玳玳黄酮自微乳化软胶囊剂在SD大鼠体内的药动学比较

目的： 考察比较玳玳黄酮自微乳化软胶囊、玳玳黄酮有效部位及普通硬胶囊在SD大鼠体内的药代动力学和口服生物利用度。 方法： SD大鼠分别灌胃玳玳黄酮有效部位、玳玳黄酮普通硬胶囊和玳玳黄酮自微乳化软胶囊，选择玳玳黄酮有效部位主要药效成分柚皮苷和新橙皮苷为评价指标，采用UPLC-MS/MS联用色谱法，同时测定大鼠血浆中柚皮苷与新橙皮苷的浓度。用DAS 3.0药动学软件处理血药浓度数据，用SPSS统计软件独立样本t检验对所得的药动学数据进行显著性差异分析。 结果： 采用非房室模型分析方法，分别给药玳玳黄酮有效部位与普通硬胶囊后，C_max、AUC_（0-∞）无显著性差异（P > 0.05），而给药自微乳化软胶囊后，C_max、AUC_（0-∞）显著增加（P<0.05）。 结论： 与玳玳黄酮有效部位及其普通硬胶囊相比，玳玳黄酮自微乳化软胶囊可以提高玳玳黄酮的口服生物利用度。

Objective: To research the pharmacokinetics and oral bioavailability of the effective parts of Daidai flavones,Daidai flavones hard capsule and Daidai flavones self-microemulsifying(SME) soft capsule in SD rats. Methods: SD rats were intragastrically administrated with the effective parts of Daidai flavones,Daidai flavones hard capsule and Daidai flavones SME soft capsule.The concentrations of naringin and neohesperidin in plasma,which were the index components of the effective parts of Daidai flavones,were measured by UPLC-MS chromatography.Blood concentration data were processed using DAS 3.0 pharmacokinetic software and the pharmacokinetic data were analyzed using SPSS statistical software. Results: Noncompartmental analysis was carried out after oral administration of the effective parts of Daidai flavones,Daidai flavones hard capsule and Daidai flavones SME soft capsule.C_max and AUC_(0-∞) of the effective parts of Daidai flavones,hard capsule had no significant difference (P > 0.05),whereas C_max and AUC_(0-∞) of Daidai flavones SME soft capsule showed a significant increase (P<0.05). Conclusion: Compared with the effective parts of Daidai flavones and the hard capsule,Daidai flavones SME soft capsule can improve oral bioavailability of Daidai flavones.