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An external preparation for improving transdermal absorption of usnic acid and its application in promoting skin wound healing

An external preparation, the technology of usnic acid, which is applied in the field of external preparations, can solve the problems of small drug loading and difficulty in absorbing usnic acid, achieve good activity, improve the effect of promoting skin wound healing, and improve transdermal absorption

Active Publication Date: 2020-01-24
北京昊坤康源医疗科学技术发展有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0010] In order to overcome the problem that usnic acid is difficult to absorb and the drug load of the existing new drug delivery system of usnic acid is small, the present invention provides an external preparation for improving the transdermal absorption of usnic acid and promoting skin wound healing. The formula is usnic acid, egg yolk lecithin, carbomer 940, glycerol, triethanolamine, water

Method used

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  • An external preparation for improving transdermal absorption of usnic acid and its application in promoting skin wound healing
  • An external preparation for improving transdermal absorption of usnic acid and its application in promoting skin wound healing
  • An external preparation for improving transdermal absorption of usnic acid and its application in promoting skin wound healing

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] The preparation of embodiment 1 usnic acid different lipid carrier transdermal gel preparation

[0026] 1. Sample Preparation

[0027] 1.1 Preparation of usnic acid phospholipid complex gel

[0028] 1.1.1 Effect of different elution solvents on the recombination rate of phospholipid complexes

[0029] The reaction time, the mass concentration of usnic acid, the ratio of usnic acid to phospholipids, and the reaction temperature were fixed, and the effects of different types of elution solvents on the recombination rate were investigated. The results are shown in Table 1.

[0030] Table 1: Effects of different elution solvents on the recombination rate of phospholipid complexes

[0031]

[0032]

[0033] The experimental results show that acetone is the best elution solvent.

[0034] 1.1.2 Effect of different reaction solvents on the recombination rate of phospholipid complexes

[0035] The elution solvent, mass concentration of usnic acid, reaction time, usnic ...

Embodiment 2

[0088] The in vitro transdermal absorption measurement of embodiment 2 usnic acid different lipid carrier gels

[0089] 1 Test method

[0090] The skin used for in vitro percutaneous penetration experiments is preferably isolated human skin from the site of clinical administration, but human skin is not only difficult to obtain, but also difficult to maintain consistent conditions, so suitable animal skin is often used instead . In this study, mouse skin and medium-sized rabbit skin were used for the in vitro transdermal determination of different lipid carrier preparations of usnic acid.

[0091] 1.1 Preparation of main reagents

[0092] 1.1.1 pH 7.4 Phosphate Buffer: Accurately weigh 1.36g of potassium dihydrogen phosphate, add 79mL of 0.1mol / L sodium hydroxide solution, shake gently, mix well, add purified water to dilute to 200mL.

[0093] 1.1.2 Physiological saline: Accurately weigh 0.90g of sodium chloride, add purified water to make up to 100mL.

[0094] 1.1.3 Mobil...

Embodiment 3

[0151] The active investigation of each preparation of embodiment 3 usnic acid to skin healing

[0152] Establishment of skin injury model: 70 SD rats, weighing 180-220g, male and female, rats were intraperitoneally anesthetized with 1% pentobarbital sodium (30mg / kg), electric clippers were used on the back, and 10% sodium sulfide was depilated , after the skin was disinfected with strong iodine, a special punch was used to cut the back of the rat with a diameter of about 1.2 cm and an area of ​​1.44 cm. 2 2 wounds in the hospital, the circular full-thickness excision of the skin was performed, and the bleeding was stopped to form an animal model of mechanical injury. All rats were fed in single cages and provided with sufficient water. 10 animals in each group, 20 wounded surfaces. In the first group of normal saline blank control group, 100 μL / d normal saline was applied to the wound surface; in the second group, the UA control group was administered (UA dissolved, 2g / 10ml ...

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Abstract

The invention aims to solve the problems of difficulty in absorbing usnic acid and small drug loading capacity of the conventional usnic acid novel dosing system, and provides an external preparation for improving transdermal absorption of usnic acid and promoting skin injury healing. A formula of the external preparation comprises the usnic acid, egg yolk lecithin, carbomer 940, glycerol, triethanolamine and water. By adopting the external preparation for improving transdermal absorption of the usnic acid and promoting skin injury healing provided by the invention, the technical problems of poor usnic acid solubility and small drug loading capacity of the conventional usnic acid novel dosing system are solved. Meanwhile, the invention provides a technical scheme of applying the usnic acid to the external preparation, thereby providing a novel usnic acid dosing manner. Moreover, usnic acid phospholipid compound gel has high activity on the aspect of promotion of skin injury healing.

Description

technical field [0001] The invention relates to an external preparation, in particular to an external preparation for improving transdermal absorption of usnic acid and application thereof. [0002] technical background [0003] Usnea acid is the dry lichen body of Usnea diffracta Vain. and Usnea longissima Ach. in the family Usneaceae (Usne aceae). Properties: yellow orthorhombic prism crystal (acetone). The melting point is 204°C. Optical rotation +509.4° (c=0.697, chloroform). Solubility at 25°C (g / 100ml water) <0.01, acetone 0.77, ethyl acetate 0.88, ethanol 0.02, furfural 7.32, sugar alcohol 1.21. It can be produced by chemical synthesis or biosynthesis. [0004] Usnea and many other lichens contain antibacterial substances, among which the antibacterial effect of usnenic acid is particularly prominent. Its antibacterial spectrum is mainly Gram-negative bacteria and Mycobacterium tuberculosis. In the test tube, usnic acid has a strong antibacterial effect on pne...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/06A61K31/343A61K47/24A61K47/32A61P17/02
CPCA61K9/0014A61K9/06A61K31/343A61K47/24A61K47/32
Inventor 赵颖宋丹宋婷李智豪
Owner 北京昊坤康源医疗科学技术发展有限责任公司
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