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WO2006087629A2 - Composition de medicament antipsychotique a delitement rapide - Google Patents

Composition de medicament antipsychotique a delitement rapide Download PDF

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Publication number
WO2006087629A2
WO2006087629A2 PCT/IB2006/000330 IB2006000330W WO2006087629A2 WO 2006087629 A2 WO2006087629 A2 WO 2006087629A2 IB 2006000330 W IB2006000330 W IB 2006000330W WO 2006087629 A2 WO2006087629 A2 WO 2006087629A2
Authority
WO
WIPO (PCT)
Prior art keywords
olanzapine
dosage form
cellulose
combination
rapidly disintegrating
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/IB2006/000330
Other languages
English (en)
Other versions
WO2006087629A3 (fr
Inventor
Chandra Sekhara Reddy Nagareddy
Ramesh Cheruvu
Kishor Dattatray Deo
Sivakumaran Meenakshisunderam
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.)
Aurobindo Pharma Ltd
Original Assignee
Aurobindo 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 Aurobindo Pharma Ltd filed Critical Aurobindo Pharma Ltd
Publication of WO2006087629A2 publication Critical patent/WO2006087629A2/fr
Publication of WO2006087629A3 publication Critical patent/WO2006087629A3/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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • 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
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates

Definitions

  • the present invention relates to rapidly disintegrating compositions of antipsychotic drug or its pharmaceutically acceptable salts. More particularly, the present invention relates to rapidly disintegrating dosage forms of olanzapine or its pharmaceutically acceptable salts.
  • the present invention also relates to a process for the preparation of rapidly disintegrating compositions of olanzapine or its pharmaceutically acceptable salts.
  • Olanzapine is an antipsychotic drug and is chemically known as 2- methyl-4-(4-methyl- 1 -piperazinyl)- 10H-thieno[2,3- ⁇ ] [ 1 ,5]benzodiazepine. Olanzapine is disclosed and claimed in US Patent No. 4,115,574 and is marketed under the trademark Zyprexa ® and Zyprexa Zydis ® for the treatment of Schizophrenia Sc Bipolar Mania. ' j - 1
  • Rapidly disintegrating tablets are known to be prepared by tablet molding, spray drying, vacuum drying and freeze drying techniques.
  • the orally disintegrating tablets of Olanzapine marketed under trade name of Zyprexa Zydis ® is manufactured by freeze-drying technology.
  • Rapidly disintegrating dosage forms have become popular in the recent past because of their ease of administration.
  • Various patents and publications disclose rapidly disintegrating dosage forms and process for their preparation. Examples of few patents and patent publications which discloses rapidly disintegrating dosage forms are given below:
  • US 5,501,861 discloses a fast dissolving tablet composition containing water-soluble carbohydrate made by compression-molded method.
  • US 5,464,632 discloses rapidly disintegratable multiparticulate tablet, which disintegrates in the mouth in less than sixty seconds, wherein the active agent is in the form of coated microcrystals or coated or uncoated micro granules.
  • US 5,762,961 discloses method of making rapidly soluble tablets comprising active ingredient, diluent, binder, and volatile salt.
  • US 5,919,485 discloses solid oral formulation comprising olanzapine, wherein the formulation is coated with a polymer selected from hydroxypropyl methyl cellulose, hydroxyethyl cellulose, methyl hydroxyethyl cellulose, sodium carboxymethyl cellulose, hydroxypropyl cellulose, polyvinylpyrrolidone, dimethylaminoethyl methacrylate, methyl acrylate acid ester copolymer, ethyl acrylate-methyl methacrylate copolymer, methyl cellulose, and ethyl cellulose.
  • US 6,149,938 discloses a process for rapidly disintegrating tablets, containing polyalcohol, an active ingredient, edible acid, optionally, other solid components selected from the group consisting of lubricants, sweetening agents, and flavors.
  • US 6,316,029 discloses an oral solid dose rapidly disintegrating nanoparticulate formulation.
  • US 6,350,469 discloses rapidly disintegrating tablet using methylcellulose having viscosity of > 1000 centipoise and an edible calcium salt.
  • US 2002/0071864 discloses a tablet for oral administration, which disintegrates in the oral cavity within 60 seconds, comprising a therapeutically effective amount of an active ingredient, (ii) spray-dried mannitol (iii) crospovidone, and (iv) one or more pharmaceutically acceptable excipients, the tablet containing no microcrystalline cellulose.
  • WO 02/47607 discloses a process for the preparation of a fast dissolving solid dosage form, comprising active agent, a cementing agent and other excipients.
  • WO 03/026610 discloses fast dissolving dosage form using an effervescent mixture.
  • WO 03/086343 discloses mouth dissolving solid dosage forms by dry granulation technique comprising pharmaceutical agent with a moisture absorber and a disintegrating agent.
  • WO 03/086361 discloses rapidly dispersing oral composition
  • Olanzapine in an amount of 1 mg to 25 mg, with at least one pharmaceutically acceptable excipients selected from the group consisting of binder, dispersing agent, filler, glidants or lubricant and sweetener.
  • WO 03/103629 discloses orally administered tablet that disintegrates quickly in the oral cavity in less than 60 seconds, comprising: drug, spray-dried mannitol, microcrystalline cellulose, sodium croscarmellose and lubricant.
  • WO 04/091585 discloses orally disintegratable tablet comprising drug and silicified microcrystalline cellulose.
  • Freeze drying processes have been used to prepare rapidly disintegrating dosage forms. Although this technology produces a product which rapidly disintegrates in water or in the oral cavity, a drawback is represented by the poor physical integrity of its physical structure which severely limits further manufacturing operations such as forming blister packs. Another significant drawback of the freeze drying technology is high production costs because of the lengthy duration of each freeze drying cycle (normally from 24 to 48 hours). Rapidly disintegrating tablets are also prepared by effervescent tablet technology. ⁇ The formulations prepared by this technology are hygroscopic in nature and requires special equipments and conditions and also require special directions for usage.
  • the above prior art discloses various methods for preparing rapidly disintegrating tablets such as, freeze drying, compression molding, effervescent and conventional tableting processes and discloses use of various excipients such as effervescent mixture, binders.
  • Commonly occurring problems while preparing rapidly disintegrating tablets are poor physical integrity and insufficient taste masking.
  • the preparation of rapid disintegrating tablets also requires special packaging material or equipment, special equipment like freeze dryer or spray dryer, use of expensive or time consuming processes.
  • the rapid disintegrating tablets prepared by conventional methods produce tablets, which have unpleasant mouth- feel and are sensitive to humidity and temperature.
  • the inventors of the present invention during their continuous effort to develop rapidly disintegrating tablet dosage forms of Olanzapine, found that rapid disintegration of tablets can be made without binders & using high concentrations of fillers meeting the USP standards as well as other in vitro and in vivo results matching the reference product.
  • the main objective of the present invention is to provide a hard, compressed, orally disintegrate dosage form of olanzapine with adequate hardness and good reproducibility.
  • Another objective of the present invention is to provide simple, cost effective and efficient process for preparing the solid dosage forms of olanzapine on a commercial scale rapidly disintegrating dosage forms.
  • the present invention provides rapidly disintegrating dosage form of olanzapine with no binding agent comprising of about 1-10% olanzapine, about 1-10% of disintegrant, about 70-85% of filler, about 0.4-7% of lubricant.
  • a process for the production of an orally disintegrating tablet dosage form of olanzapine comprising blending the excipients and optionally granulating the blend and then lubricating the mixture and compressing the lubricated blend.
  • the rapidly disintegrating tablets of the present invention comprise Olanzapine in the dosage range of from about 1 to 50 mg.
  • the rapidly disintegrating tablets of the present invention further comprise sweeteners and flavoring agents.
  • the disintegrating agent used in accordance with the present invention is selected from crosscarmellose sodium, crospovidone, sodium starch glycolate, sodium carboxymethyl cellulose, hydroxypropyl cellulose, alginic acid, alginates, polacrilin potassium, and the like or combination thereof.
  • the diluents used according to the present invention are selected from calcium phosphate-dibasic, cellulose-microcrystalline, cellulose powdered, calcium silicate, maltodextrin, polyols such as mannitol, sorbitol, xylitol, maltitol, starlac, silicified microcrystalline cellulose, sucrose, lactose, starch and combination thereof.
  • Suitable lubricants according to the present invention are selected from sodium lauryl sulfate, talc, magnesium stearate, sodium stearyl fumarate, stearic acid, glyceryl behenate, hydrogenated vegetable oil, zinc stearate and suitable glidants include colloidal silicon dioxide and talc.
  • Suitable sweeteners according to the present invention are selected from sugars such as sucrose, lactose and glucose; saccharin and salts thereof; mannitol, acesulfame potassium, glycerrhizinate salt and aspartame or mixture thereof.
  • Suitable flavoring agents include strawberry guarana, peppermint, cherry, mint, caramel, raspberry, lemon, orange, tuttifruity, banana, bubble gum, preferably strawberry guarana, juicy orange, peppermint flavor or combination thereof.
  • a process for the preparation of a rapidly disintegrating dosage form of olanzapine with no binding agent comprising of about 1-10% olanzapine, about 1-10% of disintegrant, about 70-85% of filler, about 0.4-7% of lubricant, comprises the steps of : i) sifting olanzapine, disintegrant, diluents, sweetener, flavoring agent, glidant, ii) mixing the sifted ingredients of step (i) in a blender, iii) lubricating the blend obtained in step (ii) and iv) compressing the lubricated blend of step (iii) to obtain orally disintegrating tablets.
  • step (i) olanzapine, polacrilin potassium, crospovidone, microcrystalline cellulose, mannitol, colloidal silicon dioxide, talc, aspartame, saccharin sodium and juicy orange flavor were sifted through suitable sieves and collected in separate containers, ii) sifted ingredients of step (i) were mixed in a blender, iii) lubricated the blend obtained in step (ii) with sodium stearyl fumarate and iv) compressed the lubricated blend of step (iii) to obtain orally disintegrating tablets.

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

Abstract

La présente invention concerne une forme posologique d'olanzapine à délitement rapide ne contenant pas d'agent liant qui renferme environ 1 à 10 % d'olanzapine, environ 1 à 10 % de délitant, environ 70 à 85 % de matière de charge et environ 0,4 à 7 % de lubrifiant.
PCT/IB2006/000330 2005-02-21 2006-02-20 Composition de medicament antipsychotique a delitement rapide Ceased WO2006087629A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN143/CHE/2005 2005-02-21
IN143CH2005 2005-02-21

Publications (2)

Publication Number Publication Date
WO2006087629A2 true WO2006087629A2 (fr) 2006-08-24
WO2006087629A3 WO2006087629A3 (fr) 2006-11-02

Family

ID=36644929

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2006/000330 Ceased WO2006087629A2 (fr) 2005-02-21 2006-02-20 Composition de medicament antipsychotique a delitement rapide

Country Status (1)

Country Link
WO (1) WO2006087629A2 (fr)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2246046A1 (fr) * 2009-04-28 2010-11-03 Sanovel Ilac Sanayi ve Ticaret A.S. Comprimé d'olanzapine à désintégration orale
WO2012153347A3 (fr) * 2011-05-04 2013-01-03 Zentiva K.S. Composition pharmaceutique d'olanzapine de forme 1 à administration par voie orale
CN104510717A (zh) * 2013-09-27 2015-04-15 江苏豪森药业股份有限公司 奥氮平口崩片及其制备方法
CN105377303A (zh) * 2013-07-19 2016-03-02 株式会社三和化学研究所 口腔崩解片
CN108261399A (zh) * 2016-12-30 2018-07-10 江苏豪森药业集团有限公司 奥氮平口腔崩解片及其制备方法
CN110151718A (zh) * 2019-06-13 2019-08-23 厦门医学院 一种奥氮平口腔崩解片及其制备方法
CN113730365A (zh) * 2021-08-10 2021-12-03 杭州新诺华医药有限公司 一种奥氮平口腔崩解片及其制备方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000057857A1 (fr) * 1999-03-25 2000-10-05 Yuhan Corporation Comprimé à administrer oralement se désagrégeant rapidement
AU2002255196A1 (en) * 2002-04-18 2003-10-27 Dr. Reddy's Laboratories Ltd. Rapidly dispersing solid oral compositions
ES2199061B1 (es) * 2002-06-10 2005-02-16 Laboratorios Vita, S.A. Comprimidos bucodispersables y procedimiento para su obtencion.

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2246046A1 (fr) * 2009-04-28 2010-11-03 Sanovel Ilac Sanayi ve Ticaret A.S. Comprimé d'olanzapine à désintégration orale
TR200903293A1 (tr) * 2009-04-28 2010-11-22 Sanovel İlaç San. Ve Ti̇c. A.Ş. Oral yolla dağılan olanzapin tablet.
WO2012153347A3 (fr) * 2011-05-04 2013-01-03 Zentiva K.S. Composition pharmaceutique d'olanzapine de forme 1 à administration par voie orale
CN105377303A (zh) * 2013-07-19 2016-03-02 株式会社三和化学研究所 口腔崩解片
US20160136091A1 (en) * 2013-07-19 2016-05-19 Sanwa Kagaku Kenkyusho Co., Ltd. Orally Disintegrating Tablet
CN104510717A (zh) * 2013-09-27 2015-04-15 江苏豪森药业股份有限公司 奥氮平口崩片及其制备方法
CN104510717B (zh) * 2013-09-27 2019-02-05 江苏豪森药业集团有限公司 奥氮平口崩片及其制备方法
CN108261399A (zh) * 2016-12-30 2018-07-10 江苏豪森药业集团有限公司 奥氮平口腔崩解片及其制备方法
CN110151718A (zh) * 2019-06-13 2019-08-23 厦门医学院 一种奥氮平口腔崩解片及其制备方法
CN113730365A (zh) * 2021-08-10 2021-12-03 杭州新诺华医药有限公司 一种奥氮平口腔崩解片及其制备方法

Also Published As

Publication number Publication date
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