Percutaneous absorption patch containing gestodene and/or estrogen

A gestodene and estrogen technology, applied in the field of pharmaceutical preparations, can solve the problem of not mentioning gestodene, etc., and achieve the effects of improving compliance and ensuring contraceptive effect

Inactive Publication Date: 2008-07-30
刘建平 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The progestin used in this patent is a metabolite of the third generation synthetic progesterone, which requires twice the dosage of the progestin used in the invention, and the invention does not mention gestodene alone or with any estrogen Any prior art for transdermal drug delivery

Method used

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  • Percutaneous absorption patch containing gestodene and/or estrogen
  • Percutaneous absorption patch containing gestodene and/or estrogen
  • Percutaneous absorption patch containing gestodene and/or estrogen

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Composition in the first layer (outer layer): polyvinyl alcohol (PVA17-88) 4.5g, polyvinylpyrrolidone (PVP) 0.5g, azone (Azone) 1.0g, propylene glycol 0.2g, glycerin 1.0g, pregnane Ketone (GSD) 26.83mg, ethinyl estradiol (EE) 5.3mg.

[0040] The composition of the second layer (the inner layer close to the protective film): polyvinyl alcohol (PVA17-88) 6g, polyvinylpyrrolidone (PVP) 1g, azone (Azone) 2g, propylene glycol 0.3g, glycerin 1.5g , gestodene (GSD) 6.5mg, ethinyl estradiol (EE) 2.5mg.

[0041] Preparation method: fully dissolve gestodene and ethinyl estradiol with 120 g of 50% ethanol, add polyvinyl alcohol, polyvinyl pyrrolidone, etc. to fully swell, add azone and glycerin in a water bath, ultrasonically dissolve, and stand still until the bubbles disappear. Lay the film separately, dry and cool, then compound, cover the backing layer of polyethylene aluminum-polyethylene composite film and polyethylene protective film, and prepare a product containing GSD0....

Embodiment 2

[0044] The composition of the first layer: polyvinyl alcohol (PVA17-88) 4g, polyvinylpyrrolidone (PVP) 0.5g, isopropyl myristate 1g, propylene glycol 0.5g, glycerin 0.6g, GSD 27.8mg, EE 10mg.

[0045] The composition of the second layer: polyvinyl alcohol (PVA17-88) 6g, polyvinylpyrrolidone (PVP) 1.3g, isopropyl myristate 2g, propylene glycol 0.5g, glycerin 0.8g, GSD 6mg, EE 3.0mg.

[0046] Prepared as in Example 1, prepared to contain GSD0.3mg / cm 2 , EE0.1mg / cm 2 patch. And carry out transdermal diffusion test on it, the penetration rate of GSD is 0.61μg / cm 2 / h, the permeation rate of EE is 0.25μg / cm 2 / h. The in vitro skin release curve is shown in Figure 2.

Embodiment 3

[0048] First layer: polyvinyl alcohol (PVA17-88) 9g, polyvinylpyrrolidone (PVP) 2g, glycerin 3g, isopropyl myristate 2g, propylene glycol 1.5g, 48mgGSD and 11.5mgEE.

[0049] Second layer: polyvinyl alcohol (PVA17-88) 6g, polyvinylpyrrolidone (PVP) 1g, glycerin 2g, isopropyl myristate 2g, propylene glycol 0.5g, 12mgGSD and 1.5mgEE.

[0050] The patch preparation method is the same as in Example 1, prepared to contain GSD0.33mg / cm 2 , EE0.08mg / cm 2 patch. The penetration rate of GSD in this patch is 0.8 μg / cm 2 / h, the permeation rate of EE is 0.26μg / cm 2 / h. The release curve through the skin in vitro is shown in Figure 3.

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Abstract

The invention relates to the technical field of pharmaceutical preparation, in particular to a percutaneous absorption patch containing gestodene and (or) estrogen, and also discloses the preparation method. The patch style medicine of the invention can be released by constant rate for a long time.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a transdermal absorption patch containing gestodene and / or estrogen, and the invention also discloses a preparation method thereof. Background technique [0002] Progestin alone or in combination with estrogen has shown its reliable contraceptive effect and is one of the most widely used contraceptive methods in the world. The contraceptive principle of compound contraceptives is that the contained progesterone and estrogen have the following effects: inhibit the development and maturation of ovaries and ovulation, change the shape of endometrium, change the nature of cervical mucus and change the normal peristalsis of fallopian tubes. Compared with the second-generation progesterone, the third-generation gestodene is closer to natural progesterone, has stronger progesterone receptor affinity, has almost no androgenic effect, no estrogenic activity, and has anti-estroge...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/565A61K47/10A61K47/14A61K47/22A61K47/32A61K47/34A61P15/18
Inventor 刘建平王广基梁金英张肖敏李瑛张春延
Owner 刘建平
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