EP4626407A1 - Compositions pharmaceutiques à libération prolongée contenant de la prégabaline ou des sels pharmaceutiquement acceptables de celle-ci - Google Patents

Compositions pharmaceutiques à libération prolongée contenant de la prégabaline ou des sels pharmaceutiquement acceptables de celle-ci

Info

Publication number
EP4626407A1
EP4626407A1 EP23818075.6A EP23818075A EP4626407A1 EP 4626407 A1 EP4626407 A1 EP 4626407A1 EP 23818075 A EP23818075 A EP 23818075A EP 4626407 A1 EP4626407 A1 EP 4626407A1
Authority
EP
European Patent Office
Prior art keywords
sustained release
pregabalin
release film
coated tablet
pharmaceutically acceptable
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
EP23818075.6A
Other languages
German (de)
English (en)
Inventor
Hetalbahen PATEL
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Orbit Pharma Ltd
Original Assignee
Orbit Pharma 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 Orbit Pharma Ltd filed Critical Orbit Pharma Ltd
Publication of EP4626407A1 publication Critical patent/EP4626407A1/fr
Pending legal-status Critical Current

Links

Classifications

    • 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
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • 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
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
    • 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
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Definitions

  • pregabalin is (35)-3-(aminomethyl)-5-methylhexanoic acid.
  • Pregabalin is marketed as an oral tablet, capsule, solution, and powder.
  • the commercially marketed products of pregabalin in tablet form are available in three dosage strengths: 82.5 mg, 165mg, and 330 mg for oral administration.
  • the dosage strength of the Pregabalin capsule is available in 25, 50, 75, 100, 150, 200, 225, and 300 mg capsules, as well as in an oral solution containing 20 mg / mL.
  • Pregabalin oral bioavailability is reported to be >90% regardless of the dose.
  • the elimination half-life of pregabalin is 6.3 hours.
  • the mean renal clearance is estimated to be 67.0 to 80.9 mL /min.
  • US 8,945,620 B2 discloses an oral tablet containing pregabalin, matrix forming agent including mixtures of polyvinyl acetate and polyvinylpyrrolidone, and the swelling agent includes cross-linked polyvinylpyrrolidone and polyethylene oxide.
  • the Pregabalin was dry blended with matrix-forming agents, followed by the addition of other excipients.
  • the compressed dosage forms may undergo further processing such as polishing and coating.
  • WO 2010/115612A2 discloses an oral capsule that comprises 100 parts of pregabalin and 15 parts of pregelatinized starch, wherein said blend is free of lactose, mannitol, or microcrystalline cellulose.
  • the process comprises sieving and blending the pregabalin with pregelatinized starch to a homogenous blend. To the blend, talc was added and the mixture was blended again. The final mixture was filled in a size 0 capsule in an amount of 400 mg of the blend per capsule.
  • the present invention of pregabalin or pharmaceutically acceptable salts thereof provides sustained release film-coated tablet composition for once-daily (QD) dosing.
  • QD once-daily
  • the Pregabalin continuously releases while being retained in the stomach for a longer period of time.
  • the liquid dosage form is bulky, difficult to transport, and takes up a lot of space. Due to their inherent instability, liquid dosage forms often have shorter shelf lives.
  • the patient's measurement of the exact volume determines whether the dose is administered appropriately, which increases the chance for variability.
  • the dosing regimen of 2-3 daily doses is problematic which results from the sharp increase in blood plasma levels of the drug.
  • Pregabalin is not uniformly absorbed in the gastrointestinal tract, in the small intestine and ascending colon, but rarely in intestine segments outside the hepatic flexure of the colon.
  • the average absorption window of pregabalin is about 6 hours or less, and thus if pregabalin is prepared in a conventional sustained release formulation, the released drug cannot be effectively absorbed after the formulation passes through the colonic hepatic flexure after more than 6 hours. Therefore, there is a need to develop a sustained release film-coated tablet of pregabalin that can be retained in the stomach for a longer period of time, improve patient compliance and ensure the sustained and stable release of the drug.
  • the primary object of the present invention is to provide a stable once-daily Sustained release film-coated tablet of pregabalin or pharmaceutically acceptable salts thereof for oral administration.
  • the present invention relates to a Sustained release of a film-coated tablet comprising pregabalin or a pharmaceutically acceptable salt thereof, suitable for oral administration.
  • Sustained release dosage forms are designed to release drugs at a predetermined rate while maintaining a consistent drug level for a specified period of time with the minimum possible side effects.
  • the basic principle behind a sustained release drug delivery system is to optimize the biopharmaceutical, pharmacokinetic, and pharmacodynamic properties of a drug in such a way that its utility is maximized, side effects are reduced and a cure for the disease is achieved.
  • the Sustained release film-coated tablet of the present invention comprises pregabalin and release retarding agents.
  • the Sustained release film-coated tablet further comprises at least one pharmaceutically acceptable excipient selected from a diluent and lubricant.
  • the pregabalin is present in the range of about 20 %w/w to about 80 %w/w, preferably in the range of about 30 %w/w to about 50 %w/w, and is administered as an oral solid dosage form.
  • Magnesium stearate is preferred as a lubricant for the present invention and is present in the range from about 0.15 %w/w to about 15%w/w, preferably in the range from about 0.5 %w/w to about 5%w/w.
  • pregabalin containing sustained release film-coated tablet preparation for oral administration once-daily, reduce administration times, and have pharmacokinetic properties of reducing side effects while increasing patient compliance and extending the efficacy time duration, as compared to conventional pregabalin containing preparations for oral administration twice daily.
  • Pregabalin is used for the treatment or prevention of neuropathic pain, epilepsy, fibromyalgia, diabetic peripheral neuropathy, postherpetic neuralgia, or generalized anxiety disorder.
  • a combination of polyvinyl acetate, povidone, sodium lauryl sulphate, and silica is present in the range from about 5 %w/w to about 65 % w/w, preferably from about 9%w/wto about 50 % w/w.
  • Mannitol is preferred as a diluent in the range of about 0.05 %w/w to about 60 %w/w, preferably in the range from about 0.20 %w/w to about 40 %w/w.
  • 80 % of the pregabalin is released in 24 hours, preferably more than 90 % is released within 24 hours.
  • the Sustained release film-coated tablet was made according to the method defined below using the formulation having the ingredients shown in table I:
  • the Sustained release film-coated tablet was prepared according to the procedure described below using the formulation having the ingredients shown in table II: TABLE-II
  • Pregabalin, Mannitol, Hydroxy Ethyl Cellulose, Carbopol 71G, and Kollidon SR are sieved separately through a 40# sieve, and magnesium stearate separately, through a 60# sieve.
  • Magnesium stearate was added to the mixture and blended for an additional 15 minutes at 20 RPM.
  • the lubricated blend was compressed by a compression machine to form a tablet.
  • the Sustained release film-coated tablet was prepared according to the procedure described below using the formulation having the ingredients shown in table III:
  • Pregabalin, Mannitol, Hydroxy Ethyl Cellulose, Carbopol 71G, and Kollidon SR are sieved separately through a 40# sieve, and magnesium stearate separately, through a 60# sieve. Preblending of all ingredients except magnesium stearate was done for 15 minutes at 20 RPM. Magnesium stearate was added to the mixture and blended for an additional 15 minutes at 20 RPM. The lubricated blend was compressed by a compression machine to form a tablet. The Compressed uncoated tablets are coated in which the coating material is dispersed with purified water in an S.S container under stirring for 45 minutes until the white color suspension is obtained. The tablet is coated at a maximum of 30°C temperature.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Inorganic Chemistry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne un comprimé stable enrobé d'un film, à libération prolongée, à prendre une fois par jour, contenant de la prégabaline ou des sels pharmaceutiquement acceptables de celle-ci, une combinaison d'au moins deux agents retardateurs de libération, un diluant et un lubrifiant. La présente invention assure un taux de libération uniforme du médicament et améliore l'adhésion du patient au traitement en réduisant la fréquence d'administration de médicament.
EP23818075.6A 2022-11-28 2023-11-28 Compositions pharmaceutiques à libération prolongée contenant de la prégabaline ou des sels pharmaceutiquement acceptables de celle-ci Pending EP4626407A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB2217820.6A GB2624861A (en) 2022-11-28 2022-11-28 Sustained release pharmaceutical compositions comprising pregabalin or pharmaceutically acceptable salts thereof
PCT/GB2023/053074 WO2024115889A1 (fr) 2022-11-28 2023-11-28 Compositions pharmaceutiques à libération prolongée contenant de la prégabaline ou des sels pharmaceutiquement acceptables de celle-ci

Publications (1)

Publication Number Publication Date
EP4626407A1 true EP4626407A1 (fr) 2025-10-08

Family

ID=84889643

Family Applications (1)

Application Number Title Priority Date Filing Date
EP23818075.6A Pending EP4626407A1 (fr) 2022-11-28 2023-11-28 Compositions pharmaceutiques à libération prolongée contenant de la prégabaline ou des sels pharmaceutiquement acceptables de celle-ci

Country Status (4)

Country Link
EP (1) EP4626407A1 (fr)
AU (1) AU2023402585A1 (fr)
GB (1) GB2624861A (fr)
WO (1) WO2024115889A1 (fr)

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6197819B1 (en) 1990-11-27 2001-03-06 Northwestern University Gamma amino butyric acid analogs and optical isomers
EP1543831A1 (fr) 2003-12-18 2005-06-22 Pfizer GmbH Arzneimittelwerk Gödecke Composition de pregabaline
NL2000281C2 (nl) 2005-11-02 2007-08-07 Pfizer Prod Inc Vaste farmaceutische samenstellingen die pregabaline bevatten.
WO2009087682A2 (fr) 2007-12-28 2009-07-16 Intas Pharmaceuticals Limited Nouvelle formulation de prégabaline injectable stabilisée
WO2010115612A2 (fr) 2009-04-10 2010-10-14 Synthon B.V. Compositions de prégabaline
KR101317592B1 (ko) * 2009-10-28 2013-10-15 씨제이제일제당 (주) 프레가발린, 폴리에틸렌옥사이드 및 폴리비닐알코올-폴리에틸렌글리콜 그라프트 공중합체를 함유하는 위체류형 서방성 제제
WO2013100874A1 (fr) 2011-12-19 2013-07-04 Mahmut Bilgic Formulation de prégabline effervescente
AU2013213769A1 (en) * 2012-01-30 2014-08-21 Sun Pharmaceutical Industries Limited Gastroretentive tablets
KR102221846B1 (ko) * 2014-04-07 2021-02-26 영진약품 주식회사 안정성이 개선된 프레가발린을 함유하는 약제학적 조성물 및 이의 제조방법
CN106606495A (zh) * 2015-10-27 2017-05-03 四川海思科制药有限公司 一种普瑞巴林缓释片药物组合物及其制备方法
US20210251906A1 (en) * 2018-06-28 2021-08-19 Mylan Inc. Pregabalin extended-release formulations
HUE063492T2 (hu) * 2019-07-03 2024-01-28 Alvogen Inc Szabályozott hatóanyagleadású pregabalin tabletták, azok elõállítása és alkalmazási módszerei
CN113577036B (zh) * 2021-05-31 2023-04-04 石药集团欧意药业有限公司 一种普瑞巴林胃漂浮缓释片及其制备方法
CN114028355A (zh) * 2021-12-09 2022-02-11 南京海京康医药科技有限公司 一种普瑞巴林缓释片及其制备方法

Also Published As

Publication number Publication date
AU2023402585A1 (en) 2025-07-10
GB202217820D0 (en) 2023-01-11
GB2624861A (en) 2024-06-05
WO2024115889A1 (fr) 2024-06-06

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