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Chemical preparation method for micronizing adapalene
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A micropowder and particle technology, which is applied in the separation/purification of carboxylic acid compounds, organic chemistry and other directions, can solve the problems of low yield, high cost and large loss in the pulverization process, and achieve high yield, easy operation and low cost. Effect
Pending Publication Date: 2021-03-12
WUHAN NUOAN PHARMACY
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Problems solved by technology
[0006] There are great problems in the industrial production of medicines by means of mechanical pulverization. One is to rely on expensive pulverization equipment, such as jet pulverizers, and the cost is relatively high; The batch size is generally small, the loss in the crushing process is large, and the yield is low; and the crushing process produces dust and noise, which is harmful to human health and pollutes the environment
[0007] At present, a kind of preparation method of adapalene micronization that is economical, convenient, environmentally friendly and easy to industrialize has not been found yet.
Method used
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Embodiment 1
[0037] Take 10 g of adapalene, add it into a reaction flask, add 200 ml of tetrahydrofuran, heat to 65-70° C., adapalene is completely dissolved, and a tetrahydrofuran solution containing adapalene is obtained. Add 600ml of toluene to another reaction flask, stir mechanically, control the stirring speed at 400 rpm, add the tetrahydrofuran solution containing adapalene dropwise to the reaction flask, dropwise for 1 hour, drop the temperature to 5°C, and stir After 4 hours, it was filtered, and the product was vacuum-dried to obtain 9.12 g of adapalene microparticles, with a yield of 91.2%. The particle size was measured, D90 was 12.6 μm, and D99 was 20.7 μm. see results figure 1 .
Embodiment 2
[0039] Take 10 g of adapalene, add it into a reaction flask, add 200 ml of tetrahydrofuran, heat to 65-70° C., adapalene is completely dissolved, and a tetrahydrofuran solution containing adapalene is obtained. Add 400ml of methanol into another reaction flask, stir mechanically, control the stirring speed at 350 rpm, add the tetrahydrofuran solution containing adapalene dropwise to the reaction flask, dropwise for 1 hour, after the drop is completed, cool down to 10°C and stir After 4 hours, it was filtered, and the product was vacuum-dried to obtain 9.35 g of adapalene microparticles, with a yield of 93.5%. The particle size was measured, D90 was 15.1 μm, and D99 was 25.6 μm.
Embodiment 3
[0041] Take 10 g of adapalene, add it into a reaction flask, add 200 ml of tetrahydrofuran, heat to 65-70° C., adapalene is completely dissolved, and a tetrahydrofuran solution containing adapalene is obtained. Add 500ml of ethanol to another reaction flask, stir mechanically, control the stirring speed at 350 rpm, add the tetrahydrofuran solution containing adapalene dropwise to the reaction flask, dropwise for 1 hour, after the drop is completed, cool down to 10°C and stir After 4 hours, it was filtered, and the product was vacuum-dried to obtain 9.28 g of adapalene microparticles, with a yield of 92.8%. The particle size was measured, D90 was 13.8 μm, and D99 was 22.5 μm.
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Abstract
The invention relates to a chemical preparation method of adapalenemicronization, in particular to a chemical preparation method of adapalenemicronization. The method comprises the following steps:dissolving adapalene in tetrahydrofuran to prepare a solution, and dropwisely adding the prepared tetrahydrofuran solution containing adapalene into an organic solvent while stirring; after dropwise adding is finished, performing cooling, stirring, crystallizing, filtering and drying in vacuum to obtain adapalene particles of which the D90 is less than 20 microns and the D99 is less than 50 microns. Compared with a mechanical crushing method, the method is high in product yield, low in production cost, simple and convenient to operate, environment-friendly and easy for industrial production.
Description
technical field [0001] The invention belongs to the field of pharmaceutical synthesis, and in particular relates to a chemical preparation method of adapalene micronization. In particular, methods for preparing microparticles with D90 less than 20 μm and D99 less than 50 μm. Background technique [0002] Adapalene, its chemical name is 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid, the structural formula is as follows, adapalene belongs to the third generationRetinoic acid drugs are clinically applicable to the skin treatment of acne vulgaris mainly manifested by acne, papules and pustules, and can also be used to treat acne on the face, chest and back. [0003] . [0004] Adapalene is difficult to dissolve in water and is a substance with low solubility and high absorption. In order to make adapalene absorbed quickly by the human body and exert its drug effect, it is necessary to increase its release rate in the preparation. The particle size is the key factor...
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