Tros de Ilarduya M C, Martín C, Goñi M M, Martínez-Ohárriz M C
Department of Pharmacy and Pharmaceutical Technology, School of Pharmacy, University of Navarra, Pamplona, Spain.
Drug Dev Ind Pharm. 1998 Mar;24(3):295-300. doi: 10.3109/03639049809085623.
In this report the interactions of sulindac with polyvinylpyrrolidone K30 (PVP K30), both in the solid state and in aqueous solution, have been investigated. Solid dispersions of sulindac with PVP K30 were prepared by the solvent method in ethanol from various drug-to-polymer weight ratios. X-ray powder diffraction and differential scanning calorimetry have shown that PVP inhibits the crystallization of sulindac. The stabilization of the noncrystalline state of sulindac was shown by x-ray diffractometry after a 1-year storage. There was a considerable increase in the release rate of the drug when the polymer content was increased and the intrinsic dissolution rate values of these systems were calculated. From the UV spectra a bathochromic shift and a well-defined isosbestic point were observed at pH 2 and 6, which confirmed an interaction between the drug and the polymer in solution. Moreover, the apparent solubility of sulindac has been modified as a function of the polymer concentrations. The binding process between the drug and PVP was exothermic from the stability constant values at 25, 30, and 37 degrees C at pH 2.
在本报告中，研究了舒林酸与聚乙烯吡咯烷酮K30（PVP K30）在固态和水溶液中的相互作用。通过溶剂法在乙醇中以不同的药物与聚合物重量比制备了舒林酸与PVP K30的固体分散体。X射线粉末衍射和差示扫描量热法表明，PVP抑制舒林酸的结晶。储存1年后，通过X射线衍射法显示舒林酸非晶态的稳定性。当聚合物含量增加时，药物释放速率显著增加，并计算了这些体系的固有溶解速率值。从紫外光谱中，在pH 2和6时观察到红移和明确的等吸收点，这证实了溶液中药物与聚合物之间的相互作用。此外，舒林酸的表观溶解度已根据聚合物浓度进行了调整。在pH 2时，根据25、30和37℃下的稳定常数，药物与PVP之间的结合过程是放热的。
