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A kind of zeaxanthin dipalmitate liposome eye drops and preparation method thereof

A technology of palmitate and zeaxanthin, which is applied in liposome delivery, pharmaceutical formulations, active ingredients of esters, etc., can solve the problems of different, unclear use effects, no safety testing and efficacy verification, etc., to achieve the effect Diversification, enhanced bioavailability, enhanced ability to resist changes in external conditions

Active Publication Date: 2022-07-15
宁夏全通枸杞供应链管理股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Chinese invention patent (patent application number 201810471700.7, publication number CN110496170A, application date: 2018-05-17), the title of the invention is "an eye protection solution for preventing myopia", which discloses an eye drop, which is mainly used For the prevention of myopia, the effect of the present invention is obviously different; and the patent has not carried out relevant safety testing and efficacy verification, making the final use effect unclear

Method used

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  • A kind of zeaxanthin dipalmitate liposome eye drops and preparation method thereof
  • A kind of zeaxanthin dipalmitate liposome eye drops and preparation method thereof
  • A kind of zeaxanthin dipalmitate liposome eye drops and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0048] Dissolve zeaxanthin dipalmitate with a small amount of absolute ethanol (see attached for the structural formula) figure 1 ) 20mg, Tween 800.5mg and compound lecithin 400mg, steamed under reduced pressure to form a film; Measure 10mL of water for injection and preheat at 50°C; under the same conditions, add water for injection for hydration, and ultrasonicate to the solution after complete dissolution Uniform clarification, 0.22 μm filter sterilization to obtain 2 mg / mL zeaxanthin dipalmitate liposomes (attached figure 2 ), and its particle size distribution is shown in the appendix image 3 . Then, zeaxanthin dipalmitate liposomes were diluted to 1.6 mg / mL, 1.2 mg / mL, 0.8 mg / mL, 0.4 mg / mL with MEM medium containing double antibody and serum.

[0049] The compound lecithin described in the above embodiment 1 comprises egg yolk lecithin, anhydrous butter, and cholesterol, and the mass ratio thereof is 3:2:1.

Embodiment 2

[0051] Weigh the raw materials glycerol 0.05% and phenoxyethanol 0.20% by mass percentage and mix them on a magnetic stirrer, set the rotating speed to 800rpm and 35°C, dissolve and stir until uniform; Sodium phosphate 0.10%, panthenol 0.10%, vitamin B120.05%, vitamin B6 0.05% and sodium chloride 0.5% were added to the above raw materials in small amounts for several times, dissolved and stirred until uniform; the raw material zeaxanthin double palm was weighed by mass percentage Add 5.00% of ester liposome to the above-mentioned raw materials, stir until uniform to obtain a light yellow clear and transparent liquid, adjust the pH value of the liquid to 5.1-6.5 with boric acid, filter sterilize, and bottle, namely the zeaxanthin double palm Acetate liposome eye drops.

Embodiment 3

[0053] Weigh the raw material glycerol 0.05% and phenoxyethanol 0.20% by mass percentage and mix them on a magnetic stirrer, set the rotating speed to 800rpm and 35°C, dissolve and stir until uniform; weigh the raw material water for injection 88.95%, transparent Sodium phosphate 0.10%, panthenol 0.10%, vitamin B120.05%, vitamin B6 0.05% and sodium chloride 0.5% were added to the above raw materials in small amounts for several times, dissolved and stirred until uniform; the raw material zeaxanthin double palm was weighed by mass percentage Add 10.00% of ester liposome to the above-mentioned raw materials, stir until uniform to obtain a light yellow clear and transparent liquid, adjust the pH value of the medicinal liquid to 5.1-6.5 with boric acid, filter sterilize, and bottle, namely the zeaxanthin double palm Acetate liposome eye drops.

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Abstract

The invention utilizes liposome technology to prepare eye drops, and particularly relates to a formulation of zeaxanthin dipalmitate liposome eye drops and a preparation method thereof. A zeaxanthin dipalmitate liposome eye drop is prepared from the following raw materials by mass percentage: water for injection 78.00-94.00%, zeaxanthin dipalmitate liposome 5.00-25.00%, sodium hyaluronate 0.05-0.30% %, Panthenol 0.05‑0.15%, Boric Acid 0.05‑0.10%, Vitamin B12 0.01‑0.05%, Vitamin B60.01‑0.05%, Glycerol 0.01‑0.05%, Sodium Chloride 0.50‑0.70%, Phenoxyethanol 0.10‑0.30%. The eye drops of the present invention have relatively simple formula, good stability, and no irritation to human eyes. The zeaxanthin dipalmitate is encapsulated in liposomes, which fundamentally solves the problems of poor water solubility and low bioavailability, and can make It is easier to enter the corneal cells, reduce its leakage and increase its stability, fully realize the efficient delivery of zeaxanthin dipalmitate, and achieve the effect of brightening the purpose.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an eye drop using zeaxanthin dipalmitate liposome as a carrier and a preparation method thereof. Background technique [0002] As the primary sensory organ of human beings, the human eye processes a large amount of information and reads a large amount of words every day. Once the eyes are unhealthy and unhygienic, good work and rest habits cannot be developed, which is especially likely to cause various visual fatigue, dry and sore eyes, heavy eyelids, red and swollen eyes, blurred vision and other visual fatigue symptoms, which greatly trouble people's life and healthy. The reason is that the symptoms of fatigue are most prominently affected by the eyes themselves and environmental factors. In addition, the bad surrounding environment will also exacerbate the occurrence and development of visual fatigue symptoms. [0003] At present, the eye drop formulations on the...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/23A61K31/728A61K47/24A61K47/26A61K47/28A61P27/02A61P39/06A61K31/164A61K31/4415A61K31/714
CPCA61K31/23A61K9/0048A61K9/127A61K47/24A61K47/28A61K47/26A61P27/02A61P39/06A61K31/728A61K31/164A61K31/4415A61K31/714A61K2300/00
Inventor 李明媛李萌王珊珊贾琳包莉媛李媛王志遥谢焱博苏雯郁彭
Owner 宁夏全通枸杞供应链管理股份有限公司
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