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Dronedarone or powder of salt thereof and pharmaceutical composition prepared therefrom

A technology of dronedarone and dronedarone hydrochloride, which is applied in the field of antiarrhythmic drugs, can solve problems such as the dissolution rate of dronedarone hydrochloride, the influence of drug release and stability, and the difficulty in controlling the properties of mixture excipients. Facilitate the preparation operation, improve the dissolution rate and solubility, and the effect of good dissolution effect

Inactive Publication Date: 2013-06-26
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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  • Dronedarone or powder of salt thereof and pharmaceutical composition prepared therefrom
  • Dronedarone or powder of salt thereof and pharmaceutical composition prepared therefrom
  • Dronedarone or powder of salt thereof and pharmaceutical composition prepared therefrom

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Add soybean lecithin, Tween-20, Tween-80, lauric acid macrogol glyceride in the weight ratio as shown in Table 1 based on the weight of dronedarone hydrochloride, dissolve in the phosphate buffer solution of pH 4.5 to prepare. A solution containing 2 mg / mL of dronedarone hydrochloride was prepared, incubated at 37 °C for 2 hours, then the solution was diluted 10 times with neutral phosphate buffer, and the final pH of the solution was 6.8. The solution was filtered with a filter, and the solution was measured with a UV spectrophotometer at a wavelength of 217 nm. The absorbance value A of the solution was measured at a wavelength of 217 nm; another pH 4.5 phosphate buffer was taken to make a solution containing 2 mg / mL of dronedarone hydrochloride, and the solution was incubated at 37 °C for 2 hours. Then the solution was diluted 10 times with phosphate buffer of pH 4.5, the final pH of the solution was 4.5, after incubation at 37 °C for 2 hours, filtered through a 5 μm ...

Embodiment 2

[0045] Example 2 Dronedarone hydrochloride powder

[0046] 42.6 g of dronedarone hydrochloride and 4 g of soybean lecithin were dispersed in 500 mL of 70% ethanol, and spray-dried with a spray dryer to obtain 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; air inlet temperature: 90°C; air outlet temperature: 43°C; feed volume: 5mL / min; needle penetration frequency: 15 seconds / time.

Embodiment 3

[0048] Example 3 Dronedarone hydrochloride powder

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

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

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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 an antiarrhythmic drug dronedarone or a salt thereof and a pharmaceutical composition prepared therefrom. Background technique [0002] Dronedarone, chemical name N-[2-n-butyl-3-[4-[3-(dibutylamino)propoxy]benzoyl]-5-benzofuranyl] Methanesulfonamide, molecular formula C 31 H 44 N 2 O 5 S, molecular weight 556.76, its structural formula is shown as follows: [0003] [0004] Dronedarone hydrochloride is a newly developed drug for the treatment of arrhythmia by Sanofi-Synthelabo. This product is a benzofuran derivative with similar structure and characteristics to amiodarone, but dronedarone does not contain iodine and has low 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 solvent is...

Claims

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Application Information

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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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