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Ibuprofen-loaded rivaroxaban functional particles and preparation method thereof

A functional technology of rivaroxaban, applied in pharmaceutical formulations, organic active ingredients, non-central analgesics, etc., can solve the problems of complex equipment, high economic cost, poor mobility, etc., to reduce industrialization costs and economic investment The effect of low and excellent filling

Active Publication Date: 2021-06-08
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] 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
CN2016102432348 proposes a kind of ibuprofen granule and preparation method thereof, and adopts partial fusion stirring cutting method to prepare ibuprofen granule, but granulation process still needs to use more auxiliary materials and process is complicated
Rivaroxaban mainly exists in the form of regular flaky or polygonal massive crystals, which has the characteristics of low bulk density, poor fluidity, and easy agglomeration, which seriously affects downstream processing and product quality
CN2019111299645 and CN2016100714782 propose a preparation method of rivaroxaban tablet pharmaceutical composition, but the process involves multiple preparation steps and needs to be dried and granulated in fluidized bed equipment, and the time and economic costs are high, which is not necessary. Conducive to the promotion of industrialization

Method used

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  • Ibuprofen-loaded rivaroxaban functional particles and preparation method thereof
  • Ibuprofen-loaded rivaroxaban functional particles and preparation method thereof
  • Ibuprofen-loaded rivaroxaban functional particles and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] (1) At 80°C, prepare an aqueous solution with an ibuprofen concentration of 5.0 mg / 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 rivaroxaban to the ibuprofen-water solution, wherein the concentration of rivaroxaban is 2.0mg / mL; continue stirring for 0.5h to make the rivaroxaban particles and cloth Profen oil droplets fully contact;

[0037] (3) Cool the solution to 1°C at a cooling rate of 80°C / 10min, and maintain a stirring power per unit volume of 2.093kW / m 3 To crystallization, add surfactant sodium stearate 0.02% (based on the quality of ibuprofen-rivaroxaban-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 25° C. for 12 hours, the ibuprofen-loaded rivaroxaban functional gra...

Embodiment 2

[0043] (1) At 85°C, prepare an aqueous solution with an ibuprofen concentration of 5.0 mg / mL, and stir until stratification occurs and the ibuprofen oil droplets are evenly distributed in the water;

[0044] (2) Keep the temperature and stirring rate constant, add rivaroxaban to the ibuprofen-water solution, wherein the concentration of rivaroxaban is 3.0mg / mL; continue stirring for 1.5h to make the rivaroxaban particles and cloth Profen oil droplets fully contact;

[0045] (3) Cool the solution to 5°C at a cooling rate of 60°C / 10min, and maintain a stirring power per unit volume of 0.732kW / m 3 To crystal out, add surfactant sodium hexametaphosphate 0.15% (based on the quality of ibuprofen-rivaroxaban-water mixed solution) at this temperature. Continue to stir for 2 hours to make the crystals coalesce into compact particles;

[0046] (4) After vacuum filtration, washing with water, and drying at 40° C. under normal pressure for 24 hours, the ibuprofen-loaded rivaroxaban func...

Embodiment 3

[0049] (1) At 90°C, prepare an aqueous solution with an ibuprofen concentration of 5.0 mg / mL, and stir until stratification occurs and the ibuprofen oil droplets are evenly distributed in the water;

[0050] (2) Keep the temperature and stirring rate constant, add rivaroxaban to the ibuprofen-water solution, wherein the concentration of rivaroxaban is 6.0mg / mL; continue stirring for 3h to make the rivaroxaban particles and ibuprofen The fen oil drops are in full contact;

[0051] (3) Cool the solution to 10°C at a cooling rate of 50°C / 10min, and maintain a stirring power per unit volume of 0.138kW / m 3 To crystal out, add surfactant sodium dodecylbenzene sulfonate 0.40% (based on the quality of ibuprofen-rivaroxaban-water mixed solution) at this temperature. Continue to stir for 3 hours to make the crystals coalesce into compact particles;

[0052] (4) After vacuum filtration, washing with water, and drying at normal pressure at 50° C. for 36 hours, the ibuprofen-loaded rivar...

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Abstract

The invention provides ibuprofen-loaded rivaroxaban functional particles and a preparation method thereof. The functional particles are spherical composite particles, and the mass ratio of ibuprofen to rivaroxaban in the functional particles is (0.76-3.80): 1. The ibuprofen-loaded rivaroxaban functional particles have good uniformity and fluidity, are not easy to coalesce, have an adjustable ratio of components, and have a good application prospect in the aspect of postoperative complication prevention of hip or knee replacement surgeries, and ibuprofen and rivaroxaban both exist in a stable crystal form. The ibuprofen-loaded rivaroxaban functional particles are simple in preparation method, 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 a functional granule containing ibuprofen containing rivaroxaban 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. Rivaroxaban (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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5377A61K31/192A61K9/16A61K47/12A61K47/02A61K47/20A61P7/02A61P29/00
CPCA61K31/5377A61K31/192A61K9/1617A61K9/1611A61P7/02A61P29/00A61K2300/00
Inventor 龚俊波刘岩博陈明洋闫辉彭浩宇孙萌萌侯宝红尹秋响
Owner TIANJIN UNIV
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