Intravenous nanometer suspension injection contg. oxaliplatin platinum phospholipid compound
A technology for oxaliplatin phospholipids and intravenous administration, which is applied to the active ingredients of heavy metal compounds, drug combinations, antineoplastic drugs, etc., and can solve the problems of oxaliplatin insoluble in water, clinical application limitations, and oxaliplatin intractability. and other problems, to achieve the effect of simple and easy preparation method, large drug loading capacity and good needle penetration
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Embodiment 1
[0042] Dissolve 1.5 g of oxaliplatin in 30 ml of dimethyl sulfoxide in a round bottom flask, dissolve 4.5 g of soybean lecithin and 30 mg of vitamin E in 100 ml of chloroform, and rotate the resulting mixture at 40°C for rotary evaporation under reduced pressure. A thin film is formed on the surface, and then vacuum dried under reduced pressure for 1 to 2 days. Weigh 7.5 mg of sodium oxalate, 3.0 g of glycerin, and 0.05 g of disodium edetate, and dissolve them together in 150 ml of distilled water to form an aqueous phase. The dried film was suspended in the above aqueous phase. The suspension is transferred to an ultrasonic processor for treatment until transparent, and then homogenized by a homogenizer to prepare a suspension injection. After being sterilized and filtered through a 0.22 μm microporous membrane, the aliquot volume is 5ml, and potted. The final product contained 10 mg / ml oxaliplatin.
Embodiment 2
[0044] Add 1.0 g of oxaliplatin to 1000 ml of methanol in a round-bottomed flask, process it in a tank ultrasonic processor until it is completely dissolved, add egg yolk lecithin in dichloromethane solution (4.0 g in 100 ml of dichloromethane) . Take 5.0 mg of oxalic acid, 5.0 g of glucose, and 0.03 g of disodium edetate, and dissolve them together in 100 ml of distilled water to obtain an aqueous phase. Add the water phase to the mixture of the above-mentioned drug and phospholipid, mix evenly, evaporate the solvent under reduced pressure and rotary evaporation at 40°C, transfer the suspension to an ultrasonic processor for treatment until it is transparent, and then homogenize it through a homogenizer to obtain a mixture suspension injection. After being sterilized and filtered through a 0.22μm microporous membrane, it is divided into 10ml volumes.
Embodiment 3
[0046] Add 1.0 g of oxaliplatin to 1000 ml of methanol in a round-bottomed flask, process it in a tank-type ultrasonic processor until it is completely dissolved, add a chloroform solution of egg yolk lecithin (4. g in 100 ml of chloroform), and obtain The mixture was rotary evaporated at 40°C under reduced pressure, and a film was formed on the flask. Dissolve 3.0 mg of oxalic acid, 1.0 g of mannitol, and 0.02 g of disodium edetate in 100 ml of distilled water to obtain an aqueous phase. Suspend the film in the above water phase, transfer the suspension to a high-speed milk homogenizer to homogenize, prepare the suspension, filter it through a 0.22 μm microporous membrane, and divide it into 3ml volume, freeze Dry to make lyophilized suspension injection.
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