摘要
研究葛根总黄酮生物黏附漂浮微丸在Caco-2细胞模型的转运及大鼠体内生物利用度。采用Caco-2细胞模型,用HPLC测定转运后药液中葛根素含量,比较不同生物黏附材料组成的葛根总黄酮生物黏附漂浮微丸表观穿透系数P_app的异同。SD大鼠分别口服给予葛根总黄酮、葛根总黄酮生物黏附漂浮微丸(100 mg·kg-1,以葛根素计),HPLC法测定葛根素血药浓度,绘制药-时曲线并计算药动学参数。结果表明,以羟丙基甲基纤维素(HPMC)与卡波姆组合材料制备的生物黏附漂浮微丸P_app最大,差异具有显著性(P<0.05)。葛根总黄酮生物黏附漂浮微丸曲线下面积(AUC0-t)为原料药的1.79倍;达峰质量浓度为6.39μg·m L^(-1),较原料药(3.65μg·m L^(-1))高,且具有显著性差异(P<0.05);体内的平均滞留时间延长。研究表明,HPMC与卡波姆组合黏附材料促进葛根总黄酮Caco-2跨膜转运最好,葛根总黄酮生物黏附漂浮微丸(HPMC与卡波姆组合)与葛根总黄酮原料药相比生物利用度更高,且具有缓释效果。
To study the bioavailability of pueraria flavonoids bio-adhesive and floating pellets, the absorption of puerarin was studied using Caco-2 cell monolayer by liquid chromatography（HPLC） method, comparing the Papp of pueraria flavonoids bio-adhesive and floating pellets with different bio-adhesive materials. Drugs were administered at a dose of 100 mg·kg～（-1） via ig. The plasma concentration of puerarin was determined by HPLC, the pharmacokinetics were calculated with the Win Nonlin 6.0 software. The results showed that the Papp of bio-adhesive and floating pellets with hydroxypropyl methylcellulose（HPMC）-cabomer was largest, which had a significant difference（P〈0.05）. The AUC_（0-t） of pueraria flavonoids bio-adhesive and floating pellets was 1.79 times of pueraria flavonoids, the Cmax of pueraria flavonoids bio-adhesive and floating pellets and pueraria flavonoids had a significant difference（P〈0.05）. What＇s more the MRT had prolonged. In conclusion, pueraria flavonoids bio-adhesive and floating pellets with HPMC-cabomer could significantly facilitate the transport of puerarin on Caco-2 cellular monolayers. The bioavailability of pueraria flavonoids bio-adhesive and floating pellets with HPMC-cabomer was increased more than pueraria flavonoids with a sustained release effect.
出处
《药学学报》
CAS
CSCD
北大核心
2016年第7期1144-1149,共6页
Acta Pharmaceutica Sinica
基金
国家自然科学基金资助项目(81274094)
