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A kind of melatonin nano composition and its preparation method and application

A nano-composition, melatonin technology, applied in the direction of drug combination, pharmaceutical formula, food science, etc., can solve the problems of easy crystallization of melatonin, low oral bioavailability, poor skin permeability, etc., to achieve excellent Skin permeability, process is easy to control, and the effect of fast skin absorption

Active Publication Date: 2019-08-23
刘卫 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Oral melatonin products have significant hepatic "first-pass effect" and low oral bioavailability
At present, there are a small amount of commercially available skin care products that directly add melatonin. However, because melatonin is a highly crystalline substance with low solubility and poor water dispersibility, the content of melatonin in commercially available skin care products is low, and the skin penetrates Poor performance, difficult to effectively play its role
At the same time, melatonin is easy to crystallize and precipitate during the placement process of ordinary preparations, and the placement stability is poor.

Method used

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  • A kind of melatonin nano composition and its preparation method and application
  • A kind of melatonin nano composition and its preparation method and application
  • A kind of melatonin nano composition and its preparation method and application

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preparation example Construction

[0033] The present invention provides the preparation method of above-mentioned melatonin nano composition, comprises the following steps:

[0034] (1) dissolving melatonin, emulsifier, co-emulsifier and liquid lipid to obtain an oil phase;

[0035] (2) Stirring and dissolving the stabilizer, humectant and water, and filtering the obtained solution to obtain an aqueous phase;

[0036] (3) mixing the water phase obtained in the step (2) with the oil phase obtained in the step (1) while stirring, to obtain the melatonin nano composition of the present invention;

[0037] (4) The finished product is obtained after filtering the melatonin nanoemulsion obtained in the step (3);

[0038] There is no time sequence limitation between the steps (1) and (2).

[0039] The invention dissolves melatonin, emulsifier, co-emulsifier and liquid lipid to obtain oil phase. In the present invention, the temperature of the dissolution is preferably 35-80°C, more preferably 38-70°C, further pref...

Embodiment 1

[0049] Dissolve 0.1% melatonin, 1.0% Tween 60, 2.0% polyoxyethylene castor oil-20, 15.0% propylene glycol, and 1.0% isopropyl myristate in a water bath at 35°C to obtain an oil phase for later use;

[0050] Add 0.05% hydroxypropylmethylcellulose and 4.0% allantoin to 76.85% water, stir at 15 rpm for 10 min in a water bath at 35°C, filter through a 0.45 μm microporous membrane to obtain the water phase, and set aside ;

[0051] Add the water phase to the oil phase, stir in a water bath at 35° C. at a speed of 15 rpm for 10 minutes, and then filter through a 0.45 μm microporous membrane to obtain a finished melatonin nano composition.

[0052] The particle size of the melatonin nanocomposition is detected, and the particle size of the melatonin nanocomposition is 10.8nm.

Embodiment 2

[0054] 1.0% melatonin, 2.0% Tween 40, 2.0% polyoxyethylene castor oil-30, 1.0% polyethylene glycol 400 monoglyceride, 5.0% dipropylene glycol, 11.0% 1,2-hexanediol, 3.0 % polyethylene glycol, 3.0% 1,2-pentanediol, 1.0% isopropyl palmitate, 2.0% caprylic capric macrogolglyceride, dissolved in a water bath at 50°C to obtain an oil phase, set aside;

[0055] Add 0.1% polyvinylpyrrolidone, 1.0% ethyl tyrosine hydrochloride, 0.5% chitosan, and 2.0% vitamin B5 to 65.4% water, stir at 30 rpm for 15 min in a water bath at 50 ° C, and use 0.45 μm microporous membrane filtration to obtain the aqueous phase, set aside;

[0056] Add the water phase to the oil phase, stir in a water bath at 50° C. at a speed of 30 rpm for 10 min, and then filter through a 0.45 μm microporous membrane to obtain a finished melatonin nano composition.

[0057] The particle size of the melatonin nanocomposition is detected, and the particle size of the melatonin nanocomposition is 25.5nm.

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Abstract

The invention relates to the preparation preparing technical field, and discloses a melatonin nano-composition, and a preparing method and an application thereof. The melatonin nano-composition comprises the following components by the mass percentage: 0.1%-8.0% of melatonin, 2.0%-12.0% of an emulsifier, 10.0%-50.0% of a coemulsifier, 1.0%-10.0% of liquid lipid, 0.01%-5.0% of a moisturizing agent, 0.01%-5.0% of a stabilizer, and the balance water. The melatonin nano-composition provided by the invention has the advantages of large drug loading amount, high stability and good safety, can efficiently promote melatonin to penetrate skin, and has the good whitening, abirritative and sleep-improving efficacies. Meanwhile, the preparing method is simple and easy to control, and is suitable for industrialized production.

Description

technical field [0001] The invention relates to the field of preparation preparation, in particular to a melatonin nano composition for whitening, calming and improving sleep. Background technique [0002] Melatonin is a natural indole hormone secreted from the "pineal gland", which is as big as a pinecone, deep in the brain of mammals, known as "pineal gland". According to research, melatonin can hinder the growth of human melanocytes, inhibit the activity of tyrosinase to reduce melanin, and promote cell metabolism; protect the cell structure by scavenging free radicals, anti-oxidation and inhibiting lipid peroxidation. Prevent injury, reduce the content of peroxide in the body, have obvious protective effect on the damage caused by exogenous poisons, and have a wide range of physiological activities to participate in activities such as sedation, hypnosis, analgesia and immune effects. [0003] Oral melatonin has a significant hepatic "first-pass effect" and low oral bioa...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4045A61K8/49A23L33/10A61Q19/00A61Q19/02A61P25/20
Inventor 许琦闻庆刘卫郭凤凤吕萌钮元良杨达峰
Owner 刘卫