SBA-15增溶非洛地平的双层渗透泵片的制备

发布时间：2018-06-05 16:50

本文选题：非洛地平 + SBA-　；参考：《中国新药杂志》2016年07期

【摘要】：目的:用介孔材料SBA-15改善非洛地平(felodipine,FDP)的水溶性,并结合双层渗透泵技术控制药物的释放。方法:通过溶剂挥发法将FDP载入SBA-15介孔孔道中制备固体分散体(FDP-SBA-15)。使用透射电镜观察SBA-15的形态结构,采用差示扫描量热法(differential scanning calorimetry,DSC),X射线衍射法(X-ray diffraction,XRD)和傅里叶红外光谱法(Fourier transform infrared spectroscopy,FTIR)表征药物在介孔孔道中的存在状态。利用溶出试验考察SBA-15对FDP的增溶能力和双层渗透泵片的体外释放度。通过高相液相色谱法(HPLC)测得双层渗透泵片和市售缓释片在体内药动学参数。结果:SBA-15能显著抑制药物结晶度,使药物以无定型形式存在。溶出试验表明SBA-15明显提高了FDP的溶出速率,双层渗透泵技术有效地控制了药物释放。体内试验表明自制的双层渗透泵片的口服生物利用度明显提高。结论:固体分散体与双层渗透泵技术联合在有效改善难溶性药物水溶性的同时,控制药物释放,提高口服吸收。
[Abstract]:Aim: to improve the water solubility of felodipine (felodipine) with mesoporous material SBA-15 and to control the drug release by double osmotic pump. Methods: FDP was loaded into SBA-15 mesoporous channel by solvent volatilization to prepare the solid dispersion, FDP-SBA-15. The morphology and structure of SBA-15 were observed by transmission electron microscope (TEM). The existence of SBA-15 in mesoporous channels was characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD) and Fourier transform infrared spectroscopy (FTIR). The solubilization ability of SBA-15 to FDP and the in vitro release of double-layer osmotic pump tablets were investigated by dissolution test. The pharmacokinetic parameters of double-layer osmotic pump tablets and commercial sustained-release tablets were measured by high phase liquid chromatography (HPLC). Results: 1: SBA-15 could significantly inhibit the crystallinity of the drug and make the drug exist in an amorphous form. The dissolution test showed that SBA-15 significantly increased the dissolution rate of FDP, and the double-layer osmotic pump technology effectively controlled the drug release. In vivo tests showed that the oral bioavailability of self-made double-layer osmotic pump tablets was significantly improved. Conclusion: the combination of solid dispersion and double-layer osmotic pump can effectively improve the water solubility of insoluble drugs, control drug release and increase oral absorption.
【作者单位】：辽宁医学院;
【基金】：校长基金-奥鸿博泽基金-医药创新专项(XZJJ20130104-07)
【分类号】：R943

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