RESUMO
Objective: Biopharmaceutics classification system (BCS) of five main pharmacological/toxic components (gallic acid, emodin, stilbene glycoside, physcion, and emodin-8-O-β-D-glucoside) of Polygoni Multiflori Radix Praeparata (PMRP) were carried out. Methods: The solubility and permeability of each representative component were studied by equilibrium solubility method and everted intestinal sac method, respectively. Using two softwares (Pipeline Pilot 7.5, ChemDraw 7.0) to predict the solubility and permeability parameters of each component. Classical BCS classification of measured and predicted values of representative components was conducted according to Food and Drug Administration (FDA) standards, and their correlation was evaluated. Results: The emodin, emodin-8-O-β-D-glucoside, and physcion in PMRP was preliminary determined as BCS IV drugs. THSG and gallic acid belong to BCS III drugs, and permeability was the main limiting factor in their absorption process. There was software which predicts false positives of anthraquinone in BCS classification studies. Conclusion: In this study, five main pharmacodynamic/toxic components of PMRP were classified by BCS method, which provided data support and technical reference for in vivo absorption prediction and in vitro safety evaluation of traditional Chinese medicine.
RESUMO
OBJECTIVE: To study the absorption kinetics of baicalin phospholipid complex in rats stomach and intestine. METHODS: Using rats in vivo stomach and intestinal absorption mode, the drug concentration by in situpefusion in rats were determined by HPLC to comparise the stomach, whole intestine absorption and metabolism characteristics among baicalin, baicalin phospholipid complex and physical mixture, and the sub-bowel absorption and metabolism characteristics of baicalin phospholipid complex. RESULTS: The percentage of per hour absorpion in the stomach of baicalin, baicalin phospholipid complex and physical mixture shows little difference among them. The whole intestine absorption of baicalin phospholipid complex was better than the baicalin and physical mixture, which is (2 940.87±1.45) μg,(1 373.23±3.21) μg, (992.66±3.65) μg, respectively. Baicalin phospholipid complex has extensive absorption window in the whole intestine and duodenum is the best. The absorption percentage of duodenum, jejunum, ileum and colon is 51.81%, 32.29%, 29.56%, 11.80%,respectively. CONCLUSION: Baicalin phospholipid complex can significantly enchance absorption of baicalin in rat gastrointestinal tract.