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WO2024115889A1 - 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 Download PDF

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Publication number
WO2024115889A1
WO2024115889A1 PCT/GB2023/053074 GB2023053074W WO2024115889A1 WO 2024115889 A1 WO2024115889 A1 WO 2024115889A1 GB 2023053074 W GB2023053074 W GB 2023053074W WO 2024115889 A1 WO2024115889 A1 WO 2024115889A1
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Prior art keywords
sustained release
pregabalin
release film
coated tablet
pharmaceutically acceptable
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Ceased
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PCT/GB2023/053074
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Inventor
Hetalbahen PATEL
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Orbit Pharma Ltd
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Orbit Pharma Ltd
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Priority to AU2023402585A priority Critical patent/AU2023402585A1/en
Priority to EP23818075.6A priority patent/EP4626407A1/fr
Publication of WO2024115889A1 publication Critical patent/WO2024115889A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • 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
    • 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
    • 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

  • compositions comprising pregabalin or pharmaceutically acceptable salts thereof
  • the present invention relates to a pharmaceutical composition of Pregabalin.
  • the present invention relates to a sustained release film-coated tablet of Pregabalin or pharmaceutically acceptable salts thereof, suitable for once-daily oral administration.
  • the present invention also relates to the process of the preparation of the same.
  • Pregabalin was first disclosed in the U.S. Pat. No. 6,197,819.
  • Pregabalin is also called P-isobutyl-y-aminobutyric acid or isobutyl-GABA.
  • Pregabalin is a structural derivative of the inhibitory neurotransmitter GABA, however, it does not bind to GABAA, GABAB, or benzodiazepine receptors and does not enhance GABAA responses in cultured neurons.
  • Pregabalin enhances the density of GABA transporter protein and increases the rate of functional GABA transport in cultured neurons when it is administered for a prolonged period of time. When the concentration of GABA diminishes below a threshold level appears to terminate seizures.
  • Pregabalin inhibits the calcium-dependent release of pro-nociceptive neurotransmitters in the spinal cord, possibly by interfering with the movement of calcium channels that contain alpha2-delta and reducing calcium currents.
  • the antinociceptive effects of pregabalin may interact with descending noradrenergic and serotonergic pathways, which originate in the brainstem and influence spinal cord pain transmission, pregabalin is indicated for the treatment of postherpetic neuralgia, fibromyalgia, and as adjunctive therapy for the treatment of partial-onset seizures in adults. It is also indicated for the management of neuropathic pain related to spinal cord injury and diabetic peripheral neuropathy or generalized anxiety disorder.
  • 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.
  • WO 2013/100874 Al discloses an effervescent powder, tablet, and granule comprising of pregabalin and at least one pharmaceutically acceptable excipient selected from the effervescent couple, flavoring agent, binder, lubricant, sweetener, and taste regulating agent.
  • the effervescent formulation was prepared by the wet granulation method. The process of this invention involves mixing a binder, solvent, and active agent to prepare a granulation solution. Mix pregabalin with another pharmaceutically acceptable excipient. Wet granulating the mixture with the granulation solution and then granules are dried and sieved. The granules are compressed into a tablet, bottle-filled, or sachet filled to produce the specified dosage form.
  • US 2005/0171203A1 discloses the oral liquid pharmaceutical composition of pregabalin contains at least each preservative, taste-masking agent, and viscositycontrolling agent.
  • the process involves adding sterile water to a vessel and then the contents of the vessel are heated to 80° C. Methylparaben and ethylparaben is stirred into the hot water. After a clear solution is obtained, Sodium Saccharin and hydroxyethylcellulose are added. The resulting liquid mixture is cooled to 30°C.
  • the pregabalin and flavoring agent are added in small portions with Stirring.
  • the solution is filtered using a Millipore (R) membrane filter and Stored in Sealed containers.
  • WO 2009/087682A2 discloses an injectable formulation of pregabalin which is stable between pH 4.0 to 8.0. The process involves taking water for injection into an SS container and sparge with 0.2p filtered nitrogen until the level of dissolved oxygen falls below 1 ppm. Dissolve sodium chloride, citric acid monohydrate, and pregabalin with continuous nitrogen sparging. Make up the volume with nitrogen- sparged water for injection. Filter the bulk solution through a 0.2 p polyvinylfluoridine filter by using nitrogen gas. Fill the filtered bulk solution into 5ml clear glass USP type 1 ampoules.
  • 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 present invention provides a sustained release film-coated tablet containing pregabalin or pharmaceutically acceptable salts thereof, that is useful for once-daily (QD) oral dosing. While it is retained in the stomach, the tablet continuously releases pregabalin.
  • QD once-daily
  • Another embodiment of the present invention provides a sustained release film- coated tablet containing pregabalin or pharmaceutically acceptable salts thereof, and the excipients include at least two release retarding agents, a diluent, and a lubricant.
  • another embodiment of the present invention involves a process for preparing the sustained release film-coated tablet for oral administration.
  • Another embodiment of the present invention can effectively treat postherpetic neuralgia, fibromyalgia, and as adjunctive therapy for the treatment of partial-onset seizures in adults. It is also indicated for the management of neuropathic pain related to spinal cord injury and diabetic peripheral neuropathy.
  • 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.
  • Another object of the present invention is to provide a therapeutically effective amount of pregabalin or pharmaceutically acceptable salts thereof, hydroxy ethyl cellulose, carbomer (Carbopol 71G), and a combination of polyvinyl acetate, povidone, sodium lauryl sulphate, and silica (kollidon SR) as release retarding agents, and one or more pharmaceutically acceptable excipients.
  • a further object of the present invention relates to the sustained release film-coated tablet preparation of pregabalin or pharmaceutically acceptable salts thereof, for oral administration once-daily, reducing administration times, and having pharmacokinetic properties of reducing side effects while increasing patient compliance and extending the efficacy time duration.
  • Yet another object of the present invention provides taste-masking properties such that the administration of the sustained release film-coated tablet is not unpleasant for elderly patients.
  • 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.
  • Sustained release drug delivery improves patient compliance by reducing the frequency of drug administration, reducing steady-state fluctuation of drug levels, increasing the safety margin of low therapeutic index drugs, maximizing the utilization of the drug, lowering healthcare costs through improved therapy, and shortening the treatment regimen.
  • Sustained release dosage forms provide sustained drug levels in plasma that frequently eliminate the need for night dosing, which is beneficial for patient compliance.
  • 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.
  • the composition comprises a diluent selected from dextrates, microcrystalline cellulose, dextrose, fructose, Sorbitol, pregelatinized starch, xylitol, sucrose, maltodextrin, maltose, mannitol or combinations thereof.
  • 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.
  • mannitol in the development of tablets, the use of mannitol as a filler has increased due to its physicochemical properties, such as its lower hygroscopicity, chemical inertness, and advantageous tableting behavior, including compactability and the ability to produce extremely robust tablets.
  • the composition comprises a release retarding agent selected from the group consisting of hydroxypropyl methylcellulose, hydroxyethyl methylcellulose, hydroxypropyl cellulose, hydroxymethyl cellulose, Hypromellose, Hypromellose acetate succinate, hydroxyethyl cellulose, carboxymethyl cellulose, cellulose acetate, cellulose acetate phthalate, calcium carboxymethyl cellulose, sodium carboxymethyl cellulose, methylcellulose, ethylcellulose, chitosan, gelatin, poloxamer, polyvinyl alcohol, polyvinyl acetate phthalate, polyethylene glycol, polyvinyl pyrrolidone-polyvinyl acrylate copolymer, polyvinyl alcoholpolyethylene glycol copolymer, polyvinyl pyrrolidone-polyvinyl acetate copolymer, kollidon SR, hydroxypropyl starch, magnesium aluminium silicate, polydextrose, poly
  • hydroxyethyl cellulose, carbomer (Carbopol 71G), and the combination of polyvinyl acetate, povidone, sodium lauryl sulphate, and silica (kollidon SR) is preferred as a release retarding agent present in the range of about 2%w/w to about 80 %w/w, preferably in the range from about 4%w/w to about 75 %w/w.
  • Hydroxyethyl cellulose is present in the range from about 4 %w/w to about 40 % w/w, preferably from about 8% w/w to about 20 % w/w
  • carbomer Carbopol 71G
  • Carbopol 71G is present in the range from about 1 %w/w to about 10 % w/w, preferably from about 4 %w/w to about 8 % w/w.
  • a combination of polyvinyl acetate, povidone, sodium lauryl sulphate, and silica (kollidon SR) is present in the range from about 5 %w/w to about 65 % w/w, preferably from about 9%w/w to about 50 % w/w.
  • a release retarding agent refers to those substances that retard or delay the release of a drug and provide a longer duration of therapeutic response after administration of the dosage form.
  • at least one further pharmaceutically acceptable excipient is a lubricant selected from boric acid, magnesium stearate, Sodium Stearyl fumarate, micronized polyoxy ethylene glycol, leucine, sodium benzoate, sodium acetate, sodium lauryl sulphate, steric acid, sodium stearate, sodium oleate, calcium stearate, waxes or combinations thereof.
  • 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.
  • the pregabalin sustained release film-coated tablet may further comprise a film coating material such as vinyl polymers like polyvinylpyrrolidone, polyvinyl alcohol and acetate, cellulosics such as methyl and ethyl cellulose, hydroxyethyl cellulose, hydroxypropyl methylcellulose, hydroxypropyl cellulose, acrylates and methacrylates, copolymers such as the vinyl-maleic acid and styrene-maleic acid, and natural gums and resins such as zein, gelatin, shellac, acacia or combinations thereof.
  • a film coating material such as vinyl polymers like polyvinylpyrrolidone, polyvinyl alcohol and acetate, cellulosics such as methyl and ethyl cellulose, hydroxyethyl cellulose, hydroxypropyl methylcellulose, hydroxypropyl cellulose, acrylates and methacrylates, copolymers such as the vinyl-maleic acid and s
  • the preferred embodiment of the present invention is to provide a stable once-daily Sustained release film-coated tablet of pregabalin or pharmaceutically acceptable salts thereof, and the excipients include hydroxy ethyl cellulose, carbomer (Carbopol 71G), and a combination of polyvinyl acetate, povidone, sodium lauryl sulphate, and silica (kollidon SR) as release retarding agents.
  • the Sustained release film-coated tablet further comprises at least one pharmaceutically acceptable excipient selected from a diluent and lubricant.
  • 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.
  • the present invention comprising pregabalin or pharmaceutically acceptable salts thereof, present in an amount from about 20 %w/w to about 80 %w/w, preferably in the range of about 30 %w/w to about 50 %w/w, the release retarding agent such as hydroxy ethylcellulose is present in the range from about 4 %w/w to about 40 % w/w, preferably from about 8% w/w to about 20 % w/w, carbomer (Carbopol 71G) is present in the range from about 1 %w/w to about 10 % w/w, preferably from about 4 %w/w to about 8 % w/w.
  • the release retarding agent such as hydroxy ethylcellulose
  • carbomer Carbopol 71G
  • 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.
  • 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 is present in an amount of about 165 mg, about 330 mg, or about 660 mg per tablet.
  • 80 % of the pregabalin is released in 24 hours, preferably more than 90 % is released within 24 hours.
  • 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 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.
  • the Sustained release film-coated tablet was made according to the method defined below using the formulation having the ingredients shown in table I:
  • 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 is compressed to form tablets.
  • 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:
  • the Sustained release film-coated tablet was prepared according to the procedure described below using the formulation having the ingredients shown in table IV: TABLE-IV
  • 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.
  • Example 5 The tablet prepared according to example 4 was subjected to a stability study of 40°C ⁇ 2°C/75%RH ⁇ 5%RH for 1 month. Results are tabulated below.

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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.
PCT/GB2023/053074 2022-11-28 2023-11-28 Compositions pharmaceutiques à libération prolongée contenant de la prégabaline ou des sels pharmaceutiquement acceptables de celle-ci Ceased WO2024115889A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2023402585A AU2023402585A1 (en) 2022-11-28 2023-11-28 Sustained release pharmaceutical compositions comprising pregabalin or pharmaceutically acceptable salts thereof
EP23818075.6A 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

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
GB2217820.6 2022-11-28

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US6197819B1 (en) 1990-11-27 2001-03-06 Northwestern University Gamma amino butyric acid analogs and optical isomers
US20050171203A1 (en) 2003-12-18 2005-08-04 Pfizer Inc. Pregabalin composition
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WO2010115612A2 (fr) 2009-04-10 2010-10-14 Synthon B.V. Compositions de prégabaline
WO2013100874A1 (fr) 2011-12-19 2013-07-04 Mahmut Bilgic Formulation de prégabline effervescente
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