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Preparation method for cyclodextrin inclusion levonorgestral tablets

A technology for levonorgestrel tablets and levonorgestrel is applied in the field of preparation of cyclodextrin inclusion levonorgestrel tablets, which can solve the problems of low bioavailability, low tablet dissolution rate and low dissolution rate, etc. question

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 the drug is a poorly soluble drug, insoluble in water, ethanol, isopropanol, acetone, ethyl acetate and other solvents, the dissolution rate and dissolution rate of tablets prepared by conventional preparation technology are low, resulting in low bioavailability

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073] a. Preparation of cyclodextrin inclusion compound: Weigh 75g of dry levonorgestrel raw material, weigh 75g of β-cyclodextrin, mix evenly, add to 1500g of 30% ethanol solution and stir for 200min to obtain levonorgestrel Norgestimate cyclodextrin inclusion complex;

[0074] B, mixing: get 4500g starch, join in the levonorgestrel cyclodextrin inclusion compound solution, fully mix, then add 4425g lactose and 190g carboxymethyl starch sodium, add 1900g10% polyvinylpyrrolidone aqueous solution and mix, Granulate, dry, add 47.5g magnesium stearate, fully mix to obtain cyclodextrin inclusion levonorgestrel tablet intermediate;

[0075] C, tabletting, measure the content of cyclodextrin inclusion levonorgestrel tablet intermediate, calculate sheet weight according to the specification of 0.75mg / tablet or 1.5mg / tablet, be respectively 95.1mg and 190.2mg, compress respectively to obtain 0.75mg / tablet cyclodextrin-included levonorgestrel tablets 30928 tablets, 1.5mg / tablet cyclo...

Embodiment 2

[0077] a. Preparation of cyclodextrin inclusion compound: Weigh 75g of dry levonorgestrel raw material, weigh 375g of β-cyclodextrin, mix evenly, add to 1500g of 50% ethanol solution and stir for 200min to obtain levonorgestrel Norgestimate cyclodextrin inclusion complex;

[0078] b. Mixing: Take 4500g of microcrystalline cellulose, add it to the levonorgestrel cyclodextrin inclusion compound solution, mix thoroughly, then add 4313g of lactose and 190g of crospovidone, mix, add 1900g of purified Mix after water, granulate, dry, add 47.5g of magnesium stearate, and mix well to obtain the intermediate of cyclodextrin inclusion levonorgestrel tablets;

[0079] C, tabletting, measure the content of cyclodextrin inclusion levonorgestrel tablet intermediate, calculate tablet weight according to the specification of 0.75mg / tablet or 1.5mg / tablet, be respectively 95.0mg and 190.0mg, compress respectively to obtain 0.75mg / tablet cyclodextrin-included levonorgestrel tablets 31478 table...

Embodiment 3

[0081] a. Preparation of cyclodextrin inclusion compound: Weigh 75g of dry levonorgestrel raw material, weigh 750g of β-cyclodextrin, mix evenly, add to 1500g of 70% ethanol solution and stir for 100min to obtain levonorgestrel Norgestimate cyclodextrin inclusion complex;

[0082] b. Mixing: Take 4125g of pregelatinized starch, add it to the levonorgestrel cyclodextrin inclusion compound solution, mix thoroughly, then add 4075g of lactose and 285g of croscarmellose sodium, mix, add 1900g 5% aqueous solution of povidone was mixed, granulated, dried, and 95g of magnesium stearate was added, and fully mixed to obtain the cyclodextrin inclusion levonorgestrel tablet intermediate;

[0083] C, tabletting, measure the content of cyclodextrin inclusion levonorgestrel tablet intermediate, calculate sheet weight according to the specification of 0.75mg / tablet or 1.5mg / tablet, be respectively 95.2mg and 190.4mg, compress respectively to obtain 0.75mg / tablet cyclodextrin-included levonor...

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Abstract

The invention provides a preparation method for cyclodextrin inclusion levonorgestral tablets. The preparation method comprises stirring beta-cyclodextrin and levonorgestrel in an appropriate solvent for some time; and mixing and tabletting with appropriate accessories. Compared with common levonorgestrel tablets obtained by directly tabletting, 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, high in bioavailability, and the like, 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 cyclodextrin-included levonorgestrel tablets, which belongs 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 the drug is a poorly soluble drug, insoluble in water, ethanol, isopropanol, acetone, ethyl acetate and other solvents, the dissolution rate and dissolution rate of tablets prepared by conventional preparation technology are low, resulting in low bioavailability. [0003] Cyclodextrin inclusion technology refers to a kind of drug molecular structure is fully or partly included into the cyclodextrin molecular cavity to form a unique form of complex, also known as molecular capsules, making inclusion compounds can inc...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K47/48A61K31/567A61P15/18
Inventor 胡向青贾卫东郝福
Owner BEIJING YILING BIOENG
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