Method of preparing ultra-fine danazol powder

A technology of danazol and azole powder, which is applied in the direction of non-active ingredient medical preparations, medical preparations containing active ingredients, powder delivery, etc., which can solve the problem of affecting the quality of danazol powder and the narrow particle size distribution of danazol , uneven mixing and other problems, to achieve the effect of easy packaging, shortened reaction time, and uniform particles

Inactive Publication Date: 2008-10-29
BEIJING UNIV OF CHEM TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] However, the method introduced in this patent cannot prepare danazol with controllable particle size, controllable shape and narrow particle size distribution, and the solvent precipitation method carried out in the traditional stirred tank still has problems of uneven mixing and partial supersaturation problems, thus affecting the quality of danazol powder

Method used

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  • Method of preparing ultra-fine danazol powder
  • Method of preparing ultra-fine danazol powder
  • Method of preparing ultra-fine danazol powder

Examples

Experimental program
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Effect test

Embodiment 1

[0041] Take by weighing 20g of danazol crude drug, dissolve and prepare 1000ml of danazol solution with ethanol, place in storage tank, get deionized water 40L (liter) and place another storage tank as anti-solvent, two storage tanks pass through respectively The pipeline is connected with the solution inlet 4 and the anti-solvent inlet 5 of the high-gravity rotating packed bed reactor. At room temperature, the two liquids are pumped in respectively from the solution inlet 4 and the anti-solvent inlet 5, and sprayed into the filler 3 through the liquid distributor. The temperature in the rotating bed is controlled at 4°C. Precipitation crystallizes to generate white danazol precipitate, which flows out from the outlet 1 of the rotary bed, is filtered, washed, and dried to obtain danazol granules. During operation, the flow ratio of danazol solution / anti-solvent was 1:40, and the rotational speed of the rotating bed was 3000 rpm. from image 3 It can be seen from the scanning...

Embodiment 2

[0043]Weigh 80 g of danazol raw material, dissolve and prepare 1000 ml of danazol solution with acetone, take 20 L of deionized water as anti-solvent, control the temperature in the rotating bed at 4 ° C, and the ratio of danazol solution to anti-solvent is 1: 20, Prepared ultrafine amorphous danazol particles from Figure 4 It can be seen from the scanning electron microscope photos that the average particle size is about 1 μm.

Embodiment 3

[0045] Weigh 400g of danazol bulk drug, prepare 2 liters of danazol solution with dichloromethane, take 10L of cyclohexane as anti-solvent, control the temperature in the rotating bed at 30°C, and the flow ratio of danazol solution / anti-solvent is 1:5, the rotating bed rotating speed is 1000rpm, all the other are with embodiment 1, make superfine amorphous danazol particle, from Figure 5 It can be seen from the scanning electron microscope photos shown that the average particle size is about 20 μm in length and about 4 μm in width, and the shape is uniform needle-shaped particles.

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Abstract

A preparation method of ultra-fine danazol powder belongs to the method of drug micronization. The method is that danazol solution and desolvation are first put into a supergravity rotating bed through a solution entrance 4 and a desolvation entrance 5 respectively at the same time, and the recrystallized danazol paste by the desolvation flows out from a discharge hole 1; the danazol paste is collected, filtered and dried to obtain the ultra-fine danazol powder. The method can obtain the ultra-fine danazol powder of controlled average grain size, controlled shape and narrow grain size distribution.

Description

technical field [0001] The invention belongs to a medicine manufacturing method, in particular to a medicine micronization method. Background technique [0002] Danazol, namely 17α-pregna-2,4-dien-20-yno[2,3-d]isoxazol-17β-ol. It is a gonadotropin inhibitor, used for the treatment of endometriosis, and can also be used for the treatment of fibrocystic breast disease, spontaneous thrombocytopenic purpura, hereditary angioedema, systemic erythropoiesis, men and women Sexual breasts, precocious puberty. Its structure is as follows: [0003] [0004] Danazol is a poorly water-soluble drug whose bioavailability is limited by its dissolution rate. The finer the powder, the higher its bioavailability. [0005] In U.S. Patent 20020081334, 20040067251, a preparation method of micron or nanometer danazol is described: the danazol solution is sprayed into the aqueous solution with surfactant, and then the organic solvent is volatilized to form danazol Dispersion of fine azole p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/58A61K47/34A61K47/38A61K47/10A61K47/26A61P5/24
Inventor 陈建峰赵宏王洁欣沈志刚甄崇礼
Owner BEIJING UNIV OF CHEM TECH
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