WO2011049773A1 - Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with pioglitazone - Google Patents

Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with pioglitazone Download PDF

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Publication number
WO2011049773A1
WO2011049773A1 PCT/US2010/052225 US2010052225W WO2011049773A1 WO 2011049773 A1 WO2011049773 A1 WO 2011049773A1 US 2010052225 W US2010052225 W US 2010052225W WO 2011049773 A1 WO2011049773 A1 WO 2011049773A1
Authority
WO
WIPO (PCT)
Prior art keywords
layer
weight
diluent
lubricant
disintegrant
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/US2010/052225
Other languages
English (en)
French (fr)
Inventor
Nicholas Birringer
Christopher T. John
Zhen Liu
Adam Procopio
Bhagwant Rege
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.)
Organon Pharma UK Ltd
Merck Sharp and Dohme LLC
Original Assignee
Merck Sharp and Dohme Ltd
Merck Sharp and Dohme LLC
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 Merck Sharp and Dohme Ltd, Merck Sharp and Dohme LLC filed Critical Merck Sharp and Dohme Ltd
Priority to CA2777231A priority Critical patent/CA2777231A1/en
Priority to CN2010800477129A priority patent/CN102573476A/zh
Priority to EP10825413.7A priority patent/EP2490534A4/en
Priority to AU2010308433A priority patent/AU2010308433A1/en
Priority to RU2012121185/13A priority patent/RU2012121185A/ru
Priority to US13/501,252 priority patent/US20120201885A1/en
Priority to IN3271DEN2012 priority patent/IN2012DN03271A/en
Priority to BR112012009496A priority patent/BR112012009496A2/pt
Priority to MX2012004673A priority patent/MX2012004673A/es
Priority to JP2012535230A priority patent/JP2013508370A/ja
Publication of WO2011049773A1 publication Critical patent/WO2011049773A1/en
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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • A61K9/209—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin

Definitions

  • Embodiments of Opadry® useful in the present invention include, but are not limited to, Opadry® I (HPC/HPMC), Opadry® 20A18334, Opadry® II, Opadry ⁇ II HP (PVA-PEG), or another suitable Opadry® suspension (such as polyvinyl alcohol,
  • the first layer additionally comprises one or more excipients selected from the group consisting of: (i) about 40-80 % by weight of a diluent; (ii) about 0.5-6 % by weight of a disintegrant; and (iii) about 0.75-10 % by weight of a lubricant.
  • the first layer additionally comprises one or more excipients selected from the group consisting of: (i) about 40-80 % by weight of two diluents; (ii) about 0.5-6 % by weight of a disintegrant; and (iii) about 0.75-10 % by weight of two lubricants.
  • the first layer additionally comprises one or more excipients selected from the group consisting of: (i) about 20-40 % by weight of a first diluent; (ii) about 20-40% of a second diluent; (iii) about 0.5-6 % by weight of a disintegrant; (iv) about 0.25-4 % by weight of a first lubricant and (v) about 0.5-6 % by weight of a second lubricant.
  • excipients selected from the group consisting of: (i) about 20-40 % by weight of a first diluent; (ii) about 20-40% of a second diluent; (iii) about 0.5-6 % by weight of a disintegrant; (iv) about 0.25-4 % by weight of a first lubricant and (v) about 0.5-6 % by weight of a second lubricant.
  • the dipeptidyl peptidase-4 inhibitor is sitagliptin, or the dihydrogen phosphate salt thereof.
  • the second layer about 16.53 % by weight of the second layer of Pioglitazone HC1; about 74 % by weight of the second layer of a diluent, about 6 % by weight of the second layer of a disintegrant; about 3 % by weight of the second layer of a binding agent; and about 0.5 % by weight of the second layer of a lubricant.
  • the first layer about 32.12 % by weight of the first layer of the dipeptidyl peptidase-4 inhibitor or a pharmaceutically acceptable salt thereof; about 62 % by weight of the first layer of a diluent; about 2 % by weight of the first layer of a disintegrant; and about 4 % by weight of the first layer of a lubricant.
  • the first layer about 32.12 % by weight of the first layer of the dipeptidyl peptidase-4 inhibitor or a pharmaceutically acceptable salt thereof; about 60-62 % by weight of the first layer of a diluent; about 2-3 % by weight of the first layer of a disintegrant; and about 4 % by weight of the first layer of a lubricant.
  • the second layer about 16.53 % by weight of the second layer of Pioglitazone HQ, about 71-75 % by weight of the second layer of a diluent, about 3-11 % by weight of the second layer of a disintegrant; about 0.5-1.5 % by weight of the second layer of a lubricant; and about 3-5 % by weight of the second layer of a binding agent.
  • the bilayer tablets are coated with Opadry I (HPC/HPMC).
  • Sitagliptin Powder Blend Layer Sitagliptin phosphate monohydrate, microcry stall ine cellulose, anhydrous dibasic calcium phosphate and croscarmellose sodium were blended in a bin blender for 10 minutes. Sodium stearyl fumarate and magnesium stearate were sieved through #60 sieve. The sieved sodium stearyl fumarate and magnesium stearate were blended with the sitagliptin blend for additional 5 minutes to give the lubricated sitagliptin powder blend.
  • the bilayer tablets were compressed on the Piccola bilayer tablet press using sitagliptin powder blend as the first layer and pioglitazone granulation as the second layer.
  • the tablets were film coated with a suitable Opadry® suspension (such as Opadry ® 20A18334) to an approximate 3% weight gain to provide a 618 mg coated tablet.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Inorganic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
PCT/US2010/052225 2009-10-23 2010-10-12 Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with pioglitazone Ceased WO2011049773A1 (en)

Priority Applications (10)

Application Number Priority Date Filing Date Title
CA2777231A CA2777231A1 (en) 2009-10-23 2010-10-12 Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with pioglitazone
CN2010800477129A CN102573476A (zh) 2009-10-23 2010-10-12 二肽基肽酶-4抑制剂与吡格列酮的复合药的药物组合物
EP10825413.7A EP2490534A4 (en) 2009-10-23 2010-10-12 PHARMACEUTICAL COMPOSITIONS OF COMBINATIONS OF DIPEPTIDYL-PEPTIDASE-4 INHIBITORS WITH PIOGLITAZONE
AU2010308433A AU2010308433A1 (en) 2009-10-23 2010-10-12 Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with pioglitazone
RU2012121185/13A RU2012121185A (ru) 2009-10-23 2010-10-12 Фармацевтические композиции комбинаций ингибиторов дипептидилпептидазы-4 с пиоглитазоном
US13/501,252 US20120201885A1 (en) 2009-10-23 2010-10-12 Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with pioglitazone
IN3271DEN2012 IN2012DN03271A (enExample) 2009-10-23 2010-10-12
BR112012009496A BR112012009496A2 (pt) 2009-10-23 2010-10-12 composição farmacêutica, e, método para tratar diabetes tipo 2
MX2012004673A MX2012004673A (es) 2009-10-23 2010-10-12 Composiciones farmaceuticas de combinaciones de inhibidores de dipeptidil peptidasa 4 con pioglitazona.
JP2012535230A JP2013508370A (ja) 2009-10-23 2010-10-12 ジペプチジルペプチダーゼ−４阻害剤とピオグリタゾンとの組み合わせの医薬組成物

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US25429909P 2009-10-23 2009-10-23
US61/254,299 2009-10-23

Publications (1)

Publication Number Publication Date
WO2011049773A1 true WO2011049773A1 (en) 2011-04-28

Family

ID=43900618

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2010/052225 Ceased WO2011049773A1 (en) 2009-10-23 2010-10-12 Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with pioglitazone

Country Status (12)

Country Link
US (1) US20120201885A1 (enExample)
EP (1) EP2490534A4 (enExample)
JP (1) JP2013508370A (enExample)
KR (1) KR20120104523A (enExample)
CN (1) CN102573476A (enExample)
AU (1) AU2010308433A1 (enExample)
BR (1) BR112012009496A2 (enExample)
CA (1) CA2777231A1 (enExample)
IN (1) IN2012DN03271A (enExample)
MX (1) MX2012004673A (enExample)
RU (1) RU2012121185A (enExample)
WO (1) WO2011049773A1 (enExample)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012173877A1 (en) * 2011-06-14 2012-12-20 Merck Sharp & Dohme Ltd. Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with simvastatin
WO2013062902A3 (en) * 2011-10-24 2015-06-18 Merck Sharp & Dohme Corp. Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with atorvastatin
JP2016510065A (ja) * 2013-03-06 2016-04-04 ノバルティス アーゲー 有機化合物の製剤
WO2022074664A1 (en) * 2020-10-05 2022-04-14 V-Ensure Pharma Technologies Private Limited An immediate release composition of sitagliptin hydrochloride
CN115227661A (zh) * 2022-09-22 2022-10-25 北京惠之衡生物科技有限公司 一种利格列汀片及其制备方法

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9937153B2 (en) * 2013-08-30 2018-04-10 Merck Sharp & Dohme Ltd. Oral pharmaceutical formulation of omarigliptin
TR201402685A1 (tr) * 2014-03-06 2015-09-21 Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi Vildagliptinin farmasotik formulasyonları.
CN105030724A (zh) * 2015-08-20 2015-11-11 杭州成邦医药科技有限公司 一种抗糖尿病药物的组合物
CN108096227A (zh) * 2018-01-25 2018-06-01 河北科技大学 阿格列汀口腔溶膜制剂
JP7109748B2 (ja) * 2018-12-11 2022-08-01 日本ジェネリック株式会社 アジルサルタンとアムロジピンベシル酸塩含有固形製剤及び固形製剤の製造方法
JP7423264B2 (ja) * 2019-10-17 2024-01-29 日本ジェネリック株式会社 シタグリプチン含有錠剤
TR202022612A2 (tr) * 2020-12-31 2022-07-21 Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi Alogli̇pti̇ni̇n farmasöti̇k kapsül kompozi̇syonlari

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060205675A1 (en) * 2000-06-19 2006-09-14 Arch Jonathan R S Combinations of dipeptidyl peptidase iv inhibitors and other antidiabetic agents for the treatment of diabetes mellitus
WO2006135723A2 (en) * 2005-06-10 2006-12-21 Novartis Ag Modified release 1-[(3-hydroxy-adamant-1-ylamino)-acetyl]-pyrrolidine-2(s)-carbonitrile formulation
US20080227825A1 (en) * 2005-09-29 2008-09-18 Yatindra Joshi Formulation
WO2009121945A2 (en) * 2008-04-03 2009-10-08 Boehringer Ingelheim International Gmbh New formulations, tablets comprising such formulations, their use and process for their preparation
US20090253752A1 (en) * 2004-10-25 2009-10-08 Bryan Burkey Combination of dpp-iv inhibitor, ppar antidiabetic and metmorfin

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101208085B (zh) * 2005-06-10 2011-01-05 诺瓦提斯公司 1-[(3-羟基-金刚烷基-1-基氨基)-乙酰基]-吡咯烷基-2(s)-腈的调释制剂

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060205675A1 (en) * 2000-06-19 2006-09-14 Arch Jonathan R S Combinations of dipeptidyl peptidase iv inhibitors and other antidiabetic agents for the treatment of diabetes mellitus
US20090253752A1 (en) * 2004-10-25 2009-10-08 Bryan Burkey Combination of dpp-iv inhibitor, ppar antidiabetic and metmorfin
WO2006135723A2 (en) * 2005-06-10 2006-12-21 Novartis Ag Modified release 1-[(3-hydroxy-adamant-1-ylamino)-acetyl]-pyrrolidine-2(s)-carbonitrile formulation
US20080227825A1 (en) * 2005-09-29 2008-09-18 Yatindra Joshi Formulation
WO2009121945A2 (en) * 2008-04-03 2009-10-08 Boehringer Ingelheim International Gmbh New formulations, tablets comprising such formulations, their use and process for their preparation

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of EP2490534A4 *

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012173877A1 (en) * 2011-06-14 2012-12-20 Merck Sharp & Dohme Ltd. Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with simvastatin
US20140093564A1 (en) * 2011-06-14 2014-04-03 Merck Sharp & Dohme Ltd. Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with simvastatin
EP2720685A4 (en) * 2011-06-14 2014-12-03 Merck Sharp & Dohme PHARMACEUTICAL COMPOSITIONS OF COMBINATIONS OF DIPEPTIDYL-PEPTIDASE-4-INHIBITORS WITH SIMVASTATIN
WO2013062902A3 (en) * 2011-10-24 2015-06-18 Merck Sharp & Dohme Corp. Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with atorvastatin
JP2016510065A (ja) * 2013-03-06 2016-04-04 ノバルティス アーゲー 有機化合物の製剤
WO2022074664A1 (en) * 2020-10-05 2022-04-14 V-Ensure Pharma Technologies Private Limited An immediate release composition of sitagliptin hydrochloride
CN115227661A (zh) * 2022-09-22 2022-10-25 北京惠之衡生物科技有限公司 一种利格列汀片及其制备方法
CN115227661B (zh) * 2022-09-22 2022-12-13 北京惠之衡生物科技有限公司 一种利格列汀片及其制备方法

Also Published As

Publication number Publication date
KR20120104523A (ko) 2012-09-21
AU2010308433A1 (en) 2012-06-07
EP2490534A1 (en) 2012-08-29
US20120201885A1 (en) 2012-08-09
CN102573476A (zh) 2012-07-11
IN2012DN03271A (enExample) 2015-10-23
BR112012009496A2 (pt) 2015-09-29
RU2012121185A (ru) 2013-11-27
CA2777231A1 (en) 2011-04-28
MX2012004673A (es) 2012-06-14
EP2490534A4 (en) 2013-06-12
JP2013508370A (ja) 2013-03-07

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