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WO2009109990A2 - Composition pharmaceutique de pramipexole - Google Patents

Composition pharmaceutique de pramipexole Download PDF

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Publication number
WO2009109990A2
WO2009109990A2 PCT/IN2009/000056 IN2009000056W WO2009109990A2 WO 2009109990 A2 WO2009109990 A2 WO 2009109990A2 IN 2009000056 W IN2009000056 W IN 2009000056W WO 2009109990 A2 WO2009109990 A2 WO 2009109990A2
Authority
WO
WIPO (PCT)
Prior art keywords
pharmaceutical composition
composition
pramipexole
pharmaceutically acceptable
weight
Prior art date
Application number
PCT/IN2009/000056
Other languages
English (en)
Other versions
WO2009109990A3 (fr
Inventor
Vaishali Vijay Dhavse
Nitin Bhalachandra Dharmadhikari
Original Assignee
Sun Pharmaceutical Industries Ltd.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Sun Pharmaceutical Industries Ltd. filed Critical Sun Pharmaceutical Industries Ltd.
Publication of WO2009109990A2 publication Critical patent/WO2009109990A2/fr
Publication of WO2009109990A3 publication Critical patent/WO2009109990A3/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets

Definitions

  • the present invention relates to a pharmaceutical composition
  • a pharmaceutical composition comprising pramipexole or its pharmaceutically acceptable salts or its hydrates or solvates thereof.
  • Pramipexole (S)-2-amino-4, 5, 6, 7 - tetrahydro-6-(propylamino) benzole, is a non ergot dopamine agonist with high relative in vitro specificity and full intrinsic activity at the D 2 subfamily of dopamine receptors. It is indicated in the treatment of signs and symptoms of idiopathic Parkinson's disease.
  • United States patent application number 20070129329 discloses a stabilized pharmaceutical composition of pramipexole comprising one or more dextrin.
  • the present invention provides a pharmaceutical composition
  • a pharmaceutical composition comprising a mixture of pramipexole or its pharmaceutically acceptable salts or its hydrates or solvates thereof, sugar alcohol (s) and a pharmaceutically acceptable carrier medium substantially free of polyvinyl pyrrolidone.
  • the term 'labeled amount' as used herein, refers to the amount of therapeutically active ingredient present in a pharmaceutical product.
  • a unit dose of the therapeutically active ingredient is present in the pharmaceutical product, it is often termed as a unit dosage form.
  • Detailed monographs, often called label, of the marketed dosage form contain its description, pharmacology, clinical studies, indication, contraindications, warnings, precautions, adverse events, dosage and administration and other details of the marketed product.
  • the dosage form may be available in various doses, specified in the label, for example, pramipexole tablets are available as 0.125, 0.25, 0.5, 1.0 and 1.5 mg of pramipexole dihydrochloride monohydrate. These various doses in the tablets are herein referred to as the 'labeled amount' of pramipexole dihydrochloride monohydrate.
  • the dosage form should be chemically 'stable' and retain the labeled amount of the iheiapeuiieall) active ingredient upon storage and the impurities in the pharmaceutical product should remain low.
  • a 'stable' pharmaceutical composition comprising a mixture of pramipexole or its pharmaceutically acceptable salts or hydrates or solvates thereof, sugar alcohol (s) and a pharmaceutically acceptable carrier medium substantially free of polyvinyl pyrrolidone.
  • compositions when stored in high density polyethylene containers at a temperature of about 40 0 C + 2 0 C and relative humidity of about 75 % + 5 % for a period of three months, showed the content of pramipexole dihydrochloride monohydrate ranging from about 95 % to about 105 % by weight of the labeled amount of pramipexole dihydrochloride monohydrate and the total impurities (known and unknown) were less than I % of the labeled amount of pram ⁇ pe ⁇ le d ⁇ h) di udil ⁇ J ⁇ .
  • these impurities were separated by High performance liquid chromatography (HPLC) and quantified by measuring the absorption in the ultraviolet region.
  • HPLC High performance liquid chromatography
  • any other suitable analytical method may also be employed to determine the pramipexole content and to quantify the known and unknown impurities.
  • composition of the present invention comprises a mixture of pramipexole or its pharmaceutically acceptable salts or its- hydrates or solvates thereof, sugar alcohol (s) and a pharmaceutically acceptable carrier medium substantially free of polyvinyl pyrrolidone.
  • mixture' as used herein means pramipexole or its pharmaceutically acceptable salts or its hydrates or solvates thereof is intimately blended or is in physical contact with the pharmaceutically acceptable carrier medium.
  • the pharmaceutical composition of the present invention is considered to be stable ' when the ⁇ hu ⁇ iiciceuiieul composition upon storage in suitable containers with or without desiccants at a temperature of about 40° C ⁇ 2° C and a relative humidity of about 75 % ⁇ 5 %, shows the pramipexole dihydrochloride monohydrate content in the range of about 95 % to about 105 % of the labeled amount and total impurities are less than about 1 % by weight of pramipexole dihydrochloride monohydrate.
  • the composition of the present invention comprises pramipexole or its pharmaceutically acceptable salts or its hydrates or solvates thereof.
  • the pharmaceutically acceptable acid salts of pramipexole include, but are not limited to, acid addition salts of inorganic acids or organic acids such as hydrobromide, sulfuric, phosphoric, lactic, citric, tartaric, succinic, maleic and formic acid and the like.
  • the pramipexole is used as the dihydrochloride salt, more preferably pramipexole is used as dihydrochloride monohydrate.
  • the amount of pramipexole dihydrochloride monohydrate ranges from about 0.05 mg to about 2.0 mg per tablet. More preferably, the amount of pramipexole dihydrochloride monohydrate ranges from about 0.09 mg to about 1 .8 mg per tablet.
  • T he composition of the present invention comprises a pharmaceutically acceptable carrier medium substantially free of polyvinyl pyn olidone Although it may be possible to prepare a stable pharmaceutical composition with trace amount of polyvinyl pyrrolidone, preferably the composition is completely devoid of polyvinyl pyrrolidone
  • the pharmaceutical composition comprises sugar alcohol (s) as one of the fillers or diluents
  • sugar alcohols may be in any stereoisomers or geometric isomers or/and optical isomers forms They may be straight chain or cyclic in nature
  • the straight chain sugar alcohols may be ti ihyd ⁇ c to hexafn d ⁇ c sugar alcohol
  • Examples of the straight chain sugai alcohols that ma ⁇ be used in (he composition of the present invention include, but are not limited to, hexitols such as sorbitol, mannitol, glycerol, alhtol, talitol, glucitol, iditol and dulcitol, pentitols such as xylitol, adonitol (also called ⁇ bitol) and arabitol, teti itols such as eryth ⁇ tol and threitol, and t ⁇ ols such
  • fillers or diluents that may be used in the pharmaceutically acceptable carrier medium substantially free of polyvinyl pyrrolidone, include, but are not limited to, starch and its derivatives like corn staich, pi egelatmized staicli and the like, cal ⁇ um phosphate dibasic, calcium phosphalc u ibasic, m ⁇ uuu ) -.idlli ⁇ iL cellulose, silicified microcrystalline cellulose, powdered cellulose, lactose, dextrose, dextrin, sugar compressible and the like and mixture thereof
  • the amount of fillers that may be used in the pharmaceutical composition of the present invention ranges from about 5 % to about 90 % by weight of the composition, preferably 15 % to about 30 % by weight of the composition
  • binders examples include, but are not limited to, methyl cellulose, hydioxypropyl cellulose gelatin, tragacanth sodium alginate and the like and mixture thereof
  • the amount of bindei that may be used ranges from about 0 % to about 10 % by weight of the composition
  • purified water is used as the sole granulating agent
  • lubricants/ glidants examples include, but are not limited to, silicon dioxide, colloidal silicon dioxide, magnesium stearate, calcium stearate, sodium stearyl fumarate, stearic acid, zinc stearate, talc and the like or mixture thereof
  • the amount of lub ⁇ cants/glidants that may be used in the pharmaceutical composition of the present invention ranges from about 0 1 % to about 5 %, preferably about 2 % by weight of the composition
  • the pharmaceutical composition consists essentially of a mixtuie oi p ⁇ am ⁇ pe ⁇ ole oi its phdi maceutiuillv dn.cpt.ible salts oi its lnduks oi ->oU ak -> ll ⁇ ol it ti di * ⁇ it derivatives sugai alcohol (s) and a pharmaceutically acceptable carrier medium
  • the pharmaceutically acceptable carrier medium is substantially free of polyvinyl pyrrolidone
  • the composition is completely devoid of polyvinyl pyrrolidone
  • compositions prepared according to Example 1 , 2, 5 were packed and sealed in high density polyethylene containeis with desiccant and were stored at a temperature of about 40 0 C ⁇ 2 0 C and relative humidity of about 75 % ⁇ 5 % for three months
  • the compositions were analyzed for the pramipexole content by High performance liquid chromatography (HPLC) Related substances were separated by HPLC and quantified by measuring the absorption in the Ultraviolet region The details of the results are given in table 2 Table 2
  • composition according to comparative examples 1-5 of pramipexole were packed and sealed in black-lined high density polyethylene containers without desiccant and weie st ⁇ ied at a lempeidlun. ⁇ i about 40 'C -- 2 L and relative humidity of about 75 % ⁇ 5 % for three months
  • HPLC high performance liquid chromatography
  • compositions of comparative examples 6-9 were prepared using the ingredients listed in table no 7 and the composition of comparative example 10 was prepared using the ingredients given in table no 8
  • the tablets wei e prepared according to the procedure described in comparative examples 1 -5 except use of butylated hydroxy I anisole and butylated hydroxyl toluene dissolved in mixture of isopropyl alcohol and water instead of purified water alone
  • composition according to comparative examples 6-9 of pramipexole were packed and sealed in black lined high density polyethylene containers without desiccant and were stored at a temperature of about 40 0 C ⁇ 2° C and relative humidity of about 75 % ⁇ 5 % for a period of three months
  • the composition of the comparative example 10 was packed and sealed in white high density polyethylene bottles and was stored at a temperature of about 40 ⁇ C ⁇ 2 0 C and relative humidity of about 75 % ⁇ 5 % for three months
  • the compositions were analyzed foi the pramipexole dihydrochlo ⁇ de monohydrate content by HPLC techniques Related substances were separated by HPLC and quantified by measuring the absorption in the UV region The details of the results are given in table 9

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

L’invention concerne une composition pharmaceutique comportant du pramipexole ou ses sels pharmaceutiquement acceptables ou ses hydrates ou les solvats de ce composé, un (des) alcool(s) de sucre et un milieu véhicule pharmaceutiquement acceptable ne contenant pratiquement pas de pyrrolidone de polyvinyle.
PCT/IN2009/000056 2008-01-24 2009-01-22 Composition pharmaceutique de pramipexole WO2009109990A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN176MU2008 2008-01-24
IN176/MUM/2008 2008-01-24

Publications (2)

Publication Number Publication Date
WO2009109990A2 true WO2009109990A2 (fr) 2009-09-11
WO2009109990A3 WO2009109990A3 (fr) 2009-12-10

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2009/000056 WO2009109990A2 (fr) 2008-01-24 2009-01-22 Composition pharmaceutique de pramipexole

Country Status (1)

Country Link
WO (1) WO2009109990A2 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102772403A (zh) * 2011-05-10 2012-11-14 浙江京新药业股份有限公司 普拉克索制剂及其制备方法
EP3600291A4 (fr) * 2017-03-27 2020-12-23 Chase Therapeutics Corporation Compositions et méthodes de traitement des synucléinopathies
EP3648756A4 (fr) * 2017-07-03 2021-03-31 Chase Therapeutics Corporation Compositions à base de statine et procédés destinés à être utilisés dans le traitement de synucléinopathies

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004100857A2 (fr) * 2003-05-07 2004-11-25 Akina, Inc. Granules a teneur elevee en plastique, destines a la fabrication de comprimes a dissolution rapide
US20070148238A1 (en) * 2005-06-23 2007-06-28 Spherics, Inc. Dosage forms for movement disorder treatment
US20070196494A1 (en) * 2006-02-17 2007-08-23 Arnaud Grenier Low-friability, patient-friendly orally disintegrating formulations
WO2007137071A2 (fr) * 2006-05-16 2007-11-29 Knopp Neurosciences, Inc. Compositions de r(+) et s(-) pramipéxole et procédés d'utilisation de celles-ci

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102772403A (zh) * 2011-05-10 2012-11-14 浙江京新药业股份有限公司 普拉克索制剂及其制备方法
CN102772403B (zh) * 2011-05-10 2015-11-25 浙江京新药业股份有限公司 普拉克索制剂及其制备方法
EP3600291A4 (fr) * 2017-03-27 2020-12-23 Chase Therapeutics Corporation Compositions et méthodes de traitement des synucléinopathies
US11547700B2 (en) 2017-03-27 2023-01-10 Chase Therapeutics Corporation Compositions and methods for treating synucleinopathies
EP3648756A4 (fr) * 2017-07-03 2021-03-31 Chase Therapeutics Corporation Compositions à base de statine et procédés destinés à être utilisés dans le traitement de synucléinopathies

Also Published As

Publication number Publication date
WO2009109990A3 (fr) 2009-12-10

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