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番茄红素-泊洛沙姆188固体分散体的制备及溶出度和生物利用度研究

Preparation,dissolution and bioavailability of lycopene-Poloxamer 188 solid dispersion

  • 摘要: 目的 : 采用固体分散体技术,提高番茄红素在水中的溶解度和体外溶出度,从而提高其体内的生物利用度。 方法 : 以泊洛沙姆188为载体,溶剂法制备番茄红素固体分散体,应用光谱分析和DSC考察其分散特征,溶出度试验测定其体外溶出度,大鼠灌胃后测定其体内生物利用度,用HPLC法测定血药浓度,采用Kinetica软件计算药动学参数。 结果 : 番茄红素可能以分子复合物状态存在于固体分散体中,且显著提高了番茄红素的溶出度,与市售番茄红素油混悬液为对照,其相对生物利用度为(312.2±96.9)%。 结论 : 番茄红素-泊洛沙姆188固体分散体制备工艺简单,成本较低,能显著改善难溶性药物番茄红素的生物利用度,具有较好的实际应用价值。

     

    Abstract: Aim :To improve the solubility,dissolution and bioavailability of lycopene by preparing lycopene solid dispersion. Methods :Lycopene solid dispersion was prepared by the solvent method using Poloxamer 188 as carrier.The physicochemical characteristics of the dispersion were determined by DSC,ultraviolet-visible spectra and the Dissolution Apparatus II(Paddle).The oral bioavailability of lycopene was estimated in rat after oral dosing of lycopene solid dispersion or oil preparation.The plasma concentrations of lycopene in rats were determined by HPLC.The pharmacokinetic parameters were estimated by Kinetica software package. ResultsIn vitro dissolution of lycopene solid dispersion was greater than those of lycopene(raw material),and the physical mixture of lycopene and Poloxamer 188,partly due to the existing molecular state of lycopene in the dispersion.It was also found that the relative bioavailability of lycopene solid dispersion to lycopene oil preparation was (312.2±96.9)%. The optimal ratio of lycopene to carrier in the dispersion was about 1∶5. Conclusion :Lycopene-Poloxamer 188 solid dispersion could be prepared by the proposed simple,low-costly procedure resulting in improved bioavailability of lycopene,which is worthy of further development.

     

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