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L-menthol loaded indomethacin composite particle and preparation method thereof

A technology of indomethacin and composite granules, which is applied in the direction of drug combinations, pharmaceutical formulas, active ingredients of hydroxyl compounds, etc. It can solve the problems of poor product powder performance, difficulty in industrialization, and high equipment requirements, and achieve good fluidity and excellent performance. The effect of filling and low economic investment

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

AI Technical Summary

Problems solved by technology

[0003] CN107074703A mentions a kind of method that utilizes outer cylinder, nozzle bar, drop shaper and cooling belt combination equipment to prepare L-menthol spherical particles, but this method has long process flow, high equipment requirements, and needs to prepare seed crystals in advance
CN102772372A proposes a preparation method of indomethacin inclusion compound microspheres, the process includes two aspects of inclusion compound preparation and microsphere preparation, the process is complicated and difficult to realize industrialization
CN111511367A proposes the use of a pharmaceutical composition of indomethacin and menthyl ester as an anti-inflammatory agent, but its equipment is more complicated and the performance of the product powder is poor, which is not conducive to the operation of downstream processes

Method used

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  • L-menthol loaded indomethacin composite particle and preparation method thereof
  • L-menthol loaded indomethacin composite particle and preparation method thereof
  • L-menthol loaded indomethacin composite particle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] (1) At 70°C, prepare an aqueous solution with an L-menthol concentration of 0.015g / mL and an indomethacin concentration of 0.006g / mL, and stir until separation occurs and the L-menthol-indomethacin oil The drops are evenly distributed in the water;

[0036] (2) Cool the solution to 1°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 stearate 0.02% (based on the quality of L-menthol-indomethacin-water mixed solution) under this temperature condition. Stir continuously for 0.5h to make the crystals coalesce into compact particles;

[0037] (3) After vacuum filtration, washing with water, and drying at normal pressure at 25° C. for 12 hours, L-menthol-loaded indomethacin granules were obtained.

[0038] The solid infrared absorption spectrum of product (product) (model ALPHA, Bruker, Germany) sees figure 1 , the infrared spectrum of the product is at 2866cm -1 ~2956cm -1 The absorption...

Embodiment 2

[0042] (1) At 80°C, prepare an aqueous solution with an L-menthol concentration of 0.015g / mL and an indomethacin concentration of 0.01g / mL, and stir until layering occurs and the L-menthol-indomethacin oil The drops are evenly distributed in the water;

[0043] (2) Cool the solution to 5°C at a cooling rate of 45°C / 10min, and maintain a stirring power per unit volume of 0.231kW / m 3 Until crystallization, 0.15% of the surfactant sodium hexametaphosphate (based on the quality of the L-menthol-indomethacin-water mixed solution) was added under the temperature condition. Continue to stir for 2 hours to make the crystals coalesce into compact particles;

[0044] (3) After vacuum filtration, washing with water, and drying at 40° C. under normal pressure for 24 hours, L-menthol-loaded indomethacin granules were obtained.

[0045] According to the solid infrared absorption spectrum of product and the result of Raman spectrum (test method is the same as embodiment 1), judge product i...

Embodiment 3

[0047] (1) At 90°C, prepare an aqueous solution with an L-menthol concentration of 0.015g / mL and an indomethacin concentration of 0.02g / mL, and stir until layering occurs and the L-menthol-indomethacin oil The drops are evenly distributed in the water;

[0048] (2) Cool the solution to 10°C at a cooling rate of 40°C / 10min, and maintain a stirring power per unit volume of 0.138kW / m 3 Until crystallization, 0.40% of surfactant sodium dodecylbenzenesulfonate (based on the quality of the L-menthol-indomethacin-water mixed solution) was added under the temperature condition. Continue to stir for 3 hours to make the crystals coalesce into compact particles;

[0049] (3) After vacuum filtration, washing with water, and drying at normal pressure at 50° C. for 36 hours, L-menthol-loaded indomethacin granules were obtained.

[0050] According to the solid infrared absorption spectrum of product and the result of Raman spectrum (test method is the same as embodiment 1), judge product i...

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Abstract

The invention provides an L-menthol loaded indomethacin composite particle and a preparation method thereof. The composite particle is spherical, and the mass ratio of L-menthol to indomethacin in the composite particle is (0.63-3.55): 1. The composite particle has good uniformity and liquidity, and is not easy to coalesce and adjustable in proportion between components in a product. The L-menthol exists in a stable alpha crystal form, and the indomethacin exists in a medical gamma crystal form. The composite particle can significantly increase percutaneous rates so as to enhance treatment effects. The preparation method of the composite particle is simple, low in cost, easy to realize without using ingredients, round in particle, low in energy consumption and high in efficiency; the composite particle merely uses water as a solvent, so that the composite particle is green and environment-friendly, and can be highly mixed, therefore industrialization and low economic investment can be realized.

Description

technical field [0001] The invention belongs to the technical field of crystallization in the chemical engineering industry, and in particular relates to an L-menthol-loaded indomethacin composite granule and a preparation method thereof. Background technique [0002] L-menthol (CAS: 2216-51-5), the main component of peppermint oil, also known as L-menthol, natural menthol, menthol (L-rotary), etc., the English name is L-Menthol, molecular formula C 10 h 20 O, molecular weight 156.27, usually white needle-like crystals, with a cool mint aroma. Menthol is mostly extracted from plants, and its α crystal form is a thermodynamically stable crystal form. At the same time, it is slightly soluble in water, but easily soluble in alcohol, chloroform, ether, glacial acetic acid, liquid paraffin and petroleum ether. L-menthol can be used as a flavoring agent for toothpaste, perfume, beverages and candies, etc. It is used as a stimulant in medicine, acting on the skin or mucous membra...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/20A61K31/405A61K31/045A61P29/00
CPCA61K9/145A61K9/2095A61K31/405A61K31/045A61P29/00A61K2300/00
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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