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Ofloxacin liquid crystal gel nano-particle eye drop and preparation method thereof

An ofloxacin and nanoparticle technology, applied in the field of ofloxacin liquid crystal gel nanoparticle eye drops and preparation thereof, can solve the problems of poor effect, poor biological sensation, and high viscosity of eye drops, and achieves therapeutic effect. Better results, less discomfort, less side effects

Active Publication Date: 2018-07-24
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

The problem of common ofloxacin eye drops is obvious. Because its main active ingredient (ie levofloxacin) is very water-soluble, after being dropped into the eye, the first contact is the corneal epithelium with high hydrophobicity. According to similar According to the principle of compatibility, the active ingredients of the drug will be prevented from moving into the eye and entering the eye, so as to flow out quickly; for this reason, some patients have to repeatedly use eye drops in large quantities in order to achieve better therapeutic effects, resulting in The consequences of adverse reactions are also serious, and the effect is not ideal; those skilled in the art try to increase the viscosity of the solution by adding an appropriate amount of thickening substances in the eye drops, thereby indirectly increasing the residence time of the drug in the eye, but the effect bad
However, the eye drops disclosed by the present invention have high viscosity and poor biological sense, so continuous improvement is still needed.

Method used

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  • Ofloxacin liquid crystal gel nano-particle eye drop and preparation method thereof
  • Ofloxacin liquid crystal gel nano-particle eye drop and preparation method thereof
  • Ofloxacin liquid crystal gel nano-particle eye drop and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0063] This embodiment provides a kind of ofloxacin liquid crystal gel nanoparticle eye drops, which is prepared from the following components: 0.12% ofloxacin, 20% glycerol dioleate, 50% soybean lecithin Acylcholine, 8% polysorbate 80, 5% ethanol, 0.35% sodium hyaluronate, and the rest are water for injection.

[0064] A kind of preparation method of ofloxacin liquid crystal gel nanoparticle eye drops provided by the present embodiment comprises the following steps:

[0065] S1. Weigh soybean phosphatidylcholine and glycerol dioleate, add polysorbate 80 and ethanol respectively, stir evenly, and obtain the oil phase;

[0066] S2. Drop the oil phase obtained in S1 into a small amount of water for injection, stir and disperse evenly;

[0067] S3. Add active ingredient ofloxacin to the mixed solution of S2, stir evenly to obtain a coarse dispersion;

[0068] S4. Rotate and mix the coarse dispersion formed in S3, and place it overnight;

[0069] S5. Add the mixed solution of S...

Embodiment 2

[0072] This embodiment is basically the same as Embodiment 1, the difference lies in the following aspects:

[0073] A kind of ofloxacin liquid crystal gel nanoparticle eye drops, prepared from the following components: 0.2% ofloxacin, 50% glycerol dioleate, 20% soybean phosphatidylcholine, 5 % polysorbate 80, 7% mixture of ethanol and propylene glycol, 0.28% sodium hyaluronate, and the rest is water for injection.

Embodiment 3

[0075] This embodiment is basically the same as Embodiment 1, the difference lies in the following aspects:

[0076] A kind of ofloxacin liquid crystal gel nano particle eye drop is prepared from following components: 0.16% ofloxacin, 25% glycerol dioleate, 45% soybean phosphatidylcholine, 10 80% polysorbate, 6% propylene glycol, 0.32% sodium hyaluronate, and the rest are water for injection.

[0077] The power of the ultrasonic probe used in S5 is 40W, and the ultrasonic dispersion time is 5min.

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Abstract

The invention relates to an ofloxacin liquid crystal nano-particle eye drop and a preparation method thereof. The ofloxacin liquid crystal nano-particle eye drop is prepared from 0.12-0.2% of ofloxacin, 20-50% of at least one neutral lipid and / or tocopherol, 20-50% of at least one phosphatidylcholine, 0.2-20% of a nonionic surfactant, 0.1-10% of at least one solvent, 0.28-0.35% of at least one thickener, and the balance of injection water. The liquid crystal gel nano-particle has a small and uniform particle size, so the endocytosis and the transport of cells are benefited; and the unique adhesion and the liquid crystal phase structure of the liquid crystal gel are used to prolong the retention time of drug active ingredients in eyes and effectively control the release of an entrapped substance, so the bioavailability is improved. Additionally, the preparation method of the ofloxacin liquid crystal gel nano-particle eye drop has the advantages of simple process steps, easiness in industrial large-scale production, and low production cost.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to an ofloxacin liquid crystal gel nano particle eye drop and a preparation method thereof. Background technique [0002] With the development of science and technology, more and more electronic products appear in people's lives, and prolonged exposure to electronic products can easily cause dry eye syndrome, keratitis, etc. Big data shows that corneal disease blindness has become one of the main causes of blindness in my country, among which infectious keratitis ranks first. [0003] Today, many eye conditions are still treated with traditional pharmaceutical preparations such as eye drops or ointments. However, due to the particularity of the physiological structure of the eye (such as tear film renewal, corneal permeability and other factors), it is difficult to achieve effective concentrations of eye drugs, and the bioavailability of drugs is too low, resulting in uns...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/5383A61K9/51A61K47/24A61P27/02A61P31/04A61P31/02A61P31/10
CPCA61K9/0048A61K9/08A61K9/5123A61K31/5383
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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