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WO2016042568A1 - Formulation à libération prolongée de gliclazide - Google Patents

Formulation à libération prolongée de gliclazide Download PDF

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Publication number
WO2016042568A1
WO2016042568A1 PCT/IN2014/000603 IN2014000603W WO2016042568A1 WO 2016042568 A1 WO2016042568 A1 WO 2016042568A1 IN 2014000603 W IN2014000603 W IN 2014000603W WO 2016042568 A1 WO2016042568 A1 WO 2016042568A1
Authority
WO
WIPO (PCT)
Prior art keywords
gliclazide
solid pharmaceutical
release
pharmaceutical composition
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/IN2014/000603
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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/IN2014/000603 priority Critical patent/WO2016042568A1/fr
Publication of WO2016042568A1 publication Critical patent/WO2016042568A1/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
    • A61K9/2004—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
    • A61K31/64—Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide

Definitions

  • the present invention relates to a dry ready to use modified release dosage for- mulation for Gliclazide dosage forms and its sai ls and derivatives (hereof, a process for preparing extended release tablet using INSTAMODEL (A43D00048) 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 coin- positions.
  • Invention also relates to ready-to-use modified release compositions capable of regulating release of gliclazide at various dosage strengths , a process for production thereof and also use thereof as formulated pharmaceutical composi tions.
  • Gliclazide are indicated for use as a hypo -glycaem ic drug or commonly known as anti-diabetic drug . In stave of art it is classified as a sulfonylurea . Gliclazide is a white or almost white powder which is practically in»oiobit:,i n water. The solubility in water increases with increase in pH. It belongs to class H of the biophar- maceutical classification (BCS) in which dissol ution rate is the controlling step . in. drag absorption. In general m inor changes within a pH range of from 5.8 to 8 can alter the solubility of Gliclazide. The characteristic of pH dependent solubility causes the ab- sorption problems for the active ingredient, Gliclazide between pH 6.2 and 7.4 has been controlled by the characteristic combination of polymer and glucose syrup m tablet composition.
  • BCS biophar- maceutical classification
  • Gliclazide is administered through solid dosage ranges- from SO mg to 320 mg dai ly. In standard doses of 1 60 mg and above should be taken m t wo equal ly di vided doses. Prescription of gliclazide recommends that it should be taken with meais if possible and daily. Dosage generally should not exceed 320 nig daily.
  • the daily close may vary from 1 to 4 tablets per day. i .e. from 30 to 120 mg taken orally in a single intake at breakfast time. If a dose is forgotten, there must be no increase in the dose taken the next day.
  • Gl iclazide is a BCS Class-! ! drug (B iophannaccutical Classification System) i.e. Low solubil ity and High permeability. Furt her as Gl iclazide has poor sol- ublility in water, this leads to i ts eu auc dissolution, oral absorption and therefore poor bioavailabi lity.
  • 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 polymers are used in the modified release compositions e.g. HPMC polymer. These polymers extend the release of drug by showing osmosis nature in aqueous conditions.
  • Cellulosic matrix based system work by the swelling and gelling function i.e. these polymer swel l through influx of liquids and a gel like physical structure is formed which provides extended release effect fa- cilitated by diffusion of the Gliclazide.
  • Prior art disclosing matrix based systems comprise US ' 6056977, US 200321948 1 and US 2003 1 1337 ! .
  • the object of the present invention is to provide a ready-to-use matrix system and method of preparation for Gliclazide extended release or modified release formulation. Pisdosure of Invention
  • the present invention provides hydrophilic matrix system based ready to use technology for Modified or Extended Release Formulation of Gliclazide Hy- drochloride using INSTAMODEL (A43D00048) manufactured by ideal Cures Private Limited Mumbai India.
  • the present invention also provides method for maki ng ready to use Gliclazide modified or extended release formulation, involving steps of aqueous granulation,- drying, lubrication and punching of tablets.
  • present invention also provides once and twice a day Gliclazide table dosage form.
  • Extended release 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.
  • 'modified release' is in context of the invention as a way of active drug delivery where the rate of release of the acti ve drug from the composition. is not ex- clusi vely dependent on the concentration of active drug remain ing in the dosage form and / or the solubility of the active drug in the liquid surrounding the composition, and where the time course with or without respecti ve location of release o f acti ve drug from an .oral dosage form are chosen to accomplish therapeutic or convenience ob jectives not offered by conventional dosage forms.
  • active drug is selected from Gliclazide, its intermediates and derivatives thereof.
  • the term 'G liclazide' is in context of the invention includes its polymorphic: forms, the pharmaceutically acceptable salts, including salts esters and pother chemical derivatives or intermediates etc.
  • the solid pharmaceutical composition comprises Gliclazide. from 1 to 50 w/w % of dosage form.
  • the term 'dosage', 'solid pharmaceutical composition' may. i nclude one or more of tablet, capsule, powder, disc, caplet, granules, pel lets, granules in capsule, minitab!ets, minitablets in capsule, pellets in capsule, sachet and the like.
  • the solid pharmaceutical composition also includes multilayer tablets. The solid pharmaceutical compositions are meant for oral administration.
  • tablette includes pharmaceutical compositions o f a ll 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.
  • Gl idant in the context of the present invention, is taken to mean that an ingredient which enhance product flow by reducing inter-particulate friction.
  • Gl idant 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 in- gredient 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 pyrrol idone K30 (PVP K30) and there derivatives thereof.
  • extended release solid oral dosage form for Gliclazide can be created with ready to use Instamodel (A43 D00048) system and dosage form have advantageous modified release properties.
  • the ready to use composition in accordance with present invention comprise INSTA MO DEL (A43D00048).
  • Gliclazide is formulated with ready to use composition to prepare modified release dosage form.
  • different salts., derivatives, polymorphs o f Gliclazide could be combined, to achieve ready-to-use composition to achieve extended or modified release dosage form.
  • Gliclazide is blended with the ready to use polymer and aqueous granulated further the granulated mi xture is compressed to produce a solid, formulation.
  • the ingredients are blended to form a uni form powder and then compressed with means generally known to skilled in the art.
  • Gliclazide 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 finally coated.
  • Gliclazide and .I NSTAMODEL 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 effecti ve 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 Gliclazide, their derivati ves or combination thereof along with ready to use composition. Therefore inventive for- mulation preparation comprise steps as:-
  • inventive dosage form is prepared by blending ready to use composition (instarnodel A43 D00048), process blending is performed by conventional dry blender or a food processor or 'V -blender' or a sirni!ai function device. Further Gliclazide are processed using aqueous sol vent with binder ⁇ through wet granulation or a similar wet. mixing method to generate dosage for- mulation. Dosage formulation is further dried, sieved and compressed optionally with addition of lubricant, binder, glidant to form modified release oral dosage form.
  • inventive dosage formulations are prepared by blending Gliclazide along with instarnodel (A43 D00048). I nit ia l ly al l 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 ac- ceptability and oral dosage compression quality. Subsequently un iform mixed inventive formulation is compressed in standard pharmacopoeial 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 2 .
  • oral dosage forms produced by inventive composition having human admin istrate active ingredient is suitable for human use.
  • drug suitable for veterinary purpose formulated in accordance with present composition will be suitable for veterinary use. . .
  • Gliclazide is formulated in oral dosage form for modified or extended release delivery.
  • Inventive composition comprising 10 to 30 mg or 50 mg of Gliclazide in plurality 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; an- tibacterial; antibiotic; anticoagulant; anticonvulsant; antidepressant; antifungal ; anti- histamine; antimalarial; antimicrobial agent; antipsychotic agent; Antiviral agents; blood glucose lowering drug; calcium channel modulator; diuretic; erectile dys- function; gastric acid secretion inhibitor; histamine H2-receptor antagonist; inhibitor of steroid Type II 5[alpha]- reductase including; lipid regulating agents; selective Hl- receptor antagonist; vasodilator; vitamins.
  • andrenergic blocking agent include, but are not limited to: andrenergic blocking agent; acetyl-cholin-esterase inhibitor; analgesic or antipyretics; an
  • the dosage formulation for 1 00,000 (20.00 kg) T ablets of G lic lazide is prepared using composition as stated in table: - 1 wherein Gl iclazide is 3.0 kg, 6.8 kg of Dicalcium phosphate dihydrate and 2.0 kg of Maltodextrin are weighed, sifted in rapid ' mixture granulated accordingly, subsequently sieved to get uni formly granulated powder through 40 mesh screen. It is noted that other size screen could be used to get similar results. Sieved Gliclazide with above ingredient is granulated using water as granulating solvent in rapid mixture granulator (RMG) .
  • RMG rapid mixture granulator
  • RMG should be at slow speed for 10 min followed by high speed for 2 - 3 ruins (Total qty of water used approx. 0.80 - 0.90 kg).
  • Granulation step requires proper optimization 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 -mi l l/ F itzmil l) dried in tray drier (or Fluidized bed dryer) at temperature not more than 50°C-55°C keeping loss on drying' at 1 -2%.
  • Time interval 1 , 4, 8, and 1 2 hour
  • the dnig dissolved profile of the Reference products and Gl iclazide having dose strength of 30 mg using Instamodel (A.4.3 D0Q048) formulations are compared.
  • the release exponents for the Reference and formulated Gliclazide 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)
  • 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 gliclazide et de ses sels et dérivés, un procédé de préparation de comprimé à libération prolongée 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 gliclazide à diverses concentrations de dose, un procédé pour les produire et leur utilisation en tant que compositions pharmaceutiques formulées.
PCT/IN2014/000603 2014-09-16 2014-09-16 Formulation à libération prolongée de gliclazide Ceased WO2016042568A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
PCT/IN2014/000603 WO2016042568A1 (fr) 2014-09-16 2014-09-16 Formulation à libération prolongée de gliclazide

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/IN2014/000603 WO2016042568A1 (fr) 2014-09-16 2014-09-16 Formulation à libération prolongée de gliclazide

Publications (1)

Publication Number Publication Date
WO2016042568A1 true WO2016042568A1 (fr) 2016-03-24

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Application Number Title Priority Date Filing Date
PCT/IN2014/000603 Ceased WO2016042568A1 (fr) 2014-09-16 2014-09-16 Formulation à libération prolongée de gliclazide

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116162053A (zh) * 2023-01-10 2023-05-26 山东省分析测试中心 一种格列齐特-哌嗪共晶及其制备方法

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000018373A1 (fr) * 1999-02-01 2000-04-06 Adir Et Compagnie Comprime matriciel permettant la liberation prolongee de gliclazide apres administration par voie orale
US20040081697A1 (en) * 1998-11-12 2004-04-29 Smithkline Beecham P.L.C. Pharmaceutical composition for modified release of an insulin sensitiser and another antidiabetic agent
WO2006061697A1 (fr) * 2004-12-06 2006-06-15 Themis Laboratories Private Limited Compositions de sulfonyluree et procede de preparation de ces dernieres
WO2008062470A2 (fr) * 2006-10-19 2008-05-29 Torrent Pharmaceuticals Limited Forme posologique à libération contrôlée stabilisée de gliclazide
WO2009082359A1 (fr) * 2007-12-26 2009-07-02 Ali Raif Ilac Sanayi Ve Ticaret A.S. Comprimé de gliclazide à libération prolongée
EP2181705A1 (fr) * 2008-10-31 2010-05-05 Disphar International B.V. Formulation à libération prolongée de gliclazide

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040081697A1 (en) * 1998-11-12 2004-04-29 Smithkline Beecham P.L.C. Pharmaceutical composition for modified release of an insulin sensitiser and another antidiabetic agent
WO2000018373A1 (fr) * 1999-02-01 2000-04-06 Adir Et Compagnie Comprime matriciel permettant la liberation prolongee de gliclazide apres administration par voie orale
WO2006061697A1 (fr) * 2004-12-06 2006-06-15 Themis Laboratories Private Limited Compositions de sulfonyluree et procede de preparation de ces dernieres
WO2008062470A2 (fr) * 2006-10-19 2008-05-29 Torrent Pharmaceuticals Limited Forme posologique à libération contrôlée stabilisée de gliclazide
WO2009082359A1 (fr) * 2007-12-26 2009-07-02 Ali Raif Ilac Sanayi Ve Ticaret A.S. Comprimé de gliclazide à libération prolongée
EP2181705A1 (fr) * 2008-10-31 2010-05-05 Disphar International B.V. Formulation à libération prolongée de gliclazide

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
890/MUM/2004 A, 26 January 2007 (2007-01-26), pages 6 - 7 *
ELIAS-AL-MAMUN ET AL.: "Development and Evaluation of Combined Gliclazide and Enalapril Maleate Immediate Release Tablet Md.", J. PHARM. SCI. & RES., vol. 3, no. 3, 2011, pages 1103 - 1109 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116162053A (zh) * 2023-01-10 2023-05-26 山东省分析测试中心 一种格列齐特-哌嗪共晶及其制备方法

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