Abstract
AbstractIn this study, we introduce a method to formulate Ginkgolide B lipid microemulsion (GB-LM). We have assessed its general characteristics and pharmacokinetics in animals. Soybean oil (10.0%) and oleic acid (2.4%) were chosen as the oil phase, refined egg yolk lecithin (PC98T) (1.8%) as the surfactant, and glycerol (2.25%) as the co-surfactant. The optimized formulation process resulted in particles with average diameter of 185.9 ± 52.5 nm and the zeta potential of −19.8 ± 1.3 mV. The GB-LM remained steady for three months at room temperature. Giving each dose of 4 mg/kg to rats through the vein, a clearance rate of CL (L/h): 2.594 and C max (ng/mL) was achieved: 353.8 through pharmacokinetic analysis and statistical analysis. The AUC of GB-LM was about 1.57-fold higher than that of the products available in the market. In addition, brain tissue distribution studies show that after 0.5 h administration of GB, the concentration of GB in brain tissue can reach its maximum, and then significantly decrease after 2 hours. Therefore, the improved formulation of GB-LM shows encouraging results compared with present products in several features.
Highlights
In this study, we introduce a method to formulate Ginkgolide B lipid microemulsion (GBLM)
Ginkgolide, oleic acid and refined egg yolk lecithin phospholipid (PC98T) were added to soybean oil, stirred about 2 minutes at 6000rpm until phospholipid was completely dissolved, this process was protected by nitrogen during heating, it was used as oil phase, heat preservation; According to the prescription, water phase was heated to 50-60°C, oil phase was added to water phase slowly, stirred about 10 minutes at 3000-10000 rpm high speed to form colostrum
In order to explore the effects of the preparation method on the physicochemical properties of GB-Lipid microemulsion (LM), the Ginkgolide B-Lipid microemulsion (GB-LM) were prepared with the following composition: soybean oil (10.0%), GB (0.2%), PC98T (1.8%), oleic acid (2.4%) and glycerol (2.25%)
Summary
Abstract: In this study, we introduce a method to formulate Ginkgolide B lipid microemulsion (GBLM). GB’s CAS number is [15291-77-7], C20H24O10 with molecular weight 424.40 It has a high melting point (about 300°C); it is soluble in many organic solvents, such as acetone and ethanol. Lipid microemulsion (LM) is a vegetable oil based nanosphere covered with phospholipid It is a stable Oil/ Water disperse system consisting of oil phase, emulsifier, water phase, the diameter of particle size is between 100~200 nm, which is called submicroemulsion. We designed a drug delivery system based on LM to transport medicament, and developed an optimized formulation of Ginkgolide B-Lipid microemulsion (GB-LM) using single factor and orthogonal experiment design, the physicochemical properties and pharmacokinetic parameters of GB-LM in rats were established. Shimadzu LC-2010A HT high performance liquid chromatograph, Artorius CRA225D2 electronic balance of one in one hundred thousand, SEDERE LT-ELSD SEDEX80 evaporative light scattering detector, Kunshan KQ3200DB ultrasonic cleaner
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