Li Ying, Song Yi-qun, He Ya-li, Zhu Chun-yan
Yao Xue Xue Bao. 2016 Jul;51(7):1144-9.
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 P(app) 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 WinNonlin 6.0 software. The results showed that the P(app) 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 C(max) 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.
为研究葛根黄酮生物黏附性漂浮微丸的生物利用度，采用高效液相色谱（HPLC）法，以Caco-2细胞单层模型研究葛根素的吸收情况，比较不同生物黏附材料的葛根黄酮生物黏附性漂浮微丸的表观渗透系数（P(app)）。药物按100 mg·kg(-1)剂量灌胃给药。采用HPLC法测定血浆中葛根素的浓度，并用WinNonlin 6.0软件计算药代动力学参数。结果表明，含羟丙基甲基纤维素（HPMC）-卡波姆的生物黏附性漂浮微丸的P(app)最大，差异有统计学意义（P < 0.05）。葛根黄酮生物黏附性漂浮微丸的AUC(0-t)是葛根黄酮的1.79倍，葛根黄酮生物黏附性漂浮微丸与葛根黄酮的C(max)差异有统计学意义（P < 0.05）。此外，平均滞留时间（MRT）延长。综上所述，含HPMC-卡波姆的葛根黄酮生物黏附性漂浮微丸能显著促进葛根素在Caco-2细胞单层上的转运。含HPMC-卡波姆的葛根黄酮生物黏附性漂浮微丸的生物利用度比葛根黄酮提高，且具有缓释作用。
