Application of phospholipid-Vitamin E tocopherol acid polyethylene glycol succinate micelle

A technology of polyethylene glycol ester and polyethylene glycol succinate, applied in the field of water-soluble micelle freeze-dried water-soluble powder, can solve the problems of insufficient stability of vesicles and micelles, small molecular weight of phospholipids, and application limitations. , to achieve the effect of simple and operable preparation process, reducing the degree of densification, increasing stability and safety

Inactive Publication Date: 2013-06-12
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the molecular weight of phospholipids is small, and the stability of the formed vesicles and micelles is not enough, so the application as long-circulation and sustained-release materials is greatly limited.

Method used

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  • Application of phospholipid-Vitamin E tocopherol acid polyethylene glycol succinate micelle
  • Application of phospholipid-Vitamin E tocopherol acid polyethylene glycol succinate micelle
  • Application of phospholipid-Vitamin E tocopherol acid polyethylene glycol succinate micelle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Prescription: Phospholipids 40mg, TPGS2000mg

[0022] Preparation process: Dissolve 40 mg of phospholipids and 2000 mg of vitamin E polyethylene glycol succinate in 50 ml of ethanol, stir for 30 minutes to mix evenly, slowly pour into distilled water, heat and rotary steam to recover ethanol, and obtain a mass ratio of 1:50 A solution of phospholipid-tocopherol polyethylene glycol succinate mixed micelles. The reacted solution was pre-frozen in a -20°C refrigerator for 12 hours, quickly transferred into a freeze dryer, and freeze-dried under vacuum for 48 hours to obtain phospholipid-TPGS micellar water-soluble powder with a mass ratio of 1:50.

Embodiment 2

[0024] Prescription: Phospholipids 50mg, TPGS2000mg

[0025] Preparation process: Dissolve 50 mg of phospholipids and 2000 mg of vitamin E polyethylene glycol succinate in 50 ml of ethanol, stir for 30 minutes to mix evenly, slowly pour into distilled water, heat and rotary steam to recover ethanol, and obtain a mass ratio of 1:40 Phospholipid-TPGS mixed micelles. The reacted solution was pre-frozen in a -20°C refrigerator for 12 hours, quickly transferred into a freeze dryer, and freeze-dried under vacuum for 48 hours to obtain phospholipid-TPGS micellar water-soluble powder with a mass ratio of 1:40.

[0026] Prescription: Phospholipids 60mg, TPGS 1800mg

[0027] Preparation process: Dissolve 60 mg of phospholipids and 1800 mg of vitamin E polyethylene glycol succinate in 50 ml of ethanol, stir for 30 minutes to mix evenly, slowly pour into distilled water, heat and rotary steam to recover ethanol, and obtain a mass ratio of 1:30 Phospholipid-TPGS mixed micelles. The reac...

Embodiment 4

[0029] Prescription: Phospholipids 90mg, TPGS 1800mg

[0030]Preparation process: Dissolve 90 mg of phospholipids and 1800 mg of vitamin E polyethylene glycol succinate in 50 ml of ethanol, stir for 30 minutes to mix evenly, slowly pour into distilled water, heat and rotary steam to recover ethanol, and obtain a mass ratio of 1:20 Phospholipid-TPGS mixed micelles. The reaction mixture was placed on a rotary evaporator, and the reaction solvent was evaporated under reduced pressure at 40° C., and the residue was dried under reduced pressure overnight at room temperature to obtain phospholipid-TPGS water-soluble powder with a mass ratio of 1:20.

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Abstract

The invention discloses an application of a transdermal enhancer with phospholipid and Vitamin E tocopherol acid polyethylene glycol succinate (TPGS) micelle as medicines or functional compositions of cosmetics. A cuticle of a skin epidermis has a multi-layer compact film structure and consists of cuticle cells and lipid compositions among the cuticle cells, the cuticle cells and the lipid compositions together form a compact barrier to prevent influences from the external factors such as the medicines, and therefore, transdermal absorption of the cosmetic compositions needs to overcome the barrier function of the cuticle. According to the application disclosed by the invention, an ethanol injection method is adopted on the phospholipid and the TPGS with a certain proportion to prepare a water soluble micelle, and the water soluble micelle is frozen and dried to prepare a phospholipid-TPGS water soluble powder; the phospholipid-TPGS water soluble powder is self assembled into nano-micelle with the average grain diameter being about 25nm after being dissolving into water and can enter the internals of skin cuticle cells to mutually react with keratin, so that the compact degree of the cuticle cells is lowered, and meanwhile, the phospholipid carried by the nano-micelle can form a lipid channel; and the stability of the micelle is very good, and the micelle has better transdermal promotion effect on various functional compositions of the cosmetics.

Description

technical field [0001] The present invention relates to the application of a phospholipid-vitamin E polyethylene glycol succinate micelle in the preparation of a penetration enhancer for promoting the transdermal absorption of functional components, in particular to a mixture of phospholipid and vitamin E polyethylene glycol succinate Water-soluble micelles freeze-dried water-soluble powder. Belonging to the pharmaceutical or cosmetic field. Background technique [0002] Micelle (micelles) is a thermodynamically stable system, which is widely used to solubilize poorly soluble drugs and improve bioavailability. Micelles have been used in pharmacy for the solubilization of insoluble drugs for a long time. After solubilization, the drug can reach the concentration required for clinical treatment. After the surfactant is placed in the solution, it will quickly reduce the interfacial tension of the solution, but as the amount increases, the concentration of surfactant molecules...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K9/19A61K47/34A61K47/24A61K47/22A61K8/02A61K8/06A61K8/86A61K8/67A61K8/55
Inventor 吕慧侠张振海程凤仪周建平
Owner CHINA PHARM UNIV
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