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Preparation method for ultra-micro co-grinding levonorgestrel tablets

A technology of levonorgestrel tablets and levonorgestrel, which is applied in the field of preparation of ultrafine co-pulverized levonorgestrel tablets, can solve the problems of low bioavailability, tablet dissolution rate and dissolution rate, etc.

Active Publication Date: 2012-11-14
BEIJING YILING BIOENG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Levonorgestrel is generally administered orally, but this medicine is a poorly soluble medicine, insoluble in water, ethanol, isopropanol acetone, solvents such as ethyl acetate, and its dissolution rate and dissolution rate of the prepared tablet of conventional preparation technology are all average. lower, resulting in lower bioavailability

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] a, superfine co-grinding: take 75g of dry levonorgestrel raw material, mix with 750g microcrystalline cellulose, add absolute ethanol, after making the mixture wet, superfine pulverization, make 90% particle diameter reach below 20 microns, drying to obtain the ultrafine mixture of levonorgestrel;

[0078] b. Mixing: Add 2475g of direct-pressed lactose, 412.5g of pregelatinized starch, and 82.5g of hydroxypropyl methylcellulose to the levonorgestrel ultrafine mixture, then add 19g of talcum powder, fully mix, add 19g of magnesium stearate, mixed evenly, to obtain the superfine co-pulverized levonorgestrel tablet intermediate;

[0079] c. Tablet compression: measure the content of the intermediate of ultrafine co-pulverized levonorgestrel tablets, calculate the tablet weight according to the specifications of 0.75 mg / tablet or 1.5 mg / tablet, and compress tablets respectively to obtain 0.75 mg / tablet superfine co-pulverized 32518 tablets of levonorgestrel tablets, 30443 ...

Embodiment 2

[0081] a. Superfine co-grinding: Weigh 75g of dry levonorgestrel raw material, mix it with 1000g starch, add 95% ethanol solution, make the mixture wet, superfine pulverize, make 90% of the particle size reach below 20 microns, and dry , to obtain the ultrafine mixture of levonorgestrel;

[0082] b. Mixing: Add 4950g of direct-pressed lactose, 1000g of pregelatinized starch, and 375g of hydroxypropyl methylcellulose to the levonorgestrel ultrafine mixture, then add 50g of talcum powder, mix well, and add 50g of Magnesium stearate, mixed evenly to obtain the intermediate of ultrafine co-pulverized levonorgestrel tablets;

[0083] c. Tablet compression: measure the content of the intermediate of ultrafine co-pulverized levonorgestrel tablets, calculate the tablet weight according to the specifications of 0.75 mg / tablet or 1.5 mg / tablet, and compress tablets respectively to obtain 0.75 mg / tablet superfine co-pulverized 30185 tablets of levonorgestrel tablets, 32077 tablets of 1....

Embodiment 3

[0085] a. Ultrafine co-grinding: Weigh 75g of dry levonorgestrel raw material, mix it with 1500g dextrin, add 60% ethanol solution, after making the mixture wet, ultrafine milling, make 90% particle size reach below 20 microns, bake Dry to obtain the ultrafine mixture of levonorgestrel;

[0086] b. Mixing: add 12600g of direct-pressed lactose, 3150g of pregelatinized starch, 787.5g of hydroxypropyl methylcellulose to the levonorgestrel ultrafine mixture, then add 181g of talcum powder, mix well, and add 181g Magnesium stearate, mixed evenly, to obtain the superfine co-pulverized levonorgestrel tablet intermediate;

[0087] c. Tablet compression: measure the content of the intermediate of ultrafine co-pulverized levonorgestrel tablets, calculate the tablet weight according to the specifications of 0.75 mg / tablet or 1.5 mg / tablet, and compress tablets respectively to obtain 0.75 mg / tablet superfine co-pulverized 30554 levonorgestrel tablets, 31665 levonorgestrel tablets of 1.5m...

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Abstract

The invention provides a preparation method for ultra-micro co-grinding levonorgestrel tablets. The method employs an ultra-micro co-grinding technology, ultra-micro co-grinding levonorgestrel and appropriate fillers according to a certain proportion, and mixing and tabletting with appropriate accessories. Compared with common levonorgestrel tablets obtained by ultra-micro grinding bulk pharmaceutical chemicals and tabletting directly, the levonorgestrel tablets of the invention are significantly increased in dissolution rate, so that the levonorgestrel tablets prepared by the method of the invention are convenient to take, fast in absorption and high in bioavailability, and can improve patient adaptability and increase choices of clinical medication for doctors and patients.

Description

technical field [0001] The invention relates to a preparation method of ultrafine co-pulverized levonorgestrel tablets, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Levonorgestrel is currently a widely used oral contraceptive. It suppresses ovulation and prevents a fertile egg from implanting, while thickening the cervical mucus to stop sperm from advancing. Levonorgestrel is generally administered orally, but this medicine is a poorly soluble medicine, insoluble in water, ethanol, isopropanol acetone, solvents such as ethyl acetate, and its dissolution rate and dissolution rate of the prepared tablet of conventional preparation technology are all average. lower, resulting in lower bioavailability. [0003] Ultrafine co-pulverization can make the crystalline structure of the drug become an amorphous drug under physical action, which can effectively improve its absorption in the body. At the same time, due to the addition of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/567A61P15/18
Inventor 胡向青贾卫东赖丽芳彭丽娇
Owner BEIJING YILING BIOENG
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