A kind of insoluble active ingredient particle, particle preparation and preparation method thereof

Abstract

An insoluble active ingredient particulate, a particulate preparation and a preparation method therefor. The preparation method for the particulate comprises the following steps: dissolving an insoluble active ingredient and an ionic polymer into an alkaline solution or an acidic solution, then mixing the alkaline solution and the acidic solution, and co-precipitating the insoluble active ingredient and the ionic polymer originally dissolved in the solution from the mixed solution to form the particulate by changing the pH value of the solution.

Description

technical field

[0001] The invention relates to a microparticle of an insoluble active ingredient, a microparticle preparation and a preparation method thereof. Background technique

[0002] Active ingredient, also known as active ingredient, refers to a monomer compound that has medical utility or physiological activity, can be expressed by molecular formula and structural formula, and has physical and chemical data. Drugs are also active ingredients, which refer to substances that can temporarily or permanently change or ascertain the physiological functions and pathological states of the body, and have the functions of medical treatment, diagnosis, disease prevention and health care. Drugs include natural drugs, chemically synthesized drugs and biotechnology drugs. The active ingredients need to be prepared into suitable preparations according to different requirements, different ways of use and different places of use before they can be applied.

[0003] In the field of...

Examples

Embodiment 1

[0147] Embodiment 1 domperidone microparticles

[0148] Disperse 3g of domperidone in 300ml of 30% ethanol, put it in a constant temperature water bath at 25°C, use a stirrer to disperse it at a linear speed of 190 m / min, add a dilute hydrochloric acid solution with a concentration of 8.9% until the domperidone is dissolved, and add acrylic resin Eudragit EPO 0.15g, filter the solution after it dissolves; add sodium hydroxide solution with a concentration of 9.8% to the solution at a rate of 0.75ml / min, control the pH of the solution to 7.2, continue stirring for 30min, and filter with suction to obtain The eutectoid was washed 3 times with water, dried at 40°C for 48 hours, then gently ground, and passed through an 80-mesh sieve to obtain a sample (referred to as 1A), with a content of 99.79%.

[0149] Using the above method, only change the amount of acrylic resin Eudragit EPO to 3g, the product obtained is marked as 1B, and the sample content is 102.6%.

Embodiment 1

[0150] Comparative example 1 domperidone microparticles

[0151] Disperse 3g of domperidone in 300ml of 30% ethanol, put it in a constant temperature water bath at 25°C, use a stirrer to disperse it at a linear speed of 190 m / min, add a dilute hydrochloric acid solution with a concentration of 8.9% until the domperidone is dissolved, and add PVP K301 .5g, filter this solution after it dissolves; In this solution, add concentration with the speed of 0.75ml / min and be 9.8% sodium hydroxide solution, control solution pH to 7.2 and continue to stir 30min, suction filtration obtains eutectic, Wash with water for 3 times, dry at 40°C for 48 hours, grind lightly, and pass through an 80-mesh sieve to obtain a sample (denoted as Comparative 1A), with a content of 99.67%.

[0152] Adopt the above-mentioned method to prepare 3 kinds of domperidone microparticles in addition as contrast, add PVP K30 to 9g in the sample that is recorded as contrast 1B, other conditions are all unchanged; A...

Embodiment 2

[0153] Embodiment 2 Estradiol microparticles

[0154] Disperse 1g of estradiol in 120ml of 30% ethanol, use a stirrer to disperse it at a linear speed of 250m / min, then add 0.5g of acrylic resin Eudragit L100 to it, and disperse it at a speed of 15ml / min Add 9.8% sodium hydroxide solution at a high speed, and continue to stir until the two are completely dissolved; add 8.9% hydrochloric acid solution to the solution at a speed of 15ml / min until the pH of the mixed solution is 5; After washing with water for 5 times, dry under reduced pressure at 55°C for 5 hours; gently grind in a mortar, and pass through an 80-mesh sieve to obtain a sample (denoted as 2A), with a content of 101.5%.

[0155] Using the above method, only change the amount of acrylic resin Eudragit L100 to 0.2g to obtain a sample, denoted as 2B, and the content of the sample is 99.4%.

technical field

[0001] The invention relates to a microparticle of an insoluble active ingredient, a microparticle preparation and a preparation method thereof. Background technique

[0002] Active ingredient, also known as active ingredient, refers to a monomer compound that has medical utility or physiological activity, can be expressed by molecular formula and structural formula, and has physical and chemical data. Drugs are also active ingredients, which refer to substances that can temporarily or permanently change or ascertain the physiological functions and pathological states of the body, and have the functions of medical treatment, diagnosis, disease prevention and health care. Drugs include natural drugs, chemically synthesized drugs and biotechnology drugs. The active ingredients need to be prepared into suitable preparations according to different requirements, different ways of use and different places of use before they can be applied.

[0003] In the field of...

Examples

Embodiment 1

[0147] Embodiment 1 domperidone microparticles

[0148] Disperse 3g of domperidone in 300ml of 30% ethanol, put it in a constant temperature water bath at 25°C, use a stirrer to disperse it at a linear speed of 190 m / min, add a dilute hydrochloric acid solution with a concentration of 8.9% until the domperidone is dissolved, and add acrylic resin Eudragit EPO 0.15g, filter the solution after it dissolves; add sodium hydroxide solution with a concentration of 9.8% to the solution at a rate of 0.75ml / min, control the pH of the solution to 7.2, continue stirring for 30min, and filter with suction to obtain The eutectoid was washed 3 times with water, dried at 40°C for 48 hours, then gently ground, and passed through an 80-mesh sieve to obtain a sample (referred to as 1A), with a content of 99.79%.

[0149] Using the above method, only change the amount of acrylic resin Eudragit EPO to 3g, the product obtained is marked as 1B, and the sample content is 102.6%.

Embodiment 1

[0150] Comparative example 1 domperidone microparticles

[0151] Disperse 3g of domperidone in 300ml of 30% ethanol, put it in a constant temperature water bath at 25°C, use a stirrer to disperse it at a linear speed of 190 m / min, add a dilute hydrochloric acid solution with a concentration of 8.9% until the domperidone is dissolved, and add PVP K301 .5g, filter this solution after it dissolves; In this solution, add concentration with the speed of 0.75ml / min and be 9.8% sodium hydroxide solution, control solution pH to 7.2 and continue to stir 30min, suction filtration obtains eutectic, Wash with water for 3 times, dry at 40°C for 48 hours, grind lightly, and pass through an 80-mesh sieve to obtain a sample (denoted as Comparative 1A), with a content of 99.67%.

[0152] Adopt the above-mentioned method to prepare 3 kinds of domperidone microparticles in addition as contrast, add PVP K30 to 9g in the sample that is recorded as contrast 1B, other conditions are all unchanged; A...

Embodiment 2

[0153] Embodiment 2 Estradiol microparticles

[0154] Disperse 1g of estradiol in 120ml of 30% ethanol, use a stirrer to disperse it at a linear speed of 250m / min, then add 0.5g of acrylic resin Eudragit L100 to it, and disperse it at a speed of 15ml / min Add 9.8% sodium hydroxide solution at a high speed, and continue to stir until the two are completely dissolved; add 8.9% hydrochloric acid solution to the solution at a speed of 15ml / min until the pH of the mixed solution is 5; After washing with water for 5 times, dry under reduced pressure at 55°C for 5 hours; gently grind in a mortar, and pass through an 80-mesh sieve to obtain a sample (denoted as 2A), with a content of 101.5%.

[0155] Using the above method, only change the amount of acrylic resin Eudragit L100 to 0.2g to obtain a sample, denoted as 2B, and the content of the sample is 99.4%.

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