Pharmaceutical compositions of ranolazine and dronedarone

一种决奈达隆、决奈达隆碱的技术，应用在雷诺嗪和决奈达隆的药物组合物领域，能够解决心悸或胸痛等问题

Inactive Publication Date: 2016-06-15
GILEAD SCI INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although atrial fibrillation is often asymptomatic, it can cause palpitations or chest pain

Method used

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  • Pharmaceutical compositions of ranolazine and dronedarone
  • Pharmaceutical compositions of ranolazine and dronedarone
  • Pharmaceutical compositions of ranolazine and dronedarone

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0132] Preparation operation

[0133] For the preparation of spray-dried solid dispersions (formulations) of dronedarone in the form of phosphate salt formulations, the equipment train consisted of a glass reactor, a spray dryer (MobileMinor ,GEANiro, Denmark) and a tray drying vacuum oven.

[0134] Preparation of Feed Solutions

[0135] A batch of dronedarone feed solution at 15.0% (w / w) solids content was prepared on a scale of 62.8 kg solution, corresponding to 9.42 kg spray-dried powder. Drug solution and polymer solution were prepared separately in two glass reactors. To prepare the drug solution, the dronedarone drug substance is dispersed in a dilute phosphoric acid solution and gradually dissolves due to its reaction with phosphoric acid. Initially, 95% of theoretical phosphoric acid was added to prepare the feed solution. After the drug solution was dissolved, the pH of the drug solution was adjusted to 4.0 ± 0.4 with the remaining phosphoric acid solution. Not...

Embodiment 2

[0147] method

[0148] Feed solutions for laboratory experiments were prepared by: 1) preparing an aqueous solution of counterions (e.g., phosphate, citrate, acetate); 2) adding dronedar to the acid solution from the previous step 3) Separately prepare an aqueous solution of the polymer (eg, HPMCE3LV, HPMCE5LV, PVP, PVPVA, or HPMCAS); and (4) Combine the solutions from steps (2) and (3). The total solids content of the feed solution ranges from about 10% to 20% w / w. Optionally, the feed solution can be prepared by stepwise addition of the ingredients (phosphoric acid, dronedarone and polymer) to the chosen solvent.

[0149] Spray drying feed solution:

[0150] The dronedarone feed solution was spray dried using a Buchi Mini Spray Dryer B-290 in a sealed ring configuration. Compressed nitrogen was used as both drying and nebulizing gas. Dry gas fans run at 100% power. The temperature of the condenser was set at about 4°C to remove water from the recirculated drying gas. T...

Embodiment 2A

[0164] method

[0165] Additional laboratory experiments were performed to develop various feed solution compositions. Feed solutions for laboratory experiments were prepared by (1) preparing solutions of phosphoric acid in water and / or solvents; (2) dry blending dronedarone and polymer (HPMCE3); (3) ) adding the dry blend to the phosphoric acid solution from step (1); the total solids content of the feed solution ranges from about 15% to 30% w / w. Optionally, the feed solution can be prepared by stepwise addition of ingredients (phosphoric acid, dronedarone and polymer) to the chosen solvent.

[0166] Spray drying feed solution:

[0167] Feed solution of dronedarone with Mini Spray Dryer B-290 (Buchi Corporation) spray dried in a sealed or open ring configuration. Compressed nitrogen was used as both drying and nebulizing gas. Dry gas fans run at 100% power. The temperature of the condenser was set at about 4°C to 10°C to remove water from the recirculated drying gas. ...

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Abstract

The present disclosure relates to a solid composition comprising ranolazine and a spray-dried phosphoric acid salt of dronedarone in a bilayer tablet.

Description

[0001] Cross References to Related Applications [0002] This application claims priority under 35 U.S.C. §119(e) to U.S. Provisional Application 61 / 861,862, filed August 2, 2013, which is hereby incorporated by reference in its entirety. technical field [0003] The present invention relates to solid pharmaceutical compositions comprising ranolazine and dronedarone and methods for the treatment and / or prevention of atrial fibrillation and / or atrial flutter. Background technique [0004] Atrial fibrillation (AF) is the most common cardiac arrhythmia, and its incidence increases with age. It is estimated that 8% of all persons over the age of 80 experience this type of abnormal heart rhythm and that AF accounts for one-third of hospitalizations for heart rhythm disorders. It is believed that more than 2.2 million people are living with AF in the United States alone. Fuster et al., Circulation2006114(7):e257–354. Although atrial fibrillation is often asymptomatic, it can ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/20A61K9/24A61K31/343A61K31/495
CPCA61K9/146A61K9/2027A61K9/2054A61K9/209A61K9/2095A61K31/343A61K31/495A61P43/00A61P9/04A61P9/06A61P9/10A61K2300/00A61K47/38A61J3/10
Inventor M.格伯N.黄J.M.科齐亚拉F.张
Owner GILEAD SCI INC
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