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Preparation method for solid dispersion levonorgestrel tablets

A technology of levonorgestrel tablets and levonorgestrel, which is applied in the direction of non-active ingredient medical preparations, active ingredient-containing medical preparations, pharmaceutical formulas, etc., and can solve the problem of low dissolution rate and dissolution rate of tablets , low bioavailability and other issues

Inactive 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 dispersion: take polyethylene glycol 4000 750g, heat and melt, add dry levonorgestrel raw material 75g, fully stir, take out after cooling to complete solidification, pulverize, obtain levonorgestrel dispersion ;

[0074] b. Mixing: Take 8250g of spray-dried lactose, add levonorgestrel dispersion and 285g sodium carboxymethyl starch, mix well, then add 47.5g magnesium stearate and 95g talcum powder, mix well to obtain solid dispersion left Norgestrel tablet intermediate;

[0075] c, tablet compression, measure the content of the solid dispersion levonorgestrel tablet intermediate, calculate the sheet weight according to the specification of 0.75mg / tablet or 1.5mg / tablet, be respectively 95.0mg and 190.0mg, compress respectively to get 0.75mg / tablet 31008 tablets of solid-dispersed levonorgestrel tablets, 31613 tablets of 1.5 mg / tablet solid-dispersed levonorgestrel tablets.

Embodiment 2

[0077] a. Preparation of dispersion: Weigh 750g of poloxamer, heat and melt, add 75g of dry levonorgestrel raw material, fully stir, take out after cooling to complete solidification, and pulverize to obtain levonorgestrel dispersion;

[0078] b. Mixing: Take 8250g of spray-dried lactose, add levonorgestrel dispersion and 285g sodium carboxymethyl starch, mix well, then add 47.5g talcum powder and 95g magnesium stearate, mix well to obtain solid dispersion left Norgestrel tablet intermediate;

[0079] c, tablet compression, measure the content of the solid dispersion levonorgestrel tablet intermediate, calculate the sheet weight according to the specification of 0.75mg / tablet or 1.5mg / tablet, be respectively 95.2mg and 190.4mg, compress respectively to get 0.75mg / tablet 31417 tablets of solid-dispersed levonorgestrel tablets, 30921 tablets of 1.5 mg / tablet solid-dispersed levonorgestrel tablets.

Embodiment 3

[0081] a, dispersion preparation: take polyethylene glycol 6000 1500g, heat and melt, add dry levonorgestrel raw material 75g, fully stir, take out after cooling to complete solidification, pulverize, obtain levonorgestrel dispersion ;

[0082] B. Mixing: Get 7545 parts by weight of spray-dried lactose, add levonorgestrel dispersion and 285g crospovidone, fully mix, then add 47.5g magnesium stearate and 47.5g talcum powder, fully mix to obtain Solid dispersion levonorgestrel tablet intermediate;

[0083] c, tablet compression, measure the content of the solid dispersion levonorgestrel tablet intermediate, calculate the sheet weight according to the specification of 0.75mg / tablet or 1.5mg / tablet, be respectively 95.0mg and 190.0mg, compress respectively to get 0.75mg / tablet 31068 tablets of solid-dispersed levonorgestrel tablets, 30983 tablets of 1.5 mg / tablet solid-dispersed levonorgestrel tablets.

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Abstract

The invention provides a preparation method for solid dispersion levonorgestrel tablets. The preparation method employs a melting method to prepare a solid dispersion of the levonorgestrel; 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 solid-dispersed 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 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] Solid dispersion (solid dispersion) refers to the dispersion system formed by uniformly dispersing drugs in a certain solid carrier substance in the state of molecules, colloids, microcrystals, etc. The formulation technology used to make drugs into solid d...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/567A61K47/34A61K47/38A61P15/18
Inventor 胡向青贾卫东魏改芹王畅
Owner BEIJING YILING BIOENG
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