Zhao Na, Augsburger L L
University of Maryland School of Pharmacy, Baltimore, MD 21201, USA.
Pharm Dev Technol. 2006;11(2):179-85. doi: 10.1080/10837450600561281.
The purpose of this study is to investigate factors influencing croscarmellose sodium functionality with special emphasis on developing a discriminating model tablet formulation to evaluate product brand-to-brand variability. The particle size distribution, water uptake, and swelling properties of five brands of croscarmellose sodium in either neutral water or 0.1 N HCl were studied. Differences were observed in all properties between brands. Media with acidic pH had a negative impact, but to different extents, on both the water uptake and swelling of all croscarmellose sodium brands due to the presence of carboxymethyl sodium substituents. A tablet matrix composed of lactose (75% w/w) and dicalcium phosphate (25% wt/wt) was used to compare the functional equivalency of the five brands of croscarmellose sodium. The tablet disintegration times were inversely proportional to the swelling ability of superdisintegrant in the testing medium regardless of medium temperature and disintegrant concentration. In conclusion; the particle size, total degree of substitution, and the ratio of basic to acidic substituents are important factors that should be considered during product optimization. The tablet matrix composed of lactose and dicalcium phosphate at a weight ratio of 3:1 can be used as a model formulation for product lot-to-lot consistency and product brand-to-brand comparison purposes.
本研究的目的是调查影响交联羧甲基纤维素钠功能的因素，特别着重于开发一种有区分能力的模型片剂配方，以评估不同品牌产品之间的差异。研究了五个品牌的交联羧甲基纤维素钠在中性水或0.1 N盐酸中的粒度分布、吸水性和膨胀特性。各品牌之间在所有特性上均观察到差异。由于存在羧甲基钠取代基，酸性pH介质对所有交联羧甲基纤维素钠品牌的吸水性和膨胀均有负面影响，但程度不同。使用由乳糖（75% w/w）和磷酸氢钙（25% wt/wt）组成的片剂基质来比较五个品牌交联羧甲基纤维素钠的功能等效性。无论介质温度和崩解剂浓度如何，片剂崩解时间与测试介质中超级崩解剂的膨胀能力成反比。总之，粒度、总取代度以及碱性与酸性取代基的比例是产品优化过程中应考虑的重要因素。由乳糖和磷酸氢钙按3:1重量比组成的片剂基质可作为一种模型配方，用于产品批次间一致性和产品品牌间比较。
