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A powder of dronedarone or its salt and pharmaceutical composition prepared therefrom

A technology of dronedarone and its composition, which is applied in the field of antiarrhythmic drugs, can solve problems such as the dissolution rate of dronedarone hydrochloride, difficulty in controlling the properties of mixture excipients, drug release and stability effects, etc., to facilitate the preparation operation , good dissolution effect, the effect of improving dissolution rate and solubility

Inactive Publication Date: 2016-08-17
SHENZHEN SALUBRIS PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, the disclosed amphiphilic lipid surfactant, such as macrogol glyceride laurate, is a mixture of various substances. Due to factors such as the composition ratio of each substance in the mixture and its own unique physical and chemical properties, the auxiliary material of the mixture The properties in the preparation process are difficult to control, which will affect the release and stability of the drug; in addition, because some amphiphilic lipid surfactants can only be partially dissolved in water or oil, it also brings certain effects to the preparation. difficulty
[0008] Because of the low water solubility of dronedarone hydrochloride and the pH dependence in the dissolution medium, after oral administration, the process from the stomach to the intestinal tract must experience a gradual increase in pH, which can easily lead to the formation of dronedarone hydrochloride. Inability to dissolve or have a very low dissolution rate from solid dosage forms in the high pH environment of the intestinal tract, this process seriously affects the absorption of dronedarone in the body and leads to low bioavailability

Method used

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  • A powder of dronedarone or its salt and pharmaceutical composition prepared therefrom
  • A powder of dronedarone or its salt and pharmaceutical composition prepared therefrom
  • A powder of dronedarone or its salt and pharmaceutical composition prepared therefrom

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Based on the weight of dronedarone hydrochloride, add soybean lecithin, Tween-20, Tween-80, and macrogol glyceride laurate in the weight ratio shown in Table 1, and dissolve in the phosphate buffer of pH 4.5 to prepare into a solution containing dronedarone hydrochloride 2mg / mL, incubated at 37°C for 2 hours, then diluted the solution 10 times with neutral phosphate buffer, the final pH of the solution was 6.8, and incubated at 37°C for 2 hours, and passed through a 5 μm Filter the solution, use a UV spectrophotometer to measure the absorbance value A of the solution at a wavelength of 217nm; take another phosphate buffer solution with pH 4.5 to make a solution containing dronedarone hydrochloride 2mg / mL, and keep it warm at 37°C for 2 hours. Then the solution is diluted 10 times with the phosphate buffer solution of pH 4.5, the final pH of the solution is 4.5, and after being incubated at 37°C for 2 hours, it is filtered through a filter of 5 μm. Absorbance value B, ca...

Embodiment 2

[0045] Embodiment 2 dronedarone hydrochloride powder

[0046] Disperse 42.6 g of dronedarone hydrochloride and 4 g of soybean lecithin in 500 mL of 70% ethanol, and spray dry it with a spray dryer to obtain a powder. (Wherein, the weight of soybean lecithin accounts for about 8.6% of the powder weight)

[0047] Spray drying conditions: spray dryer; nitrogen flow pressure: 600L / h; inlet air temperature: 90°C; outlet air temperature: 43°C; feed rate: 5mL / min; needle pass frequency: 15 seconds / time.

Embodiment 3

[0048] Example 3 Dronedarone Hydrochloride Powder

[0049] Disperse 42.6 g of dronedarone hydrochloride and Tween-804 g in 500 mL of absolute ethanol, and spray dry it with a spray dryer to obtain a powder. (Wherein, the weight of Tween-80 accounts for about 8.6% of powder weight)

[0050] Spray drying conditions: spray dryer; nitrogen flow pressure: 1200L / h; air inlet temperature: 80°C; air outlet temperature: 32°C; feed rate: 15mL / min; needle pass frequency: 30 seconds / time.

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PUM

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Abstract

The invention provides dronedarone or powder of a pharmaceutically acceptable salt thereof and a pharmaceutical composition prepared therefrom. The pharmaceutical composition is prepared by the steps of: dispersing dronedarone or a salt thereof, and more than one compound selected from phospholipid, or phospholipid and a water-soluble auxiliary material and a surfactant into an organic solvent; and removing the solvent by using a spray drying method or a drying method under reduced pressure. The obtained dronedarone or the powder of the pharmaceutically acceptable salt thereof and the pharmaceutical composition prepared therefrom have excellent dissolvability in a medium with the pH value of about 7, thus the bioavailability of a medicine is effectively guaranteed.

Description

technical field [0001] The invention relates to a powder of antiarrhythmic drug dronedarone or a salt thereof and a pharmaceutical composition prepared therefrom. Background technique [0002] Dronedarone, the chemical name is N-[2-n-butyl-3-[4-[3-(dibutylamino)propoxy]benzoyl]-5-benzofuryl] Methanesulfonamide, formula C 31 h 44 N 2 o 5 S, molecular weight 556.76, its structural formula is shown in the following formula: [0003] [0004] Dronedarone hydrochloride is a newly developed drug for the treatment of arrhythmia by Sanofi-Synthelabo. This product is a benzofuran derivative, similar in structure and characteristics to amiodarone, but dronedarone does not contain iodine and has lower lipophilicity. Therefore, it not only maintains the similar efficacy of amiodarone, but also has an elimination half-life of 13 -19 hours, more convenient to use as medicine. [0005] The water solubility of dronedarone hydrochloride is low, and its dissolution effect in the sol...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/343A61K47/24A61K47/32A61K47/34A61K47/40A61K47/44A61P9/06
Inventor 张宣杨睿李洪张小杰陈金脱
Owner SHENZHEN SALUBRIS PHARMA CO LTD
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