AIM: To provide primarily pharmacokinetic profiles and reveal potentially pharmacological components after oral administration of the extractum for Compund Danshen Dripping Pill (CDDP) in rats, which was mainly compos...AIM: To provide primarily pharmacokinetic profiles and reveal potentially pharmacological components after oral administration of the extractum for Compund Danshen Dripping Pill (CDDP) in rats, which was mainly composed of protocatechuic aldehyde (PAL), Danshensu (DSS), lithospermic acid A, lithospermic acid B, salvianolic acid D, rosmarinic acid, salvianolic acid B and salvianolic acid A. METHODS: After orally administration of 200 mg CDDP extractum for 1 h, the portal vein blood, the femoral artery blood, the bile and urine samples were separately collected. The gastrointestinal (GI) contents and mucosa were washed with physiological saline and the washing solution was pooled. The whole GI tract was removed and homogenized for analysis. The constituents and concentrations of all above samples were determined by the LC-MS analysis combined with the β-glucuronidase and sulfatase treatment. RESULTS: The investigation after oral administration of CDDP extractum for 1 h in rats indicated that: (1)Most of polyphenolic acids have been degraded into caffeic acid (CA) and DSS in the GI tract. Next, CA could be easily absorbed into blood circulation and a trace of DSS was also transported into the portal vein. The remains of undegraded polyphenolic acids and Danshensu were detained in the GI tract lumen. (2)Part of PAL was firstly oxidized into PAC in GI epithelial cells before absorption into the portal vein. Next, PAC and the rest PAL were further transported into blood circulation. (3)PAC and PAL were distributed in blood circulation in free and conjugated forms after being glucuronidated in the liver and the kidney while only free CA and DSS appeared in vivo. After that, all of these metabolites were gradually secreted into bile and urine. CONCLUSION: The results suggest that DSS, PAL, PAC, CA and their conjugated forms may be potential pharmacological components for CDDP extractum.展开更多
文摘AIM: To provide primarily pharmacokinetic profiles and reveal potentially pharmacological components after oral administration of the extractum for Compund Danshen Dripping Pill (CDDP) in rats, which was mainly composed of protocatechuic aldehyde (PAL), Danshensu (DSS), lithospermic acid A, lithospermic acid B, salvianolic acid D, rosmarinic acid, salvianolic acid B and salvianolic acid A. METHODS: After orally administration of 200 mg CDDP extractum for 1 h, the portal vein blood, the femoral artery blood, the bile and urine samples were separately collected. The gastrointestinal (GI) contents and mucosa were washed with physiological saline and the washing solution was pooled. The whole GI tract was removed and homogenized for analysis. The constituents and concentrations of all above samples were determined by the LC-MS analysis combined with the β-glucuronidase and sulfatase treatment. RESULTS: The investigation after oral administration of CDDP extractum for 1 h in rats indicated that: (1)Most of polyphenolic acids have been degraded into caffeic acid (CA) and DSS in the GI tract. Next, CA could be easily absorbed into blood circulation and a trace of DSS was also transported into the portal vein. The remains of undegraded polyphenolic acids and Danshensu were detained in the GI tract lumen. (2)Part of PAL was firstly oxidized into PAC in GI epithelial cells before absorption into the portal vein. Next, PAC and the rest PAL were further transported into blood circulation. (3)PAC and PAL were distributed in blood circulation in free and conjugated forms after being glucuronidated in the liver and the kidney while only free CA and DSS appeared in vivo. After that, all of these metabolites were gradually secreted into bile and urine. CONCLUSION: The results suggest that DSS, PAL, PAC, CA and their conjugated forms may be potential pharmacological components for CDDP extractum.
