中国中药杂志

2019, v.44(15) 3305-3311

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HPMCAS/姜黄素无定型态固体分散体增强姜黄素的溶出和化学稳定性
Effect of HPMCAS/curcumin amorphous solid dispersion in enhancing dissolution and chemical stability of curcumin

梁淇;王一茹;邓月义;
LIANG Qi;WANG Yi-ru;DENG Yue-yi;College of Pharmacy,Guilin Medical University;

摘要(Abstract):

制备姜黄素(curcumin,Cur)无定型态固体分散体,从而提高Cur的体外溶出度。通过超饱和测试考察醋酸羟丙基甲基纤维素琥珀酸酯(HPMCAS-HF,HPMCAS-MF,HPMCAS-LF分别简称为HF,MF,LF)和聚乙烯吡咯烷酮PVPK30 (K30)维持Cur超饱和溶液的能力。采用溶剂法制备Cur的无定型态固体分散体。运用差示扫描量热法(DSC)和红外光谱(IR)对Cur固体分散体进行表征,并对其体外溶出效果进行考察。DSC和红外结果表明在1∶3和1∶9 Cur固体分散体中Cur均以无定型态分散于载体中,药物与载体之间存在相互作用。超饱和测试表明高分子抑制Cur结晶的能力顺序为MF>HF>LF>K30。溶出结果显示,Cur-K30无定型态固体分散体药物释放率最高; Cur-K30和Cur-LF无定型态固体分散体的溶出速率较快但不稳定,4 h后药物浓度都呈现下降趋势; Cur-MF和Cur-HF固体分散体的溶出度较低,但溶出稳定增加,这与其强的结晶抑制能力有关。HPMC-AS比K30更能抑制Cur的降解,其中MF和HF抑制效果更好。制备的Cur无定型态固体分散体显著地增强了Cur的溶出,提高了Cur的化学稳定性。该研究结果可为Cur固体分散体高分子载体的合理选择提供依据。
To enhance in vitro dissolution of Cur by preparing Cur solid dispersions. The ability of HPMCAS-HF,HPMCAS-MF,HPMCAS-LF and PVPK30 to maintain supersaturated solution was investigated by supersaturation test. Amorphous solid dispersions were prepared by the solvent-evaporation method. The prepared samples were characterized using infrared spectroscopy( IR) and differential scanning calorimetry( DSC),and in vitro dissolution was investigated. DSC and IR results showed that in 1 ∶3 and 1 ∶9 solid dispersions,Cur was amorphously dispersed in the carrier,and the interaction existed between drug and carrier. The supersaturation test showed that the order of the ability of polymer to inhibit crystallization of Cur was MF>HF>LF>K30. The dissolution results showed that Cur-K30 amorphous solid dispersion had the highest drug release rate; Cur-K30 and Cur-LF amorphous solid dispersions had a quicker but not stable dissolution rate,and the drug concentration decrease after 4 h; Cur-MF and Cur-HF solid dispersions had a low dissolution,which however increased steadily,attributing to the strong ability of the polymers to inhibit the crystallization of Cur. HPMCAS could inhibit the degradation of Cur better than K30,especially MF and HF. The amorphous solid dispersions of cur significantly enhanced the dissolution of Cur and improved the chemical stability of Cur. This study can provide a basis for the rational selection of the polymer used for Cur solid dispersion.

关键词(KeyWords): 姜黄素;无定型固体分散体;稳定性;体外溶出
curcumin;amorphous solid dispersion;stability;in vitro dissolution

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基金项目(Foundation): 广西壮族自治区自然科学基金项目(2014GXNSFBA118052,2016GXNSFAA380266)

作者(Author): 梁淇;王一茹;邓月义;
LIANG Qi;WANG Yi-ru;DENG Yue-yi;College of Pharmacy,Guilin Medical University;

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