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Percutaneous absorption composition and use thereof in preparation of percutaneous absorption preparation

A composition and preparation technology, which is applied in the field of transdermal drug delivery preparations, can solve the problems of limited permeation enhancement effect, achieve the effects of reducing toxic side effects and skin irritation, improving stability and prolonging release

Active Publication Date: 2018-10-23
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] However, this method also has certain limitations. It is more suitable for some pharmaceutical or cosmetic active ingredients with relatively small molecular weight and good stability. still relatively limited

Method used

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  • Percutaneous absorption composition and use thereof in preparation of percutaneous absorption preparation
  • Percutaneous absorption composition and use thereof in preparation of percutaneous absorption preparation
  • Percutaneous absorption composition and use thereof in preparation of percutaneous absorption preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] (1) Pre-treatment of pigskin: take fresh pigskin, remove the subcutaneous fat layer, shave the pig hair to a length no longer than 2mm, and use it immediately or freeze it at -20°C to -80°C for later use.

[0052] (2) Preparation of flexible nanoliposomes: phospholipid 90G (100mg / ml), surfactant polyoxyethylene (20) oleyl ether (100mg / ml) and methanol / chloroform=1:1 were added to the In a round flask, it was evaporated to dryness by a rotary evaporator to form a uniform film on the bottom surface of the round flask. Then add 1 to 5 ml of ANTS-Fucoidan (fucoidan) drug solution, and perform hydration by shaking / ultrasound and other steps. Use the imported special extrusion device for liposomes, squeeze 21 times, and finally transfer to a new EP tube to obtain ANTS-Fucoidan flexible nano-liposome solution of 1-100 mg / ml, ready for use.

[0053] (3) Preparation of sponge spicule solution: add a certain amount of PBS phosphate buffer saline, deionized water, normal saline o...

Embodiment 2

[0059] (1) Pretreatment of pigskin: with embodiment 1.

[0060] (2) Preparation of ordinary nanoliposomes: add phospholipid 90G (100mg / ml) and methanol / chloroform=1:1 into a round flask in a certain ratio, evaporate to dryness by a rotary evaporator, and make it in a round shape Form a uniform film on the bottom surface of the flask; then add 1 to 5ml of FITC-Hyaluronic acid (hyaluronic acid) drug solution, hydrate through oscillation / ultrasound and other steps, use imported liposome special extrusion device, and squeeze 21 times , and finally transferred to a new EP tube to obtain a 1-100 mg / ml FITC-Hyaluronicacid common nanoliposome solution for use.

[0061] (3) Preparation of flexible nanoliposomes: similar to Example 1.

[0062] (4) Preparation of sponge spicule solution: same as Example 1.

[0063] (5) In vitro skin penetration test: similar to Example 1. Add 150 μL of FITC-Hyaluronic acid (average molecular weight: 250KDa) solution containing 1 to 100 mg / ml, or FITC-...

Embodiment 3

[0071] (1) Pretreatment of pigskin: with embodiment 1.

[0072] (2) Preparation of solid lipid nanoparticles: prepared with reference to conventional techniques in the art.

[0073] (3) Preparation of sponge spicule solution: same as in Example 1.

[0074] (4) In vitro transdermal test: carried out with reference to Example 1. The results showed that the spongy spicules combined with solid lipid nanoparticles had obvious penetration-promoting effect compared with other groups.

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Abstract

A percutaneous absorption composition comprising a sponge bone needle and nanoparticles, and uses thereof in the preparation of a percutaneous absorption preparation are disclosed. Release of active ingredients of drugs or cosmetics is prolonged by utilizing the slow and controlled release characteristics of various nanoparticles, the stability of the active ingredients of drugs or cosmetics is improve, and toxic side effects and skin irritation of the active ingredients of drugs or cosmetics are reduced while the percutaneous absorption composition overcomes the skin stratum corneum barriers.

Description

technical field [0001] The present invention relates to the field of transdermal drug delivery preparations, in particular to a transdermal absorption composition and its application in the preparation of transdermal absorption preparations. Sponge spicules, as a skin physical penetration enhancer, are synergistic with different types of nano-medicines effect, thereby greatly increasing the application of drugs and active ingredients in skin drug delivery systems. Background technique [0002] The skin is the largest organ in the human body and the most direct route of drug delivery. Compared with other routes of administration (such as: oral administration, injection, etc.), skin administration has many unique advantages, including avoiding the first-pass effect of the liver, damage to the gastrointestinal tract, and infection and infection caused by injection. Pain, etc.; at the same time, it can also directly act on local skin lesions, and can be administered in a sustai...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/51A61K47/46A61K8/02A61K8/11A61K8/98A61M37/00A61Q19/00
CPCA61K8/0204A61K8/11A61K8/987A61K9/0021A61K9/51A61K47/46A61K2800/10A61M37/0015A61M2037/0053A61Q19/00
Inventor 陈铭王德祥刘春云张赛曼张驰
Owner XIAMEN UNIV
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