School of Pharmacy, Shanghai Jiao Tong University, Dongchuan Road, People's Republic of China.
Int J Nanomedicine. 2011;6:1237-43. doi: 10.2147/IJN.S20903. Epub 2011 Jun 20.
The effect of eugenol on colchicine transport across an isolated rat intestinal membrane was studied using an in vitro diffusion chamber system. We found that eugenol increased the absorptive transport of the drug efficiently. The effect of eugenol on intestinal absorption of colchicine in an oral administrative nanoemulsion formulation was also demonstrated in vivo. The colchicine nanoemulsion was prepared with isopropyl myristate, eugenol, Tween80, ethanol and water, and eugenol was used as an oil phase in the formulation; an average particle size of this nanoemulsion was 41.2 ± 7.2 nm. The permeation of colchicine in the nanoemulsion across the intestinal membrane was significantly different from that of the control group (0.2 mM colchicine). Finally, co-administration of eugenol in colchicine nanoemulsion to enhance the colchicine bioavailability was investigated by an oral administration method. After oral administration of colchicine (8 mg/kg) in the form of either the nanoemulsion or in free colchicine solution, the relative bioavailability of nanoemulsion and eugenol-nanoemulsion were enhanced by about 1.6- and 2.1-fold, respectively, compared with free colchicine solution. The procedure indicated that the intestinal absorption of colchicine was enhanced significantly by eugenol in the tested nanoemulsion. All the results suggested that eugenol is an efficient component in an oral administrative formulation for improving the intestinal absorption of colchicine.
我们使用体外扩散室系统研究了丁香酚对秋水仙碱跨大鼠肠膜转运的影响。结果发现，丁香酚能有效地促进药物的吸收转运。体内实验也证明了丁香酚在口服 administration 纳米乳剂配方中对秋水仙碱肠吸收的影响。秋水仙碱纳米乳剂由肉豆蔻酸异丙酯、丁香酚、吐温 80、乙醇和水制成，丁香酚用作配方中的油相；该纳米乳剂的平均粒径为 41.2±7.2nm。秋水仙碱在纳米乳剂中的渗透穿过肠膜与对照组（0.2mM 秋水仙碱）有显著差异。最后，通过口服给药方法研究了丁香酚在秋水仙碱纳米乳剂中的共同给药以增强秋水仙碱生物利用度。以纳米乳剂或游离秋水仙碱溶液的形式口服给予秋水仙碱（8mg/kg）后，纳米乳剂和丁香酚纳米乳剂的相对生物利用度分别比游离秋水仙碱溶液提高了约 1.6 倍和 2.1 倍。该过程表明，丁香酚在测试的纳米乳剂中显著增强了秋水仙碱的肠吸收。所有结果表明，丁香酚是提高秋水仙碱肠内吸收的口服 administration 制剂中的有效成分。
