Division of Pharmaceutical Sciences, Arnold and Marie Schwartz College of Pharmacy and Health Sciences, 75 Dekalb Avenue, HS Building 605, Brooklyn, NY 11201, USA.
AAPS PharmSciTech. 2013 Jun;14(2):620-8. doi: 10.1208/s12249-013-9947-z. Epub 2013 Mar 15.
Colloidal solid dispersion is an innovative breakthrough in the pharmaceutical industry that overcomes the solubility-related issue of poorly soluble drugs by using an amorphous approach and also the stability-related issue by means of a complex formation phenomenon using different carrier materials. In the present study, a newly developed adsorption method is introduced to incorporate a high-energy sulfathiazole-polyvinylpyrrolidone (Plasdone® K-29/32) solid dispersion on porous silicon dioxide (Syloid® 244FP). Different ternary systems of sulfathiazole-Plasdone® K-29/32-Syloid® 244FP were prepared (1:1:2, 1:1:3, and 1:2:2) and categorized depending on the mechanism by which Syloid® 244FP was incorporated. Modulated differential scanning calorimetry (MDSC), X-ray diffraction, Fourier transform infrared spectroscopy, and in vitro dissolution studies were conducted to characterize the ternary systems. The X-ray diffraction and MDSC data showed a lack of crystallinity in all internal and external ternary systems, suggesting a loss of the crystallinity of sulfathiazole compared to the physical mixtures. USP apparatus II was used to measure the in vitro dissolution rate of the prepared systems at 75 rpm in different media. The dissolution rate of the optimum ratio (1:2:2) containing an internal ternary solid dispersion system was found to be three times higher than that of the external and physical systems. Thus, the porous silicon dioxide incorporated into the conventional binary solid dispersion acted as a carrier to disperse the complex and increase the dissolution rate.
胶态固体分散体是制药行业的一项创新突破,它采用无定形方法克服了难溶性药物的溶解度相关问题,通过使用不同载体材料的络合现象克服了稳定性相关问题。在本研究中,引入了一种新的吸附方法,将高能量的磺胺噻唑-聚乙烯吡咯烷酮(Plasdone® K-29/32)固体分散体结合到多孔二氧化硅(Syloid® 244FP)上。制备了不同的磺胺噻唑-Plasdone® K-29/32-Syloid® 244FP 三元体系(1:1:2、1:1:3 和 1:2:2),并根据 Syloid® 244FP 的加入机制进行了分类。对三元体系进行了调制差示扫描量热法(MDSC)、X 射线衍射、傅里叶变换红外光谱和体外溶解研究。X 射线衍射和 MDSC 数据表明,所有内部和外部三元体系均缺乏结晶度,表明磺胺噻唑的结晶度相对于物理混合物有所损失。采用 USP 仪器 II 在 75 rpm 下在不同介质中测量了制备体系的体外溶解速率。发现含有内部三元固体分散体系统的最佳比例(1:2:2)的溶解速率比外部和物理系统高 3 倍。因此,掺入常规二元固体分散体的多孔二氧化硅起到了载体的作用,分散了复合物并提高了溶解速率。