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Mifepristone slow release preparation characterized by gastric stasis and preparation method thereof

A technology of mifepristone and sustained-release preparation, applied in the field of medicine, can solve the problems of low efficiency and the like

Active Publication Date: 2012-10-03
REGENEX PHARMA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These research results have improved the bioavailability to a certain extent, but they cannot overcome the problems of large individual differences and low effective rates

Method used

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  • Mifepristone slow release preparation characterized by gastric stasis and preparation method thereof
  • Mifepristone slow release preparation characterized by gastric stasis and preparation method thereof
  • Mifepristone slow release preparation characterized by gastric stasis and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Melt 600g of PEG-6000 at 75°C, add 250g of micronized mifepristone (particle size<2μm) to mix and disperse, vacuumize and cool at room temperature, then pulverize, add 100g of fumaric acid and 700g of microcrystalline fiber to the crushed powder Vegetable, 15g PVP K30, mix evenly, add water to make soft material, extrude and spheronize to make pellets. Take half of the amount of the pellet package slow-release layer (Eudragit RS PO:Eudragit RLPO=40:60) and adhesion layer (carbomer). The coated and uncoated pellets are blended and filled into capsules.

Embodiment 2

[0042]Melt 600g of PEG-6000 at 75°C, add 250g of micronized mifepristone (particle size<5μm) to mix, disperse, spray and condense to obtain crushed powder, add 100g of fumaric acid and 700g of microcrystalline cellulose to the crushed powder , 15g PVP K30, mix evenly, add water to make soft material, extrude and spheronize, and make micropills. A slow-release layer (Eudragit RS PO:Eudragit RL PO=40:60) and an adhesive layer (carbomer) were included. Another mixed powder that has not been made into pellets was wet granulated and coated pellets were blended at a weight ratio of 40:60 and then compressed into tablets.

Embodiment 3

[0044] 600g of 2-hydroxypropyl-β-cyclodextrin and 250g of micronized mifepristone (particle size <3 μm) were simultaneously dissolved in 1mol / L hydrochloric acid solution, ground uniformly, and vacuum-dried at room temperature. Then pulverize the dried mixture, add 100g of fumaric acid, 700g of microcrystalline cellulose, and 15g of HPMCK100, mix evenly, add water to make a soft material, extrude and spheronize to obtain pellets. Take half of the pellets and pack the slow-release layer (Eudragit RS PO:Eudragit RL PO=40:60) and the adhesive layer (hydroxypropyl methylcellulose). The coated and uncoated pellets are blended and filled into capsules.

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Abstract

The invention relates to a mifepristone slow release preparation characterized by gastric stasis and a preparation method thereof. The preparation comprises a quick release mifepristone system and a slow release mifepristone cellular system. The quick release mifepristone system accounts for 10-80 wt% of the total weight and the balance is the slow release mifepristone celluar system. The slow release preparation consists of micronized mifepristone, solubilizer, pH regulator, diluent, bond, slow release material and adhesion material. The experimental results show that the bioavailability of the mifepristone slow release preparation characterized by gastric stasis is increased by more than 50% in comparison with the bioavailability of common mifepristone tablets, and the individual difference is obviously reduced. Therefore, the mifepristone slow release preparation characterized by gastric stasis can enhance the bioavailability and improve the individual difference so that the dosagereduction is possible.

Description

technical field [0001] The invention relates to a pharmaceutical preparation and a preparation method thereof, in particular to a mifepristone sustained-release preparation with gastric retention properties and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Mifepristone, its English name is mifepristone, and its chemical name is 11β-[4-(N,N-dimethylamino)]phenyl-17β-hydroxyl-17α-(1-propynyl)-estro- 4,9-Dien-3-one. Its structural formula is as follows: [0003] [0004] Molecular formula is C 29 h 35 NO 2 , with a molecular weight of 429.61. [0005] Mifepristone is a progesterone receptor antagonist, which was synthesized for the first time in 1980 by Rousel-Ucalf Company in France, and has been widely used clinically for anti-early pregnancy emergency contraception and menstruation-inducing anti-pregnancy. New indications for the treatment of uterine fibroids, endometriosis, breast cancer, depression, etc. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K9/22A61K9/52A61K31/567A61P15/18A61P15/00A61P35/00A61P25/24
Inventor 黄芳
Owner REGENEX PHARMA LTD
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