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Dpp iv inhibitor formulationsDpp iv inhibitor formulations description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20080107731, Dpp iv inhibitor formulations. Brief Patent Description - Full Patent Description - Patent Application Claims
BACKGROUND OF THE INVENTION [0001]This Application claims priority of EP 06 009 201, which is hereby incorporated by reference in its entirety. [0002]1. Field of the Invention [0003]The present invention relates to pharmaceutical compositions of selected DPP IV inhibitors, their preparation and their use to treat selected medical conditions. [0004]2. Description of the Prior Art [0005]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. DETAILED DESCRIPTION OF THE INVENTION [0006]In attempts to prepare pharmaceutical compositions of selected DPP-IV inhibitors it has been observed, that the 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. Though 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. The amino group appears to react with reducing sugars and with other reactive carbonyl groups and with carboxylic acid functional groups formed for example at the surface of microcrystalline cellulose by oxidation. These unforeseen difficulties are primarily observed in low dosage ranges which are required due to the surprising potency of the selected inhibitors. Thus, pharmaceutical compositions are required so solve these technical problems associated with the unexpected potency of selected DPP-IV inhibitor compounds. [0007]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. Additionally the compositions can be used to treat rheumatoid arthritis, obesity and osteoporosis as well as to support allograft transplantation. [0008]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. [0009]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. [0010]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. [0011]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. [0012]The above mentioned binders pregelatinized starch and L-HPC show additional diluent and disintegrant properties and can also be used as the second diluent or the disintegrant. [0013]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. [0014]As an optional glidant colloidal silicon dioxide can be used. [0015]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. [0016]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. [0017]Typical pharmaceutical compositions comprise (% by weight) TABLE-US-00001 0.5-20% active ingredient 40-88% diluent 1, 3-40% diluent 2, 1-5% binder, 5-15% disintegrant, and 0.1-4% lubricant. [0018]Preferred pharmaceutical compositions comprise (% by weight) TABLE-US-00002 0.5-7% active ingredient 50-75% diluent 1, 5-15% diluent 2, 2-4% binder, 8-12% disintegrant, and 0.5-2% lubricant [0019]The pharmaceutical 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. Typically 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. [0020]Preferred active ingredients in the context of the present invention are DPP-IV inhibitors with a primary amino group and salts thereof such as any DPP-IV inhibitor and salt thereof defined by formula (I) Continue reading about Dpp iv inhibitor formulations... Full patent description for Dpp iv inhibitor formulations Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Dpp iv inhibitor formulations patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored. 3. Each week you receive an email with patent applications related to your keywords. Start now! - Receive info on patent apps like Dpp iv inhibitor formulations or other areas of interest. ### Previous Patent Application: Sustained release pharmaceutical preparations and methods for producing the same Next Patent Application: Gastric retention system Industry Class: Drug, bio-affecting and body treating compositions ### FreshPatents.com Support Thank you for viewing the Dpp iv inhibitor formulations patent info. 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