Novel penetration-promoting agent composition and application thereof to transdermal administration system

Abstract

The invention provides a novel penetration-promoting agent composition and the application thereof to a transdermal administration system. The penetration-promoting agent provided by the invention contains an etheric compound and an alcohol compound and more preferably contains fatty acid having 6 to 18 carbon atoms or fatty alcohol having 6 to 18 carbon atoms. In the penetration-promoting agent of the invention, dimethylsulfoxide (DMSO) with controversial potential toxicity to a human body is not used; and an obtained product has the advantages of high transdermal rate, high adhesion, no potential toxic or side effect to the human body and safe and comfortable use. The transdermal administration system provided by the invention is applied by being stuck to the skin of a woman so as to fulfill the aims of effectively controlling birth and realizing conception control. The novel penetration-promoting agent composition can also be used for preventing and treating osteoporosis, climacteric metancholia of women and the like.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a novel penetration enhancer composition and its application in a transdermal drug delivery system. Background technique [0002] A combination of synthetic estrogen and progestin, often used for contraception. If a combination of natural estrogen (17-beta estradiol) and progesterone (progesterone) is used in the form of an oral contraceptive pill, these two hormones undergo extensive primary metabolism in the liver requiring the use of very large doses. The resulting metabolites often cause undesired side effects. Therefore, synthetic progesterone and estrogen compositions are now mainly used as oral contraceptives to overcome these defects. Among them, one of the most representative combinations in oral contraceptives is the combination of levonorgestrel and ethinyl estradiol. [0003] Although the combination of synthetic progesterone and estrogen is very effective in suppressing ov...

AI Technical Summary

Problems solved by technology

In order to solve the problem of dissolving levonorgestrel and estrogen, some dissolution-promoting and penetration-promoting systems use dimethyl sulfoxide (DMSO) to increase the dissolution of levonorgestrel and increase the penetration of levonorgestrel. The publication number is CN1399533 The Chinese patent disclosed a transdermal contraceptive drug delivery system. The skin penetration enhancer composition of this system uses dimethyl sulfoxide (DMSO). This system has a good transdermal rate for human skin, but due to the current The potential toxicity of dimethyl sulfoxide to the human body is still controversial. For safety reasons, the use of dimethyl sulfoxide (DMSO) should be avoided in penetration enhancer compositions.

There are also many fatty ester penetration enhancers that have been proven to have good penetration enhancement effects on levonorgestrel, for example, methyl laurate, polyethylene glycol monolaurate, poly Propylene glycol monolaurate (Polypropylene glycolmonolaurate), but these penetration enhancers, as plasticizers, have a serious damage to the viscosity or cohesion of the acrylic matrix system, and the dissolution of levonorgestrel is very limited

In order to ensure the penetration-enhancing effect, it is often necessary to use high-concentration levonorgestrel and estrogen in the viscous matrix of the transdermal drug delivery device in a supersaturated dissolved state. When using the above-mentioned high-ratio fatty ester penetration enhancers in norgestimate and estrogen transdermal drug delivery devices, they often cause severe cold flow or loss of viscosity, making it impracticable for practical use

[0022] In addition, the existing disclosed technical schemes for transdermal drug delivery all use mouse skin as the experimental object to achieve a certain transdermal amount of the given drug through the mouse skin. Differently, the permeability of mouse skin is much higher than that of human skin, and the given transdermal rate is very high, but it is not practical, and the patch prepared on this basis often cannot really be applied on the human body. Reach the amount of treatment required by medicine

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