| Oral medications is the most common administration of drug therapy. As its primary absorption sites is the small intestine,the intestinal absorption played an important barrier for drugs entering into the systemic. Baicalin is the active ingredients of the traditional Chinese medicine,baicalensis, which has a wide range of pharmacological activities,such as antioxidant, antibacterial, antiviral, anti-radiation, anti-tumor. Recent study of baicalin on scavenging free radical and antioxidant effects, can be used for treatment of ischemic cerebral vascular diseases. Oral preparations of currently market have baicalin mainly as the main ingredient, and bioavailability is not ideal. In previous studies,we made baicalin into baicalin-Phospholipid to improve its fat-soluble and water-soluble.Understanding and comparison of baicalin and baicalin-Phospholipid in oral absorption and pharmacokinetics is of great significance for oral preparation used for clinical research preparation of baicalin in gastrointestinal fluid blank lower gastrointestinal absorption, metabolism and uptake of baicalin nothing rational.First part of the paper used single-pass intestinal perfusion to comparise the rat gastrointestinal absorption characteristics of baicalin (BG), of baicalin-Phospholipid (BP), as well as a physical mixture of both (B+P).The result showed all simples have a certain degree of absorption in the stomach, but the absorption rate of each hour is not significantly different. In vivo experiment of single-pass intestinal perfusion, the absorption of baicalin-phospholipid complex showed a distinct advantage, with its accumulated uptake is2940.87μg, physical mixture is1373.23μg, and baicalin is992.66μg. The absorption percent of the three samples is54.67%、26.4%and19.92%,respectively. The absorption of baicalin-phospholipid complex has improved about twice times by baicalin, one time by physical mixture, and the differences has statistics significance, thus baicalin-phospholipid complex can promote the gastrointestinal absorption of baicalin, at the same time, significantly improve the bioavailability of baicalin. Form the each intestinal absorption rate of Baicalin-Phospholipid complex, the highest absorption is the duodenum, followed by the jejunum, ileum and colon.Second part of the paper used animal models to comparise the pharmacokineticsn characteristics of baicalin (BG), baicalin-phospholipid (BP), as well as a physical mixture of both (B+P). After oral administration Baicalin, all the three samples can be seen by the drug curves and can be detected in the blood after30min. The content of each sample is very low in the brain. Acording to blood medicine curves, three samples reached peak at120min, peak concentration of BP is higher than the rest, followed by physical mixture, baicalin.Then,the blood concentration of each samplesr gradually reduced, approached0at480min. According to brain medicine curves, drugs can be transported into brain very soon after absorbing into the blood, but the contents transported into brain tissue is very low, three samples all reached peak at180min. BP has the highest contents in brain tissue than the other two drugs, followed by physical mixture and finally the baicalin. According to the AUC values of the three samples,the order of brain and blood is as follows:BP-blood (1446.72ug),>B+P-blood (1181.13μg)>BG-blood (399.96μg)>BP-brain (135.3μg)>B+P-brain (93.48μg)> BG-brain (64.16μg). The plasma AUC value of BP has improved near3times times by BG,1.15times times by physical mixture; The brain samples AUC value of BP has improved near1.5times times by BG,1.5times times by physical mixture. According the previous study, the oral bioavailability percent of baicalin is only4%-6%.By being made into Phospholipid comples, it can improve to17.38%, and increase the content in brain., which shows infinite potential for the treatment of cerebral ischemic diseases.This paper use t two models to study how to improve utilization of baicalin in vivo, further confirmate of the Phospholipid’s improvion of membrane permeability and baicalin complex can improve bioavailability. The results of this paperhas results great significance.for research of selecting for dosage forms, process design, formulation and so on... |
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