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Objective :To fabricate resveratrol nanoemulsions and probe their pharmacokinetics profiles in rats in vivo. Methods The nanoemulsions of resveratrol were tailored by using aethylis oleas as the oil phase, Cremophor RH40 as emulsifiers, absolute alcohol as co-emulsifiers, respectively. The formulation was optimized by pseudo-ternary phase diagrams and their physicochemical properties of nanoemulsions were characterized by particle size distribution, transmission electron microscope (TEM), and Fourier transform infrared spectroscopy (FTIR). The pharmacokinetics experiments were also performed in rats after gavage and the plasm concentration of resveratrol were determined by HPLC as well as the profiles of pharmacokinetic parameters were obtained by Drug and Statistics (DAS) software. Results: The formula of nanoemulsions were as follows: the ratio of resveratrol-aethylis oleas-mixture surfactant- distilled water was 1:10:24:65. The average particle size diameters of prepared resveratrol nanoemulsions were about 40 nm and the droplets of nanoemulsions were in spherical shape observed by TEM. The results of IR disclosed that the active trans-resveratrol presented in the oil droplet of the nanoemulsions. Compared with resveratrol suspensions, the bioavailability of resveratrol nanoemulsions was increased 1.45-fold, and Cmax reached to 1.93-fold. Conclusion : These results indicated that nanoemulsions may be a promising tool for the delivery of resveratrol.
ABSTRACT
OBJECTIVE： To establish content determination method of Triptolide-glycyrrhetic acid compound microemulsion， optimize the formula and investigate its physicochemical properties and release rate in vitro. METHODS： The content of Triptolide- glycyrrhetic acid compound microemulsion was determined by UPLC. The determination was performed on ACQUITY UPLC BEH C18 column with mobile phase consisted of 0.1％ formic acid aqueous solution-acetonitrile （gradient elution） at the flow rate of 0.4 mL/min. The column temperature was 40 ℃. The detection wavelength was set at 218 nm， and sample size was 5 μL. Pseudo-ternary phase diagrams were drawn by water titration method. Using oil phase， surfactants and co-surfactants as index， the formula was optimized， and in intro release characteristics was investigated by in vitro release test. RESULTS： The linear range of triptolide and glycyrrhetinic acid were 1-40 μg/mL（r＝0.999 7） and 10-400 μg/mL（r＝0.999 8）， respectively. The limits of quantitation were 0.5 and 0.8 μg/mL； the limits of detection were 0.1 and 0.2 μg/mL. RSDs of precision， stability and reproducibility tests were all less than 2％. Average recoveries were 100.32％-101.15％ （RSD＝0.36％， n＝6）， 99.78％-101.42％ （RSD＝0.59％，n＝6）. The optimal formula included that medium chain triglyceride as oil phase， polyethylene glycol hydroxy stearate as surfactants， ethanol as co-surfactants， water as water phase， the proportion of them was 8 ∶ 28 ∶ 14 ∶ 50. The obtained microemulsion was O/W type， being transparent and clear， with average diameter， average polydispersity index and average viscosity of （62.38±3.44） nm， 0.096±0.001 and （26.84±1.10） mPa·S. Within 24 h， cumulative release rates of triptolide and glycyrrhetinic acid in obtained microemulsion were 99.8％ and 99.7％ （in PBS pH 2.0）， 99.3％ and 99.4％ （in PBS pH 7.4）， 98.9％ and 98.4％ （in PBS pH 9.0）， respectively. Triptolide and glycyrrhetinic acid released faster in the single microemulsion than in the compound microemulsion. CONCLUSIONS： Established content determination method is simple and stable. The optimized formula is stable and feasible. Obtained iriptolide-glycyrrhetinic acid compound microemulsion show better sustained-release effect than sigle microemulsion.
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OBJECTIVE: To investigate the O/W submicron emulsion injection formulation, and investigate its pharmacokinetics in the rat. METHODS: Pseudo-ternary phase diagrams were established using the water titration method. The effects of different surfactants, cosurfactants and Km values on the phase diagram were investigated, and the prescription of submicron emulsion formulation was optimized. Stability of coenzyme Q10 submicron emulsion was evaluated, and the pharmacokinetics in the rat after intravenous injection was study. RESULTS: Coenzyme Q10 submicron emulsion consisting of Poloxamer188/Lipoid S100/ethanol/PEG400/water has the lower viscosity, the smaller size and the higher encapsulation efficiency. An obvious sustained-release effect of coenzyme Q10 submicron emulsion was observed after iv injection in the pharmacokinetics experiment, and mean residence time is 6. 55 h. CONCLUSION: The optimized coenzyme Q10 submicron emulsion consumes smaller quantities of auxiliary materials and shows good stability. Moreover, it is easy to manufacture and convenient for clinical use. Copyright 2012 by the Chinese Pharmaceutical Association.