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A kind of emergency contraceptive pharmaceutical composition containing levonorgestrel and its preparation method

A technology of levonorgestrel and emergency contraception, which is applied in the directions of drug combinations, medical preparations containing active ingredients, and pharmaceutical formulations, and can solve the problem of failure to reduce the dosage of levonorgestrel and the irrelevance of bioavailability It can not reflect the real dissolution rate, etc., to achieve the effect of low equipment requirements, reduction of individual differences, and the same dissolution rate

Active Publication Date: 2011-12-07
REGENEX PHARMA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The oral solid preparations of levonorgestrel prepared by existing methods usually have the following defects: low dissolution rate (the dissolution rate of levonorgestrel from some manufacturers only has 30% to 45% of the labeled amount), poor drug absorption, and bioavailability Low, poor emergency contraceptive effect after the event, etc.
However, the in vitro dissolution rate in this patent is measured in a cosolvent sodium lauryl sulfate solution, and the in vitro dissolution rate containing a cosolvent is not related to the in vivo bioavailability, so it cannot reflect Its true dissolution profile
At the same time, the invented product also failed to reduce the dosage of emergency contraception after the event of levonorgestrel

Method used

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  • A kind of emergency contraceptive pharmaceutical composition containing levonorgestrel and its preparation method
  • A kind of emergency contraceptive pharmaceutical composition containing levonorgestrel and its preparation method
  • A kind of emergency contraceptive pharmaceutical composition containing levonorgestrel and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] prescription:

[0053] Levonorgestrel 2.0g

[0054] Organic solvent Trichloromethane 30ml

[0055] Crystallization Inhibitor Povidone K30 20g

[0056] Inert carrier hydroxypropyl cellulose 10g, mannitol 70g, dextrin 20g and microcrystalline cellulose 50g Pharmaceutically acceptable drug carrier sodium carboxymethyl starch 4.8g and magnesium stearate 1.6g

[0057] Preparation:

[0058] (1) adding levonorgestrel to the organic solvent and dissolving to form mixed solution A;

[0059] (2) adding a crystallization inhibitor in A to form a mixed solute B;

[0060] (3) B is slowly added to the inert carrier, granulated (cutting 1500rpm / min, stirring paddle 250rpm / min) to form mixture C;

[0061] (4) Dry C at 75°C for 2 to 3 hours, and the solvent residue should not exceed the limit to obtain mixture D, which is sieved through a 40-mesh sieve to granulate;

[0062] (5) mixture D is mixed with pharmaceutically acceptable medicine, mixes 10min, obtains mixture E;

[0063]...

Embodiment 2

[0065] prescription

[0066] Levonorgestrel 2.0g

[0067] Organic solvent Dichloromethane 30ml

[0068] Crystallization Inhibitor Povidone K30 20g

[0069] Inert carrier methyl cellulose 10g, mannitol 70g, dextrin 20g and microcrystalline cellulose 50g Pharmaceutically acceptable pharmaceutical carrier sodium carboxymethyl starch 4.8g and magnesium stearate 1.6g

[0070] Preparation:

[0071] Steps (1) to (5) are as in Example 1, and step (6) is to press E into tablets with a specification of 1.10 mg (B1) or 1.20 mg (B2) or fill them into capsules B3 and B4 of corresponding specifications. .

Embodiment 3

[0073] prescription

[0074] Levonorgestrel 2.0g

[0075] Organic solvent dimethyl sulfoxide 30ml

[0076] Crystallization Inhibitor Povidone K17 10g

[0077] Inert carrier ethyl cellulose 10g, mannitol 70g, dextrin 20g and microcrystalline cellulose 50g Pharmaceutically acceptable pharmaceutical carrier sodium carboxymethyl starch 4.8g and magnesium stearate 1.6g

[0078] Preparation:

[0079] Steps (1) to (5) are as in Example 1, and step (6) is to press E into tablets with a specification of 1.10 mg (C1) or 1.20 mg (C2) or fill them into capsules C3 and C4 of corresponding specifications. .

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PUM

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Abstract

The invention relates to a post-event emergency contraceptive pharmaceutical composition containing low-dose levonorgestrel without reducing the contraceptive effect. In the described pharmaceutical composition, the dosage of levonorgestrel contained in the single-dose pharmaceutical dosage unit for emergency contraception is reduced from the conventional 1.5 mg to 1.00-1.25 mg, and the double-administered pharmaceutical dosage unit The dosage of levonorgestrel contained is reduced from the conventional 0.75mg to 0.50-0.625mg. Compared with the conventional dosage, the present invention reduces the dosage of levonorgestrel, reduces individual differences and adverse reactions, and has important clinical significance. The invention also provides the preparation method of the pharmaceutical composition and the use of the pharmaceutical composition in the preparation of a medicine for treating emergency contraception.

Description

technical field [0001] The invention relates to an emergency contraceptive pharmaceutical composition containing levonorgestrel, which is used for emergency contraception after sexual intercourse, and provides a preparation method of the pharmaceutical composition. Background technique [0002] Levonorgestrel, its English name is Levonorgestrel, its chemical name is (-)-13-ethyl-17 hydroxy-18,19-bisdesmethyl-17a-pregna-4-ene-20 -Alkyn-3-one, its structural formula is as follows: [0003] [0004] Molecular formula: C 21 H 28 O 2 , molecular weight: 312.47 [0005] Levonorgestrel is a progestogen that can negatively feedback inhibit the production of follicle-stimulating hormone and luteinizing hormone, thereby inhibiting ovulation and increasing the viscosity of cervical secretions. It is widely used in clinical emergency contraception and has good effects. . [0006] The oral solid preparations of levonorgestrel prepared by the existing methods usually have the fol...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/567A61P15/18
Inventor 卢智俊李晖莹彭贵子
Owner REGENEX PHARMA LTD