AIM:To clarify both the character of the absorption and the stability of crocin in various sites along the intestinal tract,and also to determine the partition coefficient of crocin-1 in water/n-caprylic alcohol syste...AIM:To clarify both the character of the absorption and the stability of crocin in various sites along the intestinal tract,and also to determine the partition coefficient of crocin-1 in water/n-caprylic alcohol system. METHOD:The intestinal absorption and stability was investigated using in situ perfusion method in rats; Shaking flask test was used to determine the partition coefficient of crocin-1;Concentration of crocin-1 was detected by HPLC.RESULT:Decrease of Crocin-1 in various intestine segments is as follows:Duodenum 13.81%,Jejunum 9.89%,Ileum 10.07%,and Colon 10.04%,but crocin-1 can’t be found in blood; Degradation of Crocin-1 during incubation in refluxing solution of various intestinal segments is as follows:Duodenum 13.01%,Jejunum 10.11%,Ileum 9.95%,and Colon 10.45%; The partition coefficient of crocin-1 P =0.093±0.004,log P =-1.03±0.02.CONCLUSION:The results suggest that crocin is unstable and can’t be absorbed in the whole intestinal tract.展开更多
The purpose of this study was to quantify the effect of the fatty acid alkyl-chain length of a polyethylene glycol(PEG)glyceryl ester,which was used as a microemulsion oil component,on the partitioning of highly lipop...The purpose of this study was to quantify the effect of the fatty acid alkyl-chain length of a polyethylene glycol(PEG)glyceryl ester,which was used as a microemulsion oil component,on the partitioning of highly lipophilic compounds to the mesenteric lymph after oral administration.Oil blue N,a highly lipophilic anthraquinone derivative,was orally administered to lymph duct-cannulated and untreated rats in two kinds of different microemulsions.Gelucire®50/13 and Gelucire®44/14 were used as the oil component with long chain and medium chain fatty acid portions,respectively,of PEG glyceryl esters in microemulsions.The cumulative amount of oil blue N in lymph fluid was almost the same between the two microemulsions,although the transferred amount of oil component(triglyceride)in the lymph after administration of the Gelucire®50/13 microemulsion was significantly higher than that of the Gelucire®44/14 microemulsion.On the other hand,the solubility of oil blue N in Gelucire®44/14 was much higher than that in Gelucire®50/13.No significant differences were observed between microemulsions in the bioavailability of oil blue N.From these data,the partitioning of oil blue N to the lymph was calculated using a mathematical model,showing that the partitioning ratios of oil blue N to the lymph fluid were almost the same for both microemulsions.The solubility of oil blue N to the oil component of the microemulsions and the transfer of triglycerides to the lymph after administration of the microemulsions counteract each other,leading to similar partitioning ratios of oil blue N to the lymph.展开更多
文摘AIM:To clarify both the character of the absorption and the stability of crocin in various sites along the intestinal tract,and also to determine the partition coefficient of crocin-1 in water/n-caprylic alcohol system. METHOD:The intestinal absorption and stability was investigated using in situ perfusion method in rats; Shaking flask test was used to determine the partition coefficient of crocin-1;Concentration of crocin-1 was detected by HPLC.RESULT:Decrease of Crocin-1 in various intestine segments is as follows:Duodenum 13.81%,Jejunum 9.89%,Ileum 10.07%,and Colon 10.04%,but crocin-1 can’t be found in blood; Degradation of Crocin-1 during incubation in refluxing solution of various intestinal segments is as follows:Duodenum 13.01%,Jejunum 10.11%,Ileum 9.95%,and Colon 10.45%; The partition coefficient of crocin-1 P =0.093±0.004,log P =-1.03±0.02.CONCLUSION:The results suggest that crocin is unstable and can’t be absorbed in the whole intestinal tract.
文摘The purpose of this study was to quantify the effect of the fatty acid alkyl-chain length of a polyethylene glycol(PEG)glyceryl ester,which was used as a microemulsion oil component,on the partitioning of highly lipophilic compounds to the mesenteric lymph after oral administration.Oil blue N,a highly lipophilic anthraquinone derivative,was orally administered to lymph duct-cannulated and untreated rats in two kinds of different microemulsions.Gelucire®50/13 and Gelucire®44/14 were used as the oil component with long chain and medium chain fatty acid portions,respectively,of PEG glyceryl esters in microemulsions.The cumulative amount of oil blue N in lymph fluid was almost the same between the two microemulsions,although the transferred amount of oil component(triglyceride)in the lymph after administration of the Gelucire®50/13 microemulsion was significantly higher than that of the Gelucire®44/14 microemulsion.On the other hand,the solubility of oil blue N in Gelucire®44/14 was much higher than that in Gelucire®50/13.No significant differences were observed between microemulsions in the bioavailability of oil blue N.From these data,the partitioning of oil blue N to the lymph was calculated using a mathematical model,showing that the partitioning ratios of oil blue N to the lymph fluid were almost the same for both microemulsions.The solubility of oil blue N to the oil component of the microemulsions and the transfer of triglycerides to the lymph after administration of the microemulsions counteract each other,leading to similar partitioning ratios of oil blue N to the lymph.
