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Levodopa/carbidopa/entacapone pharmaceutical preparation

A technology of entacapone and pharmacy, applied in the direction of drug combination, drug delivery, oil/fat/wax non-active ingredients, etc., can solve the problem of not describing the oral solid composition containing entacapone

Inactive Publication Date: 2002-07-10
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] After a single oral administration to 15 healthy volunteers, we tested entacapone / levodopa / carbidopa 200 / 100 / 25mg tablets containing different excipients and prepared by different methods. Benzene, levodopa and carbidopa are absorbed. The tablets are prepared by wet granulating all the active ingredients at the same time (formulation 1), and compacting and granulating all the active ingredients at the same time (formulation 2). The formulations are as described in Table 1.

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

Embodiment 2

[0088] Examples of suitable entacapone / levodopa / carbidopa 200 / 100 / 25 mg tablets are shown in Table 2. The tablet is prepared by adding carbidopa granules (formulation 3) and its own powder form (formulation 4) separately to the formulation. Therefore, in order to prepare formulation 3, entacapone and levodopa were granulated together with corn starch, mannitol, croscarmellose sodium and povidone in a conventional high-shear mixer by wet granulation . Carbidopa, corn starch, mannitol, croscarmellose sodium and povidone were wet-granulated in a conventional high-shear mixer. The dried entacapone / levodopa granules, dried carbidopa granules, croscarmellose sodium, mannitol and magnesium stearate were mixed together, and the resultant was compressed into oval tablets. HPMC-coating agent coating with pigment. The preparation of Formulation 4 is similar to Formulation 3, but the powder form of Carbidopa itself is added.

[0089] After a single oral administration, 15 healthy volunteers t...

Embodiment 3

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

[0097] Ingredient name

[0098] The tablet core is coated with a colored HPMC-coating agent to increase the weight by 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

Invention field [0001] The present invention relates to a novel pharmaceutical composition comprising entacapone, levodopa and carbidopa or a pharmaceutically acceptable salt or hydrate thereof, and a preparation method of the composition and the composition The use of substances in treatment methods. The present invention also relates to the use of entacapone, levodopa and carbidopa or their pharmaceutically acceptable salts or hydrates 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-dihydroxybenzene)propionic acid and (-)-L-α-hydrazino-α-methyl-β- (3,4-Dihydroxybenzene)propionic acid, for example in the form of the monohydrate. Entacapone is described as a catechol-O-methyltransferase (COMT) inhibitor in US Patent No. 5,446,194. US Patent No. 5,446,194 discusses the enteral and par...

Claims

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Application Information

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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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