Oral controlled release tablet with reduced burst effect

A technology of controlled-release tablets and excipients, applied in pill delivery, coating, pharmaceutical formulations, etc.

Inactive Publication Date: 2011-04-20
SUN PHARMA INDS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, any release that occurs at a significantly increased rate that increases the incidence of undesired side effects or adverse effects may be considered a "dose burst"

Method used

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  • Oral controlled release tablet with reduced burst effect
  • Oral controlled release tablet with reduced burst effect
  • Oral controlled release tablet with reduced burst effect

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0175] Table 1

[0176]

[0177]

[0178] The amount of alcohol-soluble excipients in the upper compression layer, such as polyvinylpyrrolidone and acrylic resin L-100 55, is 13.5% by weight of the upper compression layer.

[0179] Metoprolol succinate, hydroxypropyl methylcellulose, lactitol monohydrate and povidone K-30 were passed through ASTM (American Society for Testing and Materials) sieve #40 and mixed properly. The mixture thus obtained is granulated with pure water to a suitable size, and the granules obtained are dried to a moisture content of 1-2%. The dried granules are suitably ground and lubricated with a mixture of sodium ethoxide starch, colloidal silicon dioxide, talc and magnesium stearate to obtain a lower compressive layer mixture.

[0180] Silicified microcrystalline cellulose, crospovidone, sodium lauryl sulfate, and appropriate colorants were passed through ASTM sieve #40 and mixed properly. The mixture thus obtained was lubricated with a mixtu...

Embodiment example 2

[0185] Table 2

[0186]

[0187]

[0188] Paroxetine hydrochloride hemihydrate, hydroxypropyl methylcellulose, lactose monohydrate and povidone K-30 (the amount of alcohol-soluble excipient accounts for 5.71% of the weight of the lower compression layer) passed ASTM (American Society for Testing and Materials) sieve #40 and mix properly. The mixture thus obtained is granulated with pure water to a suitable size, and the granules obtained are dried to a moisture content of 1-2%. The dried granules are properly milled and lubricated with an optimized mixture of Prosolv SMCC90, colloidal silicon dioxide and magnesium stearate to obtain a mixture for the first layer. Silicified microcrystalline cellulose, crospovidone, sodium lauryl sulfate, and appropriate colorants were passed through ASTM sieve #40 and mixed properly. The mixture thus obtained was lubricated with a mixture of colloidal silicon dioxide, talc and magnesium stearate (previously passed through ASTM sieve #...

Embodiment 2

[0191] The lower compressive layer begins to gel upon contact with an aqueous environment. The coating on the bottom and sides of the lower compressive layer is retained. The coating was substantially impermeable to paroxetine hydrochloride. Release occurs from the exposed upper surface of the gelled lower compressive layer. The released surface area remains essentially unchanged over the release time. In this example, it was observed that as the release progressed, the lower compressive layer eroded and its thickness decreased until the cup formed by the coating was fully formed into a cup at the end of the release time.

[0192] Example 3

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PUM

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Abstract

The present invention refers to an oral controlled release tablet providing a reduced risk of alcohol induced dose dumping; said tablet comprising: a core comprising a first compressed layer comprising a swelling agent, a second compressed layer comprising at least one therapeutically active ingredient, and pharmaceutically acceptable excipient wherein at least one excipient is a release rate controlling excipient and wherein the percent by weight of excipients that are soluble in alcohol does not exceed 35 % by weight of the layer, optionally a third compressed layer comprising a swelling agent; and a coating surrounding the said core, the coating comprising a polymer insoluble in an aqueous medium comprising from 0 % v / v to 40 % v / v of alcohol, whereby upon contact with aqueous gastrointestinal fluids, the upper compressed layer swells to cause removal of the coating from the upper surface of the upper compressed layer and then said upper layer disintegrates allowing the release of the active ingredient from the defined surface area of the upper surface of said lower compressed layer with the coating covering its bottom and side surfaces.

Description

technical field [0001] The present invention relates to a method of reducing the alcohol-induced risk of alcohol-induced dose-dumping of therapeutically active ingredients. Background technique [0002] Oral controlled-release drug delivery systems contain at least twice the amount of drug compared to traditional dosage forms, and thus require careful design to prevent rapid release of the drug dose. This unintentional rapid drug release of most of the drug contained in the controlled release drug delivery system over a relatively short period of time may be referred to as 'dose burst'. While dose bursts induced by the presence of food have been studied by regulatory bodies for about two decades, dose bursts induced by alcohol consumption have only recently received attention. In 2005, several drugs were recalled from the market due to ethanol's effect on controlled-release formulations. For example, the U.S. Food and Drug Administration (FDA) asked Purdue Pharma to recall...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/24A61K9/36A61K31/138A61K47/38
CPCA61K9/2866A61K9/2054A61K9/2086
Inventor 尼廷·巴拉昌哲·达玛惴卡瑞亚绍瑞亚·瑞普赛·扎拉
Owner SUN PHARMA INDS
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