Kriangkrai Worawut, Puttipipatkhachorn Satit, Sriamornsak Pornsak, Pongjanyakul Thaned, Sungthongjeen Srisagul
Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok-Nakhonsawan Road, Phitsanulok, 65000, Thailand.
AAPS PharmSciTech. 2014 Dec;15(6):1357-69. doi: 10.1208/s12249-014-0161-4. Epub 2014 Jun 14.
Tackiness caused by the gas-entrapped membrane (Eudragit(®)RL 30D) was usually observed during storage of the effervescent floating tablets, leading to failure in floatation and sustained release. In this work, common anti-tacking agents (glyceryl monostearate (GMS) and talc) were used to solve this tackiness problem. The impact of anti-tacking agent on the properties of free films and corresponding floating tablets was investigated. GMS was more effective than talc in reducing tackiness of the film. Addition and increasing amount of anti-tacking agents lowered the film mechanical strength, but the coating films were still strong and flexible enough to resist the generated gas pressure inside the floating tablet. Wettability and water vapor permeability of the film decreased with increasing level of anti-tacking agents as a result of their hydrophobicity. No interaction between anti-tacking agents and polymer was observed as confirmed by Fourier transform infrared spectroscopy, powder X-ray diffractometry, and differential scanning calorimetry studies. Increasing amount of anti-tacking agents decreased time to float and tended to retard drug release of the floating tablets. Floating properties and drug release were also influenced by type of anti-tacking agents. The obtained floating tablets still possessed good floating properties and controlled drug release even though anti-tacking agent had some effects. The results demonstrated that the tackiness problem of the floating tablets could be solved by incorporating anti-tacking agent into the gas-entrapped membrane.
在泡腾漂浮片储存过程中,通常会观察到由气体截留膜(Eudragit® RL 30D)引起的粘性,导致漂浮和缓释失败。在这项工作中,使用了常见的抗粘剂(单硬脂酸甘油酯(GMS)和滑石粉)来解决这种粘性问题。研究了抗粘剂对游离膜和相应漂浮片性能的影响。GMS在降低膜的粘性方面比滑石粉更有效。抗粘剂的添加和用量增加会降低膜的机械强度,但包衣膜仍足够坚固且柔韧,能够抵抗漂浮片内部产生的气体压力。由于抗粘剂的疏水性,随着其用量增加,膜的润湿性和水蒸气透过率降低。傅里叶变换红外光谱、粉末X射线衍射和差示扫描量热法研究证实,未观察到抗粘剂与聚合物之间的相互作用。抗粘剂用量增加会缩短漂浮时间,并倾向于延缓漂浮片的药物释放。抗粘剂的类型也会影响漂浮性能和药物释放。即使抗粘剂有一些影响,所获得的漂浮片仍具有良好的漂浮性能和控释效果。结果表明,通过在气体截留膜中加入抗粘剂,可以解决漂浮片的粘性问题。