Pharmacokinetics study of bio-adhesive tablet of Panax notoginseng saponins

Panax notoginseng (Burk.) F.H. Chen is an important traditional Chinese medicine mainly produced in Yunnan, Guangxi and Szechwan in China.Panax notoginseng saponin (PNS), the extract of Panax notoginseng, has been generally studied. PNS possesses many pharmacological active effects, including resistance against cerebral infarction and ischemia by inhibiting apoptosis and expression of caspase-1 and caspase-3 [1,2]; antioxidant property by its strong ferrous ion chelating activity scavenging activities against hydrogen peroxide, hydroxyl radicals, superoxide anion and DPPH free radicals [3]; therapeutic effect on atherosclerosis by lowering serum lipid level and regulating expression of vascular cell differentiation antigen 40 and matrix metalloproteinase 9 [4]. In recent years, increasing attention has been paid to other activities of PNS: neuroprotective activity based on its potent protective effect against blood-brain barrier damage) [5]; anti-hyperglycemic and anti-obese effects by lowering fasting blood glucose levels and improving glucose tolerance [6]; anti-platelet and anti-coagulant effects [7]; anti-inflammatory in vitro properties via blocking NF-κB signaling pathway in macrophages [8]; anti-depressive activity that may be mediated by modulation of brain monoamine neurotransmitters and intracellular Ca2+ concentration (Xiang et al.: The antidepressant effects and mechanism of action of total saponins from the caudexes and leaves of Panax notoginseng in animal models of depression, submitted).Currently, there are some commercial formulations of PNS in China, including XUESAITONG tablet, injection and lyophilized powder injection. However, the oral bioavailability of PNS is not satisfying, and it is documentarily reported that some adverse reactions such as epistasis, allergy and even anaphylactic shock might be caused by using PNS injection [9]. In order to avoid such serious adverse effects as well as to improve the oral bioavailability of PNS, developing