Solid dispersoid of poorly soluble drug CVD (carvedilol), preparation method and application

A technology for solid dispersion and insoluble drugs, applied in the field of medicine, can solve the problems of long grinding cycle, limited solubility and bioavailability of carvedilol, poor solubility, etc., and achieves improved solubility and dissolution rate, good long-term storage stability properties, improved bioavailability

Pending Publication Date: 2019-09-27
HEFEI COSOURCE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This preparation makes the insoluble drug carvedilol into nanoparticles, which can greatly improve the dissolution of carvedilol, but the grinding cycle in the preparation process is long, and the process is time-consuming and energy-consuming
[0007] Chinese invention patent CN106309434A discloses a method for preparing carvedilol solid dispersion using supercritical antisolvent technology, which also helps to increase the solubility of insoluble drugs and improve the bioavailability of insoluble drugs; It has good solubility, and its solubility is poor in alkaline environment. Carvedilol has a pH of 5.0 to 8.0 in the intestinal tract. The poor solubility of the drug makes it easy to precipitate and precipitate in the high pH gastrointestinal tract environment, which limits the Enhanced Solubility and Bioavailability of Carvedilol

Method used

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  • Solid dispersoid of poorly soluble drug CVD (carvedilol), preparation method and application
  • Solid dispersoid of poorly soluble drug CVD (carvedilol), preparation method and application
  • Solid dispersoid of poorly soluble drug CVD (carvedilol), preparation method and application

Examples

Experimental program
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Effect test

Embodiment 1

[0049] 1) Preparation of carvedilol solid dispersion intermediate product: add 10g of carvedilol and 2.78g of phosphoric acid to 50ml of 60% ethanol solution at 80°C, stir to obtain a clear liquid, then cool to room temperature, and use IKA T18 to homogenize Disperse with an instrument to control the particle size from 10 μm to 50 μm; vacuum dry to remove the solvent to obtain the co-precipitate, and sieve with 40 mesh to obtain the intermediate product of the dispersion (carvedilol + protonating reagent).

[0050] 2) Preparation of Carvedilol Solid Dispersion 1: Dissolve 20 g of Povidone K30 in 100 ml of 60% ethanol solution, stir to make the dissolution clear;

[0051] Add 10g of carvedilol and 2.78g of phosphoric acid to 50ml of 60% ethanol solution at 80°C, and stir to obtain a clear liquid; then add the above-mentioned povidone K30 solution, stir, then cool to room temperature, and use an IKA T18 homogenizer to carry out Disperse and control the particle size to 10 μm to ...

Embodiment 2

[0059] Dissolve 100g of povidone K30 in 500ml of 50% ethanol solution, stir to make the solution clear; take 2g of crospovidone and disperse it in 20ml of 50% ethanol solution, stir and suspend evenly;

[0060] Add 10g of carvedilol and 2.78g of phosphoric acid into 50ml of 50% ethanol solution at 70°C, stir to obtain a clear liquid, then add 2g of polyoxyethylene hydrogenated castor oil RH40, then add the above-mentioned povidone K30 solution, keep stirring Clarify, then cool to room temperature; then add crospovidone suspension to obtain a suspension. IKA T18 homogenizer was used for dispersion, and the particle size was controlled to be 10 μm to 50 μm; the solvent was removed by fluidized bed spray drying to obtain co-precipitates, and carvedilol solid dispersion was obtained by sieving with 80 mesh.

Embodiment 3

[0062] Dissolve 2.5g of povidone K30 in 15ml of 60% methanol solution, stir to make the solution clear; take 20g of crospovidone and disperse it in 180ml of 60% methanol solution, stir and suspend evenly;

[0063] Add 10g of carvedilol and 2.78g of phosphoric acid to 50ml of 60% methanol solution at 70°C, stir to obtain a clear solution, then add 40g of polyoxyethylene hydrogenated castor oil RH40, then add the above-mentioned povidone K30 solution, and keep stirring Clarify, then cool to room temperature; then add crospovidone suspension to obtain a suspension. The dispersion is carried out by mechanical stirring and shearing, and the particle size is controlled to be 10 μm to 50 μm; the solvent is removed by rotary evaporation to obtain a co-precipitate, and the carvedilol solid dispersion is obtained after jet milling.

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Abstract

The invention discloses a solid dispersoid of poorly soluble drug CVD (carvedilol), a preparation method and an application and relates to the technical field of medicines. With the adoption of a one-step solvent coprecipitation method, CVD and a protonation reagent are dissolved in a solvent, a dispersion material is added, a suspension is obtained for coprecipitation, and finally, the solid dispersoid is prepared after the solvent is removed. The one-step solvent coprecipitation method is adopted for in-situ production of the solid dispersoid. Detection proves that CVD is transformed into an amorphous form from an original crystal form and is dispersed in the solid dispersoid, besides, CVD is salified due to addition of the protonation reagent, thus, the solubility and the dissolution rate of free alkali drugs are improved from two aspects, and the bioavailability of the BCSII type poorly soluble drug CVD is effectively improved. a drug preparation with retention floating in the stomach and time-lag trip or release in different pH parts in a body is prepared from the CVD solid dispersoid according to a polymer coating material in cooperation with the dissolubility characteristic of pH dependency.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a solid dispersion of an insoluble drug carvedilol, a preparation method and an application thereof. Background technique [0002] After insoluble drugs are prepared into oral solid preparations by conventional preparation technology, there are problems such as low dissolution rate and poor absorption after oral administration, which affect the drug efficacy and therapeutic effect. Methods to improve the solubility and bioavailability of poorly soluble oral solid preparations include reducing the particle size of raw materials (such as micronization), adding solubilizers (such as surfactants, etc.), adding pH regulators (such as salt formation, etc.), screening or Control the crystal form and crystal form amorphization of raw materials (such as cyclodextrin inclusion, solid dispersion), etc. [0003] Solid Dispersion Technology (Solid Dispersion) is a technology that disperses ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/32A61K31/403A61P9/12A61P9/10A61P9/04A61P9/06A61P27/06
CPCA61K9/146A61K31/403A61P9/04A61P9/06A61P9/10A61P9/12A61P27/06
Inventor 孙宏张吴伟陈登俊
Owner HEFEI COSOURCE PHARMA CO LTD
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