WO2017153821A1 - Résinates de tofacitinib destinées au masquage du goût - Google Patents

Résinates de tofacitinib destinées au masquage du goût Download PDF

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Publication number
WO2017153821A1
WO2017153821A1 PCT/IB2016/055490 IB2016055490W WO2017153821A1 WO 2017153821 A1 WO2017153821 A1 WO 2017153821A1 IB 2016055490 W IB2016055490 W IB 2016055490W WO 2017153821 A1 WO2017153821 A1 WO 2017153821A1
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Prior art keywords
resinate
tofacitinib
resinates
range
resin
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PCT/IB2016/055490
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English (en)
Inventor
Milind Vinayak SATHE
Saiesh Purushottam PHALDESAI
Srikant V PIMPLE
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Unichem Laboratories Limited
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Publication of WO2017153821A1 publication Critical patent/WO2017153821A1/fr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
    • 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 resinates of Tofacitinib, fast disintegrating and or quick release pharmaceutical compositions comprising the said resinates and process for the preparation of resinates and compositions.
  • Oral dosage forms containing Tofacitinib have bitter taste. Therefore these are provided in coated form, preferably film coated. Bitter taste of Tofacitinib does not support its use without coating. Fast disintegrating and or quick release taste masked oral dosage forms of Tofacitinib are not available. Therefore there is a need to provide fast disintegrating and or quick release taste masked oral dosage forms containing Tofacitinib.
  • Taste masking is also done by various other means such as formation of new salt, various types of coatings, resinates and inclusion complexes. Rapid melt, Fast melt or quick disintegrating techniques also enable oral dispersion of compositions. Each of these methods is associated with peculiar disadvantages which are method specific.
  • the resin has to be drug compatible. It has to be drug specific otherwise desirable drug release profile may not be achieved. Formulating a stable composition is an important aspect in drug development. Composition in which an improper resin is used can jeopardize drug stability and or drug availability for absorption. Therefore formation of appropriate resinate is a problematic, complicated and challenging process.
  • a taste masked composition of a bitter tasting drug in combination with two enteric polymers comprising, a methacrylic acid copolymer and a phthalate polymer is taught by US 6565877.
  • cation-exchange resins such as polysulfonic acid and polycarboxylic acid polymers for adsorbing amine drugs.
  • Loading active substances onto an ion exchange resin is also disclosed by US 2990332 and is told to be dependent upon several factors such as equilibrium constant, temperature, the rate of diffusion and the presence of other ions.
  • IN 225628 teaches resinate complexes of Cetirizine, levocetirizine, its enantiomers salts and the compositions thereof.
  • IN 207068 teaches a manufacturing process for the preparation of mouth dispersible tablets using active pharmaceutical substance Alprazolam.
  • IN 206560 teaches a novel method for the preparation of mouth dispersible tablet of active pharmaceutical substance Ondansetron using Betacyclodextrin.
  • US 5188825 teaches freeze-dried dosage forms prepared by bonding or complexing a water- soluble active agent to or with an ion exchange resin to form a substantially water insoluble complex.
  • US 5219563 teach use of synthetic cation exchange resins such as copolymers of styrene and divinylbenzene which are sulphonated and copolymers of methacrylic acid and divinylbenzene for masking the bitter taste of ranitidine .
  • Patent application number 2842/MUM/2015 which is not published on the date of application refers to orally disintegrating tablets of Tofacitinib but is silent on resinate formation or resinates of Tofacitinib.
  • Tablets produced by Freeze drying technology have high cost of production, besides sensitive to humidity. Their soft, fragile nature renders them unsuitable for conventional blister packing. Useful only for low dose water soluble drugs, poor stability at higher temperature and humidity and very poor physical resistence are additional disadventages. Claritin, Reditab, Dimetapp, Zofran, Lorazepam, Loperamide and few more products are available based on Zydis Tecnology, freeze drying technology.
  • Tablets produced by Molding lack mechanical strength. These often get eroded and damaged during handling or opening the blister pack. Increasing hardness results into undesirable effect on disintegration. Improvement of mechanical strength and disintegration is possible but with huge investments. Orally disintegrating or fast dissolving tablets produced by other technologies necessitate use of robotic techniques such as robotic pick and pack type of packaging systems which are costly.
  • Dysphagia or difficulty in swallowing, is common among all age groups and is more pronounced in infants, small age and geriatric populations. It is also prominent in physically challenged, elderly institutionalized individuals. Swallowing with water is a difficult task for them.
  • Solid dosage forms that can be dissolved in water or suspended in the mouth, promote easy swallowing and are highly desirable for the pediatric, geriatric population and for other patients who prefer the convenience.
  • Orally disintegrating tablets have added adventage that bioavailability of drugs is enhanced due to absorption from mouth, pharynx and oesophagus, besides rapid or fast onset of therapeutic action.
  • Orally dispersible tablets have other adventages such as cost effective and simple packaging if appropriate method is selected to produce and pack it. Enhanced palatability, ease of administration and hence patient compliance are its pronounced advantages.
  • Resinate of Tofacitinib and or the fast relase or quick release compositions such as orally disintegrating tablets, dry syrups and such other dosage forms made form such resinates are not reported as yet.
  • Tofacitinib orally dispersible compositions comprising the resinates of Tofacitinib, without the use of aromatic solvents are not known.
  • the invention discloses use of non aromatic solvents to prepare resinate of Tofacitinib or its pharmaceutical salts such as Tofacitinib Citrate.
  • the main object of the invention is to provide resinates of Tofacitinib, rapid disintegrating and or quick release taste masked pharmaceutical compositions comprising the said resinates and process for the preparation of resinates and compositions.
  • Another object of the invention is to prepare stable resinates of Tofacitinib, rapid disintegrating and or quick release taste masked pharmaceutical compositions comprising the said resinates and process for the preparation of resinates and compositions.
  • Yet another object of the invention is to provide easily dispersible resinates of Tofacitinib, rapid disintegrating and or quick release taste masked pharmaceutical compositions comprising the said resinates and process for the preparation of resinates and compositions.
  • Yet another aspect of the invention is to provide resinates of Tofacitinib, a rapidly disintegrating and or quick release taste masked pharmaceutical compositions of Tofacitinib without the use of aromatic solvents and without the use of sophisticated packaging machinery.
  • Yet another object of the invention to provide taste masked rapidly disintegrating and or quick release composition of Tofacitinib with at least one more active ingredient.
  • the present invention relates to resinates of Tofacitinib.
  • the invention also relates to taste masked, stable and readily dispersible resinates of Tofacitinib, rapidly disintegrating and or quick release taste masked pharmaceutical compositions comprising the said resinates and process for the preparation of resinates and compositions. Further the invention relates to the preparation of resinates and the compositions comprising the resinates without the use of aromatic solvents and without the use of sophisticated packaging machinery.
  • the process for preparation of resinates comprises steps:
  • the process of preparation of taste masked resinates of Tofacitinib and compositions comprising these resinates comprises steps of:
  • step b) or c) or d) Processing the resinate obtained in step b) or c) or d) with at least one pharmaceutical excipient to obtain rapidly disintegrating and or quick release compositions with or without other actives.
  • Resinates prepared by the above process are stable resinates. These resinates and the compositions are prepared without the use of aromatic solvents and without the use of sophisticated packaging machinery. DETAILED DESCRIPTION OF THE INVENTION
  • the present invention relates to resinates of Tofacitinib.
  • the invention also relates to compositions comprising tofacitinib resinates.
  • the invention also relates to process to prepare the resinates and the compositions comprising the resinates.
  • the process for preparation of resinates comprises steps:
  • the process of preparation of taste masked resinates of Tofacitinib and compositions comprising these resinates comprises steps of:
  • step b) or c) or d) Processing the resinate obtained in step b) or c) or d) with at least one pharmaceutical excipient to obtain rapidly disintegrating and or quick release compositions with or without other actives.
  • Resinate formation takes place when ion exchange resin is contacted with drug solution. Thereafter depending upon the dosage form to be produced it may be washed and it may be dried or it may be washed and dried.
  • the resinate When the resinate is incorporated into dosage forms, it should be free from non aqueous solvents used in preparing and or washing. The content of solvents shold conform to ICH guidelines and the applicable pharmacopoeia. This can be achieved by drying alone, or by washing with water and then drying.
  • the process of preparation of solid dosage form compositions with the resinates of Tofacitinib comprises steps of:
  • the dried resinate is processed to obtain fast disintegrating and or quick release compositions.
  • Fast disintegrating and or quick release compositions of resinate are prepared as illustrated in the exmaples.
  • the resinate of Tofacitinib has a versatile use. It is processed to obtain several oral dosage compositions such as granules for dispersion either in sachet pack or as a dry syrup, or such granules dispersed into flavored syrupy base to obtain liquid suspension, quick dispersing tablets. Incorporation of resinate into chewing gum base gives chewing gum composition or dispersed into lozenge base to have a lozenge. The resinate when used with cooked glucose or similar base, gives a lollypop. Resinate can be incorporated into a wafer base or a soluble film base to have medicated wafer or soluble film.
  • desired composition is prepared by incorporating the resinate with other pharmaceutically acceptable excipients.
  • the cation exchange resin used for resinate formation is selected from Methacrylic acid polymer with divinylbenzene and Acrylic acid Potassium salt or Methacrylic acid polymer with divinylbenzene and Potassium salt, Methacrylic acid polymer with divinylbenzene and Acrylic acid, sulphonated copolymers of styrene and divinylbenzene, cross linked polymer of methacrylic acid and divinylbenzene.
  • These resins are commercially available including those available as Indion resins, Tulsion resins, Dowex resins, Amberlite IRP resins and their equivalents in the form of salt with alkali metals or in acid form. Resinate formation takes place even when ratio of resin to Tofacitinib is 0.5: 1.
  • Non aromatic solvent can be used singularly or in presence of another non aromatic solvent i.e. co-solvent.
  • Non aromatic solvent and or co-solvent is selected from ethanol, isopropyl alcohol, water, Dicholoromethane, organic polar and non-polar solvents, glycerin, propylene glycol and their suitable mixtures.
  • Non aromatic solvents as per the present invention includes open chain aliphatic solvents and mixtures thereof. These solvents are selected from compounds having carbon atoms ranging from CI - C6. It includes solvents such as ethers, esters, aldehydes, Ketones, alcohols, chlorinated solvents, water miscible and water immiscible solvents. Alcohols includes acohols having carbon atoms CI to C6. Aldehydes and ketones having carbon atoms from CI to C6.
  • Ethers, alcohols and esters having carbon atoms CI to C6 are covered by present invention.
  • Chlorinated solvents having carbon atoms from CI to C6 are included in the present invention.
  • Preferred alcohols are methanol, ethanol, straight and branched propyl alcohol and mixtures thereof.
  • Preferred ketone being acetone and preferred aldehyde being acetaldehyde.
  • Preferred chlorinated solvents include dichloromethane or methylelne dichloride.
  • Preferred solvent is one in which the Tofacitinib is soluble, which can be removed to conform to GMP and or ICH standards and which is physiologically acceptable.
  • Resinate is dried in one embodiment by heating in hot air oven. In another embodiment it is air dried at room or slightly elevated temperatures. Evaporation, vacuum evaporation, tray drying, microwave drying, spray drying, drum and belt film drying are other effective drying techniques. Centrifuging and optionally followed by drying is yet another methtod of removing the solvent. Drying method is selected depending on solvent to be removed.
  • Resinate is dried at a temperature less than 110°C. It is advisable to carry out drying at temperature range of above 20°C to about 110°C. Suitable temperature is selected to ensure removal of solvent from the resinate. Preferable range for drying is 30°C to 105°C, more preferable range being 40°C to 90°C, most preferable range being 50°C to 80°C. The resinates were found to be stable in the temperature range of 40°C to 70°C when exposed for 30 minutes duration. There was no impact on taste masking ability.
  • Active ingredient is Tofacitinib.
  • the process of forming resinate as illustrated by the invention provides sufficient motivation to form resinates of acid addition salts of Tofacitinib and hence other pharmaceutically acceptable acid addition salts are covered by the invention.
  • the content of active ingredient in the resinate is in the range of about 11% to about 67%w/w, preferably from about 11% to about 16.66% w/w which is approximately equal to 17% w/w.
  • Content of active in the resinate in the preferred range is useful for orally disintegrating tablets or orally disintegrating compositions.
  • Content of active ingredient can be adjusted in the range of about 18% to 50% w/w or from 51% to 67% w/w of that of resinate by taking lesser quantity of resin.
  • Resinate wherein active content is in the range of 25% to about 67% can be conveniently filled into empty hard gelatin capsules with or without other excipients.
  • addiotnal sweetening agents such as aspartame, sucralose or flavors such as Peppermint, strwbaerry, mint, orange flavours also enable incorporation of resinate with higher content of active.
  • Similar granular preparation can be prepared by known methods which is to be taken directly from the container without dilution with any solvent such as water. These are powders to be taken orally.
  • the resinate is processed with pharmaceutically acceptable excipients to obtain rapidly disintegrating or fast disintegrating and or quick release compositions such as quick dispersing tablets, granules for dispersion to prepare suspension just before consumption or as a dry syrup.
  • the resinate when dispersed into flavored syrupy base gives a liquid suspension. When mixed with chewing gum base, gives chewing gum composition. When dispersed into lozenge base, gives a lozenge.
  • Resinate with suitable active content is conveniently filled into empty hard gelatin capsules with or without other excipients. Capsule filling can be done either manually on hand filling machines or by mechanized means on automatic or semiautomatic machines.
  • Taste masked pharmaceutical compositions of Tofacitinib intended by this application / invention encompass all aforesaid compositions and dosage forms.
  • Resinate can be easily incorporated into various dosage forms in various percentages weight by weight. Resinate content from 0.1 %w/w to 99%w/w of the weight of composition provides suitable Tasteless, rapidly disintegrating and quick release dosage form.
  • the percentage of the resinate in the composition is also decided by the quantity and extent of other ingredients used and other desired attributes. Although 0.1% w/w or such lower concentrations of resinate can be incorporated to form a composition, use of 0.1% w/w or such lower concentrations of resinate in the composition would make the composition bulky or voluminous and hence not desirable. It is preferable to keep content of the resinate in the composition from 10% w/w to 90% w/w. Preferred resinate percentage in the composition is in the range of about 25% w/w to about 90% w/w. Resinate along with additional one or more active pharmaceutical ingredient provides fixed dose combination dosage form.
  • Additional sweteining agents that can be employed for preparation of Tofacitinib resinate compositions can be selected from sugars such as Mannitol, Sucrose, Maltitol, Fructose, Sorbitol, Sucralose, Dextrose; Aspartame; Saccharin Sodium, Acesulfame Potassium and the like pharmaceutically acceptable sweeteners.
  • sugars such as Mannitol, Sucrose, Maltitol, Fructose, Sorbitol, Sucralose, Dextrose; Aspartame; Saccharin Sodium, Acesulfame Potassium and the like pharmaceutically acceptable sweeteners.
  • the resinate was given to 8 volunteers for testing palatability and substantial reduction in bitter taste was noticed which is otherwise associated with Tofacitinib.
  • the compositions comprising resinate were given to 8 volunteers for testing palatability, mouth-feel, and taste.
  • compositions were found to be substantially free from the bitter taste, otherwise associated with Tofacitinib, were found to be palatable and had acceptable mouth feel. Use of taste enhancing agents improves the taste further.
  • the disintegration time of the tablet in the oral cavity was about well below 2 minutes. In some compositions it was 30 - 45 seconds.
  • Quickly disintegrating or fast release compoisitions mean disintegration in oral cavity within 2 mniutes.
  • the invention provides resinates of Tofacitinib and the process to preare the same. So prepared resinates are found to be stable at drying temperatures mentioned hereinabove. These are also easily dispersible. These resinates and the compositions comprising the resinates are prepared without the use of aromatic solvents and without the use of sophisticated packaging machinery.
  • Orally disintegrating, quick release compositions with improved palatability, mouth-feel, and taste eliminate the use of the water and support patient compliance.
  • Resinates and the compositions such as rapid disintegrating and or quick release taste masked pharmaceutical compositions comprising the said resinates and process for the preparation of resinates and compositions is described by non-limiting examples. Examples:
  • Example 1 Process to prepare the resinate of Tofacitinib base
  • the bitter taste was masked to different degree in case of different resins used and cake had acceptable taste and was not bitter like Tofacitinib base.
  • Example 4 Rapid disintegrating taste masked tablet composition of resinate of
  • Example 5 Manufacturing Process for Example 2, 3 and 4.
  • Formulae represent unit composition. Input materials taken in multiples depending upon available equipments to produce 10 tablets.
  • Example 6 Dry syrup composition comprising resinate of Tofacitinib. [Resinate w/w % is 80.16%.]
  • Tofacitinib resinate 40.078 mgs in 5 ml is equal to 5mg of Tofacitinib base or 8.078mg of Tofacitinib citrate per 5ml.
  • Tofacitinib resinate, Sodium CMC, Sucrose and Propyl Paraben were mixed. Water was added to make volume to 5 ml.
  • 500 ml were prepared without sugar.
  • the compositions were studied for 7 days. Subjective evaluation testing was done during and after 7 days. Composition with sugar had acceptable taste. Bitter taste was adequately masked. The composition without sugar had acceptable taste taste even after 7 days. The suspensions remain easily re-dispersible at the end of 7 days and were palatable.
  • Example 7 Dry syrup composition comprising resinate of Tofacitinib resinate (Indion
  • Tofacitinib resinate 50.078 mgs in 5 ml is equal to 5mg of Tofacitinib base per 5ml.
  • Tofacitinib resinate, Sodium CMC, Sucrose and Propyl Paraben were mixed in mixer. Water was added to make volume to 5 ml.
  • 500 ml were prepared without sugar.
  • the compositions were studied for 7 days. Subjective evaluation testing was done during and after 7 days. Composition with had acceptable taste. Bitter taste was adequately masked. The composition without sugar had acceptable taste taste even after 7 days. The suspensions remain easily re-dispersible at the end of 7 days and were palatable .
  • % of resinate in the composition is 85.8% or approximately 86% w/w of dry solids.
  • Example 8 Dry syrup composition comprising resinate of Tofacitinib resinate (Indion
  • Tofacitinib resinate 70.078 mgs in 5 ml is equal to 5mg of Tofacitinib base per 5ml.
  • Tofacitinib resinate, Sodium CMC, Sucrose and Propyl Paraben were mixed in mixer. Water was added to make volume to 5 ml.
  • 500 ml were prepared without sugar.
  • the compositions were studied for 7 days. Subjective evaluation testing was done during and after 7 days. Composition with sugar had acceptable taste. Bitter taste was adequately masked. The composition without sugar had acceptable taste taste even after 7 days. The suspensions remain easily re-dispersible at the end of 7 days and were palatable.
  • % of resinate in the composition is 89.4% or approximately 90% w/w of dry solids.
  • Dry Syrup compositions as listed above were prepared without sugar.
  • the composition without sugar had acceptable taste.
  • Bitter taste was adequately masked.
  • Example 10 Stability of resinates of Tofacitinib at 70°C with respect to taste.

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Abstract

La présente invention concerne des résinates de tofacitinib. L'invention concerne également des résinates de tofacitinib au goût masqué, stables et aisément dispersibles, des compositions pharmaceutiques au goût masqué à désintégration rapide et/ou à libération rapide comprenant lesdits résinates et un procédé de préparation des résinates et des compositions. Afin de former le résinate, la résine est choisie parmi des copolymères d'acide méthacrylique et de divinylbenzène, un polymère réticulé d'acide méthacrylique et de divinylbenzène, des copolymères sulfonés de styrène et de divinylbenzène. Afin de former le résinate, une résine échangeuse d'ions est mise en contact avec la solution de tofacitinib préparée dans un solvant non aromatique. Le résinate sert à formuler différentes formes posologiques pharmaceutiques telles que des comprimés, des capsules, des sirops secs.
PCT/IB2016/055490 2016-03-08 2016-09-15 Résinates de tofacitinib destinées au masquage du goût WO2017153821A1 (fr)

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IN201621007953 2016-03-08
IN201621007953 2016-03-08

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Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080095842A1 (en) * 2004-12-06 2008-04-24 Antarkar Amit K Rapidly Disintegrating Taste Masked Compositions and a Process for Its Preparations
US20130344149A1 (en) * 2011-01-27 2013-12-26 Ratiopharm Gmbh Oral Dosage Forms for Modified Release Comprising Tasocitinib
US20150336961A1 (en) * 2012-12-28 2015-11-26 Glenmark Pharmaceuticals Limited Process for the preparation of tofacitinib and intermediates thereof

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080095842A1 (en) * 2004-12-06 2008-04-24 Antarkar Amit K Rapidly Disintegrating Taste Masked Compositions and a Process for Its Preparations
US20130344149A1 (en) * 2011-01-27 2013-12-26 Ratiopharm Gmbh Oral Dosage Forms for Modified Release Comprising Tasocitinib
US20150336961A1 (en) * 2012-12-28 2015-11-26 Glenmark Pharmaceuticals Limited Process for the preparation of tofacitinib and intermediates thereof

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