Oleanolic acid liposome preparation, freeze dried powder injecta thereof and its preparation
A technology for liposome preparation and freeze-dried powder injection, which is applied in the field of oleanolic acid liposome and freeze-dried powder for injection and preparation, can solve the problems of affecting drug dissolution and absorption, low drug bioavailability, affecting curative effect, etc. problem, to achieve good biocompatibility, solve the problem of water insolubility, and the preparation method is simple and easy to implement.
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Embodiment 1
[0025] Weigh 10mg oleanolic acid, 300mg soybean lecithin (purity>90% phosphatidylcholine), 10mg cholesterol, 100mg Tween 80, place in a pear-shaped glass bottle, and use 20ml chloroform / methanol (1:2) mixed solvent In 37°C constant temperature water bath, the organic solvent was removed under reduced pressure with a rotary evaporator, so that a uniform lipid film was formed on the wall of the glass bottle, placed in a vacuum desiccator, and placed overnight at room temperature for later use. Take 10ml of pH6.8 phosphate buffer solution, add it to the above-mentioned glass bottle, rotate and wash the membrane with a rotary evaporator under the condition of an ice bath, until the lipid film is hydrated and becomes a milky white liposome suspension, and press evenly Reduce the particle size to a smaller size (5000psi, 10 times). 300 mg of mannitol was dissolved in liposomes, and after aseptic filtration (the pore size of the membrane filter was 0.22 μm), the final dispersion was ...
Embodiment 2
[0027] Weigh 10 mg of oleanolic acid, 500 mg of soybean lecithin (purity > 80% phosphatidylcholine), and 5 mg of cholesterol, place them in a pear-shaped glass bottle, and put them in a mixed solvent of 20 ml of chloroform / methanol (1:1) at 37 ° C. Use a rotary evaporator on a constant temperature water bath to remove the organic solvent under reduced pressure to form a uniform lipid film on the glass bottle wall, place it in a vacuum desiccator, and place it overnight at room temperature for later use. Take 10ml of glucose injection dissolved with 150mg of poloxamer 188, add it to the above-mentioned glass bottle, and use a rotary evaporator to wash the membrane under the condition of an ice bath until the lipid film is hydrated and becomes a milky white liposome mixture. Suspension, obtained by high-pressure homogenization with smaller particle size (5000psi, 5 times). 300 mg of lactose was dissolved in liposomes, and after aseptic filtration (membrane filter pore size 0.22 ...
Embodiment 3
[0029] Weigh 10mg of oleanolic acid and 300mg of lecithin and dissolve in 5ml of ether, then dissolve 200mg of polyoxyethylene castor oil in 10ml of 0.9% sodium chloride injection, then add the phospholipid ether solution to the chloride solution containing EL In sodium injection, the two are mixed for emulsification, and then the organic solvent is removed under reduced pressure, and probe ultrasonication is enough for 1 min. 1000 mg trehalose was dissolved in liposomes, after sterile filtration (membrane filter pore size 0.22 μm), the final dispersion was divided into vials, and then freeze-dried. The measured encapsulation efficiency is 72.8%, and the average particle diameter is 265nm.
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