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Nasal nano-preparation mometasone furoate liquid crystal gel nanoparticle and preparation method thereof

A technology of mometasone furoate and nano-preparation, which is used in anti-inflammatory agents, liquid delivery, pharmaceutical formulations, etc., can solve the problem that the moisturizing and moisturizing effect does not reach the best level, the particle size of liquid crystal nanoparticles is not suitable, and the molecular weight of furoate is not suitable. The problem of low content of metasone, etc., can achieve the effect of maintaining the relative stability of particle size, avoiding the risk of hemolysis, and improving the sustained release time and absorption rate.

Active Publication Date: 2018-07-17
武汉百纳礼康生物制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, mometasone furoate is rarely used in the treatment of bacterial rhinitis and allergic rhinitis. For example, the mometasone furoate nasal spray with thixotropic fluid properties and its preparation method provided by the invention application number CN2016106682925, its Mometasone furoate The content of metasone is low, and because the preparation process of lipid liquid crystal nanoparticles is not adopted, the nasal spray developed has a certain effect, but the effect is not strong, the duration of drug effect is short, and frequent medication is required every day, thus forming a certain drug Dependence; the selected wetting agent Tween-80 and moisturizing agent glycerin, the moisturizing effect has not reached the best level
Another example is the ibuprofen cubic liquid crystal precursor solution provided by the invention application number CN2016111796080, the cubic liquid crystal nanoparticles and the preparation method thereof, the fatty acid glyceride used contains unsaturated monoglyceride, and a certain concentration of unsaturated monofatty acid Glycerides can cause hemolysis in animals, and there are certain risks when using them; because the physical and chemical properties of ibuprofen and mometasone furoate are different, and the preparation method of this patent is to add water and stir all the raw materials together, then perform ultrasonic crushing and high-pressure homogenization , the particle size of the formed liquid crystal nanoparticles is not applicable to the present invention, and a new preparation method needs to be re-studied

Method used

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  • Nasal nano-preparation mometasone furoate liquid crystal gel nanoparticle and preparation method thereof

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Embodiment 1

[0025] This embodiment provides a nasal cavity nano-preparation mometasone furoate liquid crystal gel nanoparticles, including raw materials: mometasone furoate 0.09wt%, diacylglycerol 50wt%, soybean lecithin 20wt%, polysorbate-80 5wt%, absolute ethanol 5wt%, deionized water 19.91wt%.

[0026] The preparation method of the nasal cavity nano-preparation mometasone furoate liquid crystal gel nanoparticles provided in this embodiment comprises the following steps:

[0027] S1. Weigh mometasone furoate, diacylglycerol, soybean lecithin, polysorbate-80, heat and stir at 30-45°C to obtain a mixed solution;

[0028] S2. Add anhydrous solvent to the mixed solution obtained in S1, and perform ultrasonic dispersion for 3 to 5 minutes to obtain a clear and transparent liquid crystal gel nanoparticle precursor solution;

[0029] S3. Add deionized water to 100wt% in the liquid crystal nanoparticle gel precursor solution obtained in S2, and then further disperse through a high-shear homoge...

Embodiment 2

[0031] This embodiment is basically the same as Embodiment 1, the difference lies in the following aspects:

[0032] A nasal cavity nano-preparation mometasone furoate liquid crystal gel nanoparticles, comprising raw materials: mometasone furoate 0.06wt%, diacylglycerol 30wt%, soybean lecithin 30wt%, polysorbate-80 15wt%, anhydrous Ethanol 15wt%, deionized water 9.94wt%.

Embodiment 3

[0034] This embodiment is basically the same as Embodiment 1, the difference lies in the following aspects:

[0035] A nasal cavity nano-preparation mometasone furoate liquid crystal gel nanoparticles, comprising raw materials: mometasone furoate 0.08wt%, diacylglycerol 40wt%, soybean lecithin 25wt%, polysorbate-80 10wt%, anhydrous Ethanol 10wt%, deionized water 14.92wt%.

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Abstract

The invention discloses a nasal nano-preparation mometasone furoate liquid crystal gel nanoparticle and a preparation method thereof. The nanoparticle consists of 0.06-0.09wt% of mometasone furoate, 30-50wt% of a liquid crystal material, 20-30wt% of phosphatidylcholine, 5-15wt% of a surfactant, 5-15wt% of a solvent and 0-40wt% of de-ionized water. The preparation method of the liquid crystal gel nanoparticle comprises the following steps: firstly, uniformly mixing all raw materials except for the solvent and the de-ionized water, and adding the solvent and promoting dispersion; and then, adding the water, and implementing further dispersion via a high shear homogenizer or ultrasonic wave, so that a finished product (the liquid crystal gel nanoparticle) is obtained. The prepared mometasonefuroate liquid crystal gel nanoparticle is small in particle size, high in encapsulation efficiency, good in medicine absorption rate, good in sustained release effect and good in therapeutic effect;and the liquid crystal gel nanoparticle is obvious curative effect on allergic rhinitis and bacterial rhinitis.

Description

technical field [0001] The invention belongs to the field of gel nano preparations, in particular to a nasal cavity nano preparation mometasone furoate liquid crystal gel nanoparticles and a preparation method thereof. Background technique [0002] Mometasone furoate is a synthetic glucocorticoid with anti-inflammatory and anti-allergic effects. It is widely used in skin inflammation and Itchy skin. [0003] Lipid liquid crystal nanoparticle refers to a nanoparticle with a certain concentration of amphiphilic lipid material and surfactant dispersed in aqueous solution to self-assemble into a honeycomb or sponge structure containing double continuous water channels and closed lipid bilayers. The system is based on the cubic lattice as the structural unit. There are tiny pores (5-10nm) in the cubic lattice. It contains two bicontinuous water channels that are not connected to each other. It is closed, with double continuous water channels and closed lipid bilayers extending ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K9/14A61K47/14A61K47/26A61K31/58A61P29/00A61P37/08A61P17/00A61P25/00A61P17/08A61P17/06A61P17/04A61P11/02A61P31/04
CPCA61K9/0043A61K9/06A61K9/145A61K31/58A61K47/14A61K47/26
Inventor 罗亮黄丽萍孟凡玲
Owner 武汉百纳礼康生物制药有限公司
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