US20080107731A1 - Dpp iv inhibitor formulations - Google Patents

Dpp iv inhibitor formulations Download PDF

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Publication number
US20080107731A1
US20080107731A1 US11/744,701 US74470107A US2008107731A1 US 20080107731 A1 US20080107731 A1 US 20080107731A1 US 74470107 A US74470107 A US 74470107A US 2008107731 A1 US2008107731 A1 US 2008107731A1
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Prior art keywords
pharmaceutical composition
diluent
tablet
disintegrant
lubricant
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Abandoned
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US11/744,701
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English (en)
Inventor
Anja Kohlrausch
Patrick Romer
Gerd Seiffert
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.)
Boehringer Ingelheim International GmbH
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Boehringer Ingelheim International GmbH
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=36972901&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=US20080107731(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim International GmbH filed Critical Boehringer Ingelheim International GmbH
Publication of US20080107731A1 publication Critical patent/US20080107731A1/en
Assigned to BOEHRINGER INGELHEIM INTERNATIONAL GMBH reassignment BOEHRINGER INGELHEIM INTERNATIONAL GMBH ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: SEIFFERT, GERD, ROMER, PATRICK, KOHLRAUSCH, ANJA
Priority to US13/230,133 priority Critical patent/US20120003313A1/en
Priority to US13/467,505 priority patent/US20120219622A1/en
Priority to US13/735,078 priority patent/US20130122089A1/en
Priority to US14/877,019 priority patent/US20160022687A1/en
Priority to US15/655,269 priority patent/US20170312287A1/en
Priority to US16/357,357 priority patent/US11033552B2/en
Priority to US17/319,325 priority patent/US20210260068A1/en
Abandoned legal-status Critical Current

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    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Definitions

  • the present invention relates to pharmaceutical compositions of selected DPP IV inhibitors, their preparation and their use to treat selected medical conditions.
  • DPP-IV dipeptidyl peptidase IV
  • CD26 The enzyme DPP-IV (dipeptidyl peptidase IV) also known as CD26 is a serine protease known to lead to the cleavage of a dipeptide from the N-terminal end of a number of proteins having at their N-terminal end a prolin or alanin residue. Due to this property DPP-IV inhibitors interfere with the plasma level of bioactive peptides including the peptide GLP-1 and are considered to be promising drugs for the treatment of diabetes mellitus.
  • DPP-IV inhibitors with a primary or secondary amino group show incompatibilities, degradation problems, or extraction problems with a number of customary excipients such as microcrystalline cellulose, sodium starch glycolate, croscarmellose sodium, tartaric acid, citric acid, glucose, fructose, saccharose, lactose, maltodextrines.
  • customary excipients such as microcrystalline cellulose, sodium starch glycolate, croscarmellose sodium, tartaric acid, citric acid, glucose, fructose, saccharose, lactose, maltodextrines.
  • the compounds themselves are very stable, they react with many excipients used in solid dosage forms and with impurities of excipients, especially in tight contact provided in tablets and at high excipient/drug ratios.
  • a pharmaceutical composition according to the present invention is intended for the treatment of to achieve glycemic control in a type 1 or type 2 diabetes mellitus patient and comprises a DPP-IV inhibitor with an amino group, especially a free or primary amino group, as an active ingredient, a first and second diluent, a binder, a disintegrant and a lubricant.
  • An additional disintegrant and an additional glidant are a further option.
  • the compositions can be used to treat rheumatoid arthritis, obesity and osteoporosis as well as to support allograft transplantation.
  • Diluents suitable for a pharmaceutical composition according to the invention are cellulose powder, dibasic calciumphosphate anhydrous, dibasic calciumphosphate dihydrate, erythritol, low substituted hydroxypropyl cellulose, mannitol, pregelatinized starch or xylitol. Among those diluents mannitol and pregelatinized starch are preferred.
  • Diluents preferred as the second diluent are the above mentioned diluents pre-gelatinized starch and low-substituted hydroxypropylcellulose (L-HPC) which show additional binder properties.
  • Lubricants suitable for a pharmaceutical composition according to the invention are talc, polyethyleneglycol, calcium behenate, calcium stearate, hydrogenated castor oil or magnesium stearate.
  • the preferred lubricant is magnesium stearate.
  • Binders suitable for a pharmaceutical composition according to the invention are copovidone (copolymerisates of vinylpyrrolidon with other vinylderivates), hydroxypropyl methylcellulose (HPMC), hydroxypropylcellulose (HPC), polyvinylpyrrolidon (povidone), pregelatinized starch, low-substituted hydroxypropylcellulose (L-HPC), copovidone and pregelatinized starch being preferred.
  • binders pregelatinized starch and L-HPC show additional diluent and disintegrant properties and can also be used as the second diluent or the disintegrant.
  • Disintegrants suitable for a pharmaceutical composition according to the present invention are corn starch, crospovidone, low-substituted hydroxypropylcellulose (L-HPC) or pregelatinized starch, corn starch being preferred.
  • colloidal silicon dioxide can be used as an optional glidant colloidal silicon dioxide.
  • An exemplary composition according to the present invention comprises the diluent mannitol, pregelatinized starch as a diluent with additional binder properties, the binder copovidone, the disintegrant corn starch, and magnesium stearate as the lubricant.
  • Dosage forms prepared with a pharmaceutical compositions according to the present invention contain active ingredients in dosage ranges of 0.1-100 mg. Preferred dosages are 0.5 mg, 1 mg, 2.5 mg, 5 mg and 10 mg.
  • Typical pharmaceutical compositions comprise (% by weight)
  • active ingredient 40-88% diluent 1, 3-40% diluent 2, 1-5% binder, 5-15% disintegrant, and 0.1-4% lubricant.
  • Preferred pharmaceutical compositions comprise (% by weight)
  • compositions according to the invention are intended for oral use and can be used in the dosage form of a capsule, a tablet or a film-coated tablet.
  • the film coat represents 2-4%, preferably 3% of the composition and comprises a film-forming agent, a plasticizer, a glidant and optionally one or more pigments.
  • An exemplary coat composition may comprise hydroxypropylmethyl-cellulose (HPMC), polyethylene glycol (PEG), talc, titanium dioxide and optionally iron oxide.
  • DPP-IV inhibitors with a primary amino group and salts thereof such as any DPP-IV inhibitor and salt thereof defined by formula (I)
  • R1 is ([1,5]naphthyridin-2-yl)methyl, (quinazolin-2-yl)methyl], (quinoxalin-6-yl)methyl, (4-Methyl-quinazolin-2-yl)methyl, 2-Cyano-benzyl, (3-Cyano-quinolin-2-yl)methyl, (3-Cyano-pyridin-2-yl)methyl, (4-Methyl-pyrimidin-2-yl)methyl, or (4,6-Dimethyl-pyrimidin-2-yl)methyl, and R2 is 3-(R)-amino-piperidin-1-yl, (2-amino-2-methyl-propyl)-methylamino or (2-(S)-amino-propyl)-methylamino.
  • Preferred DPP IV inhibitor compounds are the following compounds and salts thereof:
  • compositions according to the invention can be prepared by a wet granulation process.
  • Alternative methods for granulation of active ingredient and excipients with a granulation liquid are fluid bed granulation or one-pot granulation.
  • the granulation liquid is a solvent such as water, ethanol, methanol, isopropanol, acetone, preferably purified water, and contains a binder such as copovidone.
  • the solvent is a volatile component, which does not remain in the final product.
  • the active ingredient and the other excipients with exception of the lubricant are premixed and granulated with the aqueous granulation liquid using a high shear granulator.
  • the wet granulation step is followed by an optional wet sieving step, drying and dry sieving of the granules. For example a fluid bed dryer can then be used for drying.
  • the dried granules are sieved through an appropriate sieve.
  • a suitable conventional blender such as a free fall blender followed by addition of the lubricant such as magnesium stearate and final blending in the blender.
  • an exemplary wet granulation process for the preparation of a pharmaceutical composition according to the present invention comprises
  • part of the exipients such as part of a disintegrant (e.g. corn starch) or a diluent (e.g. pregelatinized starch) or an additional disintegrant (crospovidone) can be added extragranular prior to final blending of step g.
  • a disintegrant e.g. corn starch
  • a diluent e.g. pregelatinized starch
  • an additional disintegrant crospovidone
  • the granulate produced in steps a to e is produced in a one pot high shear granulation process and subsequent drying in a one pot granulator.
  • the final blend is further filled into capsules.
  • the final blend is further compressed into tablets of the target tablet core weight with appropriate size and crushing strength, using an appropriate tablet press.
  • a coating suspension is prepared and the compressed tablet cores are coated with the coating suspension to a weight gain of about 2-4%, preferably about 3%, using a standard film coater.
  • the film-coating solvent is a volatile component, which does not remain in the final product.
  • An active DPP IV inhibitor ingredient with a primary amino group and all other excipients with exception of magnesium stearate are blended in a high shear blender. This pre-mix is sieved through a 1 mm sieve. After addition of magnesium stearate the pre-mix is blended in a free fall blender to produce the final blend. The final blend is compressed into tablets using a suitable tablet press.
  • the following compositions can be obtained:
  • Component mg/tablet %/tablet mg/tablet %/tablet Active ingredient 1.000 2.000 2.500 2.000 Mannitol 43.250 86.500 108.125 86.500 Pregelatinized starch 5.000 10.000 12.500 10.000 Magnesium stearate 0.750 1.500 1.875 1.500 Total 50.000 100.000 125.000 100.000
  • Component mg/tablet %/tablet mg/tablet %/tablet Active ingredient 5.000 2.000 10.000 2.000 Mannitol 216.250 86.500 432.500 86.500
  • An active DPP IV inhibitor ingredient with a primary amino group and all other excipients with exception of magnesium stearate are blended in a high shear blender. This pre-mix is sieved through a 1 mm sieve. After addition of magnesium stearate the pre-mix is blended in a free fall blender to produce the final blend. The final blend is compressed into tablets using a suitable tablet press.
  • the following compositions can be obtained:
  • Component mg/tablet %/tablet mg/tablet %/tablet Active ingredient 10.000 1.667 10.000 2.222 Dibasic 464.000 77.333 344.000 76.788 calciumphosphate, anhydrous Low-substituted 120.000 20.000 90.000 20.000 hydroxypropylcellulose Magnesium stearate 6.000 1.000 6.000 1.000 Total 600.000 100.000 450.000 100.000
  • Copovidone is dissolved in purified water at ambient temperature to produce a granulation liquid.
  • An active DPP IV inhibitor ingredient with a primary amino group, mannitol and part of the pregelatinized starch are blended in a suitable mixer, to produce a pre-mix.
  • the pre-mix is moistened with the granulation liquid and subsequently granulated.
  • the moist granulate is optionally sieved through a sieve with a mesh size of 1.6-3.0 mm.
  • the granulate is dried at 55 ° C. in a suitable dryer to a residual moisture content corresponding to 2-5% loss on drying.
  • the dried granulate is sieved through a sieve with a mesh size of 1.0 mm.
  • the granulate is blended with part of the pregelatinized starch in a suitable mixer.
  • Magnesium stearate is added to this blend after passing through a 1.0 mm sieve for delumping.
  • the final blend is produced by final blending in a suitable mixer and compressed into tablets.
  • the following tablet composition can be obtained:
  • Copovidone is dissolved in purified water at ambient temperature to produce a granulation liquid.
  • An active DPP IV inhibitor ingredient with a primary amino group, mannitol, pregelatinized starch and corn starch are blended in a suitable mixer to produce the pre-mix.
  • the pre-mix is moistened with the granulation liquid and subsequently granulated using a high shear mixer.
  • the moist granulate is optionally sieved through a sieve with a mesh size of 1.6-3.0 mm.
  • the granulate is dried at about 60° C. in a fluid bed dryer until a loss on the drying value of 2-4% is obtained.
  • the Final Blend is compressed into tablet cores.
  • Hydroxypropyl methylcellulose, polyethylene glycol, talc, titanium dioxide and iron oxide are suspended in purified water in a suitable mixer at ambient temperature to produce a coating suspension.
  • the tablet cores are coated with the coating suspension to a weight gain of about 3% to produce film-coated tablets.
  • the following tablet compositions can be obtained:
  • Copovidone is dissolved in purified water at ambient temperature to produce a granulation liquid.
  • An active DPP IV inhibitor ingredient with a primary amino group, mannitol and pregelatinized starch are blended in a suitable mixer to produce a pre-mix.
  • the pre-mix is moistened with the granulation liquid and subsequently granulated.
  • the moist granulate is optionally sieved through a suitable sieve.
  • the granulate is dried at about 50° C. in a suitable dryer until a loss on drying value of 3-5% is obtained.
  • the dried granulate is sieved through a sieve with a mesh size of 1.0 mm.
  • Magnesium stearate is passed through a 1.0 mm sieve and added to the granulate. Subsequently the final blend is produced by final blending in a suitable blender and the final blend is compressed into tablets.
  • the following tablet compositions can be obtained:
  • Copovidone is dissolved in purified water at ambient temperature to produce a granulation liquid.
  • An active DPP IV inhibitor ingredient with a primary amino group and a part of mannitol, pregelatinized starch and corn starch are blended in a suitable mixer, to produce a pre-mix.
  • the pre-mix is moistened with the granulation liquid and subsequently granulated.
  • the moist granulate is sieved through a suitable sieve.
  • the granulate is dried at about 60° C. inlet air temperature in a fluid bed dryer until a loss on drying value of 1-4% is obtained.
  • the dried granulate is sieved through a sieve with a mesh size of 1.0 mm.
  • Magnesium stearate is passed through a sieve for delumping and added to the granulate. Additionally the remaining part of the exipients are added extragranular at this process step. Subsequently the final blend is produced by final blending in a suitable blender and compressed into tablet cores.
  • Hydroxypropyl methylcellulose, polyethylene glycol, talc, titanium dioxide and iron oxide are suspended in purified water in a suitable mixer at ambient temperature to produce a coating suspension.
  • the tablet cores are coated with the coating suspension to a weight gain of about 3% to produce film-coated tablets.
  • the following formulation variants can be obtained:
  • Formulation E Component mg/Tablet %/Tablet mg/Tablet %/Tablet Active ingredient 1.000 1.111 1.000 1.111 Mannitol 23.300 25.889 66.950 74.389 Pregelatinized starch 4.500 5.000 4.500 5.000 Corn starch 4.500 5.000 4.500 5.000 Copovidone 1.350 1.500 2.700 3.000 Total (granulate) 34.650 38.500 79.650 88.500 Corn starch 4.500 5.000 4.500 5.000 4.500 5.000 Mannitol 45.000 50.000 Magnesium stearate 1.350 1.500 1.350 1.500 Total (tablet core) 90.000 100.000 90.000 100.000 100.000

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US13/467,505 US20120219622A1 (en) 2006-05-04 2012-05-09 Dpp iv inhibitor formulations
US13/735,078 US20130122089A1 (en) 2006-05-04 2013-01-07 Dpp iv inhibitor formulations
US14/877,019 US20160022687A1 (en) 2006-05-04 2015-10-07 Dpp iv inhibitor formulations
US15/655,269 US20170312287A1 (en) 2006-05-04 2017-07-20 Dpp iv inhibitor formulations
US16/357,357 US11033552B2 (en) 2006-05-04 2019-03-19 DPP IV inhibitor formulations
US17/319,325 US20210260068A1 (en) 2006-05-04 2021-05-13 Dpp iv inhibitor formulations

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US13/735,078 Abandoned US20130122089A1 (en) 2006-05-04 2013-01-07 Dpp iv inhibitor formulations
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US13/735,078 Abandoned US20130122089A1 (en) 2006-05-04 2013-01-07 Dpp iv inhibitor formulations
US14/877,019 Abandoned US20160022687A1 (en) 2006-05-04 2015-10-07 Dpp iv inhibitor formulations
US15/655,269 Abandoned US20170312287A1 (en) 2006-05-04 2017-07-20 Dpp iv inhibitor formulations
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US17/319,325 Pending US20210260068A1 (en) 2006-05-04 2021-05-13 Dpp iv inhibitor formulations

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