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Estradiol gel

An estradiol gel, estradiol technology, which can be used in aerosol delivery, medical preparations with inactive ingredients, endocrine system diseases, etc., can solve the problem of poor transdermal absorption of estradiol and shorten the validity period of the drug , unstable properties and other problems, to achieve the effect of improving bioavailability and curative effect, improving transdermal absorption effect and stability, and preventing degradation or destruction

Active Publication Date: 2020-03-13
JIANMIN PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, the transdermal absorption effect of estradiol is relatively poor. In order to promote the absorption of drugs to improve the curative effect, it is necessary to add penetration enhancers in externally applied drugs. There are many literature reports on this aspect. In addition, the molecular structure of estradiol contains The phenolic hydroxyl group is easily oxidized, especially unstable in a liquid environment, thus shortening the effective period of the drug

Method used

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  • Estradiol gel
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1 Influence of tyloxapol on transdermal absorption effect and stability of estradiol gel

[0026] (1) Preparation of test drugs

[0027]

[0028] Dissolving the estradiol in ethanol to obtain an ethanol solution of estradiol, then adding tyloxapol and azone, and stirring to obtain solution A; adding HPMC to water, stirring evenly, to obtain solution B; stirring solution A and solution B Mix, finally add sodium hydroxide, stir to make a gel after homogenization.

[0029] (2) In vitro transdermal absorption test

[0030] Take a mouse (about 20-25g), kill it by breaking the neck, cut off the hair on the back with surgery, remove the remaining hair with a razor, and take the back skin about 2×2cm 2 The large and small areas were soaked in saline. Subcutaneous fat was removed and stored in saline at 4°C. Using a Franz diffusion cell, fix the treated mouse skin between the supply pool and the receiving pool, with the cuticle facing the supply pool. Add 2.5 g o...

Embodiment 2

[0040]

[0041] Dissolve the estradiol in ethanol to obtain an estradiol ethanol solution, then add tyloxapol, azone, and propylene glycol, and stir to obtain solution A; add polyvinylpyrrolidone and carboxymethylcellulose to water, and stir evenly to obtain Solution B: Stir and mix solution A and solution B, and finally add sodium hydroxide, stir and homogenize to form a gel.

Embodiment 3

[0043]

[0044]

[0045] Dissolve the estradiol in ethanol to obtain an ethanol solution of estradiol, then add tyloxapol, linoleic acid, and propylene glycol, and stir to obtain solution A; add carbomer to water, and stir evenly to obtain solution B; A and solution B are stirred and mixed, and finally triethanolamine is added, stirred and homogenized to form a gel.

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PUM

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Abstract

The invention discloses an estradiol gel, which consists of an effective dose of estradiol and a gel matrix. The gel matrix contains tyloxapol which accounts for 0.05-2 wt% of the weight of the gel. By adding tyloxapol into the gel matrix, the percutaneous penetration rate and cumulative penetration amount of estradiol are improved. Therefore, the bioavailability and curative effect of the drug are improved, the stability of estradiol is also improved, and the degradation or destruction of the estradiol is prevented, thus improving the storage period of the drug.

Description

technical field [0001] The invention relates to an estradiol gel, which belongs to the field of pharmaceutical preparations. Background technique [0002] Estradiol, chemical name estrogen-1,3,5(10)-triene-3,17β-diol, its composition is suitable for the treatment of various symptoms caused by estrogen deficiency, especially for menopause-related Symptoms (hot flashes, night sweats, urinary symptoms, vaginal dryness, etc.). There are five ways of administration: oral administration, vaginal administration, subcutaneous implantation, injection administration and transdermal administration. Among them, the transdermal route of administration can reduce the dosage of the drug, overcome the side effects of the gastrointestinal tract caused by oral administration, avoid the first-pass effect, and reduce the damage to the liver, which has obvious advantages compared with other dosage forms. [0003] However, the transdermal absorption effect of estradiol is relatively poor. In or...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K47/10A61K31/565A61P5/30A61P15/12
CPCA61K9/0004A61K9/06A61K47/10A61K31/565A61P5/30A61P15/12
Inventor 吴雪英任霞赵刚郭平黄珮闻吴木琴黄志军
Owner JIANMIN PHARMA GRP CO LTD
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