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WO2016042563A1 - Formulation à libération prolongée de carbamazépine - Google Patents

Formulation à libération prolongée de carbamazépine Download PDF

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Publication number
WO2016042563A1
WO2016042563A1 PCT/IN2014/000598 IN2014000598W WO2016042563A1 WO 2016042563 A1 WO2016042563 A1 WO 2016042563A1 IN 2014000598 W IN2014000598 W IN 2014000598W WO 2016042563 A1 WO2016042563 A1 WO 2016042563A1
Authority
WO
WIPO (PCT)
Prior art keywords
carbamazepine
pharmaceutical composition
release
lubricant
instamodel
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/IN2014/000598
Other languages
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/IN2014/000598 priority Critical patent/WO2016042563A1/fr
Publication of WO2016042563A1 publication Critical patent/WO2016042563A1/fr
Anticipated expiration legal-status Critical
Ceased 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
    • A61K9/205—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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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 Carbamazepine dosage forms and its salts and derivati ves thereof, a process for preparing extended release tablet using IN STAMODEL (A43 D00047) 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 modi fied release compositions capable of regulating release of Carbamazepine at various dosage strength, a process for production thereof and also use thereof as formulated pharmaceutica l compositions.
  • Carbamazepine are indicated for use as an anticonvulsant drug or commonly known as antiepileptic drugs.
  • state of art evidence supporting efficacy of carbamazepine as an anticonvulsant was derived from acti ve drug-controlled studies that enrolled, patients, with the many seizure types namely Partial seizures, Generalized tonic-clonic seizures mixed seizures etc.
  • Partial seizures w ith complex syrnp- tomatology (psychomotor, temporal lobe) , patients with these seizures appear to show greater improvement than those with other types.
  • M i xed seizure patterns which incl ude the above, or other partial or generalized seizures.
  • Carbamazepine is administered through so lid dosage form 200 mg twice a day. Increase at weekly intervals by adding up to 200 mg/day using a thrice a day. or quarter a day. regimen until the optima l response is obta ined.
  • Dosage genera l ly shou ld not exceed 1000 mg daily in children 1 2 to 1 5 years of age, and 1 200 mg dai ly in patients above 1 5 years of age.
  • Carbamazepine is poorly soluble in water leading io erratic dissolution, oral absorption and therefore poor bioavailabil ity (less char 70% ) is olso observed.
  • Carbamazepine is a BCS Class-Il drug (Biopharmaceutical Classification System) i.e. Low solubility and H igh permeabi l ity and it is the most widely used as anticonvulsant, anti-epileptic and anti-neuralgic drag. Further as Carbamazepine. has poor solubility in water it leads to erratic d issol ution, on:!
  • modified release compositions are developed to provide relatively constant drug plasma levels and sustained efficacy for longer period of time.
  • extended 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.
  • 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 Carbamazepine.
  • the object of the present invention is to provide a ready-to-use matrix system and method of preparation for Carbamazepine extended release or modified release for- mulation.
  • the present invention provides hydrophilic matrix system based ready to use technology for Modified or Extended Release Formulation of Carbamazepine Hydrochloride using INSTAMODEL (A43 D00047) manufactured and supplied by Ideal Cures Private Limited.
  • the present invention also provides method for making ready to use Carbamazepine modified or extended release formulation, involving steps of aqueous granulation,, drying, lubrication and punching of tablets.
  • present invention also provides once a day Carbamazepine table dosage form.
  • Extended release or modified release tablet formulation cars 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.
  • composition according to the invention in the context of the 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 dispersi ng it in required quantity of water.
  • 'modified release' is in context, of the invention as a way -of active drug delivery where the rate of release of the active drug from the composition i s not ex clusively dependent on the concentration of active drug remaining in the dosage form and / or the solubility of the active drug in the liquid surrounding thexomposiiion, and where the time course with or without respective location of release of active drug from an oral dosage form are chosen to accomplish therapeutic or convenience objectives not offered by conventional dosage forms.
  • active drug is selected from Carbamazepine, its intermediates and deri vati ves thereo f
  • 'Carbamazepine' is in context of the invention includes its polymorphic forms, the pharmaceutically acceptable salts, inc luding salts esters and pother chemical derivatives or intermediates etc.
  • the solid pharmaceutical composition comprises Carbamazepine from 1 to 80 w/w % of dosage form.
  • the term 'dosage', 'solid pharmaceutical composition' may include one -or more of tablet, capsule, powder, disc, caplet, granules, pellets, granules in capsule, minitablets, minitablets in capsule, pellets in capsule, sachet and the like.
  • the solid pharmaceutica l composition also includes multilayer tablets. The solid pharmaceutical compositions are meant for oral administration.
  • tablette includes pharmaceutical compositions of all shapes and sizes, whether coated or uncoated.
  • Lubricant of present invention includes but not limited to talc, magnesium stearate, stearic acid, sodium stearyl fumarate and there derivatives thereof.
  • Glidant in the context of the present invention, is taken to mean that an ingredient which enhance product flow by reducing inter-particulate friction.
  • Glidant can be used in present invention includes but not limited to silicon di-oxide, colloidal silicon dioxide and there derivatives thereof. It is available under several brand names 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, efhanol, methylene di chloride, isopropyl alcohol, water or their mixture thereof.
  • Solvent can be used in present invention includes but not l imited to polyvinyl polymers, Polyvinyl pyrrolidone K30 (PVP K30) and there derivatives thereof.
  • the ready to use composition in accordance, with present invention comprise INSTAMODEL (A43 D00047).
  • Carbamazepine is formulated with ready to use composition to prepare modified release dosage form.
  • di fferent salts, derivatives, polymorphs of Carbamazepine could be combined to achieve ready-to-use composition to achieve extended or modified release dosage form.
  • Carbamazepine is blended with the ready to use polymer and aqueous granulated further the granu lated mix ture 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.
  • Carbamazepine. and INS TAMODEL 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 finally coated.
  • Carbamazepine 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.
  • This system of formulation uses simple and economic polymers hence, cost effective to the customer.
  • Another advantage of the present formulation is its robust and reproducible results for extended release dose form without batch to batch variations. Further by using aqueous solvent system for granulation dosage form does not have any residual solvent or hazardous effect found in many organic solvent based formulations.
  • Inventive dosage form may be prepared by blending Carbamazepine, 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 A43D00047), process blending is performed by , conventional dry blender or a food processor or 'V-blender' or a similar function device. Further Carbamazepine are processed using aqueous sol vent with binder through wet granulation or a similar wet mixing method to generate dosage formulation . Dosage formulation is further dried, sieved and compressed optional ly with addition of lubricant, binder, glidant to form modified release oral dosage form.
  • inventive dosage formulations are prepared by blending Carbamazepine along with Instamodel (A43 D00047). I nitial ly all components are blended by conventional dry blending in a food processor or 'V- b!ender' 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 pharmacopoeial equipment to get a controlled release oral dosage formulation of the correct desi red weight and strength.
  • hardness of tablets produced is in range of 7 Kg/cm 2 to 15 Kg/cm 2 .
  • oral dosage forms produced by inventive composition having human administrate active ingredient is suitable for human use.
  • drug suitable for veterinary purpose formulated in accordance with present composition will be suitable for veterinary use.
  • Carbamazepine is formulated in oral dosage form for modified or extended release delivery.
  • Inventive composition comprises 50, 100, 200, 300 mg or 500 mg of Carbamazepine in plural ity of dosage formulations.
  • 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-cholin-esterase 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 of steroid Type II 5[alpha]- reductase including; lipid regulating agents; selecti ve H l - receptor antagonist; vasodilator; vitamins.
  • the dosage formulation for 100,000 (30.00 kg) Tablets of Carbamazepine is prepared using composition as stated in table:- 1 wherein Carbamazepine is 20.0 kg and weighed accordingly, subsequently sieved to get uniformly granu lated powder through 40 mesh scree,. It is noted that other size screen could be used to get simi lar results.
  • Sieved Carbamazepine is blended with 7.90 kg of ready to use I nstainodel (A43D00047) in blender for 20 minutes (e.g. RMG granulator).
  • Solvent system for wet granulation is prepared by taking 1.2 kg PVP K -30 in 5 kg of water , in RMG granulator in low to medium speed in the duration of 10 minutes followed by 5 minutes of high speed with chopper.
  • tray drier or Fluidized bed dryer
  • coating suspenstion is prepared in water with sti rrer and mixed for about 45 minutes
  • Coated tablets are then dried and packed as per pharmacopoieal guidelines.
  • the active ingredient content for present invention is standardized for m sustained release profile is as per table 2
  • the drug dissolved profile o f the Reference products and Carbamazepine hav ing dose strength of 200 mg using Instarnodel (A43D00047) formulations are compared:
  • the release exponents for the Reference and formulated Carbamazepine is found to be having similar modified release profile indicating a predoin inan tiy di ffusion based drug release mechanism.

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

Abstract

La présente invention concerne une formulation galénique à libération modifiée sèche prête à l'emploi pour les formes galéniques de carbamazépine et 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 de carbamazépine à diverses concentrations de dose, un procédé pour les produire et leur utilisation en tant que compositions pharmaceutiques formulées.
PCT/IN2014/000598 2014-09-16 2014-09-16 Formulation à libération prolongée de carbamazépine Ceased WO2016042563A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
PCT/IN2014/000598 WO2016042563A1 (fr) 2014-09-16 2014-09-16 Formulation à libération prolongée de carbamazépine

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/IN2014/000598 WO2016042563A1 (fr) 2014-09-16 2014-09-16 Formulation à libération prolongée de carbamazépine

Publications (1)

Publication Number Publication Date
WO2016042563A1 true WO2016042563A1 (fr) 2016-03-24

Family

ID=55532648

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2014/000598 Ceased WO2016042563A1 (fr) 2014-09-16 2014-09-16 Formulation à libération prolongée de carbamazépine

Country Status (1)

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WO (1) WO2016042563A1 (fr)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030175353A1 (en) * 2002-03-14 2003-09-18 Sun Pharmaceutical Industries Limited Oral controlled drug delivery system
US20070071819A1 (en) * 2005-05-30 2007-03-29 Kesarwani Amit K Multiple unit modified release compositions of carbamazepine and process for their preparation

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030175353A1 (en) * 2002-03-14 2003-09-18 Sun Pharmaceutical Industries Limited Oral controlled drug delivery system
US20070071819A1 (en) * 2005-05-30 2007-03-29 Kesarwani Amit K Multiple unit modified release compositions of carbamazepine and process for their preparation

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