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a contraceptive

A technology for contraceptives and gestodene, which is applied in the directions of drug combinations, pharmaceutical formulations, organic active ingredients, etc., can solve the problems of inappropriate use and increase the risk of thrombosis, and achieve the effects of reducing side effects and inhibiting ovulation.

Inactive Publication Date: 2018-01-12
江华瑶族自治县金牛开发建设有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The first generation of oral contraceptives uses the combination of norethindrone, megestrol and ethinyl estradiol. Because of norethindrone and megestrol, to achieve the contraceptive effect at this time, the content of ethinyl estradiol should be more than 50 μg. Oral contraceptives are used in combination with cyproterone, levonorgestrel and ethinyl estradiol. Because the activity of cyproterone and levonorgestrel is much higher than that of norethindrone, they have obvious anti-estrogen activity. The content of ethinyl estradiol can be controlled at 30-35 μg. The third-generation oral contraceptive uses a combination of desogestrel, gestodene and ethinyl estradiol to control its dosage at 20-30 μg. The combination of norgestrel, drospirenone and ethinyl estradiol reduces the amount of estrogen used to 20 μg, which greatly reduces the side effects of contraceptives, but the use of drospirenone and dienogest will increase the risk of thrombosis, and it is not suitable to use more

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] A contraceptive, the single dose unit includes the following components: 30 μg gestodene, 3.1 mg nomegestone, 0.41 mg levonorgestrel, 3.2 mg drospirenone, 2.1 mg cyproterone, 20 μg alkyne Estrol, 60 g sucrose and 5 μg mestranol.

Embodiment 2

[0034] A contraceptive, the single dose unit includes the following components: 30 μg gestodene, 2.2 mg nomegestone, 0.3 mg levonorgestrel, 2.7 mg drospirenone, 2.5 mg cyproterone, 15 μg alkyne Estrol, 60 g of sucrose, 10 μg of mestranol, 4.5 mg of dydrogesterone and 60 mg of a cellulose derivative.

Embodiment 3

[0036] A contraceptive, the single dosage unit includes the following components: 35 μg gestodene, 2.1 mg nomegestone, 0.5 mg levonorgestrel, 8.6 mg drospirenone, 3 mg cyproterone, 15 μg ethinyl estradiol Alcohol, 70g sucrose, 10μg mestranol, 9mg dydrogesterone and 100mg cellulose derivatives.

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PUM

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Abstract

The invention relates to contraceptive. The contraceptive is characterized by comprising the following components by mass in single dosage: 10-50mu g of gestodene, 1.5-10mg of nomegestrol, 0.2-0.5mg of levonorgestrel, 1-20mg of drospirenone, 0.5-10mg of cyproterone, 10-20mu g of ethinyloestradiol, 40-80g of saccharose and 5-20mu g of mestranol. The sum of the content of the ethinyloestradiol and the content of the mestranol is not more than 30mu g; and the sum of the content of the cyproterone, the content of the ethinyloestradiol and the content of the saccharose is 2-20mg. The contraceptive adopts the means that multiple progestational hormones and estrogenic hormones are mixed for use so as to reduce the estrogenic hormones, so that the obtained contraceptive can guarantee less injury to a human body under the condition with better contraceptive effect.

Description

technical field [0001] The invention relates to a contraceptive. Background technique [0002] Since the 1960s, oral contraceptives with a combination of progestogen and estrogen have been used, and the active ingredient of the contraceptive pill is provided by the progestin component. The estrogen component mainly enhances the ovulation suppression effect of progesterone and ensures a stable cycle. . Since the advent of oral contraceptives, researchers from all over the world have been researching and developing more selective progesterone preparations to reduce the dose of progesterone while maintaining its high efficiency, good cycle regulation, and low incidence of side effects. [0003] The first generation of oral contraceptives uses the combination of norethindrone, megestrol and ethinyl estradiol. Because of norethindrone and megestrol, to achieve the contraceptive effect at this time, the content of ethinyl estradiol should be more than 50 μg. Oral contraceptives ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/585A61P15/18A61K31/57A61K31/567
CPCA61K31/567A61K31/57A61K31/585A61K2300/00
Inventor 唐凡兰
Owner 江华瑶族自治县金牛开发建设有限公司
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