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Levonorgestrel-containing emergency contraception medicament composition and preparation method thereof

A technology for levonorgestrel and emergency contraception, which is applied in drug combinations, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problem of failing to reduce the dosage of levonorgestrel and not reflecting the real dissolution rate , Bioavailability is not relevant and other issues, to achieve the effect of low equipment requirements, reduce individual differences, and facilitate production

Active Publication Date: 2010-06-16
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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  • Levonorgestrel-containing emergency contraception medicament composition and preparation method thereof
  • Levonorgestrel-containing emergency contraception medicament composition and preparation method thereof
  • Levonorgestrel-containing emergency contraception medicament composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] prescription:

[0054] Levonorgestrel 2.0g

[0055] Organic solvent Chloroform 30ml

[0056] Crystallization Inhibitor Povidone K30 20g

[0057] Inert carrier 10g of hydroxypropyl cellulose, 70g of mannitol, 20g of dextrin and 50g of microcrystalline cellulose Pharmaceutically acceptable drug carrier 4.8g of sodium carboxymethyl starch and 1.6g of magnesium stearate

[0058] Preparation:

[0059] (1) adding levonorgestrel to an organic solvent for dissolution to form a mixed solution A;

[0060] (2) adding a crystallization inhibitor to A to form a mixed solution B;

[0061] (3) Slowly add B to the inert carrier, granulate (cut at 1500rpm / min, stirrer at 250rpm / min), and form mixture C;

[0062] (4) Dry C at 75°C for 2 to 3 hours, and the residual solvent should not exceed the limit to obtain mixture D, which is passed through a 40-mesh sieve for granulation;

[0063] (5) Mix the mixture D with a pharmaceutically acceptable drug, and mix for 10 minutes to obtain t...

Embodiment 2

[0066] prescription

[0067] Levonorgestrel 2.0g

[0068] Organic solvent Dichloromethane 30ml

[0069] Crystallization Inhibitor Povidone K30 20g

[0070] Inert carrier: methylcellulose 10g, mannitol 70g, dextrin 20g and microcrystalline cellulose 50g Pharmaceutically acceptable drug carrier: sodium carboxymethyl starch 4.8g and magnesium stearate 1.6g

[0071] Preparation:

[0072] Steps (1) to (5) are as in Example 1, step (6) is to compress E into tablets with a specification of 1.10mg (B1) or 1.20mg (B2) or fill it into capsules B3 and B4 of corresponding specifications .

Embodiment 3

[0074] prescription

[0075] Levonorgestrel 2.0g

[0076] Organic solvent Dimethyl sulfoxide 30ml

[0077] Crystallization Inhibitor Povidone K17 10g

[0078] Inert carrier ethyl cellulose 10g, mannitol 70g, dextrin 20g and microcrystalline cellulose 50g pharmaceutically acceptable drug carrier sodium carboxymethyl starch 4.8g and magnesium stearate 1.6g

[0079] Preparation:

[0080] Steps (1) to (5) are as in Example 1, and step (6) is to compress E into tablets with specifications of 1.10mg (C1) or 1.20mg (C2) or fill them into capsules C3 and C4 of corresponding specifications .

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Abstract

The invention relates to an after emergency contraception medicament composition containing low-dose levonorgestrel without reducing contraceptive effect. In the medicament composition, the consumption of levonorgestrel contained by a medicament dosage unit with single-dosage medicament for emergency contraception is reduced from conventional 1.5 mg to 1.00 to 1.25 mg, and the consumption of levonorgestrel contained by the medicament dosage unit with two-dosage administration is reduced from conventional 0.75 mg to 0.50 to 0.625 mg. The composition reduces the dosage of the levonorgestrel used relative to conventional medicament dosage and reduces individual differences as well as adverse reaction, thereby having important clinical significance. The invention also provides a method for preparing the medicament composition, as well as the application of the medicament composition in the preparation of emergency contraception medicaments.

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, and its chemical name is (-)-13-ethyl-17-hydroxy-18,19-bis-demethyl-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 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 with good results . [0006] The oral solid preparations of levonorgestrel prepared by existing methods usually have the following defec...

Claims

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Application Information

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IPC IPC(8): A61K31/567A61P15/18
Inventor 卢智俊李晖莹彭贵子
Owner REGENEX PHARMA LTD
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