Cefpodoxime proxetil is a third generation cephalosporin antibiotic demonstrates pH dependent solubility and is highly soluble only in acidic pH. The purpose of this investigation was to design and develop immediate release tablets of cefpodoxime proxetil by direct compression method and determine the effect of different solid buffers (organic acids) such as fumaric acid (formulations F1-F4), maleic acid (formulations M1-M4) and citric acid (formulations C1-C4) by using cefpodoxime and acid in the ratios of 4:1, 2:1, 1:1 and 1:2 to achieve pH-independent release of the drug. Physical parameters and assay were found to be within the acceptable range as prescribed in USP 36 / NF 31. In vitro dissolution studies of each formulation were performed in distilled water, USP dissolution medium, HCl buffer solution of pH 1.2, phosphate buffer solutions of pH 4.5 and 6.8 to observe the drug release. The formulations F3, F4, M4 were selected for film coating on the basis of better drug release profile, to protect the drug from chemical degradation through hydrolysis. Film coated formulation F3, F4 and M4 showed a remarkable in vitro release of the drug (72.88±0.43 to 92.67±0.71%) within 30min of observation in all dissolution media and further evaluated by model independent and model dependent approaches. The drug release was found to be best fit to Weibull model as highest r2adjusted (0.924-0.998) and lowest AIC (18.416-54.710) values were obtained in all dissolution media. R Gui® applied for stability studies of F3 and F4 formulations, showing shelf lives of 28 & 27months at ambient and 33 months at accelerated temperatures. Formulation F4 was chosen as best formulation on the basis of physical properties, highest dissolution rate and stability studies.

译文

头孢泊肟酯是第三代头孢菌素抗生素,具有pH依赖性溶解度,仅在酸性pH下高度可溶。本研究的目的是通过直接压片法设计和开发头孢泊肟酯的速释片剂,并确定不同固体缓冲液 (有机酸) 如富马酸 (配方F1-F4) 的效果。马来酸 (制剂M1-M4) 和柠檬酸 (制剂C1-C4) 通过以4:1,2:1,1:1和1:2的比例使用头孢泊肟和酸来实现药物的pH独立释放。发现物理参数和测定在USP 36 / NF 31规定的可接受范围内。在蒸馏水,USP溶解介质,pH 1.2的HCl缓冲溶液,pH 4.5和6.8的磷酸盐缓冲溶液中进行每种制剂的体外溶出研究,以观察药物释放。基于更好的药物释放特性,选择F3,F4,M4制剂进行薄膜包衣,以保护药物免受水解化学降解。薄膜包衣制剂F3,F4和M4在所有溶解介质中观察30分钟内显示出显着的药物体外释放 (72.88 ± 0.43至92.67 ± 0.71%),并通过模型独立和模型依赖方法进行进一步评估。发现药物释放最适合Weibull模型,因为在所有溶解介质中获得最高的r2调节值 (0.924-0.998) 和最低的AIC值 (18.416-54.710)。R Gui®适用于F3和F4制剂的稳定性研究,显示在环境下的保质期为28和27个月,在加速温度下的保质期为33个月。根据物理性质,最高溶解速率和稳定性研究,选择配方F4作为最佳配方。

+1
+2
100研值 100研值 ¥99课程
检索文献一次
下载文献一次

去下载>

成功解锁2个技能,为你点赞

《SCI写作十大必备语法》
解决你的SCI语法难题!

技能熟练度+1

视频课《玩转文献检索》
让你成为检索达人!

恭喜完成新手挑战

手机微信扫一扫,添加好友领取

免费领《Endnote文献管理工具+教程》

微信扫码, 免费领取

手机登录

获取验证码
登录