇RS 30 D组合,以15%(w/w)的聚合物载量进行包衣。不同制剂的药物释放曲线存在显著差异。结果表明,尤特奇RL 30 D更显著地增加药物的初始释放,而尤特奇RS 30 D则使药物的初始释放最小化,但更显著地增加药物的终末释放。在酸性介质中,仅用尤特奇RL 30 D包衣的微丸释放约50%的药物,而用尤特奇RS 30 D包衣时仅释放5%的药物,但用尤特奇RL 30 D和尤特奇RS 30 D组合包衣的微丸最多释放10%的药物。在缓冲介质中,观察到比例为1:0、4:1、3:2的尤特奇RL 30 D和尤特奇RS 30 D包衣的微丸有突释现象。还观察到,当尤特奇RL 30 D和尤特奇RS以1:1比例包衣时,药物释放急剧增加,且释放最符合零级释放动力学,当比例为1:0和3:2时遵循 Higuchi 释放动力学。本研究结果表明,根据聚合物的物理化学性质合理选择聚合物材料对于设计具有合适溶出曲线的缓释微丸剂型很重要。