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Ibuprofen-loaded praziquantel composite particle and preparation method thereof

A technology of composite granules and praziquantel, which is applied in the direction of pharmaceutical formulations, drug combinations, and medical preparations containing active ingredients, etc., and can solve problems such as low bioavailability, poor product powder performance, and impact on clinical application

Active Publication Date: 2021-05-28
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 slow-release prodrug by direct melt copolymerization, but the equipment for melt copolymerization is complex, costly and energy-consuming
CN2016102432348 proposes a kind of ibuprofen granule and preparation method thereof, and adopts partial fusion stirring cutting method to prepare ibuprofen granule, but the granulation process still needs to use more auxiliary materials, and the process is complicated
For praziquantel, on the one hand, its needle-like crystal habit has the characteristics of low bulk density, poor fluidity, and easy agglomeration, which seriously affects downstream processing and product quality. On the other hand, due to its low solubility, high permeability and biological The low utilization rate has seriously affected its clinical application
CN110790759A proposes a method for preparing ultrasonically assisted spherical praziquantel crystals, but this method uses isopropanol as a solvent, and there is a certain amount of solvent residue, and the introduction of ultrasonic devices greatly increases the cost of equipment
CN108794466A proposes a preparation method of amorphous praziquantel solid, although the reactivity is improved, but the product powder performance is poor, and there are still problems in the follow-up preparation tabletting

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] (1) At 70°C, prepare an aqueous solution with a concentration of ibuprofen of 0.01g / mL and a concentration of praziquantel of 0.002g / mL, and stir until layering occurs and the oil droplets of ibuprofen-containing praziquantel are uniform in water distributed;

[0037] (2) Cool the solution to 1°C at a cooling rate of 70°C / 10min, and maintain a stirring power per unit volume of 0.989kW / m 3 To crystal out, add surfactant sodium stearate 0.02% (based on the quality of ibuprofen-carrying praziquantel-water mixed solution) under this temperature condition. Stir continuously for 0.5h to make the crystals coalesce into compact particles;

[0038] (3) Vacuum filtration, washing with water, and drying at normal pressure at 25° C. for 12 hours to obtain the praziquantel product contained in ibuprofen.

[0039] The solid infrared absorption spectrum of product (instrument model ALPHA, Bruker, Germany) sees figure 1 , in the infrared spectrum of the product (product) at 1707cm ...

Embodiment 2

[0044] (1) At 80°C, prepare an aqueous solution with a concentration of ibuprofen of 0.01 g / mL and a concentration of praziquantel of 0.005 g / mL, and stir until layering occurs and the oil droplets of ibuprofen-containing praziquantel are uniform in water distributed;

[0045] (2) Cool the solution to 5°C at a cooling rate of 60°C / 10min, and maintain a stirring power per unit volume of 0.358kW / m 3 To crystal out, add surfactant sodium hexametaphosphate 0.15% (based on the quality of ibuprofen-carrying praziquantel-water mixed solution) under this temperature condition. Continue to stir for 2 hours to make the crystals coalesce into compact particles;

[0046] (3) Vacuum filtration, washing with water, and drying at 40° C. under normal pressure for 24 hours to obtain the praziquantel product contained in ibuprofen.

[0047] According to the results of the solid infrared absorption spectrum, PXRD spectrum and differential scanning calorimetry spectrum of the product (test meth...

Embodiment 3

[0049] (1) At 90°C, prepare an aqueous solution with a concentration of ibuprofen of 0.01 g / mL and a concentration of praziquantel of 0.01 g / mL, and stir until layering occurs and the oil droplets of ibuprofen-containing praziquantel are uniform in water distributed;

[0050] (2) 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-carrying praziquantel-water mixed solution) under this temperature condition. Continue to stir for 3 hours to make the crystals coalesce into compact particles;

[0051] (3) Vacuum filtration, washing with water, and drying at normal pressure at 50° C. for 36 hours to obtain the praziquantel product contained in ibuprofen.

[0052] According to the results of the solid infrared absorption spectrum, PXRD spectrum and differential scanning calorimetry spectrum of the product (test ...

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Abstract

The invention provides an ibuprofen-loaded praziquantel composite particle and a preparation method thereof, the composite particle is a spherical composite particle, and the mass ratio of ibuprofen to praziquantel in the composite particle is (1.11-10.57) : 1. The ibuprofen-loaded praziquantel composite particle has better uniformity and flowability and is not easy to coalesce, wherein the proportion of each component of the product is adjustable, the ibuprofen exists in a stable crystal form, the praziquantel exists in an amorphous form, and the ibuprofen-loaded praziquantel composite particle has a better treatment prospect in the aspect of human and livestock suffering schistosomiasis. The preparation method of the ibuprofen-loaded praziquantel composite particles is simple, low in price, easy to implement, free of auxiliary materials, round and full in particles, low in energy consumption and high in efficiency. The process only uses water as a solvent, so that the method is green and environment-friendly, is highly mixed, can realize industrialization and is low in economic investment.

Description

technical field [0001] The invention belongs to the technical field of crystallization in the chemical engineering industry, and in particular relates to a composite particle of ibuprofen-loaded praziquantel and a preparation method 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. Praziquantel (CAS: 55268-74-1), chemical name 2-cyclohexylcarbonyl-1,3,4,6,...

Claims

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Application Information

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IPC IPC(8): A61K31/4985A61K9/16A61K31/192A61P33/12
CPCA61K31/192A61K31/4985A61K9/16A61P33/12A61K2300/00
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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