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Self-assembly system based on hydrophilic polymer and medicine and preparation method thereof

A hydrophilic polymer and self-assembly technology, which is applied in the direction of pharmaceutical formulations, non-active ingredients of polymer compounds, medical preparations of non-active ingredients, etc., to achieve the effects of simple preparation, ensuring safety in the body, and reducing solvent residues

Active Publication Date: 2012-12-12
ARMY MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, work in this area has not been reported in the literature so far.

Method used

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  • Self-assembly system based on hydrophilic polymer and medicine and preparation method thereof
  • Self-assembly system based on hydrophilic polymer and medicine and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Dissolve polyethyleneimine with a molecular weight of 800 Da in 1 ml of deionized water, and the concentration of the polymer aqueous solution is 10 mg / ml; dissolve ibuprofen in methanol, where the concentration of ibuprofen is 20 mg / ml; ultrasonic Under the action, slowly add 0.5 ml of ibuprofen methanol solution into the polymer aqueous solution; then place the mixed solution in a dialysis bag with a molecular weight cut-off of 3500 Da, dialyze in deionized water under magnetic stirring, keep the temperature at room temperature, and The deionized water was replaced at intervals; after 12 hours, the dialysate was filtered and freeze-dried to obtain the drug-loaded polymer assembly. The drug loading in the resulting assembly was 38.7%. After oral administration to rats, the area under the plasma concentration-time curve (AUC) of the assembly system was 5 times that of the same dose of the raw drug.

Embodiment 2

[0029] Dissolve polyethyleneimine with a molecular weight of 1000 Da in 0.5 ml deionized water, and the concentration of the polymer aqueous solution is 20 mg / ml; dissolve ketoprofen in ethanol, where the drug concentration is 20 mg / ml; , slowly add 1 ml of ketoprofen ethanol solution into the polymer aqueous solution; then place the mixed solution in a dialysis bag with a molecular weight cut-off of 7000 Da, dialyze in deionized water under magnetic stirring, keep the temperature at room temperature, and keep the temperature at room temperature for a certain time interval The deionized water was replaced; after 24 hours, the dialysate was filtered and freeze-dried to obtain the drug-loaded polymer assembly. The drug loading in the resulting assembly was 60.8%.

Embodiment 3

[0031] Dissolve polyethyleneimine with a molecular weight of 1200 Da in 1 ml of deionized water, and the concentration of the polymer aqueous solution is 10 mg / ml; dissolve fenoprofen in acetone, where the drug concentration is 50 mg / ml; ultrasonication 0.2 ml fenoprofen acetone solution was slowly added to the polymer aqueous solution; then the mixed solution was placed in a dialysis bag with a molecular weight cut-off of 12000 Da, dialyzed in deionized water under magnetic stirring, and the temperature was kept at room temperature. The deionized water was replaced at intervals; after 24 hours, the dialysate was filtered and freeze-dried to obtain the drug-loaded polymer assembly. The drug loading in the resulting assembly was 43.5%.

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Abstract

The invention relates to a self-assembly system based on hydrophilic polymer and medicine and a preparation method thereof. The system consists of a hydrophilic polymer and a carboxyl-containing medicine, wherein the hydrophilic polymer is polymine or beta-cyclodextrin modified polymine; and the carboxyl-containing medicine is selected from ibuprofen, ketoprofen, fenoprofen, flurbiprofene, oxaprozin, naproxen, indometacin, sulindac, etodolac, diclofenac, pontal, meclofenamic acid, flufenamic acid, tolfenamic acid, lumiracoxib, licofelone, diflunisal and aspirin. The system is prepared by dissolving the hydrophilic polymer in a certain amount of water, dissolving the medicine in a water soluble solvent, slowly adding the organic solution of the medicine into the aqueous solution of the polymer under the action of ultrasound, placing the mixed solution in a dialysis bag, dialyzing in deionized water with magnetic stirring, replacing the deionized water at certain time interval, filtering dislysate after 5 to 48 hours, cooling and drying.

Description

technical field [0001] The invention relates to a high-efficiency drug delivery system based on a hydrophilic polymer-drug self-assembly and a preparation method thereof. Especially ibuprofen, ketoprofen, fenoprofen, flurbiprofen, oxaprozin, naproxen, indomethacin, sulindac, etodolac, diclofenac, mefenamic acid, meclofenac A method for preparing a polymer assembly delivery system for carboxyl-containing non-steroidal anti-inflammatory drugs such as fenamic acid, flufenamic acid, tolfenamic acid, lumiracoxib, ricofenol, diflunisal, and aspirin. Background technique [0002] Many important therapeutic compounds are widely used in clinic due to their extremely small water solubility, so it is a very important work to develop effective delivery systems. As an ideal drug delivery system, it must be able to transport the drug to a specific site in the body and release the drug at that site. At the same time, the carrier itself must be able to degrade into non-toxic products and ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61K47/32A61K47/40A61K47/58A61K47/69
Inventor 李晓辉张建祥李淑慧
Owner ARMY MEDICAL UNIV
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