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Ethinyl estradiol gas permeable absorbing paste

An ethinyl estradiol and transdermal technology is applied in the field of pharmacy to achieve the effects of prolonging the action time of the drug, meeting the treatment requirements and increasing the transdermal rate.

Inactive Publication Date: 2007-05-30
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently on the market for the palliative treatment of prostate cancer, only oral tablets are available, and no other dosage forms are on the market

Method used

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  • Ethinyl estradiol gas permeable absorbing paste
  • Ethinyl estradiol gas permeable absorbing paste
  • Ethinyl estradiol gas permeable absorbing paste

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Polyacrylate pressure sensitive adhesive (PSA) 390mg, dibutyl sebacate 175mg, succinic acid 35mg, drug ethinyl estradiol 20mg, oleic acid 160mg, solvent (acetone:isopropanol:ethanol=21:2.3:11.7) 2400mg , together into the bottle, the bottle mouth is closed, until completely dissolved, spread on 40cm 2 on the backing layer, followed by drying at 60°C for 30min. The dried matrix layer contains 50% polyacrylate, 2.6% ethinyl estradiol, and 20.5% oleic acid. After cooling, it covers the upper lining layer. The improved Franz diffusion cell device is used to measure its permeability to human skin in vitro. The receiving solution is 20% polyethylene glycol 400 (PEG400) saline solution in water. 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 0.76ug / cm 2 h. Fig. 1 is the cumulative drug penetration-time ...

Embodiment 2

[0022] Polyacrylate pressure sensitive adhesive (PSA) 390mg, dibutyl sebacate 175mg, succinic acid 35mg, drug ethinyl estradiol 20mg, oleic acid 100mg, solvent (acetone:isopropanol:ethanol=21:2.3:11.7) 2400mg , as in 1 operation, the matrix layer after drying contains 54% polyacrylate, 2.8% ethinyl estradiol, 13.9% oleic acid, covers the upper lining layer after cooling, and uses the modified Franz diffusion cell device to measure its penetration to human skin in vitro rate, the receiving fluid is 20% polyethylene glycol 400 (PEG400) saline aqueous solution, and the penetration rate is 0.50ug / cm 2 h. Fig. 2 is the cumulative drug penetration-time curve of this embodiment.

Embodiment 3

[0024] Polyacrylate pressure sensitive adhesive (PSA) 300mg, dibutyl sebacate 135mg, succinic acid 27mg, drug ethinyl estradiol 20mg, oleic acid 230mg, solvent (acetone:isopropanol:ethanol=21:2.3:11.7) 1848mg , as in 1 operation, the matrix layer after drying contains polyacrylate 42%, ethinyl estradiol 2.8%, oleic acid 32.3%, after cooling, cover the upper lining layer, and adopt the modified Franz diffusion cell device to measure its penetration to human skin in vitro rate, the receiving fluid is 20% polyethylene glycol 400 (PEG400) saline aqueous solution, and the penetration rate is 0.43ug / cm 2 h. Fig. 3 is the cumulative drug penetration-time curve of this embodiment.

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PUM

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Abstract

A percutaneous absorbing disk of eston-E for treating prostatic cancer is composed of substrate layer, medicinal matrix layer and protecting film. Its advantage is high percutaneous speed.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to a drug transdermal absorption patch, in particular to an ethinyl estradiol transdermal absorption patch. 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 ligands. Test...

Claims

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Application Information

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