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Micronized composition containing Levonorgestrel

A technology of levonorgestrel and its composition, which is applied in the field of micronized levonorgestrel-containing composition, can solve the problems of affecting the effect of emergency contraception, prolonging the drug absorption time, etc., and achieve rapid onset and accelerated release , Improve the effect of release

Active Publication Date: 2010-01-20
CHINA RESOURCES ZIZHU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In order to solve the problem in the prior art that the delayed release of the enteric solvent type of levonorgestrel prolongs the drug absorption time and thus affects the effect of emergency contraception, the present invention provides a method that can reduce the incidence of vomiting and can A micronized levonorgestrel-containing composition that enables levonorgestrel to be released rapidly in the body, and works better to better achieve the purpose of emergency contraception

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Drug core:

[0037] Micronized Levonorgestrel 1.5g

[0038] Lactose 5g

[0039] Starch 45g

[0040] Sucrose 35g

[0041] Dextrin 5g

[0042] 5% starch slurry appropriate amount

[0043] Sodium carboxymethyl starch 2g

[0044] Magnesium Stearate 1g

[0045] Isolation gown layer:

[0046] Opadry YS-1-7027 3g

[0047] water 22g

[0048] Enteric coating layer:

[0049] Opadry 93063209 5g

[0050] water 20g

[0051] Micronize the levonorgestrel powder with 70%-90% particles less than or equal to 10 microns, mix it with lactose, sucrose, starch, and dextrin in equal amounts, and add an appropriate amount of 5% starch slurry to make granules, 60 Ventilated and dried at ℃, granulated, added sodium carboxymethyl starch and magnesium stearate, mixed evenly, pressed into tablets, coated with isolation coat and enteric coating on the tablets, and made 1000 tablets.

Embodiment 2

[0053] Drug core:

[0054] Micronized Levonorgestrel 1.5g

[0055] Lactose 60g

[0056] Microcrystalline Cellulose 30g

[0057] 10% ethanol solution of povidone K30

[0058]Magnesium Stearate 1g

[0059] Isolation gown layer:

[0060] Hypromellose 3g

[0061] Polyethylene glycol 0.5g

[0062] Titanium dioxide 0.7g

[0063] Talc powder 0.6g

[0064] Enteric coating layer:

[0065] Acrylic resin 8g

[0066] Triethyl citrate 0.8g

[0067] Talc powder 1.6g

[0068] Micronized 50%-70% levonorgestrel powder with particles less than or equal to 10 microns is uniformly mixed with lactose and microcrystalline cellulose according to the method of equal volume addition, and an appropriate amount of ethanol solution of 10% povidone K30 is added. Granules, ventilated and dried at 60°C, granulated, added with magnesium stearate, mixed evenly, compressed into tablets, coated with isolation coats and enteric coatings on the tablets to obtain 1000 tablets.

Embodiment 3

[0070] Drug core:

[0071] Micronized Levonorgestrel 0.75g

[0072] Sucrose 55g

[0073] Dextrin 20g

[0074] Sodium carboxymethyl starch 2g

[0075] 2% hypromellose solution appropriate amount

[0076] Magnesium Stearate 1g

[0077] Enteric coating layer:

[0078] Polyvinyl acetate phthalate 10g

[0079] Talc powder 1.6g

[0080] Micronize the levonorgestrel powder with 70%-100% particles less than or equal to 20 microns, mix it with sucrose, dextrin, sodium carboxymethyl starch, and add an appropriate amount of 2% hypromellose The solution is made into granules, ventilated and dried at 60°C, sized, added with magnesium stearate, mixed evenly, filled into No. 3 capsules, and coated with enteric coating to obtain 1000 granules.

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Abstract

The invention relates to a micronized composition containing Levonorgestrel, and aiming at the problem of low dissolution rate of the Levonorgestrel enteric coated preparation in the prior art, the invention provides the micronized composition containing Levonorgestrel. In the invention, 70 to 100 percent of Levonorgestrel is micronized to particles, and the grain diameter of each particle is less than or equal to 20 nanometers; the particles are combined with 60 to 97.9 percent of excipient to be prepared into a medicine core; and the medicine core is coated by a coating layer. The composition greatly improves the releasing degree and the peak time of the Levonorgestrel and Tmax.

Description

technical field [0001] The invention relates to a micronized pharmaceutical composition for contraception, in particular to a micronized levonorgestrel-containing composition. Background technique [0002] Levonorgestrel is used as a progestogen for contraception, especially emergency contraception. Emergency contraception refers to remedial measures taken to prevent pregnancy after intercourse without any contraceptive measures or after contraceptive failure: or taking emergency contraceptive pills within 72 hours after intercourse without contraceptive measures; or placing intrauterine within 5 days IUD. The purpose of taking emergency contraception is to prevent fertilization or implantation of fertilized eggs in the shortest possible time. The dissolution rate of the drug is an important factor affecting the time of action of the drug, so in order to better achieve the purpose of emergency contraception, the dissolution rate of the emergency contraceptive drug should b...

Claims

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Application Information

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IPC IPC(8): A61K31/567A61K9/14A61K9/20A61K9/48A61P15/18
Inventor 周敏李源郑焱张明赵红欣
Owner CHINA RESOURCES ZIZHU PHARMA
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