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Sustained release pharmaceutical formulations comprising ranolazine

A slow-release drug, ranolazine technology, used in drug combination, pill delivery, metabolic diseases, etc., can solve the problem of not being able to provide ranolazine plasma

Inactive Publication Date: 2008-01-02
GILEAD PALO ALTO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In clinical trials, such formulations were not successful in providing satisfactory plasma levels of ranolazine over an extended period of time

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Preparation of 40% Ranolazine SR Formulation

[0018] step

[0019] Ranolazine (400 g), Avicel(R) (212.3 g) were mixed in a granulator (KG-5 high shear mixer) at an impeller speed of 250 rpm and a chopper speed of 2500 rpm , Eudragit(R) L100-55 (350 g) and hydroxypropyl methylcellulose (HPMC) (10.7 g) were mixed together for five minutes.

[0020] Sodium hydroxide (6.67g) was dissolved in 230ml of water and this solution was added to the powder mixture at a rate of 50ml / min at a propulsion speed of 500rpm and a cutting speed of 1000rpm.

[0021] Further water (30ml) was added at a rate of 100ml / min at a propulsion speed of 500rpm and a pelletizing speed of 1000rpm.

[0022] To facilitate agglomeration, the powder was aggregated for 15 minutes at a propulsion speed of 250 rpm and a cutting speed of 5000 rpm.

[0023] The granules prepared in the previous step were dried for 25 minutes in a fluidized bed dryer with an inlet air temperature of 60°C and a rated airfl...

Embodiment 2

[0036] Preparation of ranolazine SR formulations with pH-independent polymers

[0037] step

[0038] In a granulator (KG-5 high shear mixer), ranolazine (750 g) was mixed with hydroxypropyl methylcellulose (HPMC E10M Premium CR, 230 g ) were mixed together for five minutes.

[0039] 260 ml of water were added to the powder mixture at a rate of 100 ml / min at a propulsion speed of 250 rpm and a pelletizing speed of 2500 rpm.

[0040] To facilitate aggregation, the powder was aggregated for 5 minutes at a propulsion speed of 250 rpm and a cutting speed of 5000 rpm.

[0041] The granules prepared in step 3 were dried for 25 minutes in a fluidized bed dryer with an inlet air temperature of 60 °C and a nominal airflow setting of 8.

[0042] The dried granules are sieved using a suitable mesh screen (0.083 inch mesh).

[0043] The obtained granules were taken out, weighed, and mixed with 2% magnesium stearate (20 g, pre-sieved with a 40-mesh sieve) for 3 minutes using a mixer...

Embodiment 3

[0053] Preparation of ranolazine SR formulations with pH-independent polymers

[0054] step

[0055] Ranolazine (750 g), Avicel(R) (75 g) were mixed with HPMC E10M Premium CR (155 g) in a granulator (KG-5 high shear mixer) at a propulsion speed of 250 rpm and a cutting speed of 2500 rpm Mix for five minutes.

[0056] 260 ml of water were added to the powder mixture at a rate of 100 ml / min at a propulsion speed of 250 rpm and a pelletizing speed of 2500 rpm.

[0057] To facilitate aggregation, the powder was aggregated for 5 minutes at a propulsion speed of 250 rpm and a cutting speed of 5000 rpm.

[0058] The prepared granules were dried for 25 minutes in a fluidized bed dryer with an inlet air temperature of 60°C and a nominal airflow setting of 8.

[0059] The dried granules are sieved using a suitable mesh screen (0.083 inch mesh).

[0060] The obtained granules were taken out, weighed, and mixed with 2% magnesium stearate (20 g, pre-sieved with a 40-mesh sieve) for...

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PUM

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Abstract

Disclosed are novel ranolazine sustained release pharmaceutical formulations.

Description

Background technique [0001] This application claims priority to US Provisional Patent Application Serial No. 60 / 642,168, filed January 6, 2005, which is hereby incorporated by reference in its entirety. [0002] Ranolazine (N-(2,6-dimethylphenyl)-4-[2-hydroxy-3-(2-methoxyphenoxy)-propyl]-1-piperazineacetamide ) is an agent that has been found useful in the treatment of various disease conditions including heart failure, arrhythmia, angina pectoris, diabetes, myocardial infarction, intermittent claudication, and the like. Ranolazine has been the subject of clinical trials for the treatment of some of the symptoms of these diseases, including angina, especially chronic angina. [0003] Initially, clinical trials of ranolazine in patients with angina were considered a failure because of the ineffectiveness of an immediate-release formulation of ranolazine at a dose level of 120 mg three times daily. Subsequent clinical research work with ranolazine clearly demonstrated that due...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/20
CPCA61K9/2027A61K9/2054A61P9/00A61P9/04A61P9/06A61P9/10A61P3/10A61K9/20
Inventor 斯里孔达·萨斯特里亚纳基·尼沙德哈姆
Owner GILEAD PALO ALTO
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