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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

Inactive Publication Date: 2006-11-29
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Oxaliplatin is poorly soluble in aqueous carriers and most organic solvents, and its clinical application is greatly limited
[0006] Oxaliplatin is poorly soluble in water, making its volume larger for clinical use

Method used

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  • Intravenous nanometer suspension injection contg. oxaliplatin platinum phospholipid compound

Examples

Experimental program
Comparison scheme
Effect test

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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Abstract

A nano-class suspension injection of oxaliplatin-phoshpatide composition for intravenous injection is proportionally prepared from oxaliplatin, surfactant, pH regulator, isotonic agent, antioxidant, water for injection, and optional excipient (for the freeze-dried powder injection).

Description

Technical field: [0001] The invention relates to a platinum complex antitumor drug preparation and a preparation method thereof, in particular to a nano-suspension injection of oxaliplatin-phospholipid complex for intravenous administration. Background technique: [0002] Oxaliplatin (oxaliplatin) is an optical isomer prepared by Y.Kidani in 1978 from a mixture of diaminocyclohexane derivatives (dach-platinum), namely (1R-trans)-( 1,2-ring: hexamethylenediamine-N,N')[oxalic acid (2-)-O,O']platinum. is a cytostatic antineoplastic agent used in the treatment of many types of tumors, and especially those of the colon, ovary, and upper respiratory tract, as well as epidermoid and germinal cell tumors. [0003] [0004] Oxaliplatin [0005] Oxaliplatin is poorly soluble in aqueous carriers and most organic solvents, and its clinical application is greatly limited. [0006] Oxaliplatin is poorly soluble in water, making it a relatively large volume for clin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/44A61K31/282A61P35/00
Inventor 王东凯刘伟
Owner SHENYANG PHARMA UNIVERSITY
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