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Cyproterone acetate medicinal preparation and preparation method thereof

A technology of cyproterone acetate and pharmaceutical preparations is applied in the directions of drug combinations, pharmaceutical formulations, medical preparations of non-active ingredients, etc., and can solve the problems of increasing cyproterone acetate, unstable curative effect, low dissolution rate and the like, Achieve the effects of good stability, low manufacturing cost and simple preparation method

Inactive Publication Date: 2014-04-16
武汉九珑人福药业有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, cyproterone acetate is almost insoluble in water, so the dissolution rate in water is very low, and the curative effect may be affected or unstable after taking
At present, cyproterone acetate is mostly used to be compatible with other progestogens to make compound contraceptives, but there is no report of a prescription for increasing the dissolution of cyproterone acetate, so inventing a prescription preparation for increasing the dissolution of cyproterone acetate is very necessary

Method used

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  • Cyproterone acetate medicinal preparation and preparation method thereof
  • Cyproterone acetate medicinal preparation and preparation method thereof
  • Cyproterone acetate medicinal preparation and preparation method thereof

Examples

Experimental program
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Embodiment 1

[0017] Cyproterone acetate pharmaceutical preparation, the mass percent of each component in terms of dry weight is: 30.5% of cyproterone acetate micropowder particles, 64.6% of filler, 1.2% of disintegrant, 0.9% of glidant, lubricant 0.3%, binder balance, the particle diameter of 90wt% cyproterone acetate micropowder particle in described cyproterone acetate micropowder particle is below 5 μm.

[0018] The preparation method of cyproterone acetate pharmaceutical preparation

[0019] (1) Pretreatment of cyproterone acetate

[0020] Add 10g of cyproterone acetate raw material to 60ml of ethanol, heat up to completely dissolve, concentrate to about 5-10ml, cool down and freeze for 2 hours, filter, wash the filter cake with ethanol, and then vacuum-dry at 50°C to constant weight. After drying, 6.5 g of cyproterone acetate was obtained, the content of which was detected by HPLC was 99.85%, and the melting point was 208-212°C. After crushing and sieving, more than 90% of the cypr...

Embodiment 2

[0027] Cyproterone acetate pharmaceutical preparation, the mass percent of each component in terms of dry weight is: 29.8% of cyproterone acetate micropowder particles, 57.2% of filler, 10.7% of disintegrant, 0.6% of lubricant, and glidant 1.2%, binder balance, the particle diameter of 90wt% cyproterone acetate micropowder particle in described cyproterone acetate micropowder particle is below 5 μm.

[0028] The preparation method of cyproterone acetate pharmaceutical preparation

[0029] (1) Pretreatment of cyproterone acetate

[0030] Add 10g of cyproterone acetate raw material to 40ml of toluene, heat up to fully dissolve, concentrate until about 0.5-4ml of solvent remains, cool down and freeze for 2 hours, filter, wash the filter cake with toluene, and then vacuum dry at 50°C to constant weight. After drying, 6 g of cyproterone acetate was obtained, the content detected by HPLC was 99.90%, and the melting point was 208-212°C. After crushing and sieving, more than 90% of ...

Embodiment 3

[0037] Cyproterone acetate pharmaceutical preparation, the mass percent of each component in terms of dry weight is: 31.0% of cyproterone acetate micropowder particles, 65.7% of filler, 1.2% of disintegrant, 0.9% of glidant, lubricant 0.3%, binder balance, the particle diameter of 90wt% cyproterone acetate micropowder particle in described cyproterone acetate micropowder particle is below 5 μ m.

[0038] The preparation method of cyproterone acetate pharmaceutical preparation

[0039] (1) Pretreatment of cyproterone acetate

[0040] Add 10g of cyproterone acetate raw material to 40ml of toluene, heat up to fully dissolve, concentrate until about 0.5-4ml of solvent remains, cool down and freeze for crystallization for 2 hours, filter, wash the filter cake with toluene, and then vacuum-dry at 50°C to constant weight. After drying, 6 g of cyproterone acetate was obtained, the content detected by HPLC was 99.90%, and the melting point was 208-212°C. After crushing and sieving, m...

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Abstract

The invention relates to a cyproterone acetate medicinal preparation and a preparation method thereof. The cyproterone acetate medicinal preparation is prepared by taking solutions of cyproterone acetate micro powder particles, a filler, a disintegrating agent, a lubricant, a flow aid and an adhesive as raw materials. The prepared preparation consists of the following components in percentage by mass counted by dry weight: 17-40 percent of the cyproterone acetate micro powder, 40-75 percent of the filter, 1-15 percent of the disintegrating agent, 0-2 percent of the lubricant, 0-2 percent of the flow aid and 0.5-11 percent of the adhesive. As measured by a laser particle size analyzer, the particle sizes of 90 percent by weight cyproterone acetate micro powder particles serving as raw materials are below 5 microns. The dissolution of the cyproterone acetate medicinal preparation can be increased to the maximum extent, so that the bioavailability of the cyproterone acetate medicinal preparation is enhanced; a simple process is adopted, and industrial production is easy to perform.

Description

technical field [0001] The invention relates to a pharmaceutical preparation and a preparation method thereof, in particular to a cyproterone acetate pharmaceutical preparation and a preparation method thereof. Background technique [0002] Cyproterone acetate English name: Cyproterone Acetate, chemical name: 6-chloro-1,2-methylene-4,6-diene-3,20-diproterone acetate, other names: cyproterone Acetate, Cyproterone Ester, Champron, Cyproterone Acetate, Androcur, Andro-Diane, SH-80714. It was developed by the German company Shering and first launched in 1982. Now it has been registered in 15 countries, and it is recorded in the pharmacopoeias of the United Kingdom, Italy and Europe. This product is a derivative of 17α-hydroxyprogesterone, which is an androgen antagonist with strong anti-androgen effect and progesterone activity. Clinically, it can be used to treat abnormal libido in men, prostatic hypertrophy and prostate cancer, precocious puberty, hirsutism in women, acne, m...

Claims

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Application Information

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IPC IPC(8): A61K31/57A61K47/32A61K47/38A61P15/00A61P13/08A61P17/10A61P15/12A61P15/18
Inventor 乔炜俊刘俊勇喻华耀陶曙
Owner 武汉九珑人福药业有限责任公司