ABSTRACT
Nao-Qing solution has been shown to be clinically effective in the treatment of acute ischemic stroke (AIS). The purpose of this study was to improve the pharmacokinetics and brain uptake of Nao-Qing, administered as an oil-in-water microemulsion. Sprague-Dawley (SD) rats were given Nao-Qing microemulsion by intranasal or intragastric routes. Samples of blood, brain, heart, liver, lung and kidney were collected at pre-determined time intervals, and the contents of ginsenosides Rg1 and Rb1 (active ingredients of the Nao-Qing microemulsion) were analyzed by high-performance liquid chromatography (HPLC). The results showed that contents of ginsenosides Rg1 and Rb1 in Nao-Qing microemulsion was 8475.13 ± 54.61 µg/ml and 6633.42 ± 527.27 µg/ml, respectively, and that the particle size, pH and viscosity of the microemulsion were 19.9 ± 5.07 nm, 6.1 and 3.056 × 10(-3 )Pas, respectively. Absorption of ginsenoside Rg1 was higher than that of ginsenoside Rb1, which was barely detectable after intragastric administration; furthermore, the concentration of ginsenoside Rg1 in blood and other tissues at each time point was lower for intragastric than for intranasal administration. Compared with intragastric administration, intranasal administration resulted in a shorter tmax (0.08 versus 1 h), a higher Cmax (16.65 versus 11.29 µg/ml), and a higher area under the concentration-time curve (AUC) (592.91 versus 101.70 µgch/ml) in the brain. The relative rates of uptake (Re) and the ratio of peak concentration (Ce) in the brain were 126.31% and 147.48% for ginsenoside Rg1, respectively. These data illustrate that intranasal administration can promote the absorption of drugs in Nao-Qing microemulsion and achieve fast effect.
Subject(s)
Brain/metabolism , Ginsenosides/administration & dosage , Ginsenosides/pharmacokinetics , Administration, Intranasal , Animals , Blood-Brain Barrier/metabolism , Chemistry, Pharmaceutical , Drugs, Chinese Herbal/administration & dosage , Drugs, Chinese Herbal/pharmacokinetics , Emulsions , Humans , Phytotherapy , Rats , Rats, Sprague-Dawley , Stroke/drug therapy , Stroke/metabolismABSTRACT
OBJECTIVE: To prepare PEG-PLA polymeric micelles loaded with vinpocetine (VP). METHODS: VP micelles were prepared by thin-film hydration method, single factors affecting drug loading content, encapsulation efficiency, productivity, particle size and polydispersity index (PDI) such as dosage, type of organic solvent, quantity of organic solvent, hydration temperature, hydration speed, amount of hydration water, hydration time were investigated, and the optimum technology was obtained. The mean particle size and PDI were determined by DLS. The drug loading content, encapsulation efficiency, productivity of VP micelles were investigated by UV. RESULTS: The drug loading content and particle size of VP micelles were 20.35% and 118.3 nm, respectively. CONCLUSION: The technology of VP micelles prepared by thin-film hydration method is practical and simple. It's valuable to be further studied.
