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Ibuprofen-loaded lenalidomide composite particle and preparation method thereof

A technology of composite particles and lenalidomide, which is applied in the direction of organic chemical methods, drug combinations, and pharmaceutical formulations, can solve the problems of unfavorable industrial production and application, high economic cost, and complicated equipment, so as to prevent agglomeration and reduce economic investment , Excellent filling effect

Active Publication Date: 2021-06-22
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

CN106806899A proposes a method for preparing polylactic acid bond-loaded ibuprofen sustained-release prodrug by direct melt copolymerization, but the equipment for melt copolymerization is complicated and the economic cost is high
For example, CN106806899A discloses a polylactic acid bond-loaded ibuprofen slow-release prodrug and its direct melt copolymerization preparation method and application; the preparation method of the prodrug comprises the following steps: (1) mixing lactic acid and ibuprofen, After the pre-polymerization water removal treatment, an intermediate is obtained; (2) the obtained intermediate is subjected to melt polycondensation under the action of a catalyst, and the reaction product is dissolved, precipitated, and vacuum-dried to obtain the polylactic acid bond-loaded ibuprofen slow-release Prodrug; the polylactic acid bond-loaded ibuprofen sustained-release prodrug prepared by the preparation method has good biological activity, especially has good antibacterial properties against Escherichia coli, Staphylococcus aureus, Candida albicans, etc.; However, the melt copolymerization equipment used in the preparation process of the prodrug is complex, high in cost, and high in energy consumption, which is not conducive to subsequent industrial production and application

Method used

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  • Ibuprofen-loaded lenalidomide composite particle and preparation method thereof
  • Ibuprofen-loaded lenalidomide composite particle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] (1) At 75°C, prepare an aqueous solution with an ibuprofen concentration of 0.01 g / mL, and stir until stratification occurs and the ibuprofen oil droplets are evenly distributed in the water;

[0036] (2) Keep the temperature and stirring rate constant, add lenalidomide to the ibuprofen-water solution, wherein the concentration of lenalidomide is 0.01g / mL; continue to stir for 0.5h to make the lenalidomide particles and ibuprofen The fen oil drops are in full contact;

[0037] (3) Cool the solution to 1°C at a cooling rate of 40°C / 10min, and maintain a stirring power per unit volume of 0.122kW / m 3 To crystallization, add surfactant sodium stearate 0.08% (based on the quality of ibuprofen-lenalidomide-water mixed solution) at this temperature. Stir continuously for 0.5h to make the crystals coalesce into compact particles;

[0038] (4) After vacuum filtration, washing with water, and drying at normal pressure at 20° C. for 12 hours, the ibuprofen-loaded lenalidomide co...

Embodiment 2

[0042] (1) At 80°C, prepare an aqueous solution with an ibuprofen concentration of 0.10 g / mL, and stir until stratification occurs and the ibuprofen oil droplets are evenly distributed in the water;

[0043] (2) Keep the temperature and stirring rate constant, add lenalidomide to the ibuprofen-water solution, wherein the concentration of lenalidomide is 0.08g / mL; continue to stir for 1.5h to make the lenalidomide particles and ibuprofen The fen oil drops are in full contact;

[0044] (3) Cool the solution to 5°C at a cooling rate of 60°C / 10min, and maintain a stirring power per unit volume of 0.716kW / m 3 To crystal out, add surfactant sodium hexametaphosphate 0.10% (based on the quality of ibuprofen-lenalidomide-water mixed solution) at this temperature. Continue to stir for 2 hours to make the crystals coalesce into compact particles;

[0045] (4) After vacuum filtration, washing with water, and drying at 40° C. under normal pressure for 24 hours, the ibuprofen-loaded lenal...

Embodiment 3

[0048] (1) At 85°C, prepare an aqueous solution with an ibuprofen concentration of 0.35 g / mL, and stir until stratification occurs and the ibuprofen oil droplets are evenly distributed in the water;

[0049] (2) Keep the temperature and stirring rate constant, add lenalidomide to the ibuprofen-water solution, wherein the concentration of lenalidomide is 0.18g / mL; continue stirring for 3h to make the lenalidomide particles and ibuprofen Full contact with oil droplets;

[0050] (3) Cool the solution to 10°C at a cooling rate of 80°C / 10min, and maintain a stirring power per unit volume of 1.472kW / m 3 To crystal out, add surfactant sodium dodecylbenzene sulfonate 0.35% (based on the quality of ibuprofen-lenalidomide-water mixed solution) at this temperature. Continue to stir for 3 hours to make the crystals coalesce into compact particles;

[0051] (4) After vacuum filtration, washing with water, and drying at 60° C. under normal pressure for 36 hours, the ibuprofen-loaded lenal...

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Abstract

The invention provides an ibuprofen-loaded lenalidomide composite particle and a preparation method thereof, wherein the composite particle is a spherical composite particle, and the mass ratio of ibuprofen to lenalidomide in the composite particle is (0.55-3.5):1. The ibuprofen-loaded lenalidomide composite particle has good uniformity and fluidity and is not easy to coalesce, an proportion among the components is adjustable, ibuprofen and lenalidomide both exist in stable crystal form, and the composite particle has good application prospects in treatment of tumors and complications thereof such as fever. The preparation method of the ibuprofen-loaded lenalidomide composite particle is simple, low in price, easy to implement, free of auxiliary materials, round and full in particle, low in energy consumption, high in efficiency, green, environmentally friendly, highly mixed, capable of achieving industrialization and low in economic investment, and only water is used as a solvent.

Description

technical field [0001] The invention belongs to the technical field of crystallization in the chemical engineering industry, and in particular relates to an ibuprofen-loaded lenalidomide composite particle and a preparation method thereof. Background technique [0002] Ibuprofen (CAS: 15687-27-1), chemical name 2-methyl-4-(2-methylpropyl) phenylacetic acid, alias 拉拉风, English name is Ibuprofen, molecular formula C 13 h 18 o 2 , molecular weight 206.28, usually white crystalline powder, melting point is 75°C-77°C. Insoluble in water, easily soluble in ethanol, chloroform, ether, acetone and other solvents. Ibuprofen inhibits cyclooxygenase, reduces the synthesis of prostaglandins, produces analgesic and anti-inflammatory effects, and acts as an antipyretic through the hypothalamic thermoregulatory center. Lenalidomide (CAS: 366789-02-8), chemical name 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl) Phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide, molecular ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/454A61K31/192A61P29/00A61K9/16A61K47/12A61K47/02A61K47/20C07C57/30C07C51/43C07D401/04
CPCC07C57/30C07C51/43C07D401/04A61K31/454A61K31/192A61P29/00A61K9/1617A61K9/1611C07B2200/13A61K2300/00
Inventor 龚俊波孙萌萌陈明洋刘岩博侯宝红
Owner TIANJIN UNIV
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