Ethinyl estradiol gas permeable absorbing gel

A technology of ethinyl estradiol and gel, applied in the field of pharmacy, can solve the problems such as the amount of penetration through the skin, the penetration rate cannot meet the treatment requirements, etc., and achieve the effects of increasing the penetration rate and being convenient to use.

Inactive Publication Date: 2005-10-12
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because of the dense structure of the stratum corneum, most drugs cannot penetrate the skin or the amount of penetration is very small. Although ethinyl estradiol can penetrate, the transdermal rate cannot meet the treatment requirements.

Method used

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  • Ethinyl estradiol gas permeable absorbing gel
  • Ethinyl estradiol gas permeable absorbing gel
  • Ethinyl estradiol gas permeable absorbing gel

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Weigh 200mg of Carbomer 934, add 3-4ml of water, and swell for about 1 hour. Separately weigh 20 mg of ethinyl estradiol and 2 mg of methylparaben, add 3 g of ethanol and 1.5 g of propylene glycol to dissolve them, and mix them evenly with carbomer, drop triethanolamine to cross-link until neutral, and keep stirring to make the mixture Uniform transparent gel, add water to 10g. Stir well, and use the improved Franze diffusion cell device to measure its permeability to human skin in vitro, and the receiving solution is 20% polyethylene glycol 400 (PEG400) physiological saline solution. Use HPLC to measure ethinyl estradiol, the wavelength is 281nm, the mobile phase is 70% methanol, 30% water, the flow rate is 1ml / min, for ethinyl estradiol, the retention time is about 5.5min, and the permeation rate is 6.78μg / cm 2 h, figure 1 It is the drug cumulative penetration-time curve of this embodiment.

Embodiment 2

[0021] Weigh 200mg of Carbomer 934, add 3-4ml of water, and swell for about 1 hour. In addition, weigh 20 mg of ethinyl estradiol and 2 mg of methylparaben, add 4 g of ethanol and 1.5 g of propylene glycol to dissolve them, and mix them evenly with carbomer, drop triethanolamine to cross-link until neutral, and keep stirring to make the mixture Uniform transparent gel, add water to 10g. A modified Franze diffusion cell device was used to measure its permeability to human skin in vitro, and the receiving solution was 20% polyethylene glycol 400 (PEG400) physiological saline aqueous solution. Use HPLC to measure ethinyl estradiol, the wavelength is 281nm, the mobile phase is 70% methanol, 30% water, the flow rate is 1ml / min, for ethinyl estradiol, the retention time is about 5.5min, and the permeation rate is 6.117μg / cm 2 h, figure 2 It is the drug cumulative penetration-time curve of this embodiment.

Embodiment 3

[0023] Weigh 200mg of Carbomer 934, add 3-4ml of water, and swell for about 1 hour. Separately weigh 20 mg of ethinyl estradiol and 2 mg of methylparaben, add 2 g of ethanol and 1.5 g of propylene glycol to dissolve them, and mix them evenly with carbomer, drop triethanolamine to cross-link until neutral, and keep stirring to make the mixture Uniform transparent gel, add water to 10g. A modified Franze diffusion cell device was used to measure its permeability to human skin in vitro, and the receiving solution was 20% polyethylene glycol 400 (PEG400) physiological saline aqueous solution. Use HPLC to measure ethinyl estradiol, the wavelength is 281nm, the mobile phase is 70% methanol, 30% water, the flow rate is 1ml / min, for ethinyl estradiol, the retention time is about 5.5min, and the permeation rate is 3.79μg / cm 2 h. image 3 It is the drug cumulative penetration-time curve of this embodiment.

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Abstract

A percutaneous absorbing gel of eston-E for treating amenorrhoea, climacteric syndrome and prostatic cancer, or for contraceptive purpose is prepared from eston-E, percutaneous absorption promoter, and carbomer.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a gel for transdermal absorption of ethinyl estradiol, which relates to a medicinal gel for transdermal absorption. Background technique [0002] Cancer is the biggest disease facing mankind. For men, especially men over 40 years old, the incidence of prostate cancer ranks ahead of all kinds of malignant tumors. With the aging of the population and the decline in mortality, the incidence of prostate cancer is increasing at an average rate of 8%. It is estimated that the incidence of prostate cancer will double by 2011. The United States alone will reach about 2.9 million people, and China will also have about 8 million people. For advanced metastatic prostate cancer, hormone therapy can reduce symptoms and improve quality of life. The androgen receptor of prostate cancer is located in the cytoplasm, and testosterone (T) and its metabolite dihydrotestosterone (DHT) are its most active lig...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/70A61K31/565A61P13/08A61P35/00
Inventor 梁文权刘晓昱饶跃峰
Owner ZHEJIANG UNIV
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