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Coated Tablets Of 6-(5-Chloro-2-Pyridyl)-5-[(4-Methyl-1-Piperazinyl)Carbonyloxy]-7-Oxo-6,7-Dihydro-5H-Pyrrolo[3,4-b]Pyrazine And Methods For Measuring Effectiveness Of Coating

a technology of pyrrolopyrrolo and pyrrolopyrrolo, which is applied in the direction of instruments, drug compositions, biocides, etc., can solve the problems of inability to capture the dissolution profiles of tablets, time-consuming, and large clinical studies, and none of these techniques are able to accurately determine very small amounts of material at very short time frames

Inactive Publication Date: 2010-09-02
SUNOVION PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0012]The invention is also directed towards a method for treatment, prevention, or amelioration of a sleep disorder in a subject comprising administering to a subject in need thereof, a composition described above. The invention further includes a method for treatment, prevention, or amelioration of anxiety in a subject comprising administering to a subject in need thereof, a composition described above.

Problems solved by technology

But none of these techniques are able to accurately determine very small amounts of material at very short time frames.
Human taste panel studies, such as the “Lick and Roll” testing method (a method involving direct collection of human saliva from the patients who take LUNESTA® tablets) is not only time-consuming, but also requires large and expensive clinical studies.
Further, the conventional dissolution method is not capable of capturing the dissolution profiles of the tablets in the incipient stages of dissolution because sampling requires time intervals of five minutes or longer.
On the other hand, methods such as conventional UV fiber optics and / or LC-UV methods, while rapid, are not sensitive enough to accurately quantify the trace amount of the active pharmaceutical ingredient at the ng / mL level.

Method used

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  • Coated Tablets Of 6-(5-Chloro-2-Pyridyl)-5-[(4-Methyl-1-Piperazinyl)Carbonyloxy]-7-Oxo-6,7-Dihydro-5H-Pyrrolo[3,4-b]Pyrazine And Methods For Measuring Effectiveness Of Coating
  • Coated Tablets Of 6-(5-Chloro-2-Pyridyl)-5-[(4-Methyl-1-Piperazinyl)Carbonyloxy]-7-Oxo-6,7-Dihydro-5H-Pyrrolo[3,4-b]Pyrazine And Methods For Measuring Effectiveness Of Coating
  • Coated Tablets Of 6-(5-Chloro-2-Pyridyl)-5-[(4-Methyl-1-Piperazinyl)Carbonyloxy]-7-Oxo-6,7-Dihydro-5H-Pyrrolo[3,4-b]Pyrazine And Methods For Measuring Effectiveness Of Coating

Examples

Experimental program
Comparison scheme
Effect test

example 1

Eszopiclone 3.0 mg Coated Tablets (Opadry® tm Coat)

[0093]18 kilograms of eszopiclone cores (3.0 mg per tablet) were coated with an Opadry coating dispersion. The Opadry dispersion of this example was made by mixing 14.58 kg of purified water with 1.62 kg of Opadry tm (07F99077, Blue), resulting in a 10% solids content, for 45 minutes in a vortex at 24° C. at 750 rpm. 100 g of the coating suspension was removed and found to have a viscosity of 336.5 cP (25° C.). The mixture was then de-aerated by mixing at a low speed for approximately one hour.

[0094]The 18 kg of core tablets (eszopiclone 3.0 mg, single dedusted cores) were loaded into a 24-inch O'Hara Labcoat Model IIX pan, which has 4 mixing baffles, a peristaltic pump, 96440-25 Masterflex tubing, 2 Spraying Systems guns (SUV113A), VF-3578-SS or VF-3578-316SS nozzles and VA113293-60-316SS or CO-VF-3578-SS air caps, for coating. The two spray guns were set to 35 g / min (70 g / min total spray rate). After 100 minutes, the desired 4.5% ...

example 2

[0096]A solids content range study was conducted on a 1 kg scale. The 7% and 10% solids content samples had comparable appearances, while the 13% solids content surface was rougher. The table below illustrates viscosity results and the run time required to achieve a 4% coating weight gain.

Run Time for 4%Solids Content (%)Viscosity (cP)Weight Gain (min)711663104364413118032

example 3

Taste Assessment

[0097]An open-label multiple-dose study of the taste profile of eszopiclone tablets was utilized to perform taste assessments. For the purpose of testing the compositions described above, the flavor profile panel consisted of four persons who have normal ability to smell and taste, have been trained in fundamental sensory principles and all aspects of the Flavor Profile technique and have considerable experience as panel members. The samples to be profiled were uniform and representative. Sample preparation and presentation were standardized and controlled.

[0098]The Flavor Profile is an art-recognized descriptive sensory analysis method used to measure the type and intensity of attributes in products and ingredients. [see Keane, P. The Flavor Profile Method. In C. Hootman (Ed.), Manual on Descriptive Analysis Testing for Sensory Evaluation ASTM Manual Series: MNL 13. Baltimore, Md. (1992).] It is based on the concept that flavor consists of identifiable taste, odor (...

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Abstract

Coated tablets of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) are provided. The tablets minimize the perceived bitterness of the medicament. A method for analyzing instantaneous dissolution of sub-microgram quantities of core material is also disclosed.

Description

CROSS REFERENCE TO RELATED APPLICATIONS[0001]This application is related to U.S. application Ser. Nos. 12 / 338,899, 12 / 338,903 and 12 / 338,908, all filed on Dec. 18, 2008, which are incorporated herein by reference in their entirety. This application claims priority to U.S. provisional application 61 / 148,621, filed Jan. 30, 2009, which is incorporated herein by reference in its entirety.FIELD OF THE INVENTION[0002]The present invention relates to coated oral solid dosage forms and to methods for testing the effectiveness of the coating on said solid dose.BACKGROUND OF THE INVENTION[0003]Eszopiclone, also known as (S)-zopiclone or (S)-(6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine), is formulated as the free base and is sold as LUNESTA®. It is used to treat different types of sleep problems, such as difficulty in falling asleep, difficulty in maintaining sleep during the night, and waking up too early in the morning. Most peo...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/4985A61K9/00A61K9/30A61K9/36A61P25/22A61P25/20G01N33/00
CPCA61K9/2866Y10T436/147777A61K31/4985A61P25/20A61P25/22
Inventor HSIA, RICHARDHUANG, CAI GUSARANTEAS, KONSTANTINOS E.MISRA, TUSHAR K.BONASIA, JR., PHILIP J.
Owner SUNOVION PHARMA INC
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