ABSTRACT
The intestinal absorption properties of the main effective components (glycyrrhizic acid, isoliquiritigenin, 6-gingerol, ginsenoside Rb1, atractylode-I) in Lizhong decoction (LZD) extracts were investigated with an in situ single-pass intestinal perfusion model in rats. UPLC-TQ-MS was used to determine the concentration of the five components in the intestinal perfusion. Animal welfare and experimental procedures were in accordance with the regulations of the Animal Ethics Committee of Nanjing University of Chinese Medicine. As evaluation indexes for the intestinal absorption characteristics, the absorption rate constant (Ka) and the apparent permeability coefficient (Peff) of the five main ingredients were analyzed. Results showed that the best absorption sites for glycyrrhizic acid, isoliquiritin and 6-gingerol were the ileum, colon and duodenum, respectively, and the differences between different intestinal segments were statistically significant (P <0.05). There was no notable difference in Ka and Peff between ginsenoside Rb1 and atractylode-I in the different intestinal segments (P > 0.05), suggesting that they were absorbed throughout. The five components were well-absorbed in the whole intestine (Peff > 1.0×10-3 cm·min-1), indicating that LZD is suitable for preparing sustained, controlled release and enteric-coated preparations.
ABSTRACT
Background: The present study was done to assess the blood loss during delivery even after active management of third stage of labor with oxytocin and the maternal outcomes of PPH.Methods: We studied 100 pregnant women were either in spontaneous labor or admitted for induction of labor, underwent vaginal delivery or caesarean section in our institute. Active management of third stage of labor in all 100 cases included 10 IU intramuscular oxytocin or 10 to 20 IU intravenous in 500 ml of Ringer’s Lactate. Blood loss in all cases was noted.Results: Of the included cases, 27 had to be given extra-uterotonics for atonic uterus, of which 12 parturient still had PPH. Atonic uterus was the cause of PPH in 11 of the 12 cases, while one case was of atonic uterus plus trauma. Half of all PPH cases responded to medical management alone, five cases had to undergo tamponade/stepwise devascularization and one case had to undergo obstetric hysterectomy. Blood loss was significantly higher in women aged more than 35 years, primigravida, not in labor, oligohydramnios or post-datism, elective LSCS, scarred uterus in and had more than 1 high risk factor. Among various high-risk conditions, significantly higher blood loss was observed in patients with chronic hypertension, gestational hypertension, pre-gestational diabetes mellitus, multipara with prior PPH, placenta previa, preeclampsia and sickle cell trait.Conclusions: Fifteen women avoided PPH by using a reliable method of blood loss measurement and initiating interventions early. Organized PPH management protocol morbidity and mortality of the mother and neonate can be prevented.
ABSTRACT
To determine the absorption properties and study the intestinal absorption kinetics of poncidin in rats. In situ single pass perfusion model was combined with High Performance Liquid Chromatography-Mass Spectrometry (HPLC-MS/MS) method to investigate the intestinal absorption characteristics and calculate absorption parameters with aspects of drug absorption, concentration and perfusion medium. The absorption of poncidin under acid condition at pH 6.5 was more stable, where intestinal enzymes showed little influence on metabolism, and the absorption was significantly higher than that in pH alkaline condition at pH 8.0 (<0.05). Drug concentrations had no significant influence on absorption rate constant of the same intestinal segment Ka and apparent permeability coefficient Papp values of poncidin. Different concentrations of poncidin showed no significant differences in the Ka and Papp values among duodenum, jejunum and colon, but the values were significantly lower than ileum absorption parameters, with significant differences (<0.05). There was no significant effect of verapamil on intestinal absorption of poncidin. The results showed that poncidin could be absorbed at all the studied intestinal segments while ileum seemed to be the best absorption segment in the concentration range of 10-1 000 μg·L⁻¹. The absorption was characterized by a linear dynamic process of passive transport, without absorption saturation. Weak acid environment was helpful for the intestinal absorption of poncidin, and ponicidin was not a substrate of P-glycoprotein (P-gp).
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To study the effects of compound Longmaining(FFLMN) with different combinations on the intestinal absorption of puerarin. The rat single pass intestinal perfusion model was adopted, and the concentration of puerarin in intestinal samples was determined by HPLC. The effects of different combination groups on the absorption of puerarin in duodenum, jejunum, ileum and colon were investigated. The combined drugs were GG(Puerariae Lobatae Radix), GG-CSL (Puerariae Lobatae Radix compared with Dioscoreae Nipponicae Rhizoma), GG-CX(Puerariae Lobatae Radix compared with Chuanxiong Rhizoma) and FFLMN (compound Longmaining). We found that the absorption rate constant(Ka) and the apparent coefficient(Papp) of puerarin had no significant difference between GG-CSL and FFLMN groups, but significantly higher in GG and GG-CX groups(P<0.05) in the duodenum and ileum. In jejunum and colon, Ka and Papp of puerarin showed significant differences between GG and other groups(P<0.05). At the same time, FFLMN also had significant differences with GG-CSL and GG-CX groups(P<0.05). The results showed that in the whole intestine of rats, FFLMN could significantly promote the absorption of puerarin. In the duodenum and ileum, Dioscoreae Nipponicae Rhizoma played a significant role in promoting absorption of puerarin. In jejunum and colon, Dioscoreae Nipponicae Rhizoma and Chuanxiong Rhizoma have a synergistic effect in promoting absorption of puerarin.
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Objective: To study the rat intestinal absorption characteristic of puerarin loaded O-carboxymethyl chitosan (CMCS) microspheres in situ. Methods: Single-pass intestinal perfusion (SPIP) model was used for rat in situ and HPLC to determine the concentration of puerarin. The effects of different perfusion rate, drug concentration, and intestinal segments on intestinal absorption were investigated, and the absorption characteristics of the puerarin and puerarin loaded O-CMCS microspheres were compared. Results: Perfusion rate had significant effect on the absorption rate constants (Ka) and the apparent absorption coefficient (Papp) (P 0.05); Ka and Papp of drug loaded microspheres in jejunum and ileum showed no significant difference, but they were significantly higher than that in duodenum (P < 0.05); The drug loaded microspheres and puerarin had the significant difference in Ka and Papp in jejunum (P < 0.05). Conclusion: The absorption mechanism of puerarin in the microspheres is passive diffusion, puerarin is absorbed well in jejunum and ileum, and puerarin loaded O-CMCS microspheres can significantly improve the absorption of puerarin.
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OBJECTIVE: To study the in situ intestinal absorption kinetics of senkyunolide I in rats. METHODS: The absorption of senkyunolide I in four segments of rat intestine was investigated using the in situ single-pass perfusion method, and the drug content was measured by HPLC. The absorption kinetics of senkyunolide I at different segments of intestine, drug concentration, and perfusion medium were studied. RESULTS: Drug concentration had no significant influence on the ka and the P values of senkyunolide I (P≤0.05) in the range of 128.5-514 μg · mL-1 Papp values of senkyunolide 1at duodenum were significantly higher than those atthe other three regions of intestine (P<0.001). But no significant differences in the P value (P≤0.05) were found among jejunum, ileum, and colon. CONCLUSION: The absorption of senkyunolide I complied with linear kinetics in the dose range studied, indicating that its absorption may be mediated mainly by passive transport. Senkyunolide 1could be absorbed at all the studied intestinal segments while duodenum seemed to be the best absorption segment for it.