A kind of stephenia fatty oil-bile salt mixed micelle containing stephenin and its preparation method and application
A technology of azalea and mixed micelles, which can be applied to medical preparations containing active ingredients, oil/fat/wax non-active ingredients, and non-active medical preparations, etc., which can solve the problem of poor water solubility and active Can not give full play to problems such as unsatisfactory gastrointestinal absorption effect, etc., to achieve the effect of improving solubility and improving intestinal absorption effect
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Embodiment 1
[0055] Example 1 Preparation of Fructus Stephanae Fatty Oil.
[0056] (1) Pulverize the daughter of the daughter of a daughter into a daughter of the daughter of a daughter through a 20-mesh sieve;
[0057] (2) Extract 1,000g of Fructus Rhizome powder with 20,000g of ethanol three times, and combine to obtain the ethanol extract;
[0058] (3) Recover the alcohol extract to remove ethanol, then pass it through silica gel column chromatography with a particle size of 100-200 mesh, and use petroleum ether (60-90°C) as the eluting solvent for elution, and the eluate is the fatty oil .
Embodiment 2
[0059] Example 2 Preparation of Stephaniae Fatty Oil-Bile Salt Mixed Micelle Containing Stephanin.
[0060] (1) Dissolve 200 mg of sodium deoxycholate in 0.01 M phosphate buffer (PBS) at pH=7.4 to obtain a 0.2 mg / mL sodium deoxycholate solution;
[0061] Weighed 5mg of stephartine L1, L2, L3 and L8 and dissolved in ethyl acetate to obtain a stepharutin mixed solution with the concentration of each monomer being 1 mg / mL;
[0062] Weigh 2 g of the Fructus Stephanae fatty oil obtained in Example 1 and dissolve it in ethyl acetate to obtain a 20 mg / mL fatty oil solution.
[0063] (2) Take 1 mL of the above-mentioned stephenin mixed solution and stephaezi fatty oil solution respectively, put them in the same round-bottomed flask, evaporate in a water bath at 40°C, evaporate the ethyl acetate, and put the round-bottomed flask in a vacuum drying oven , evacuated overnight at room temperature to remove residual ethyl acetate to form a lipid film.
[0064] (3) Take 80 mL of sodium de...
Embodiment 3
[0070] Example 3 Characterization of Stephaniae Fatty Oil-Bile Salt Mixed Micelle Containing Stephanin.
[0071] 3.1 Form
[0072] The solutions in Example 2 and Comparative Example 1 are characterized by a high-resolution transmission electron microscope, and the photomicrograph of the stephaezi fatty oil-bile salt mixed micelles solution containing stephenin is as follows: figure 1 As shown, the photomicrographs of the spironocin-bile salt micellar solution are shown as figure 2 shown. Depend on figure 1 and figure 2 It can be seen that the micelles formed by the diterpene alcohol esters of stephenae in sodium deoxycholate solution are more regular in shape, more uniform in particle size, and more uniform in distribution in the presence of stephatia fatty oil.
[0073] 3.2 Particle size distribution and Zeta potential
[0074] Zetasizer 3000 HS instrument (Malvern Instruments, Malvern, UK) measured the particle size and Zeta potential of the sample solution S1 of Exam...
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