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Cyclodextrin mifepristone clathrate compound, preparation method thereof, and pharmaceutical composition containing clathrate compound

A technology of cyclodextrin inclusion compound and mifepristone, which is applied in the direction of drug combination, non-active ingredient medical preparations, pharmaceutical formulas, etc., which can solve the problems of slow absorption process, lower peak blood concentration of drugs, and poor curative effect and other problems, to achieve the effect of reducing toxic and side effects, increasing adaptability, and improving water solubility

Inactive Publication Date: 2014-01-15
SHANGHAI NEW HUALIAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because the absorption process of the drug is mainly carried out in the dissolved state, and the dissolution of mifepristone is slow, so the absorption process is also very slow, and it has been excreted through metabolism before it is fully absorbed, resulting in the peak blood flow of the drug. Decreased drug concentration, poor efficacy

Method used

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  • Cyclodextrin mifepristone clathrate compound, preparation method thereof, and pharmaceutical composition containing clathrate compound
  • Cyclodextrin mifepristone clathrate compound, preparation method thereof, and pharmaceutical composition containing clathrate compound
  • Cyclodextrin mifepristone clathrate compound, preparation method thereof, and pharmaceutical composition containing clathrate compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] formula:

[0030]

[0031] Operation process:

[0032] a. Weigh 0.5 g of mifepristone according to the formula, add it into 25 ml of ethanol, and ultrasonically dissolve it completely to form a mifepristone ethanol solution.

[0033] b. Weigh 1.6g of β-cyclodextrin according to the formula, add it into 25ml of pure water, stir at constant temperature to dissolve it, and form an aqueous solution of β-cyclodextrin.

[0034] c. Slowly add mifepristone ethanol solution to the β-cyclodextrin aqueous solution under the condition of 55° C. and stirring speed not less than 2500 rpm.

[0035] d. After fully mixing the β-cyclodextrin aqueous solution and the mifepristone ethanol solution, keep the original condition and continue to stir for 4 hours, and cool to room temperature.

[0036] e. Freeze-drying at -5°C to obtain a slightly yellow powder, which is the inclusion compound of mifepristone cyclodextrin.

[0037] After detection, at 25°C, the solubility of the clathrate...

Embodiment 2

[0039] formula:

[0040]

[0041] a. Take by weighing 0.6g of mifepristone according to the formula, add it in 40g of methanol, and ultrasonically dissolve it completely to form a methanol solution of mifepristone.

[0042] b. Weigh 2.0 g of β-cyclodextrin according to the formula, add it into 60 g of pure water, and conduct ultrasonic dissolution at 50° C. to form an aqueous solution of β-cyclodextrin.

[0043] c. Keeping the above conditions, slowly add mifepristone methanol solution to the β-cyclodextrin aqueous solution.

[0044] d. Continue ultrasonic dissolution for 4 hours after adding all of the solution.

[0045] e. Spray-dry to obtain a slightly yellow powder, which is the inclusion compound of mifepristone cyclodextrin.

[0046] (2), preparation of pharmaceutical composition containing mifepristone cyclodextrin inclusion compound

Embodiment 3

[0047] Embodiment 3, prepare the dispersible tablet of mifepristone cyclodextrin inclusion compound:

[0048] formula:

[0049]

[0050] Pulverize the mifepristone cyclodextrin inclusion compound, pass through a 100-mesh sieve, mix with other auxiliary materials according to the formula ratio, and directly compress into tablets to obtain dispersible tablets.

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Abstract

The invention discloses a cyclodextrin mifepristone clathrate compound. The clathrate compound takes beta-cyclodextrin as a skeleton to include mifepristone; the ratio of the beta-cyclodextrin to the mifepristone is (1-5):1. Meanwhile, the invention discloses a preparation method of the clathrate compound, and a pharmaceutical composition containing the clathrate compound. The pharmaceutical composition is a solid preparation and comprises the cyclodextrin mifepristone clathrate compound and at least two auxiliary materials. The cyclodextrin mifepristone clathrate compound focuses on solving the problem of water-solubility of the mifepristone; the solubility of the cyclodextrin mifepristone clathrate compound in water is about 30 times of that of pure mifepristone; an oral preparation is prepared from the cyclodextrin mifepristone clathrate compound instead of the traditional mifepristone crude drug. Therefore, the absorption rate of the drug is greatly improved; the curative effect of the drug is greatly improved; the effect of drug metabolism is reduced; the toxic and side effects are reduced; the adaptability of a sufferer on the drug is increased.

Description

technical field [0001] The invention relates to an inclusion compound with β-cyclodextrin as a skeleton and a preparation method thereof, and also relates to a composition containing the inclusion compound. Background technique [0002] Mifepristone (Mifepristone, 11b-[p-(Dimethylamino)phenyl]-17b-hydroxy-17-(1-propy-nyl)estra-4,9-dien-3-one) is a new type of antiprogestin , can bind to progesterone receptors and glucocorticoid receptors, and its affinity to endometrial progesterone receptors is 5 times stronger than progesterone. medicine. Mifepristone was introduced into my country in 1986, and domestic mifepristone was used clinically in 1992. [0003] Traditional oral preparations of mifepristone are directly made from mifepristone raw materials. According to the 2010 edition of "Chinese Pharmacopoeia", mifepristone is almost insoluble in water. Because the absorption process of the drug is mainly carried out in the dissolved state, and the dissolution of mifepriston...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/567A61P15/04
Inventor 杜霑林杨光李相穆丽娟赵琴
Owner SHANGHAI NEW HUALIAN PHARMA
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