ABSTRACT
Objective To study the intestinal absorption characteristics of demethoxycurcumin hydroxypropyl/β cyclodcxtrin (DECD) and demethoxycurcumin (DE) in rats. Methods DECD was prepared by cyclodcxtrin inclusion technique and characterized by spectroscopic method. The morphology of DECD was observed by microphotograph and zeta potential was examined by Malvern laser particle sizer. In vivo single-pass intestinal perfusion rat model was adopted; the absorption rate constant (Ka), effective permeability (Papp) and percent absorption of DECD and DE were determined using the ultraviolet spectrophotometry. Results DECD was successfully prepared, with a solubility of 2. 30 g/L, which was 38. 33 times that of DE. Zeta potential of DECD was —32. 2 mV. The results of intestinal absorption experiment showed that the Ka and Papp values of DECD decreased in order in the ileum, duodenum, jejunum, and colon. In addition, the Ka, Papp values and percent absorption of DECD were higher than that of DE. Conclusion DECD can markedly improve the intestinal absorption of DE in rats.
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<.01 or P<.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.
ABSTRACT
Objective: To evaluate the pharmacokinetics of curcumin phospholipid complex (CCPC) in rats following oral administration. Methods: Blood samples were collected from the retinal venous plexus of SD rats after oral administration of CCPC or curcumin (CC), and the blood concentration of curcumin was determined by high-performance liquid chromatography (HPLC). Results: The solubility and cumulative dissolution of CCPC (0.150 g/L and 68.04%, respectively) were higher than those of CC (0.057 g/L and 50.68%, respectively). The pharmacokinetic parameter of CCPC and CC were calculated as follows: Cmax (74.34±5.57) μg/L and (61.64±4.29) μg/L, Tmax (0.17±0) h and (0.25±0) h, AUC0-t (637.38±30.04) μg·h·L-1 and (172.41±31.66) μg·h·L-1, and AUC0-∞ (857.80±223.69) μg·h·L-1 and (191.08±43.27) μg·h·L-1, respectively. The intra-day, inter-day precision, and recovery rate met the criteria for content determination. Conclusion: Compared with curcumin, CCPC can be absorbed more rapidly and eliminated more slowly.