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Sterides anti-progestogen composition and preparation method thereof

A technology of anti-progestin and composition, which is applied in the field of steroidal anti-progestin pharmaceutical composition, can solve the problems of low bioavailability, achieve the effects of avoiding side effects, reducing individual differences, and prolonging residence time

Active Publication Date: 2011-06-29
REGENEX PHARMA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The purpose of the present invention is to solve the problem of low bioavailability of anti-progestin due to the dependence of dissolution and absorption on pH in the prior art, and to provide a new anti-progestin pharmaceutical composition. Contains two parts: immediate-release pellets and sustained-release adherent pellets

Method used

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  • Sterides anti-progestogen composition and preparation method thereof
  • Sterides anti-progestogen composition and preparation method thereof
  • Sterides anti-progestogen composition and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0057] (1) Preparation of immediate-release pellets:

[0058] Take 40g of antiprogestin mifepristone with a micronized particle size of 2 μm, add it to the heated and melted dispersant polyethylene glycol 600032g, mix well, spray cooling and granulate; dry granules and disintegrant carboxymethyl starch 18g of sodium and croscarmellose sodium, 72g of lactose as a filler, 8g of low-substituted hydroxypropyl methylcellulose as a binder are mixed, and then an organic solvent, ethanol aqueous solution, is added to make a soft material, and the orifice is extruded with a thickness of 0.5mm Extruded, quickly placed in a spheronizing pot to spheroidize, discharged, and dried to obtain 188g of quick-release pellets.

[0059] (2) Preparation of slow-release adhesive pellets:

[0060] Take 4 g of polyacrylic acid resin as the sustained-release agent, and dissolve it in the organic solvent ethanol to prepare a sustained-release coating solution. Get the quick-release pellet 120g that st...

Embodiment 2

[0063] 1) Preparation of immediate-release pellets:

[0064] Get antiprogestogen mifepristone 20g, disintegrating agent carboxymethyl starch sodium and croscarmellose sodium each 10g join in the dispersing agent poloxamer 40g that heats and melts, after mixing evenly, spray cooling preparation Granules; dry granules are mixed with 380g of microcrystalline cellulose as filler and 30g of low-substituted HPMC as binder, then add a certain amount of water-based soft material, extrude with a 0.4mm extrusion orifice, and quickly place them in a spheronizing pot to spheroidize. material, dried to obtain 490g of immediate-release pellets.

[0065] 2) Preparation of slow-release adhesive pellets:

[0066] Take 40 g of sustained-release agent cellulose acetate phthalate, 10 g of foaming agent sodium bicarbonate, and 20 g of pore-forming agent sugar powder, disperse them in organic solvent ethanol, and then add water to prepare a sustained-release coating solution. In addition, 20 g of...

Embodiment 3

[0069] The preparation method is the same as in Example 1, 60g of mifepristone, wherein the dispersant is replaced by 800012g of polyethylene glycol, the disintegrant is replaced by 6g of cross-linked polyvinylpyrrolidone, the filler is replaced by 90g of powdered sugar, and the binder is replaced by PVP K3033g, slow-release agent is replaced by ethyl cellulose dispersion 9g, foaming agent is replaced by calcium carbonate 0.3g, porogen is replaced by polyethylene glycol 0.6g, adhesive agent is replaced by xanthan gum 9g.

[0070] Take 81g of immediate-release pellets and 129g of slow-release adherent pellets, mix them, and pack them into capsule shells containing the antiprogestin mifepristone 25mg per capsule to obtain sample 3.

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Abstract

The invention provides a sterides anti-progestogen composition which comprises immediate-release pellets and sustained-release adhesive pellets, wherein the immediate-release pellet contains anti-progestogen, dispersing agent, disintegrating agent, filler and binder; and the sustained-release adhesive pellet contains the immediate-release pellet, sustained-release agent, adhesive agent, foaming agent and porogen. The anti-progestogen composition provided by the invention can promote absorption of sterides anti-progestogen medicine and improve bioavailability and curative effect.

Description

technical field [0001] The invention of this product relates to a steroidal antiprogestin pharmaceutical composition and a preparation containing the composition. The composition and the pharmaceutical preparation include quick-release pellets and slow-release adhesive pellets. The antiprogestogen drug preparation of the invention can fully absorb the antiprogestogen in the stomach, improves bioavailability and reduces adverse reactions. Background technique [0002] Antiprogestins can bind to progesterone receptors, and have the functions of terminating early pregnancy, anti-implantation, inducing menstruation and promoting cervical ripening. At present, mifepristone and euriprestone acetate (CDB-2914) have been successfully developed and marketed, and cymipristone and CDB-4124 are still under study. Both mifepristone and euripristone acetate can be used as emergency contraception, benefiting most women. Cymipristone is currently being developed in combination with misopr...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K9/22A61K9/52A61K31/573A61K31/575A61K31/567A61P15/00A61P15/06A61P15/18
Inventor 杨伟谢恒杨舒隽杨丽雯
Owner REGENEX PHARMA LTD