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Sparingly soluble active component particle, particle preparation and preparation method thereof

An active ingredient and insoluble technology, which is applied in the field of insoluble active ingredient particles, particle preparations and their preparation, can solve the problems of easy aggregation of particles, poor dispersion performance and wettability, and poor dissolution performance of insoluble active ingredients.

Active Publication Date: 2016-06-08
SINOTHERAPEUTICS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The technical problem solved by the present invention is to overcome the defects of poor dissolution performance of insoluble active ingredients, easy agglomeration of particles, poor dispersion performance and wet performance, and poor stability in the prior art, and provide a kind of insoluble active ingredient particles, Microparticle preparation and its preparation method

Method used

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  • Sparingly soluble active component particle, particle preparation and preparation method thereof
  • Sparingly soluble active component particle, particle preparation and preparation method thereof
  • Sparingly soluble active component particle, particle preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

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 EPO0.15g, after it dissolves, filter the solution; add a concentration of 9.8% sodium hydroxide solution 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 25°C constant temperature water bath, 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 PVPK301. 5g, filter this solution after it dissolves; Add concentration to this solution with the speed of 0.75ml / min and be 9.8% sodium hydroxide solution, control solution pH to 7.2 and continue to stir for 30min, suction filtration obtains eutectic, water Wash 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 PVPK30 to 9g in the sample recorded as contrast 1B, other conditions are all unchanged; Add polyethylene gly...

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 250 m / min, then add 0.5g of acrylic resin Eudragit L1000 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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Abstract

The invention discloses a sparingly soluble active component particle, a particle preparation and a preparation method thereof. The preparation method of the sparingly soluble active component particle comprises the following steps: dissolving sparingly soluble active component and ionic polymer into an alkaline solution or an acidic solution, and then mixing the alkaline solution and acidic solution to change the pH value of solutions so as to precipitate the sparingly soluble active component and ionic polymer from the mixed solution to form particles; and the performance of the sparingly soluble active component particle is improved. According to the preparation method, sparingly soluble active component and ionic polymer are co-precipitated, at the same time, a preparation technology is adopted, and two technologies are tightly combined to prepare the sparingly soluble active component particle preparation. The prepared preparation has the advantages of excellent dissolving-out characteristic, high bioavailability, small individual difference, good stability, and good content uniformity.

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...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/30A61K8/02A23P10/20
CPCA61K9/14A61K9/16A61K31/19A61K31/454
Inventor 任福正郑斯骥景秋芳
Owner SINOTHERAPEUTICS
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