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Levonorgestrel drop pills and preparation method thereof

A technology of levonorgestrel and drop pills, which is applied in the field of levonorgestrel drop pills and its preparation, and can solve the problems of poor water solubility and low bioavailability of levonorgestrel

Active Publication Date: 2008-10-22
SHANDONG RUIAN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, levonorgestrel unilaterally is mainly administered in the form of oral tablets, but due to the poor water solubility of levonorgestrel and low bioavailability, the present invention prepares levonorgestrel solid dispersion enhance its bioavailability

Method used

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  • Levonorgestrel drop pills and preparation method thereof
  • Levonorgestrel drop pills and preparation method thereof
  • Levonorgestrel drop pills and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] 1. Prescription

[0045] (1) Levonorgestrel drop pill core components

[0046] Levonorgestrel 7.5g

[0047] Macrogol 6000 240g

[0048] Polysorbate 80 28g

[0049]

[0050] Makes 10000 pills

[0051] (2) Coating layer prescription

[0052] Dropping Pill Core 275.5g

[0053] Coating powder 10g

[0054] Aspartame 2g

[0055] Apple essence 2g

[0056] 80% ethanol solution 120ml

[0057] 2. The preparation method of levonorgestrel dropping pills:

[0058] (1) Put polyethylene glycol 6000 into a beaker, heat to about 80°C and stir to mix evenly after melting;

[0059] (2) Put the micronized levonorgestrel and polysorbate 80 into another beaker, heat to about 80°C and stir thoroughly to mix completely;

[0060] (3) Mix (1) and (2) evenly;

[0061] (4) Use a No. 12 standard needle to drop the mixed solution into the cooled simethicone oil, settle for about 30 minutes, filter, and remove the attached condensate;

[0062] (5) Stir the coat...

Embodiment 2

[0064] 1. Prescription

[0065] (1) Levonorgestrel drop pill core components

[0066] Levonorgestrel 7.5g

[0067] Macrogol 6000 180g

[0068] Polyoxyl(40) stearate 60g

[0069] Polysorbate 80 28g

[0070]

[0071] Makes 10000 pills

[0072] (2) Coating layer prescription

[0073] Dropping Pill Core 275.5g

[0074] Coating powder 10g

[0075] Aspartame 2g

[0076] Orange essence 2g

[0077] 80% ethanol solution 120ml

[0078] 2. The preparation method of levonorgestrel dropping pills:

[0079] (1) Put polyethylene glycol 6000 and polyoxyl (40) stearate into a beaker, heat to about 80°C and stir to mix evenly after melting;

[0080] (2) Put the micronized levonorgestrel and polysorbate 80 into another beaker, heat to about 80°C and stir thoroughly to mix completely;

[0081] (3) Mix (1) and (2) evenly;

[0082] (4) Use a No. 12 standard needle to drop the mixed solution into the cooled simethicone oil, settle for about 30 minutes, f...

Embodiment 3

[0085] 1. Prescription

[0086] (1) Levonorgestrel drop pill core components

[0087] Levonorgestrel 7.5g

[0088] Macrogol 4000 80g

[0089] Macrogol 6000 160g

[0090] Polysorbate 80 28g

[0091]

[0092] Makes 10000 pills

[0093] (2) Coating layer prescription

[0094] Dropping Pill Core 275.5g

[0095] Coating powder 10g

[0096] Neotame 0.2g

[0097] Orange essence 2g

[0098] 80% ethanol solution 120ml

[0099] 2. The preparation method of levonorgestrel dropping pills:

[0100] (1) Put polyethylene glycol 4000 and polyethylene glycol 6000 into a beaker, heat to about 80°C and stir to mix evenly after melting;

[0101] (2) Put the micronized levonorgestrel and polysorbate 80 into another beaker, heat to about 80°C and stir thoroughly to mix completely;

[0102] (3) Mix (1) and (2) evenly;

[0103] (4) Use a No. 12 standard needle to drop the mixed solution into the cooled simethicone oil, settle for about 30 minutes, filter, and re...

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Abstract

The invention provides a Levonorgestrel pill and a preparation method thereof. The Levonorgestrel pill consists of a pill core and a coating layer, wherein, the pill core comprises Levonorgestrel active ingredient, carrier used as dispersant and surface active agent with a weight ratio of 1: 10-60: 1-10; the coating material used by the coating layer consists of coating powders and correctives. The coating powders adopt gastric solubility film coating powders, the dosage of which is 2-6 percent (w / w) of the total amount of the Levonorgestrel pill; the dosage of the correctives is 0.1-2 percent (w / w) of the total amount of the Levonorgestrel pill. The preparation method of the Levonorgestrel pill is that the Levonorgestrel raw material is micronized to a grain diameter of less than 20 Mu m; in the preparation process, main medicine is evenly dispersed in the carrier to form a solid dispersoid, thus improving the drug water solubility, increasing the drug dissolution rate and bioavailability and more effectively playing a curative role.

Description

technical field [0001] The invention relates to a levonorgestrel dropping pill with high bioavailability and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] The chemical name of levonorgestrel is (-)-13-ethyl-17-hydroxy-18,19-bis-demethyl-17α-pregna-4-en-20-yn-3-one, which is a Progesterone, from January 1, 2001, began to have an over-the-counter drug status in the UK, and its oral administration is mainly used for female emergency contraception. Molecular formula C 21 h 28 o 2 , relative molecular mass 312.47. This product is white or white crystalline powder; soluble in chloroform, slightly soluble in methanol, insoluble in water. Its structural formula is: [0003] [0004] Pharmacological action: Levonorgestrel is a progestogen, which mainly acts on the hypothalamus and pituitary gland. It can reduce or disappear the peak levels of follicle-stimulating hormone and luteinizing hormone in...

Claims

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Application Information

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IPC IPC(8): A61K9/32A61K31/567A61P15/18A61P5/34
Inventor 侯金升王丽
Owner SHANDONG RUIAN PHARMA CO LTD
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