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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 transport of Pueraria total flavonoids bioadhesive floating pellets in Caco-2 cell model and the bioavailability in rats. The Caco-2 cell model was used to determine the content of puerarin in the transfused liquid by HPLC. The similarities and differences of the apparent permeability coefficient P_app of the bioadhesive buoyant pellets with different bioadhesive materials were compared. SD rats were orally administered Pueraria total flavonoids Pueraria total flavonoids bioadhesive floating pellets (100 mg · kg-1, puerarin dollars), HPLC determination of puerarin plasma concentration, draw the drug-time curve and calculate the pharmacokinetic Learning parameters. The results showed that the P_app of bioadhesive buoyancy pellets prepared with hydroxypropyl methylcellulose (HPMC) and carbomer was the largest, the difference was significant (P <0.05). Pueraria total flavonoids bioadhesive floating pellets under the curve area (AUC0-t) 1.79 times the bulk drug; peak mass concentration of 6.39μg · m L -1, compared with the bulk drug (3.65μg · m L ~ ( -1)), with significant difference (P <0.05); the average residence time in vivo was prolonged. The results showed that the combination of HPMC and carbomer adhesion material to promote Caco-2 Pueraria total flavonoids transmembrane transport the best, Pueraria total flavonoids bioadhesive floating pellets (HPMC and carbomer combination) compared with the total Pueraria lobata API Degree is higher, and has slow release effect.