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Ibuprofen-loaded o-vanillin composite particles and preparation method thereof

A technology of composite particles and o-vanillin, applied in the field of composites, can solve problems such as unfavorable industrial production application, unfavorable industrial production application, use of many auxiliary materials, etc. Effect

Active Publication Date: 2021-06-18
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] CN105816434A proposes an ibuprofen granule and a preparation method thereof. The ibuprofen granule is made of the following mass fractions of raw materials: 95% to 100% of crystals of ibuprofen or ibuprofen salt, 0 to 5% of Low melting point lipid material; however, the ibuprofen granules are prepared by partial melting, stirring and cutting, and the granulation process still needs to use more auxiliary materials, and the process is complicated, which is not conducive to industrial production and application
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 o-vanillin composite particles and preparation method thereof
  • Ibuprofen-loaded o-vanillin composite particles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] (1) At 40°C, prepare a mixed aqueous solution containing 0.01g / mL ibuprofen and 0.02g / mL o-vanillin;

[0038] (2) Stir the mixed solution in (1) until liquid-liquid phase separation occurs and the ibuprofen-o-vanillin oil droplets are evenly distributed in the water;

[0039] (3) Keep stirring to cool the solution to 1°C at a cooling rate of 30°C / 10min, and keep stirring at 0.226kW / m 3 until crystallization;

[0040] (4) adding a mass fraction of 0.02% surfactant sodium stearate, and continuously stirring for 0.5h, the crystals are coalesced into compact spheres;

[0041] (5) After vacuum filtration, washing with water, and drying at normal pressure at 15° C. for 12 hours, the ibuprofen-loaded o-vanillin functional granules were obtained.

[0042] The solid infrared absorption spectrum of product (instrument model ALPHA, Bruker, Germany) sees figure 1 , the infrared spectrum of the product is at 1707cm -1 The absorption peak of ibuprofen appears at 1635, 1688cm -1 ...

Embodiment 2

[0045] (1) At 60°C, prepare a mixed aqueous solution containing 0.08g / mL ibuprofen and 0.12g / mL o-vanillin;

[0046] (2) Stir the mixed solution in (1) until liquid-liquid phase separation occurs and the ibuprofen-o-vanillin oil droplets are evenly distributed in the water;

[0047] (3) Keep stirring to cool the solution to 5°C at a cooling rate of 45°C / 10min, and keep stirring at 0.489kW / m 3 until crystallization;

[0048] (4) adding the surfactant sodium hexametaphosphate with a mass fraction of 0.10%, and continuously stirring for 1.5 hours, so that the crystals are coalesced into compact spheres;

[0049] (5) After vacuum filtration, washing with water, and drying at normal pressure at 15° C. for 24 hours, the ibuprofen-loaded o-vanillin functional granules were obtained.

[0050] According to the solid infrared absorption spectrum result of product (test method is the same as embodiment 1), it is judged that product is the physical mixture of ibuprofen and o-vanillin, a...

Embodiment 3

[0052] (1) At 70°C, prepare a mixed aqueous solution containing 0.15 g / mL ibuprofen and 0.10 g / mL o-vanillin;

[0053] (2) Stir the mixed solution in (1) until liquid-liquid phase separation occurs and the ibuprofen-o-vanillin oil droplets are evenly distributed in the water;

[0054] (3) Keep stirring to cool the solution to 7°C at a cooling rate of 60°C / 10min, and keep stirring at 1.479kW / m 3 until crystallization;

[0055] (4) adding a surfactant sodium dodecylbenzenesulfonate with a mass fraction of 0.30%, and stirring continuously for 3.5 hours, so that the crystals are coalesced into compact spheres;

[0056] (5) After vacuum filtration, washing with water, and drying at normal pressure at 20° C. for 36 hours, the ibuprofen-loaded o-vanillin functional granules were obtained.

[0057] According to the solid infrared absorption spectrum result of product (test method is the same as embodiment 1), it is judged that product is the physical mixture of ibuprofen and o-vanil...

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Abstract

The invention provides ibuprofen-loaded o-vanillin composite particles and a preparation method thereof. The composite particles are spherical composite particles, and the mass ratio of ibuprofen to o-vanillin in the composite particles is (0.05-4.50):1. The ibuprofen-loaded o-vanillin composite particles have good uniformity and fluidity, and the spherical particles are not prone to coalescence, so that the ibuprofen-loaded o-vanillin composite particles have good stability in the storage and transportation process; the ibuprofen-loaded o-vanillin composite particles have the effects of resisting bacteria, resisting inflammation, bringing down a fever and the like, and the milk-flavored o-vanillin can reduce the bitter taste of the oral ibuprofen particles to a certain extent; the preparation method is simple, low in energy consumption and high in efficiency, only water is used as a solvent, the raw materials are single and environmentally friendly, industrialization can be achieved, and the economic input is low.

Description

technical field [0001] The invention belongs to the field of composites, and relates to composite granules loaded with ibuprofen and o-vanillin, a preparation method and application thereof. Background technique [0002] Ibuprofen (CAS: 15687-27-1), the chemical name 2-methyl-4-(2-methylpropyl) phenylacetic acid, also known as balanga, is a non-steroidal anti-inflammatory drug widely used clinically. Inflammation medicine has a history of more than 50 years of use. 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 is mainly used for analgesic and anti-inflammatory effects such as sprains, strains, headaches, low back pain, and postoperative pain. [0003] CN105816434A proposes an ibuprofen granule and a preparation method thereof. The ibuprofen granule is made of the fol...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/20A61K31/12A61K31/192A61P29/00
CPCA61K9/16A61K9/2095A61K31/192A61K31/12A61P29/00A61K2300/00
Inventor 龚俊波孙萌萌陈明洋刘岩博侯宝红
Owner TIANJIN UNIV
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