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WO2016042564A1 - Formulation à libération prolongée d'acéclofénac - Google Patents

Formulation à libération prolongée d'acéclofénac Download PDF

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Publication number
WO2016042564A1
WO2016042564A1 PCT/IN2014/000599 IN2014000599W WO2016042564A1 WO 2016042564 A1 WO2016042564 A1 WO 2016042564A1 IN 2014000599 W IN2014000599 W IN 2014000599W WO 2016042564 A1 WO2016042564 A1 WO 2016042564A1
Authority
WO
WIPO (PCT)
Prior art keywords
aceclofenac
pharmaceutical composition
solid pharmaceutical
instamodel
lubricant
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.)
Ceased
Application number
PCT/IN2014/000599
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English (en)
Inventor
Suresh Pareek
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.)
Individual
Original Assignee
Individual
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 Individual filed Critical Individual
Priority to PCT/IN2014/000599 priority Critical patent/WO2016042564A1/fr
Publication of WO2016042564A1 publication Critical patent/WO2016042564A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
    • 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

Definitions

  • the present invention relates to a dry ready to use modified release dosage formulation for Aceclofenac dosage forms and its salts and derivatives thereof, a process for preparing extended release tablet using INSTAMODEL (A43D00045) manufactured by Ideal Cures Private Limited Mumbai India thereof also use thereof as additive to animal feeds, foods and food supplements and also cosmetic and pharmaceutical compositions.
  • Invention also relates to ready-to-use modified release compositions capable ofregulating release of Aceclofenac at various dosage strength, a process for production thereof and also use thereof as formulated pharmaceutical compositions.
  • Aceclofenac are indicated for use as non-steroidal anti-inflammatory drug (NSA1D).
  • NSA1D non-steroidal anti-inflammatory drug
  • Aceclofenac is the glycolic acid ester of diclofenac. It is used for the relief of pain and inflammation in rheumatoid arthritis, osteoarthritis.and ankylosing spondylitis.
  • Aceclofenac has higher anti-inflammatory action than conventional NSAIDs. It is a cytokine inhibitor.
  • Aceclofenac works by blocking the action of a substance in the body called cyclo-oxygenase. Cyclo-oxygenase is involved in the production ofprostaglandins (chemicals in the body) which cause pain, swelling and inflammation.
  • Aceclofenac is known for Anti-inflammatory and Analgesic action. It is poorly soluble in water leading to erratic dissolution, oral absorption and therefore poor bioavailability is also observed.
  • Aceclofenac is administered through solid dosage ranges from 100 mg to 200 mg daily. In standard doses of 200 mg is taken in two equally divided doses , one tablet in the morning and one tablet in the evening . Prescription of Aceclofenac recommend that it should be taken with meals if possible and daily. Dosage generally should not exceed 200 mg daily.
  • Aceclofenac is poorly soluble in water leading to erratic dissolution, oral absorption and therefore poor bioavailability (less than 70%) is also observed.
  • Aceclofenac is a BCS Class-II drug (Biopharmaceutical Classification System) i.e. Low solubility and High permeability. Further as Aceclofenac has poor solubility in water, it leads to erratic dissolution, oral absorption and therefore poor bioavailability.
  • modified release compositions are developed to provide relatively constant drug plasma levels and sustained efficacy for longer period of time.
  • aim ofextended and modified release composition is to get required therapeutic concentration of the active in the blood stream and maintain its therapeutic concentration without deviation from strength during specified period.
  • Prior art documents disclosing such extended release compositions of aceclofenac are WO 2010090371, WO 2012141502, IN 223582 and 998/DEL/2008.
  • cellulosic polymers are used in the modified release compositions e.g. HPMC polymer. These polymers extend the release ofdaig by showing osmosis nature in aqueous conditions.
  • Cellulosic matrix based system work by the swelling and gelling function i.e. these polymer swell through influx of liquids and a gel like physical structure is formed which provides extended release effect facilitated by diffusion of the Aceclofenac.
  • the object of the present invention was to provide a ready-to-use matrix system and method ofpreparation for Aceclofenac extended release or modified release formulation.
  • the present invention provides hydrophilic matrix system based ready to use technology for Modified or Extended Release Formulation of Aceclofenac .Hydrochloride: using INSTAMODEL ( A43D00045) manufactured by ideal Cures Private Limited Mumbai India.
  • the present invention also provides method for making ready to use Aceclofenac modified or extended release formulation, involving steps of aqueous granulation, drying, lubrication and punching of tablets.
  • present invention also provides Once a day Aceclofenac table dosage form
  • Extended released or modified release tablet formulation can be in the form of single or multilayer tablets, capsule ,shaped oral dosage form,caplet, granules, disc, pellets, granules in capsule, mini-tablets in oral dosage form and other possible oral dosage form mean thereof.
  • the solid oral dosage form can optionally include one or more pharmaceutically acceptable excipients.
  • the feature 'ready-to-use' in the context ofthe present invention, is taken to mean the property that the composition according to the invention can be used directly for its purposes by the user by simply dispersing it in required quantity ofwater.
  • 'modified release' is in context ofthe invention as a way ofactive drug delivery where the rate ofrelease ofthe active drug from the composition is not exclusively dependenton the concentration ofactive drug remaining in the dosage form and /or the solubility ofthe active drug in the liquid surrounding the composition, and where the time course with or.without respective location ofrelease ofactive drug from an oral dosage form are chosen to accomplish therapeutic crconvenience objectives not offered by conventional dosage forms.
  • active drug is selected.from Aceclofenac, its intermediates and derivatives thereof,
  • 'Aceclofenac' is in context ofthe invention includes its polymorphic forms, the pharmaceutically acceptable salts, including salts esters and pother chemical derivatives-or intermediates etc
  • the solid pharmaceutical,composition comprises Ace clofeuac from I to 80 w/w % ofdosage form.
  • the term 'dosage', 'solid pharmaceutical composition' may. include one or more of tablet, capsule, powder, disc.caplet, granules, pellets, granules in capsule,niinitablets, minitablets in capsule, pellets in capsule, sachet and the like.
  • the solid pharmaceutical composition also includes multilayer tablets. The solid pharmaceutical compositions are meant fororal administration. .
  • tablette includes pharmaceutical compositions ofall shapes and sizes, whethercoatedor uncoated.
  • Lubricant ofpresent invention includes but not limited to talc, magnesium stearate;stearic acid, sodium stearyl fumarate and there derivatives thereof.
  • Glidant' in the context ofthe presentinvention, js.taken tomean that an ingredient which enhance product flow by reducing inter-panjcujale friction, Glidant can be used in present invention includes but not limited to silicon di-oxide, colloidal, silicon dioxide and there derivatives thereof. Itis available under several brandnames like AEROSIL® and CAB-O-SIL®.
  • Solvent in the context of the present invention, is taken to mean ingredient that facilitate mixing of components in wet granulation process.
  • Solvent can be used in present invention includes but not limited to Acetone, ethanol, methylene di chloride, isopropyl alcohol, water or their mixture thereof.
  • Solvent can be used in present invention includes but not limited to dextrin and their derivatives, maltodextrin, polyvinyl polymers, Polyvinyl pyrrolidone KL30 (PVP K30) and there derivatives thereof.
  • the ready to use composition in accordance with present invention comprise INSTAMODEL. (A43D00045).
  • Aceclofenac is formulated with ready to use composition to prepare modified release dosage form.
  • different salts, .derivatives, polymorphs of Aceclofenac could be .combined to achieve -ready-to use composition to achieve extended or modified release dosage form.
  • Aceclofenac is blended with the- ready to use polymer and aqueous granulated further the granulated mixture is compressed to produce a solid formulation.
  • the ingredients are blended to form a- uniform powder and then compressed with means generally known to skilled in the art.
  • Aceclofenac and I NSTAMODEL are blended together with binding agent and thereafter wetgranulated and dried. These dried, granules are then processed in presence of lubricant and glidant, and thereafter compressed to ..form, appropriate, dosage form and finally coated.
  • Aceclofenac and, INSTAMODEL. are blended together with binding agent and thereafter wet granulated and dried. These dried granules, are then processed in presence of lubricant and glidant, and thereafter compressed to form appropriate dosage form and optionally coated.
  • inventive dosage form may be prepared by blending Aceclofenac, their derivatives or combination thereof along with ready to use composition. Therefore inventive formulation preparation comprise steps as:-
  • inventive dosage form is prepared by blending ready to use composition ( Instamodel A43D00045),.
  • process blendi ng is performed by conventional dry blender or a food processor or 'V-blender' or a similar function device.
  • Further Aceclofenac are processed using aqueous solvent with binder through wet granulation or a similar wet mixing method to generate dosage formulation.
  • Dosage formulation is further dried, sieved and compressed optionally with addition of lubricant, binder, glidant to form modified release oral dosage form.
  • inventive dosage formu lations are prepared by blending Aceclofenac along with Instamodel (A43D00045). initially all components are blended by conventional dry blending in a food processor or 'V- blender' or a similar function device. Other solid oral dosage formulation components like binders, lubricants, glidants, detackifier, excipients can be added to create inventive formulation. Further mixture is then processed with appropriate quantity of aqueous solvent with, binder and wet granulated. Obtained sieved granulated is then uniformly mixed with premeasured amount of the lubricant to improve industrial acceptability and oral dosage compression quality. Subsequently uniform mixed inventive, formulation is compressed in standard pharmaeopoeial. equipment to get a controlled release oral dosage formulation. of the correct desired weight and strength.
  • hardness. of tablets produced is in range of 7 Kg/cm 2 to 15 Kg/cm 1 .
  • oral dosage forms produced by inventive composition having human administrable active ingredient is suitable for human use.
  • drug suitable for veterinary purpose formulated in accordance, with present composition will be suitable for veterinary use.
  • Aceclofenac is formulated in oral dosage form for modified or extended release delivery.
  • Inventive composition comprising 50 to 300 mg or 200 mg of Aceclofenac in plurality of dosage for- mulations.
  • Controlled release formulation can have combination of one or more additional drugs.
  • Suitable APIs that can be used with the present invention include, but are not limited to: andrenergic blocking agent; acetyl-choliivesterase inhibitor;,analgesic or antipyretics; angiotensin modulator; anthelmintic agents; anti anxiety agent; antibacterial; antibiotic; anticoagulant; anticonvulsant; antidepressant; antifungal; antihistamine; antimalarial; antimicrobial agent; antipsychotic agent; Antiviral agents; blood glucose lowering drug; calcium channel modulator; diuretic; erectile dysfunction; gastric acid secretion inhibitor; histamine H2-receptor antagonist; inhibitor o steroid Type II 5[alpha]- reductase including; lipid regulating agents; selective H1- receptor antagonist; vasodilator; vitamins.
  • andrenergic blocking agent include, but are not limited to: andrenergic blocking agent; acetyl-choliivesterase inhibitor;,analgesic or antipyretics; angiotensin modul
  • the dosage formulation for 100,000 (28.00 kg) Tablets of Aceclofenac is prepared using composition as stated in table:- 1 wherein Aceololenac is 20.0 kg and 6.5 kg of Instamodel (A43D00045) are weighed, sifted in rapid mixture granulator accordingly, subsequently sieved to get uniformly granulated powder through 40 mesh screen. It is noted that other size screen could be used to get similar results. Sieved Aceclofenac with above ingredients is granulated using 5.5 kg of water and 1.0 kg of binder (PVPK-30) as granulating solvent in rapid mixture granulator (RMG) .
  • PVPK-30 binder
  • RMG rapid mixture granulator
  • RMG should be at slow speed for 15 min followed by high speed for 3-5 mms (Total qty of water used approx.5-6 kg).
  • Granulation step requires proper op tirnization of water quantity and continuous monitoring to avoid heavy granulation. If required extra water can be added gradually under continuous observation (to avoid heavy wet mass). Generated wet mass is sieved using #20 mesh screen (Multi-mil!/ Fitzmill) dried.in tray drier (or Fluidized bed dryer) at temperature not more than 50°C-55°C keeping loss on drying. at 1-2%.
  • Coating is preformed on dosage form using INSTACOAT Pharma RnD coaler (6' pan) at 25 rpm with inlet temperature being 53 °C and.bed temperature at 40 °C. coating was done using 1mm nozzle sprayer with peristaltic pump injecting coating suspension at the rate of1ml/min. Coated tablets are then dried and packed as perphamacopoieal guidelines.
  • Aceclotenac dose form dissolution studv was performed.
  • Drugdissolution profiles of tablet prepared are measured by USP 35 dissolution test of rotating basket method ⁇ 71 1>. It is evident from standard state of the art that active ingredient may have its own dissolution testing parameters which can be found in their respective monographs.
  • the active ingredient content for present invention is standardized for sustained release profile is as per table 2:-
  • Time interval 1 , 4, 10, 16, 20 hour
  • IJV- VIS Spectrophotometer UV 2700- Thermo Fisher Scientific.
  • the drug dissolved profile of the Reference producls and Aceclofenac ha ving dos strength of 200 mg using Instamodel (A43D00045) formulations are compared.
  • the release exponents for the Reference and formulated Aceclofenac is found to be having similar modified release profile indicating a predominantly diffusion based drug release mechanism.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Emergency Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne une formulation galénique à libération modifiée sèche prête à l'emploi pour les formes galéniques d'acéclofénac et de ses sels et dérivés, un procédé de préparation de comprimé à libération prolongée en utilisant de l'INSTAMODEL (A43D00045) fabriqué par Ideal Cures Private Limited Bombay Inde ainsi que son utilisation comme additif à des aliments pour animaux, des aliments et des compléments alimentaires, ainsi que des compositions cosmétiques et pharmaceutiques. L'invention concerne également des compositions à libération modifiée prêtes à l'emploi capables de réguler la libération d'acéclofénac à diverses concentrations de dose, un procédé pour les produire et leur utilisation en tant que compositions pharmaceutiques formulées.
PCT/IN2014/000599 2014-09-16 2014-09-16 Formulation à libération prolongée d'acéclofénac Ceased WO2016042564A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
PCT/IN2014/000599 WO2016042564A1 (fr) 2014-09-16 2014-09-16 Formulation à libération prolongée d'acéclofénac

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/IN2014/000599 WO2016042564A1 (fr) 2014-09-16 2014-09-16 Formulation à libération prolongée d'acéclofénac

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WO2016042564A1 true WO2016042564A1 (fr) 2016-03-24

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Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011152652A2 (fr) * 2010-06-01 2011-12-08 한국유나이티드제약 주식회사 Préparation d'acéclofénac à libération lente présentant un effet clinique pharmacologique optimal lorsqu'elle est administrée une fois par jour

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011152652A2 (fr) * 2010-06-01 2011-12-08 한국유나이티드제약 주식회사 Préparation d'acéclofénac à libération lente présentant un effet clinique pharmacologique optimal lorsqu'elle est administrée une fois par jour

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
GHOSH S. ET AL.: "Formulation and in Vitro Evaluation of Once Daily Sustained Release Formulation of Aceclofenac", TROPICAL JOURNAL OF PHARMACEUTICAL RESEARCH, vol. 9, no. 3, June 2010 (2010-06-01), pages 265 - 273 *
GHOSH S. ET AL.: "Preparation and evaluation of aceclofenac sustained release formulation and comparison of formulated and marketed product.", INTERNATIONAL JOURNAL OF MEDICINE AND MEDICAL SCIENCES, vol. 1, no. 9, September 2009 (2009-09-01), pages 375 - 382, XP055108024 *
SUBRAMANIAM K. ET AL.: "Formulation and Evaluation of Sustained Release Tablets of Aceclofenac using Hydrophilic Matrix System.", INTERNATIONAL JOURNAL OF PHARMTECH RESEARCH, vol. 2, no. 3, September 2010 (2010-09-01), pages 1775 - 1780 *

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