Norethisterone acetate-containing compound estradiol transdermal sustained release preparation and preparation method thereof

A technology of norethisterone acetate and compound estradiol, which is applied in the field of medicine, can solve the problems of stimulation of endometrial hyperplasia, the embarrassment of popularization and use of estrogens, etc., and achieves the decrease of blood drug concentration, avoids the phenomenon of peak and valley of blood drug concentration, long-lasting effect

Active Publication Date: 2013-04-24
ZHEJIANG YATAI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to estrogen alone, stimulation of endometrial hyperplasia occurs even in the range of doses required to reduce menopausal symptoms and maintain bone mass
And any route of administration, including transdermal therapeutic systems, will have this side effect
This puts the promotion of estrogen in an embarrassing dilemma

Method used

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  • Norethisterone acetate-containing compound estradiol transdermal sustained release preparation and preparation method thereof
  • Norethisterone acetate-containing compound estradiol transdermal sustained release preparation and preparation method thereof

Examples

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Effect test

Embodiment 1

[0036] A kind of compound estradiol transdermal slow-release preparation containing norethindrone acetate of the present embodiment comprises a backing layer, a protective film and a skeleton layer between the backing layer and the protective film; the skeleton layer includes an upper layer A skeleton layer, a lower skeleton layer and a controlled-release membrane between the upper skeleton layer and the lower skeleton layer; the surface of the lower skeleton layer is covered with a backing layer made of aluminum-plastic film.

[0037] Its preparation method is: 1) 1g estradiol, 10.5g norethindrone acetate, 25.46g laurocapram, 100.97g propylene glycol, 14.05g lauric acid, 18.6g polyethylene glycol 400, 287.86g polyacrylate and Mix 46.97g of ethyl acetate, stir evenly, and place until the bubbles disappear; 2) Apply the mixture obtained in step 1) on the anti-adhesive layer with a thickness of 0.10mm, and place it in an oven to dry at a temperature of 80°C, drying time is 60 mi...

Embodiment 2

[0041] A kind of compound estradiol transdermal slow-release preparation containing norethindrone acetate of the present embodiment, a kind of compound estradiol transdermal slow-release preparation containing norethindrone acetate of the present embodiment, comprises backing layer, protection film and a skeleton layer between the backing layer and the protective film; the skeleton layer includes an upper skeleton layer, a lower skeleton layer and a controlled release membrane between the upper skeleton layer and the lower skeleton layer; the lower skeleton layer The surface is covered with a backing layer made of aluminum-plastic film.

[0042] Its preparation method is: 1) 1.5g estradiol, 12g norethindrone acetate, 24.16g laurocaprone, 79.68g propylene glycol, 10.69g lauric acid, 20.67g polyethylene glycol 400, 268.91g polyacrylate and Mix 53.98g of ethyl acetate, stir evenly, and place until the air bubbles disappear; 2) Apply the mixture obtained in step 1) on the anti-adh...

Embodiment 3

[0046] A kind of compound estradiol transdermal slow-release preparation containing norethindrone acetate of the present embodiment comprises a backing layer, a protective film and a skeleton layer between the backing layer and the protective film; the skeleton layer includes an upper layer A skeleton layer, a lower skeleton layer and a controlled-release membrane between the upper skeleton layer and the lower skeleton layer; the surface of the lower skeleton layer is covered with a backing layer made of aluminum-plastic film.

[0047] Its preparation method is: 1) 2g estradiol, 13.5g norethindrone acetate, 19.46g laurocaprone, 106.69g propylene glycol, 8.77g lauric acid, 16.27g polyethylene glycol 400, 229.39g polyacrylate and Mix 62.31g of ethyl acetate, stir evenly, and place until the bubbles disappear; 2) Coat the mixture obtained in step 1) on the anti-adhesive layer with a thickness of 0.10mm, and place it in an oven to dry at a temperature of 80°C, drying time is 60 mi...

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Abstract

The invention discloses a norethisterone acetate-containing compound estradiol transdermal sustained release preparation and a preparation method thereof. The preparation comprises a backing layer, a protective film and a frame layer between the backing layer and the protective film, wherein the frame layer comprises an upper frame layer, a lower frame layer and a controlled release film between the upper frame layer and the lower frame layer; and the backing layer covers the surface of the lower frame layer. The upper and lower frame layers are respectively wrapped by estradiol and norethisterone acetate in a certain ratio, an intermediate frame layer is wrapped by a special transdermal patch of the controlled release film, estrogen estradiol effects in relieving or eliminating climacteric syndromes and preventing osteoporosis are fully played, and the preparation also has the characteristics of small stimulus to human bodies, small side effects, quality stability and long effective time.

Description

technical field [0001] The invention relates to a compound estradiol transdermal slow-release preparation and a preparation method thereof, in particular to a compound estradiol transdermal slow-release preparation containing norethindrone acetate and a preparation method thereof, belonging to the field of medicine. Background technique [0002] The chemical name of estradiol is: estradiol-1,3,5(10)-triene-3,17β-diol; the structural formula of estradiol is: [0003] [0004] The chemical name of norethindrone acetate is: 17β-hydroxyl 19-nor-17α-pregna-4-en-20-yn-3-one acetate; the structural formula of norethindrone acetate is: [0005] [0006] Women's climacteric syndrome is a common disease in women. Its pathogenesis is related to ovarian dysfunction and decreased estrogen secretion. In 1987, the Swiss Ciba Pharmaceutical Company first successfully developed the estrogen transdermal therapy system Estraderm TTS administered through the skin route as estrogen repla...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/567A61K31/565A61K9/70A61P15/12A61P19/10A61P15/00
Inventor 吕旭幸王丽云郭光祥陈洁王一升
Owner ZHEJIANG YATAI PHARMA
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