Extended Release Pharmaceutical Composition Of Entacapone Or Salts Thereof

a technology of entacapone and pharmaceutical composition, which is applied in the direction of drug compositions, biocide, nervous disorders, etc., can solve the problems of side effects, non-compliance with the patient's regimen, and other unwanted side effects, so as to reduce the ‘wearing off’ phenomenon. , the effect of reducing the ‘wearing off’ phenomenon

Inactive Publication Date: 2016-01-21
WOCKHARDT LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0025]In another general aspect of the invention there is provided a method of reducing the ‘wearing off’ phenomena in Parkinson's patients, comprising administering to patient in need thereof, an extended release pharmaceutical composition comprising from about 200 to about 1000 mg of entacapone or salts there of in a mammal in need thereof, optionally with other pharmaceutically acceptable excipients.
[0026]In another general aspect of the invention there is provided a method of reducing the ‘wearing off’ phenomena in Parkinson's patients, comprising administering to patient in need thereof, an extended release pharmaceutical composition comprising from about 200 to about 1000 mg of entacapone or salts there of in a mammal in need thereof, optionally with other pharmaceutically acceptable excipients, wherein one tablet of the said composition exhibits no significant difference in rate and / or extent of absorption of entacapone as compared to 2-4 tablets of 200 mg of immediate release entacapone commercially marketed as Comtan® administered at the interval of 3-4 hours.
[0033]In another general aspect of the invention there is provided a method of reducing the ‘wearing off’ phenomena in Parkinson's patients, comprising administering to patient in need thereof, an extended release pharmaceutical composition comprising from about 30 mg to about 300 mg of levodopa, 10 mg to about 100 mg of carbidopa and 200 mg to about 1000 mg of entacapone or salts thereof, optionally with other pharmaceutically acceptable excipients.

Problems solved by technology

However, as Parkinson's disease gets worse, the brain has fewer cells that can take up levodopa and store it as dopamine for release when levels are low.
If someone with a reduced ability to store dopamine is given too much levodopa, it may lead to side effects (e.g. dyskinesia).
As these motor fluctuations emerge, other unwanted side effects may occur.
Further, this regimen is not patient compliant.
Another problem with entacapone formulations is for the patients having swallowing problems.
These patients cannot easily swallow the tablet.
Further, it has been observed that it is very inconvenient for the patient to take a tablet of Sinemet CR and Comtan simultaneously number of times a day, which leads to patient non-compliance especially in Parkinson's patient.
Further, literature also suggests when the three ingredients are present together vis a vis entacapone, carbidopa and levodopa, it leads to decrease in bioavailability of entacapone and levodopa.
Additionally, literature also reports destabilization of triple combination formulation in presence of microcrystalline cellulose.

Method used

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  • Extended Release Pharmaceutical Composition Of Entacapone Or Salts Thereof
  • Extended Release Pharmaceutical Composition Of Entacapone Or Salts Thereof

Examples

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Effect test

examples

[0061]The composition of batches is provided in Table 1 to 23. Following formulations are representatives of the preferred compositions of the invention. The preparation of example is detailed below.

example — i

Example—I

[0062]

TABLE 1Pharmaceutical composition of the invention% w / wIngredientsEntacapone60.1Mannitol18.0Hydroxypropyl methyl cellulose16.2Povidone0.9Magnesium Stearate0.9Talc0.2-3CoatingOpadry3.8

[0063]Procedure:

[0064]Entacapone and mannitol were sifted and co-sifted through mesh to form a bulk. Hydroxypropyl methyl cellulose was sifted and added to the above bulk to form a mixture. A part of magnesium stearate was sifted and mixed with the above mixture to form a bulk. The bulk was dry granulated using roller compactor to form the slugs. The slugs were size reduced to form granules. The granules were lubricated with remaining portion of magnesium stearate and talc to form a blend. The blend was compressed using suitable tooling to form tablets. The tablets were coated using Opadry.

TABLE 2Dissolution data of composition prepared as per example I.Time (hrs)% drug released0.528152274388496

[0065]Table 2 provides the dissolution data of composition prepared as per formula given in tab...

example — ii

Example—II

[0066]

TABLE 3Pharmaceutical composition of the inventionIngredients% w / wEntacapone57.1Lactose19.3Hydroxy ethyl cellulose12.4Hydroxypropyl methyl cellulose8.6Waterq.s.Magnesium Stearate1.4Talc1.1

[0067]Procedure: Entacapone, lactose, hydroxy ethyl cellulose and hydroxypropyl methylcellulose were co-sifted and mixed to form a bulk. The bulk was wet granulated using water to form the granules and the granules were dried. The dried granules were size reduced. Magnesium stearate and talc were sifted and added to the size reduced granules and were compressed using suitable tooling to form tablets.

TABLE 4Dissolution data of composition prepared as per example II.Time (hrs)% drug released0.533158278388497

[0068]Table 4 provides the dissolution data of composition prepared as per formula given in table 3. For determination of drug release rate, USP Type 2 Apparatus (rpm 75) was used wherein 1000 ml of pH 5.5 phosphate buffer at 37° C.±0.5° C. was used as medium.

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Abstract

There is provided an extended release pharmaceutical composition comprising from about 200 mg to about 1000 mg of entacapone or salts thereof, optionally with other pharmaceutically acceptable excipients. The invention also provides an extended release pharmaceutical composition comprising triple combination of from about 30 mg to about 300 mg of levodopa, 10 mg to about 100 mg of carbidopa and 200 mg to about 1000 mg of entacapone or salts thereof, optionally with other pharmaceutically acceptable excipients. The invention also relates to process of preparation of such compositions.

Description

FIELD OF THE INVENTION[0001]There is provided an extended release pharmaceutical composition comprising from about 200 mg to about 1000 mg of entacapone or salts thereof, optionally with other pharmaceutically acceptable excipients. The invention also provides an extended release pharmaceutical composition comprising triple combination of from about 30 mg to about 300 mg of levodopa, 10 mg to about 100 mg of carbidopa and 200 mg to about 1000 mg of entacapone or salts thereof, optionally with other pharmaceutically acceptable excipients. The invention also relates to process of preparation of such compositions.BACKGROUND OF THE INVENTION[0002]Entacapone, an inhibitor of catechol-O-methyltransferase (COMT), used in the treatment of Parkinson's disease as an adjunct to levodopa / carbidopa therapy. The chemical name of entacapone is (E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N, N-diethyl-2-propenamide. Its empirical formula is C14H15N3O5, and its structural formula is:[0003]Carbidopa, ...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/20A61K9/24A61K9/28A61K31/197A61K31/277
CPCA61K9/2054A61K31/277A61K9/209A61K9/28A61K31/197A61K9/2027A61K31/198A61P25/16A61K2300/00A61K45/06
Inventor KAPOOR, RITESHTALWAR, MUNISHMATE, SANJAYMASHALKAR, MANOJJAIN, GIRISH KUMARKODGULE, MANDAR
Owner WOCKHARDT LTD
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