Mura P, Faucci M T, Manderioli A, Bramanti G, Parrini P
Drug Dev Ind Pharm. 1999 Mar;25(3):257-64. doi: 10.1081/ddc-100102169.
Solid dispersions of 10% w/w naproxen (NAP) in poly(ethylene glycol) (PEG) (4000, 6000, or 20,000) as a carrier with or without incorporation of anionic (sodium dodecyl sulfate; SDS) or nonionic (Tween 80; Tw80) surfactant were prepared by the melting method. Physicochemical characteristics were determined by differential scanning calorimetry (DSC) and X-ray diffraction analysis. The results of dissolution studies showed that drug dissolution properties were better from ternary systems than from binary systems since in the former the wetting and solubilizing effects of surfactant and polymer were additive. No influence of the PEG molecular weight was found. The best performance given by anionic surfactant has been attributed to several factors, such as higher hydrophilicity, better solubilizing power, and most facile interaction with both drug and PEG. No important changes in solid-state characteristics or in drug dissolution properties were found after 30 months storage for dispersions with or without surfactant. Only a slight decrease in initial drug dissolution rate was observed at the highest concentration (10% w/w) of SDS.
采用熔融法制备了10%（w/w）萘普生（NAP）在聚乙二醇（PEG）（4000、6000或20000）中作为载体的固体分散体，载体中添加或不添加阴离子型（十二烷基硫酸钠；SDS）或非离子型（吐温80；Tw80）表面活性剂。通过差示扫描量热法（DSC）和X射线衍射分析确定理化特性。溶出度研究结果表明，三元体系的药物溶出特性优于二元体系，因为在前者中表面活性剂和聚合物的润湿性和增溶作用是相加的。未发现PEG分子量的影响。阴离子表面活性剂表现出的最佳性能归因于几个因素，如更高的亲水性、更好的增溶能力以及与药物和PEG最容易发生的相互作用。对于添加或未添加表面活性剂的分散体，储存30个月后，固态特性或药物溶出特性未发现重要变化。在SDS最高浓度（10% w/w）时，仅观察到初始药物溶出速率略有下降。
