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Levodopa/carbidopa/entacapone pharmaceutical preparation

A technology of entacapone and levodopa, applied in the directions of drug combination, drug delivery, oil/fat/wax inactive ingredients, etc., can solve the problem of not describing the oral solid composition containing entacapone, etc.

Inactive Publication Date: 2004-09-29
ORION CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] To the applicant's knowledge, neither the above patent nor any other patent or publication describes an oral solid composition comprising entacapone, levodopa and carbidopa, or pharmaceutically acceptable salts or hydrates thereof

Method used

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  • Levodopa/carbidopa/entacapone pharmaceutical preparation
  • Levodopa/carbidopa/entacapone pharmaceutical preparation
  • Levodopa/carbidopa/entacapone pharmaceutical preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] Entacapone / levodopa / carbidopa 200 / 100 / 25 mg tablets containing different excipients prepared by different methods were tested after a single oral administration to 15 healthy volunteers Peng, levodopa and carbidopa absorption. Tablets were prepared by wet granulation of all active ingredients simultaneously (Formulation 1), and compaction granulation of all active ingredients simultaneously (Formulation 2). The formulations are listed in Table 1.

[0084] The purpose of the absorption study was to evaluate the absorption of the active substance between two fixed-dose combination tablets and entacapone 200mg tablets administered together with levodopa / carbidopa 100 / 25mg tablets , the latter being SINEMET PLUS(R), marketed in Europe by DuPont Pharmaceuticals Ltd. The study was conducted according to an open randomized crossover design. Plasma entacapone, levodopa, and carbidopa concentrations were determined using two separate reversed-phase HPLC methods, that is, enta...

Embodiment 2

[0088] Examples of suitable entacapone / levodopa / carbidopa 200 / 100 / 25 mg tablets are described in Table 2. Tablets were prepared by adding carbidopa separately in granulated form (formulation 3) and in powder form itself (formulation 4) to the formulation. Therefore, to prepare formulation 3, entacapone and levodopa were wet granulated with corn starch, mannitol, croscarmellose sodium and povidone in a conventional high shear mixer . Carbidopa was wet granulated with corn starch, mannitol, croscarmellose sodium and povidone in a conventional high shear mixer. Mix the dry entacapone / levodopa granules, dry carbidopa granules, croscarmellose sodium, mannitol and magnesium stearate together, compress the resultant into oval tablets, and use Pigment-containing HPMC-coating agent coating. Formulation 4 was prepared similarly to Formulation 3, but with the addition of carbidopa itself in powder form.

[0089] Formulations 3 and 4 were tested for absorption in 15 healthy volunteers...

Embodiment 3

[0096] Prepare formulations 5 and 6 shown in Table 3 below according to formulation 3, but use 200mg / 50mg / 12.5mg (preparation 5) and 200mg / 150mg / 37.5mg (preparation 6) of entacapone / levodopa / carba Bidoba. Correspondingly, 200 mg / 100 mg / 10 mg of entacapone / levodopa / carbidopa were also prepared.

[0097] ingredient name

[0098] The tablet cores are coated with a colored HPMC-coating agent with a weight gain of 2-3%.

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PUM

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Abstract

The invention relates to an oral solid fixed dose composition comprising pharmacologically effective amounts of entacapone, levodopa, and carbidopa, or a pharmaceutically acceptable salt or hydrate thereof, and comprising at least one pharmaceutically acceptable excipient. The composition of the invention can be used e.g. for the treatment of Parkinson's disease.

Description

field of invention [0001] The present invention relates to a novel pharmaceutical composition, which comprises entacapone, levodopa and carbidopa or pharmaceutically acceptable salts or hydrates thereof, relates to a preparation method of the composition, and also relates to the combination Use of substances in methods of treatment. The present invention also relates to the use of entacapone, levodopa and carbidopa or pharmaceutically acceptable salts or hydrates thereof in the preparation of oral solid fixed dose combinations. Background of the invention [0002] The chemical names of entacapone, levodopa and carbidopa are (E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-di Ethyl-2-acrylamide, (-)-L-α-amino-β-(3,4-dihydroxyphenyl)propionic acid and (-)-L-α-hydrazino-α-methyl-β- (3,4-Dihydroxyphenyl)propionic acid, for example in the form of the monohydrate. Entacapone is described in US Patent No. 5,446,194 as a catechol-O-methyltransferase (COMT) inhibitor. US Patent No...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K9/16A61K9/20A61K9/26A61K31/192A61K31/195A61K31/198A61K31/275A61K31/277A61K36/47A61K47/10A61K47/26A61K47/36A61K47/44A61P25/16
CPCA61K31/275A61K9/2054A61P25/00A61P25/16A61P25/18A61P43/00A61K31/195A61K2300/00A61K31/198
Inventor S·卡里奥恩L·科维恩M·拉克森J·林图拉克索M·尼斯卡恩M·帕坦恩M·里塔拉K·瓦赫沃M·沃凯
Owner ORION CORPORATION
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