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Melatonin (MT) flexible liposome as well as preparation method and application thereof

A flexible liposome and melatonin technology, applied in the field of medicine, can solve the problems of low solubility, low absorption and availability, and limited absorption, and achieve the effects of good biocompatibility, improved bioavailability, and reduced dosage.

Active Publication Date: 2020-06-26
SHANDONG FIRST MEDICAL UNIV & SHANDONG ACADEMY OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Oral administration is usually used to supplement melatonin, but due to the first-pass effect of the liver, most of the drugs are degraded by the liver, and very little can be utilized by the human body
Moreover, the half-life of melatonin in the body is short, and its solubility is low and unstable, which limits its absorption in the body and affects the curative effect of common preparations of melatonin.
In addition, long-term oral melatonin can cause anxiety, restlessness, irritability, and suspicious situations
Therefore, to develop a new melatonin dosage form to change the way of oral administration, so as to solve the problems of strong first-pass effect of melatonin in the liver, low absorption and utilization, and large side effects, is a problem that needs to be solved at present.

Method used

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  • Melatonin (MT) flexible liposome as well as preparation method and application thereof
  • Melatonin (MT) flexible liposome as well as preparation method and application thereof
  • Melatonin (MT) flexible liposome as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] A flexible liposome of melatonin, prescribed for:

[0054] 18.90mg, lecithin 80.00mg, cholesterol 20.00mg, sodium deoxycholate 18.91mg.

[0055] Preparation:

[0056] Precisely weigh the prescribed amount of melatonin, lecithin, cholesterol and sodium deoxycholate and place them in a round bottom flask, add 10mL chloroform and 10mL absolute ethanol to dissolve them in a water bath ultrasonically, place them on a rotary evaporator at 40°C to reduce Press rotary evaporation until the organic solvent evaporates to dryness and form a thin film on the bottle wall, then add 10mL distilled water and continue vacuum rotary evaporation for 1 hour to make it fully hydrated, and finally use an ultrasonic cell pulverizer to sonicate for 15 minutes to obtain melatonin flexible liposomes .

Embodiment 2

[0058] A flexible liposome of melatonin, prescribed for:

[0059] 15.00mg, lecithin 75.00mg, cholesterol 25.00mg, sodium deoxycholate 15.00mg.

[0060] Preparation:

[0061] Precisely weigh the prescribed amount of melatonin, lecithin, cholesterol and sodium deoxycholate and place them in a round bottom flask, add 10mL chloroform and 10mL absolute ethanol to dissolve them in a water bath ultrasonically, place them on a rotary evaporator at 40°C to reduce Press rotary evaporation until the organic solvent evaporates to dryness and form a thin film on the bottle wall, then add 10mL distilled water and continue vacuum rotary evaporation for 1 hour to make it fully hydrated, and finally use an ultrasonic cell pulverizer to sonicate for 15 minutes to obtain melatonin flexible liposomes .

[0062] Example 2

[0063] A flexible liposome of melatonin, prescribed for:

[0064] 25.00mg, lecithin 85.00mg, cholesterol 15mg, sodium deoxycholate 15.00mg.

[0065] Preparation:

[0066]...

Embodiment 4

[0068] A flexible liposome of melatonin, prescribed for:

[0069] 10.00mg, lecithin 70.00mg, cholesterol 10.00mg, sodium deoxycholate 30.00mg.

[0070] The preparation method is the same as in Example 1.

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Abstract

The invention belongs to the technical field of medicine and particularly relates to a melatonin (MT) flexible liposome as well as a preparation method and application thereof. The MT flexible liposome is prepared from the following raw materials in parts by weight: 10-30 parts of MT, 70.00-90.00 parts of lecithin, 10-30 parts of cholesterol and 10-30 parts of sodium deoxycholate. The MT flexibleliposome has a better percutaneous permeation effect. Pharmacokinetic experiment results of rats show that the AUC of the flexible liposome is 1.82 times higher than that of ordinary liposome, indicating that the flexible liposome can improve the biocompatibility of percutaneous absorption of the MT. Pharmacodynamic experiment results of mice indicate that the external flexible liposome has an anti-photoaging effect. The flexible liposome enters a human body via skin and changes structures of stratum corneum lipid and keratin and can resist skin injury caused by ultraviolet sunburn.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a flexible liposome of melatonin and its preparation method and application. Background technique [0002] Melatonin (Melatonin, MT), also known as pineal gland, is commonly known as the "melatonin" of the human body. Its chemical structural formula is N-acetyl-5-methoxytryptamine, and its molecular formula is C13N2H16O2. It can be secreted by animals and plants. A hormone with antioxidant activity. In the human body, melatonin is a compound secreted by the pineal gland in the human brain. It can resist oxidation, adjust the rhythm of sleep and wakefulness, help improve sleep, enhance human immunity, maintain the balance of the internal environment of the body and improve the body's defense. ability; and can act on the secretion system to delay aging, maintain the zinc content in the blood, and resist tumor diseases and cardiovascular and cerebrovascular diseases. ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/4045A61P17/18A61P17/16A61P17/00A61K8/49A61K8/14A61Q19/08A61Q17/04
CPCA61K9/127A61K9/1277A61K9/0014A61K31/4045A61P17/18A61P17/16A61P17/00A61K8/492A61K8/14A61Q19/08A61Q17/04A61K2800/522Y02A50/30
Inventor 侯雪芹张萌张汉霆
Owner SHANDONG FIRST MEDICAL UNIV & SHANDONG ACADEMY OF MEDICAL SCI
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