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A stable pharmaceutical composition comprising ethinyl estradiol and norethindrone acetate

A technology of norethindrone acetate and composition, which is applied in the field of pharmaceutical preparations, can solve problems such as oxidative degradation and drug effect decline, and achieve the effects of improving stability, ensuring stability, and improving overall stability

Active Publication Date: 2022-05-17
北京联嘉医药科技开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Ethinyl estradiol is an orally bioavailable estrogen, which is used in almost all modern combined oral contraceptive formulations. The content in a single dose product is usually less than 100µg, and it is prone to oxidative degradation after exposure to air. decrease the effectiveness of the drug

Method used

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  • A stable pharmaceutical composition comprising ethinyl estradiol and norethindrone acetate
  • A stable pharmaceutical composition comprising ethinyl estradiol and norethindrone acetate
  • A stable pharmaceutical composition comprising ethinyl estradiol and norethindrone acetate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-5

[0051] The compound tablet of ethinyl estradiol and norethindrone acetate is prepared by fluidized bed wet granulation tablet technology, and the processing steps are as follows:

[0052] Weighing: Weigh each component according to the prescription in Table 1.

[0053] Main drug solution preparation: dissolve ethinyl estradiol, norethindrone acetate, and vitamin E in a mixed solvent of ethanol and chloroform 1:1 (v / v);

[0054] Screening: pass lactose and starch through a sieve with a pore size of 20 mesh;

[0055] Granulation and drying: Put the sieved material into a fluidized bed granulation pot, spray the main drug solution in a fluidized state, and then fluidize and dry at 40°C;

[0056] Screening: pass the dried material through a sieve with an aperture of 20 mesh;

[0057] Blending and tableting: add the prescribed amount of magnesium stearate to the sieved granules, mix evenly, and then press into 5mm round tablets.

[0058] Table 1 Example 1-5 Tablet Prescription ...

Embodiment 6

[0060] Embodiment 6 Determination of related substances

[0061] The tablet prepared by Example 1-5 was preserved for 3 months under 40°C / 75%RH condition, and the packaging condition was a heat-sealed high-density polyethylene bottle, and the high-performance liquid chromatography was used to measure 0 days and 3 tablets respectively. The amount of related substances in the monthly samples, the determination results are shown in Table 3.

[0062] The HPLC chromatographic conditions are: use octyl bonded silica gel as filler; use acetonitrile containing 0.5% phosphoric acid as mobile phase A, acetonitrile containing 0.5% phosphoric acid: water = 1:3 as mobile phase B, perform linearity according to Table 2 Gradient elution; flow rate is 1.6ml per minute; FLDex285nm, em350nm (6α-hydroxyethinylestradiol, 6β-hydroxyethinylestradiol and Δ9,11-ethinylestradiol), UV 210nm (other impurities); column temperature: 40ºC; Sample volume: 30µl.

[0063] Table 2 Gradient elution parameter ...

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Abstract

A stable pharmaceutical composition comprising ethinyl estradiol and norethindrone acetate, the stability of ethinyl estradiol is improved by adding vitamin E; and by using specific amount of vitamin E, the stability of ethinyl estradiol and norethindrone acetate is controlled The production of related substances improves the overall stability of the compound preparation.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations. The invention provides a pharmaceutical composition for female contraception or treatment and prevention of climacteric syndrome with good stability. Background technique [0002] Oral contraceptives usually contain a combination of synthetic progestin and estrogen. Both of these two hormone compounds can promote the maturation of female accessory sex organs and the emergence of secondary sexual characteristics, and maintain normal sexual desire and reproductive function. The compound preparation of estrogen ethinyl estradiol and progestin norethindrone acetate (optical rotation -32° to -38°) can be used for female contraception and treatment or prevention of menopausal syndrome. [0003] Ethinyl estradiol is an orally bioavailable estrogen, used in almost all modern combined oral contraceptive formulations, the content in single dose products is usually less than 100µg, and it is pro...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/567A61K9/32A61K9/48A61K47/22A61K47/26A61K47/36A61P15/12A61P15/18
CPCA61K9/284A61K9/2013A61K9/2018A61K9/2059A61K9/4866A61K9/4858A61K31/567A61K47/22A61P15/12A61P15/18A61K2300/00
Inventor 陈艳钱云刘见见
Owner 北京联嘉医药科技开发有限公司
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