Pharmaceutics Division, Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, India.
AAPS PharmSciTech. 2012 Jun;13(2):431-40. doi: 10.1208/s12249-012-9763-x. Epub 2012 Feb 24.
The present investigation was aimed at developing and optimizing a simple aqueous tablet-coating formulation and its process. 5-Fluorouracil (5-FU) was used to ascertain the relative lipophilic/hydrophilic behavior of the coating system. Optimization was performed by evaluating the adhesive force strength and cohesive force strength of the tablet coat using a texture analyzer. The in vitro release of 5-FU was found to decrease with an increase in (tablet surface-coat) adhesive force strength. The (tablet-tablet) cohesive force strength was reduced by the addition of magnesium silicate to the coating solution. The addition of magnesium silicate (0.2% w/v) to the carboxymethyl Cassia fistula gum-chitosan (CCG-CH) coating surface significantly inhibited the release of 5-FU possibly due to an increase in the hydrophobic character of the coated tablet surface. This was possible by coating cohesive force strength reduction coating compositions (CCG-CH (70:30) and 0.3% magnesium silicate). Further, the FTIR-ATR and DSC analyses suggested the pivotal role of magnesium silicate in modifying the release of 5-FU from CCG-CH-coated tablets due to hydrogen bonding of its Si-O-Si or Mg-O groups with -OH moieties of CCG-CH.
本研究旨在开发和优化一种简单的水性片剂包衣配方及其工艺。 5-氟尿嘧啶(5-FU)用于确定涂层系统的相对亲脂性/亲水性行为。通过使用质构分析仪评估片剂包衣的粘附力强度和内聚强度来进行优化。发现 5-FU 的体外释放随着(片剂表面包衣)粘附力强度的增加而降低。将硅酸镁添加到包衣溶液中会降低(片剂-片剂)内聚力强度。将硅酸镁(0.2%w/v)添加到羧甲基瓜儿豆胶-壳聚糖(CCG-CH)包衣表面可显著抑制 5-FU 的释放,这可能是由于包衣片剂表面疏水性的增加所致。通过降低内聚强度的包衣组合物(CCG-CH(70:30)和 0.3%硅酸镁)可以实现这一点。此外,FTIR-ATR 和 DSC 分析表明,硅酸镁在通过其 Si-O-Si 或 Mg-O 基团与 CCG-CH 的-OH 部分形成氢键来修饰 5-FU 从 CCG-CH 包衣片剂中的释放方面起着关键作用。