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Single Unit Oral Dose Pharmaceutical Composition Comprising Levodopa, Carbidopa And Entacapone Or Salts Thereof

a single-unit, oral-dosage technology, applied in the direction of drug compositions, biocide, nervous disorders, etc., can solve the problems of side effects, other unwanted side effects, and regimens that are not patient-compliant, and achieve the effect of reducing the phenomenon of “wearing off”

Inactive Publication Date: 2011-09-22
GUPTA YATENDRA KUMAR +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The invention provides a single unit oral dose pharmaceutical composition comprising levodopa, carbidopa, and entacapone in extended release and immediate release forms. This composition is effective in treating Parkinson's disease and reducing the \"wearing off\" phenomena in patients. The process for preparing the pharmaceutical composition involves coating or mixing the active ingredients with pharmaceutically acceptable excipients and converting it into a suitable dosage form. The details of the patent text are set forth in the description below."

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.
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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  • Single Unit Oral Dose Pharmaceutical Composition Comprising Levodopa, Carbidopa And Entacapone Or Salts Thereof
  • Single Unit Oral Dose Pharmaceutical Composition Comprising Levodopa, Carbidopa And Entacapone Or Salts Thereof
  • Single Unit Oral Dose Pharmaceutical Composition Comprising Levodopa, Carbidopa And Entacapone Or Salts Thereof

Examples

Experimental program
Comparison scheme
Effect test

examples

[0045]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

[0046]

TABLE 1Pharmaceutical composition of the inventionIngredients% w / wEntacapone IR layer / PortionEntacapone38.41Mannitol6.73Sodium starch glycolate3.85Corn Starch9.42Croscarmellose sodium4.62Povidone1.51Purified waterq.s.Extragranular IngredientsMagnesium stearate0.77Levodopa and Carbidopa CR layer / PortionLevodopa19.22Carbidopa5.19Microcrystalline Cellulose4.62Povidone3.46Purified Waterq.s.Extragranular IngredientsPoly Vinyl Pyrrolidone1.73Magnesium Stearate0.38

Procedure:

Entacapone Layer / Portion:

[0047]Entacapone and mannitol were co-milled and sifted. Cornstarch, croscarmellose sodium and sodium starch glycolate were co-sifted separately. The materials were placed in granulator and mixed. Povidone was dissolved in purified water and granulated with the mixed material. The granulated contents were dried. Magnesium stearate was sifted and mixed with the dried granules.

Levodopa and Carbidopa Layer / Portion:

[0048]Levodopa, Carbidopa and microcrystalline cellulose were co-sifted and mix...

example-ii

[0051]

TABLE 3Pharmaceutical composition of the inventionIngredients% w / wEntacapone layer / PortionEntacapone28.57Mannitol5.00Sodium starch glycolate2.86Corn Starch7.00Croscarmellose sodium3.43Povidone1.14Purified waterq.s.Extragranular IngredientsMagnesium stearate0.57Levodopa and Carbidopa CR layer / PortionLevodopa28.57Carbidopa7.71Microcrystalline Cellulose6.86Povidone5.14Purified Waterq.s.Extragranular IngredientsPVP2.57Magnesium Stearate0.57

Procedure:

Entacapone Layer / Portion:

[0052]Entacapone and mannitol were co-milled and sifted. Corn starch, croscarmellose sodium and sodium starch glycolate were co-sifted separately. The materials were placed in granulator and mixed. Povidone was dissolved in purified water and granulated with the mixed material. The granulated contents were dried. Magnesium stearate was sifted and mixed with the dried granules.

Levodopa and Carbidopa Layer / Portion:

[0053]Levodopa, Carbidopa and microcrystalline cellulose were co-sifted and mixed. Povidone was diss...

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Abstract

There is provided a single unit oral dose pharmaceutical composition comprising a) levodopa or salts thereof from about 50 mg to about 300 mg in extended release form, b) carbidopa or salts thereof from about 10 mg to about 100 mg in extended release and c) entacapone or salts thereof from about 100 mg to about 1000 mg in immediate release form, 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 a single unit oral dose pharmaceutical composition comprising a) levodopa or salts thereof from about 50 mg to about 300 mg in extended release form, b) carbidopa or salts thereof from about 10 mg to about 100 mg in extended release and c) entacapone or salts thereof from about 100 mg to about 1000 mg in immediate release form, 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, an inhibitor of aromatic amino acid decarboxylation, is a white, crystalline compound, slightly soluble in ...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/52A61K31/277A61P25/16A61K9/24
CPCA61K9/2059A61K9/209A61K31/198A61K31/277A61K45/06A61K2300/00A61P25/16A61K9/0053
Inventor GUPTA, YATENDRA KUMARJAIN, GIRISH KUMARTALWAR, MUNISHMASHALKAR, MANOJ
Owner GUPTA YATENDRA KUMAR
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