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Contraceptive medicament preparation containing gestodene

A technology of gestodene and contraceptive drugs, which is applied in the field of contraceptive drug preparations containing gestodene to achieve the effect of high cumulative release

Active Publication Date: 2012-07-18
LIAONING AIMU MEDICAL SCI&TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The object of the present invention is to solve the problem of ensuring sustained or controlled release of the drug, and provides a contraceptive pharmaceutical preparation containing gestodene

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Gestodene vaginal ring, using a gravimetric specific surface area of ​​5000cm 2 / g~50000cm 2 Gestodene powder per g is mixed with silicone rubber or EVA carrier to make a drug core, and silicone rubber or EVA is used to make a controlled-release membrane. The content of the drug, the ratio of the drug to the silicone rubber or EVA carrier are based Daily release dose design. The minimum distance between the geometric center of all powders and the surface of the preparation is less than 5mm. The daily release dose of gestodene is 0.01mg~0.075mg, and it is released for one menstrual cycle.

Embodiment 2

[0015] Gestodene / ethinyl estradiol vaginal ring, using a gravimetric surface area of ​​5000 cm 2 / g~50000cm 2 / g of Gestodene powder, the weight specific surface area is 5000cm 2 / g~50000cm 2 / g of ethinyl estradiol powder is mixed with silicone rubber or EVA carrier to make a drug core, and silicone rubber or EVA is used to make a controlled release film. Release dose design. The minimum distance between the geometric center of all powders and the surface of the preparation is less than 5mm. The daily release dose of gestodene is 0.01 mg to 0.075 mg, and the daily release dose of ethinyl estradiol is 0.005 mg to 0.050 mg, for one menstrual cycle.

[0016] In the above examples, other estrogens equivalent to the daily release dose of ethinyl estradiol can be used instead of ethinyl estradiol, such as estradiol.

Embodiment 3

[0018] Gestodene / ethinyl estradiol vaginal ring, dissolve gestodene and ethinyl estradiol in an organic solvent, soak the ring-shaped silicone rubber or EVA carrier in an organic solvent to swell, and volatilize the organic solvent to release the drug The crystals are left in the gap of the annular silicone rubber or EVA carrier, and the controlled release film is made of silicone rubber or EVA, and the amount of drug dissolved is designed according to the selected daily release dose. The minimum distance between the geometric centers of all crystals and the formulation surface is less than 5 mm. The daily release dose of gestodene is 0.01 mg to 0.075 mg, and the daily release dose of ethinyl estradiol is 0.005 mg to 0.050 mg, for one menstrual cycle.

[0019] In the above examples, other estrogens equivalent to the daily release dose of ethinyl estradiol can be used instead of ethinyl estradiol, such as estradiol.

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PUM

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Abstract

The invention relates to a contraceptive medicament preparation containing gestodene, which is dosed through natural orifice of human beings or mammals or through transdermal or subcutaneous administration. The gestodene is in a zero order release pattern. The contraceptive medicament preparation contains 0.0005 mg to 0.100 mg of gestodene of daily dose, and one or more kinds of pharmaceutical acceptable excipient or carriers. The contraceptive medicament preparation is characterized in that the gestodene is a crystal or powders with the weight specific surface area more than 100 cm2 / g. The minimal distance between the geometric center of the crystal with more than or equal to 70% of weight proportion and the surface of the preparation is less than or equal to 5 mm. The minimal distance between the geometric center of the powders with more than or equal to 70% of weight proportion and the surface of the preparation is less than or equal to 5 mm. The contraceptive medicinal preparationcontains 0.005 mg to 0.050 mg ethinyloestradiol of daily dose. In the invention, the distribution characteristics of the size and the design of the drug is selected, the drug can be in a better zero order release pattern, and the cumulative release rate is higher.

Description

technical field [0001] The invention relates to a contraceptive pharmaceutical preparation administered through the natural orifice of a human or a mammal, transdermally or subcutaneously, in particular to a contraceptive pharmaceutical preparation containing gestodene. Background technique [0002] Gestodene is the third generation progestin, also known as 15-dehydrohornorone, melting point: 197.9°C, solubility: insoluble in water, soluble in methanol, ethanol and acetone. Compared with the second-generation progesterone such as levonorgestrel currently commonly used, it has more prominent safety and effectiveness. It hardly affects the weight, blood pressure, etc. of the user. It has no significant effect on blood lipids and carbohydrate metabolism, and can regulate skin, inhibit acne, improve quality of life, and have a balanced effect on blood coagulation system. At present, gestodene has been developed as an oral tablet, such as the United States Wyeth company Desmin ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/567A61P15/18
Inventor 武小锋史凤阳
Owner LIAONING AIMU MEDICAL SCI&TECH
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