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Pharmaceutical compositions containing a dgat1 inhibitor

a technology of dgat1 and composition, which is applied in the field of pharmaceutical compositions, can solve the problems of poor flow characteristics, difficult formulation of drug substances, and fluffy sticky substances

Inactive Publication Date: 2013-07-25
NOVARTIS AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides a pharmaceutical composition comprising a compound of formula (I), or a salt thereof, and various ingredients that improve its flowability, compactability, and prevent sticking and capping issues during tabletting. The formulation is robust and can be scaled up with consistent performance. The composition comprises a therapeutically effective amount of the compound, one or more surfactants with lubricant properties, one or more dry binders with disintegrant properties, one or more fillers, and one or more disintegrants.

Problems solved by technology

However, the compound of formula (I), or a pharmaceutically acceptable salt thereof, in particular the sodium salt thereof, is a drug substance which is difficult to formulate due to its physicochemical properties.
It is also plate like, very fluffy, and sticky in nature.
It also exhibits poor flow characteristics.
These characteristics of the drug substance make it particularly problematic to develop formulations comprising the compound of formula (II) which would be amenable to withstanding the compression forces required for a tablet form of the pharmaceutical composition with an adequate hardness window.
During the course of development, it has been found to be difficult to achieve such a formulation.

Method used

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  • Pharmaceutical compositions containing a dgat1 inhibitor
  • Pharmaceutical compositions containing a dgat1 inhibitor
  • Pharmaceutical compositions containing a dgat1 inhibitor

Examples

Experimental program
Comparison scheme
Effect test

embodiment 2

[0047]A pharmaceutical composition, according to embodiment 1, wherein the surfactant with lubricant properties is selected from, sodium lauryl sulfate (SLS), stearic acid, palmitic acid, myristic acid, poloxamers and polyethylene glycols such as PEG 4000-8000, Tween series of surfactants. Brij series of surfactants (i.e., Brij 80), Triton X-100, and combinations thereof, preferably Sodium lauryl sulfate (SLS).

embodiment 3

[0048]A pharmaceutical composition, according to embodiment 1 or 2, wherein the dry binder is selected from polyethylene glycols (PEG), e.g., PEG 4000; pregelatinized starch; starch; chitosan; guar gum, microcrystalline cellulose: methyl cellulose; calcium carboxymethylcellulose; sodium carboxymethylcellulose, alginic acid and / or its sodium salt; hydroxypropylmethyl cellulose or hydroxypropyl cellulose, both preferably of medium to high viscosity, e.g., viscosity grades 3 or 6 cps, e.g. low substituted hydroxypropyl cellulose (L-HPC LH-21); and combinations thereof, most preferably, low substituted hydroxypropyl cellulose (L-HPC LH-21).

embodiment 4

[0049]A pharmaceutical composition, according to any one of embodiments 1 to 3, wherein the filler is selected from microcrystalline cellulose (e.g., cellulose MK GR and products available under the registered trade marks AVICEL, FILTRAK, HEWETEN or PHARMACEL, Vivapur, emcocel, tabulose), low-substituted hydroxypropyl cellulose, hydroxyethyl cellulose, hydroxypropyl methyl cellulose, Anhydrous Dicalcium Phosphate, Dicalcium Phosphate, lactose, Anhydrous Lactose, and combinations thereof.

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Abstract

The present invention relates to a pharmaceutical composition comprising a therapeutically effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, one or more surfactants with lubricant properties, one or more dry binders with disintegrant properties, one or more fillers and one or more disintegrants.

Description

FIELD OF THE INVENTION[0001]The present invention relates to pharmaceutical compositions comprising (4-{4-[5-(6-trifluoromethyl-pyridin-3-ylamino)-pyridin-2-yl]-pheny}-cyclohexyl)-acetic acid, or a pharmaceutically acceptable salt thereof, e.g. the sodium salt thereof, as the active ingredient in a suitable carrier. The present invention also relates to the processes for their preparation and to their use as medicaments.[0002]As disclosed in WO 2007 / 126957, a genus of compounds as DGAT1-inhibitors, including, at Example 5-1, the compound (4-{4-[5-(6-trifluoromethyl-pyridin-3-ylamino)-pyridin-2-yl]-phenyl}-cyclohexyl)-acetic acid, having the structural formula (I):and its sodium saltmay be employed in the treatment of a condition or a disorder such as inflammatory conditions, obesity, diabetes and related metabolic disorders.[0003]Administration of such pharmaceutical agents via the oral route is preferred to parenteral administration because it allows self-administration by patients...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/20A61K31/444
CPCA61K9/2009A61K9/2054A61K9/2095A61K31/444A61K9/2059A61P17/00A61P29/00A61P3/00A61P3/04A61P35/00A61P3/06A61P9/00A61P3/10A61K9/20A61K47/38A61K47/26A61K9/2013A61K9/2018A61K9/2027A61K9/2813
Inventor WEN, HONGKUMARAPERUMAL, NATRAJANNAUSE, RICHARD
Owner NOVARTIS AG
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