KGM modified lecithin loaded NADH transdermal ethosome and preparation, as well as preparation process and application thereof

An ethosome and lecithin technology, applied in the field of biopolymer materials, can solve the problems of short biological half-life, limit potential applications, frequent administration, etc., and achieve high encapsulation efficiency, stable thermodynamic properties, and fast transdermal performance Effect

Active Publication Date: 2018-10-26
HOBOOMLIFE BIO TECH SHENZHEN CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its potential application is limited due to its poor stability at room temperature, short biological half-life, easy enzymatic degradation, and immunogenicity.
[0006] At present,

Method used

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  • KGM modified lecithin loaded NADH transdermal ethosome and preparation, as well as preparation process and application thereof
  • KGM modified lecithin loaded NADH transdermal ethosome and preparation, as well as preparation process and application thereof
  • KGM modified lecithin loaded NADH transdermal ethosome and preparation, as well as preparation process and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] This embodiment provides a KGM modified lecithin-loaded NADH transdermal ethosome, which consists of the following components in terms of mass percentage: 0.05% of NADH, 0.03% of konjac glucomannan, and 1% of phospholipid , cholesterol 0.02%, stabilizer 0.1%, antioxidant 0.1%, low molecular weight alcohol 5%, and the balance is water. Wherein, the konjac glucomannan (KGM) includes an equal amount of quaternized konjac glucomannan (QKGM) and carboxymethyl konjac glucomannan (CKGM), the phospholipid is soybean lecithin, and the The stabilizer is dicetyl phosphate, the antioxidant is vitamin C, and the low molecular weight alcohol is glycerol.

[0044] The KGM modified lecithin-loaded NADH transdermal protosome gel can be used for treating Alzheimer's disease, Parkinson's disease, muscular atrophy and antioxidant drugs, and can also be used for anti-aging, anti-inflammatory and sunscreen preparations.

[0045] This embodiment also provides a KGM modified lecithin-loaded N...

Embodiment 2

[0062] This embodiment provides a KGM-modified lecithin-loaded NADH transdermal ethosome, which consists of the following components in terms of mass percentage: 1% NADH, 10% konjac glucomannan, 10% phospholipids, Cholesterol 1%, stabilizer 0.5%, antioxidant 1%, low molecular weight alcohol 50%, and the balance is water. Wherein, the konjac glucomannan (KGM) comprises quaternized konjac glucomannan (QKGM) and chitosan (CS), the mass ratio of the two is 1:1, and the phospholipid is egg yolk lecithin, Described stabilizing agent is the mixture of phospholipid phthaloglycerol and phosphoric acid ester, and the mass ratio of the two is 1:2, and described antioxidant is the mixture of vitamin E, di-tert-butyl p-cresol, and the mass ratio of the two is 1:2. 1. The low molecular weight alcohol is ethanol.

[0063] The KGM modified lecithin-loaded NADH transdermal protosome gel can be used for treating Alzheimer's disease, Parkinson's disease, muscular atrophy and antioxidant drugs, ...

Embodiment 3

[0073] This embodiment provides a KGM modified lecithin-loaded NADH transdermal ethosome, which consists of the following components in terms of mass percentage: 5% NADH, 4.5% konjac glucomannan, 5% phospholipids, Cholesterol 0.5%, stabilizer 0.3%, antioxidant 0.5%, low molecular weight alcohol 30%, and the balance is water. Wherein, the konjac glucomannan (KGM) comprises a mixture of oxidized konjac glucomannan (OKGM) and quaternized konjac glucomannan (QKGM), the mass ratio of the two is 1:2, and the phospholipid It is hydrogenated soybean lecithin, the stabilizer is phosphatidyl phthaloserine, the antioxidant is a mixture of malic acid and β-carotene, the mass ratio of the two is 1:1, and the low molecular weight alcohol is n-butanol and A mixture of ethanol, the volume ratio of the two is 1:2.

[0074] The KGM modified lecithin-loaded NADH transdermal protosome gel can be used for the treatment of Alzheimer's disease, Parkinson's disease, muscular atrophy and antioxidant dr...

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Abstract

The invention discloses a KGM modified lecithin loaded NADH transdermal ethosome, belonging to the technical field of medicinal preparation production. The ethosome is prepared from the following components by weight percent: 1.05-1 percent of NADH, 0.03-10 percent of konjac glucomannan, 1-10 percent of phospholipids, 0.02-1 percent of cholesterol, 0.1-0.5 percent of a stabilizing agent, 0-1 percent of an antioxidant, 5-50 percent of low molecular weight alcohol and the balance of water. The ethosome can be used for solving the problems that NADH is easily enzymolysed, has short biological half-life period and poor stability, has a novel multi-cell vesicle structure having a spherical or spheroidal shape, has more stable thermodynamic property, smaller grain size and higher encapsulation efficiency, has more rapid and stronger transdermal performance and skin tolerance, so that the dosage can be reduced, occurrence of adverse reaction can be reduced, and safety can be improved. The invention further discloses gel containing the ethosome and a preparation process of the ethosome and gel. The gel has fine texture and good human body absorption, and the preparation process is simple,has mild condition, and is suitable for industrial volume production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparation production, and in particular relates to a KGM-modified lecithin-loaded NADH transdermal ethosome, a preparation, a preparation process and application thereof. Background technique [0002] The transdermal drug delivery system refers to a new dosage form that is administered on the skin surface, and the drug penetrates through each layer of the skin at a certain speed, and enters the blood circulation of the whole body of the human body from the capillaries to achieve an effective blood drug concentration and achieve systemic or local therapeutic effects. Compared with oral and intravenous injection, transdermal drug absorption is not affected by pH, food, transit time and other factors in the digestive tract, so it can avoid the liver and gastrointestinal first-pass effect and reduce the fluctuation of blood drug concentration , avoid drug stimulation to the gastrointestinal t...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/06A61K47/36A61K31/7076A61P25/28A61P25/16A61P21/00A61P39/06
CPCA61K9/0014A61K9/06A61K9/1271A61K31/7076A61K47/36A61P21/00A61P25/16A61P25/28A61P39/06
Inventor 王运刘喜元方秋杰陈娜叶小舟
Owner HOBOOMLIFE BIO TECH SHENZHEN CO LTD
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