Mifepristone capsule and preparation method thereof

A mifepristone and capsule technology, which is applied in the field of mifepristone capsules and its preparation, can solve the problems of increasing stomach burden, influence on drug absorption, reducing availability, etc., so as to improve bioavailability and reduce nausea and vomiting. , the effect of increasing solubility

Active Publication Date: 2022-04-22
深圳市资福药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the problem that this invention exists is that the solubility of pure mifepristone is high in the strongly acidic gastric environment, and after reaching the intestinal tract, it causes crystallization due to the increase of pH, thereby reducing the availability. Although this invention improves However, after dissolving in the stomach, mifepristone and β-cyclodextrin dissociate, and the dissolved mifepristone may also be precipitated in the intestinal tract, resulting in reduced availability
But the problem of this invention is that in this invention, the absorption site of mifepristone is in the stomach, and mifepristone has greater irritation to the stomach, and side effects such as nausea and vomiting may occur, and the stomach is enlarged simultaneously. The burden on the stomach, eating will also have a greater impact on drug absorption, and the period of prolonging gastric retention is limited after all, and the absorption rate of mifepristone is also limited. After mifepristone enters the intestinal tract, it may also be due to crystallization resulting in decreased availability

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] A preparation method of mifepristone capsules, comprising the following steps:

[0062] N1: Grind mifepristone to a particle size of more than 90% and less than 10 μm, then mix 2.5 g of pulverized mifepristone with 15 g of melted solubilizer, mix evenly, cool and solidify, and then pulverize through a 40-mesh sieve to obtain Mifepristone mixtures containing solubilizers;

[0063] N2 Mix the mifepristone mixture containing the solubilizer obtained in the step N1 with 15g xanthan gum, 10g citric acid, and 57.5g lactose to obtain the contents of the capsule;

[0064] N3 filling 1 g of the capsule contents obtained in step N2 into enteric-coated empty capsules to obtain mifepristone capsules.

[0065] The solubilizer is polyoxyethylene sorbitan monolaurate.

Embodiment 2

[0067] A preparation method of mifepristone capsules, comprising the following steps:

[0068] N1: Grind mifepristone to a particle size of more than 90% and less than 10 μm, then mix 2.5 g of pulverized mifepristone with 15 g of melted solubilizer, mix evenly, cool and solidify, and then pulverize through a 40-mesh sieve to obtain Mifepristone mixtures containing solubilizers;

[0069] N2 Mix the mifepristone mixture containing the solubilizer obtained in the step N1 with 15g xanthan gum, 10g citric acid, and 57.5g lactose to obtain the contents of the capsule;

[0070] N3 filling 1 g of the capsule contents obtained in step N2 into enteric-coated empty capsules to obtain mifepristone capsules.

[0071] The solubilizer is multi-branched polyether.

[0072] The preparation method of described multi-branched polyether comprises the following steps:

[0073] S1 Mix 10g of diphenolic propane and 15g of tetraethylenepentamine, heat to 100°C to completely dissolve the diphenolic...

Embodiment 3

[0076] A preparation method of mifepristone capsules, comprising the following steps:

[0077] N1: Grind mifepristone to a particle size of more than 90% and less than 10 μm, then mix 2.5 g of pulverized mifepristone with 15 g of melted solubilizer, mix evenly, cool and solidify, and then pulverize through a 40-mesh sieve to obtain Mifepristone mixtures containing solubilizers;

[0078] N2 Mix the mifepristone mixture containing the solubilizer obtained in the step N1 with 15g xanthan gum, 10g citric acid, and 57.5g lactose to obtain the contents of the capsule;

[0079] N3 filling 1 g of the capsule contents obtained in step N2 into enteric-coated empty capsules to obtain mifepristone capsules.

[0080] The solubilizer is gelatin sodium oleate.

[0081] The preparation method of described gelatin sodium oleate, comprises the following steps:

[0082] M1 Dissolve 6g of sodium oleate in 60mL of water, heat to 70°C, stir for 10min, then add 0.3g of 1-ethyl-(3-dimethylaminopro...

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Abstract

The invention discloses a mifepristone capsule and a preparation method thereof. The mifepristone capsule comprises mifepristone, a solubilizer, an adhesive, an acidity regulator and a diluent. The preparation method of the mifepristone capsule comprises the following steps: firstly crushing mifepristone, and then mixing the crushed mifepristone with a solubilizer to obtain a mifepristone mixture containing the solubilizer; mixing the mifepristone mixture containing the solubilizer with an adhesive, an acidity regulator and a diluent to obtain a capsule content; and finally, filling the capsule content into an empty capsule to obtain the mifepristone capsule. The mifepristone capsule prepared by adding the self-made solubilizer has a very good slow-release effect in intestinal tracts, and the bioavailability can be remarkably improved.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a mifepristone capsule and a preparation method thereof. Background technique [0002] Mifepristone (MIF) is a norethindrone derivative, its chemical name is 11-β[4-(N,N-dimethylamino)-1-phenyl]-17β-hydroxyl-17α- (1-propynyl)-estr-4,9-dien-3-one, the molecular formula is C 29 h 35 NO 2 , with a molecular weight of 429.61. French company Rossel-Uclaf successfully developed in 1980, is the world's first synthetic anti-progestin drug. [0003] MIF can competitively bind with progesterone receptors (the affinity for endometrial progesterone receptors is 5 times stronger than that of progesterone), thereby inhibiting the activity of endogenous or exogenous progesterone. In the early days, MIF was mainly used for emergency contraception and medical abortion (often used in conjunction with prostaglandin drugs), and is now also widely used in the treatment of ectopic pregn...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/567A61K47/42A61K47/34A61P5/36A61P15/00A61P35/00C08G65/28C08H1/00
CPCA61K9/4866A61K31/567A61P15/00A61P35/00A61P5/36C08G65/2624C08H1/00Y02A50/30
Inventor 邱文吴法清凌向平姜海兵
Owner 深圳市资福药业有限公司
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