Hydrophilic amide polymer self-assembly particle drug release system suitable for hydrophobic drugs and preparation method thereof

A technology of amide polymers and hydrophobic drugs, which can be used in pharmaceutical formulations, medical preparations containing active ingredients, and medical preparations containing active ingredients. and adverse reactions, increase the cost of preparations, etc., to achieve good freeze-drying redispersibility, improve bioavailability, and low price

Active Publication Date: 2015-04-22
ARMY MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

On the one hand, this increases the cost of the preparation, on the other hand, the use of high-dose polymer carriers increases potential side effects and adverse reactions, which is not conducive to clinical application

Method used

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  • Hydrophilic amide polymer self-assembly particle drug release system suitable for hydrophobic drugs and preparation method thereof
  • Hydrophilic amide polymer self-assembly particle drug release system suitable for hydrophobic drugs and preparation method thereof
  • Hydrophilic amide polymer self-assembly particle drug release system suitable for hydrophobic drugs and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Dissolve poly(N-methacrylamide) with a molecular weight of 5000Da, flurbiprofen and cyclosporin A in 1ml methanol, where the polymer concentration is 10mg / ml and the flurbiprofen concentration is 2.5mg / ml The concentration of cyclosporin A is 5mg / ml; then the solution is placed in a dialysis bag with a molecular weight cut-off of 3500Da, and the solution is dialyzed in deionized water under magnetic stirring at a temperature of 10℃, and the deionized water is replaced every 0.5 hour interval; 6 hours The product is collected by centrifugation and freeze-dried to obtain assembly particles. The drug loading amount of cyclosporin A in the resulting assembly particles was 25.8%.

Embodiment 2

[0037] Dissolve poly(N-ethylacrylamide) with a molecular weight of 10000Da, indomethacin and rapamycin in 1ml ethanol, where the polymer concentration is 10mg / ml and the indomethacin concentration is 10mg / ml. The concentration of rapamycin is 15mg / ml; then the solution is placed in a dialysis bag with a molecular weight cut-off of 5000Da, and the solution is dialyzed in deionized water under magnetic stirring at a temperature of 20℃, and the deionized water is replaced every 3 hours; after 12 hours The product is collected by centrifugation and freeze-dried to obtain assembly particles. The drug loading amount of rapamycin in the resulting assembly particles was 30.2%.

Embodiment 3

[0039] The poly(N-n-propylacrylamide) with a molecular weight of 15000Da, sulindac and tamsulolimus were dissolved in 2ml of acetone, the polymer concentration was 8mg / ml, the sulindac concentration was 20mg / ml, The concentration of Rolimus is 30mg / ml; then the solution is placed in a dialysis bag with a molecular weight cut-off of 10000Da, and the solution is dialyzed in deionized water under magnetic stirring at a temperature of 15°C. The deionized water is replaced every 3 hours; centrifuged after 24 hours The product is collected and freeze-dried to obtain assembly particles. The drug loading amount of tamsulolimus in the resulting assembly particles was 45.9%.

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Abstract

The invention relates to a hydrophilic amide polymer self-assembly particle drug release system suitable for hydrophobic drugs and a preparation method thereof. The system comprises a hydrophilic amide polymer, a hydrophobic carboxyl-containing compound and a hydrophobic drug, wherein the hydrophilic amide polymer comprises poly(N-methacrylamide), poly(N-ethylacrylamide), poly(N-n-propylacryamide) and a copolymer of the poly(N-methacrylamide), the poly(N-ethylacrylamide) and the poly(N-n-propylacryamide). The preparation method comprises the following steps: dissolving the hydrophilic amide polymer, the hydrophobic carboxyl-containing compound and the hydrophobic drug in a water-soluble organic solvent; putting the obtained organic solution in a dialysis bag, dialyzing in deionized water under the condition of magnetic stirring and changing the deionized water at a certain time interval; and centrifuging to collect the product after 6-72 hours and carrying out freeze-drying to obtain the system.

Description

Technical field [0001] The invention relates to a hydrophilic amide polymer self-assembled microparticle drug release system suitable for hydrophobic drugs and a preparation method thereof. Especially cyclosporin A, rapamycin, tamsulolimus, everolimus, desfoslimus, zotarlimus, Darapladib, fenofibrate, clofenac, beclofibrate, diltiazem , Nicardipine, nifedipine, nimodipine, verapamil, reserpine, digoxin, digitoxin, paclitaxel, docetaxel, adriamycin, daunorubicin, epirubicin , Pirarubicin, camptothecin, hydroxycamptothecin, irinotecan, topotecan, vincristine, vindesine, vinorelbine, toremifene, exemestane and other hydrophobic drugs Preparation method of drug system. Background technique [0002] At present, most of the drugs widely used in clinical practice and the drugs under preclinical and clinical research and development are poorly water-soluble hydrophobic drugs. Due to solubility limitations, the oral bioavailability of these drugs is often extremely low. On the one han...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K9/14A61K47/32A61K45/00
Inventor 张建祥李晓辉窦寅周兴
Owner ARMY MEDICAL UNIV
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