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%)

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Summary

Introduction

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

Preparation of Ginkgolide B Lipid Microspheres
Materials and equipment
Measurement of particle size and zeta potential
Pharmacodynamics studies
Method for determination of GB in lipids
Brain tissue distribution studies
Results
Formulation optimization by orthogonal experiment design
Study on pharmacokinetics of rats in vivo
Brain tissue distribution
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