| 摘要: |
| 目的 比较去甲氧基姜黄素羟丙基-β-环糊精磷脂复合物、去甲氧基姜黄素羟丙基-β-环糊精包合物、去甲氧基姜黄素磷脂复合物、去甲氧基姜黄素原料药在大鼠体内的药代学性质,探讨去甲氧基姜黄素羟丙基-β-环糊精磷脂复合物作为药物载体的优势。 方法 SD大鼠灌胃给药50 mg/mL(以去甲氧基姜黄素原料药计)剂量制剂及游离药物后,分别于5 min、10 min、15 min、30 min、45 min、1 h、1.5 h、2 h、3 h、4 h、6 h、8 h、10 h、12 h、1 d、2 d、3 d在大鼠眼底静脉丛取血。采用高效液相法测定血浆中去甲氧基姜黄素的浓度。 结果 去甲氧基姜黄素羟丙基-β-环糊精磷脂复合物的AUC0-∞ (μg·L-1·h)为(1 424.87±258.62),较原料药去甲氧基姜黄素(370.58±2.76)、去甲氧基姜黄素磷脂复合物(716.17±123.18)、去甲氧基姜黄素羟丙基-β-环糊精包合物(1 009.35±138.64)均有提高(P<0.01或P<0.05)。 结论 去甲氧基姜黄素羟丙基-β-环糊精磷脂复合物较单一的磷脂复合物或羟丙基-β-环糊精包合物更能促进药物的吸收,有利于提高药物的生物利用度。 |
| 关键词: 去甲氧基姜黄素 去甲氧基姜黄素羟丙基-β-环糊精磷脂复合物 药代动力学 |
| DOI：10.3724/SP.J.1008.2015.1225 |
| 投稿时间：2015-03-04修订日期：2015-05-22 |
| 基金项目:重庆市科学技术委员会资助项目(CSTC2012JJB10027). |
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| Pharmacokinetics study of deme-thoxycurcumin hydroxypropyl-β-cyclodextrin phospholipid complex in rats |
| LUO Jian-chun,LI Na,HU Xue-yuan,ZHAO De-zhang,ZHANG Jing-qing* |
(Medicine Engineering Research Center, Chongqing Medical University, Chongqing 400016, China
*Corresponding author.) |
| Abstract: |
| Objective To compare the pharmacokinetics of deme-thoxycurcumin hydroxypropyl-β-cyclodextrin phospholipid complex, deme-thoxycurcumin hydroxypropyl-β-cyclodextrin, deme-thoxycurcumin phospholipid complex and deme-thoxycurcumin in rats in vivo, so as to discuss the advantages of hydroxypropyl-β-cyclodextrin phospholipid complex as drug carrier. Methods SD rats were gavaged with the preparations and free drug at 50 mg/mL (dose according to deme-thoxycurcumin). Then, blood samples were drawn from rat retinal venous plexus at 5 min, 10 min, 15 min, 30 min, 45 min, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 10 h, 12 h, 1 d, 2 d and 3 d. And the deme-thoxycurcumin concentrations in blood were determined by HPLC. Results The AUC0-∞ of deme-thoxycurcumin hydroxypropyl-β-cyclodextrin phospholipid complex was (1 424.87±258.62) μg·L-1·h, which was higher than that of deme-thoxycurcumin (370.58±2.76) μg·L-1·h, deme-thoxycurcumin phospholipid complex (716.17±123.18) μg·L-1·h and deme-thoxycurcumin hydroxypropyl-β-cyclodextrin (1 009.35±138.64) μg·L-1·h, being 3.84, 1.98, and 1.41 folds of deme-thoxycurcumin, deme-thoxycurcumin phospholipid complex and deme-thoxycurcumin hydroxypropyl-β-cyclodextrin, respectively (P<0.01 or P<0.05). Conclusion The deme-thoxycurcumin hydroxypropyl-β-cyclodextrin phospholipid complex has a better absorption property than deme-thoxycurcumin phospholipid complex and deme-thoxycurcumin hydroxypropyl-β-cyclodextrin, which can help to improve the bioavailability. |
| Key words: deme-thoxycurcumin deme-thoxycurcumin hydroxypropyl-β-cyclodextrin phospholipid complex pharmacokinetics |
