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Composition of a non-nucleoside reverse transcriptase inhibitor

A composition and polymer technology, which can be applied in the general field and can solve problems such as differences in the crystallization tendency of compounds

Active Publication Date: 2016-06-29
MERCK SHARP & DOHME BV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] Additionally, compounds often differ in their propensity to crystallize

Method used

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  • Composition of a non-nucleoside reverse transcriptase inhibitor
  • Composition of a non-nucleoside reverse transcriptase inhibitor
  • Composition of a non-nucleoside reverse transcriptase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0081] An example of the preparation of a spray-dried pharmaceutical formulation of Compound A is provided below. One goal in developing solid dispersion formulations was to achieve superior biological properties compared to conventional formulations containing crystalline Compound A. The biopharmaceutical comparison of spray-dried solid dispersion formulations containing increased concentrations of polymer was compared to conventional formulations containing the same amount of API. API is Compound A or a pharmaceutically acceptable salt thereof. Bioavailability was determined in vivo by administering to beagle dogs a test formulation of the active pharmaceutical ingredient (API) and / or other formulations at a dose of 1 mg / kg of API and then measuring the amount of API in serum or blood over time .

[0082] Preparation of spray-dried formulations

[0083] The spray-dried formulation comprises compound A (5-30% w / w); optional surfactants (1-10% w / w) such as SDS (sodium dod...

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Abstract

The invention encompasses a composition comprising the reverse transcriptase (RT) inhibitor 3-chloro-5-({1-[(4-methyl-5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl]-2-oxo-4-(trifluoromethyl)-1,2-dihydropyridin-3-yl}oxy)benzonitrile sufficiently mixed in a concentration enhancing polymer, and processes for making the same. The composition and processes of the present invention significantly improve the bioavailability of the aforementioned RT inhibitor, while maintaining physical stability.

Description

Background technique [0001] Reverse transcriptase (RT) inhibition is discussed in WO2011 / 120133A1 (published October 6, 2011) and US Patent No. 8,486,975 (issued July 16, 2013), both of which are hereby incorporated by reference in their entirety. Agent 3-chloro-5-({1-[(4-methyl-5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl]-2 -Oxo-4-(trifluoromethyl)-1,2-dihydropyridin-3-yl}oxy)benzonitrile (referred to herein as "Compound A") and a method for its preparation. [0002] Anhydrate Compound A is known to exist in at least three crystalline forms - Form I, Form II and Form III. Crystalline Anhydrate Compound A has low solubility and poor bioavailability. The solubility of the most stable anhydrous crystalline form of Compound A in water and fasted state simulated intestinal fluid is 6.3 μg / mL. At the 100 mg dose, >37 liters of water were required to dissolve the compound. [0003] There are many strategies for increasing the bioavailability of poorly soluble drugs. Oral ...

Claims

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Application Information

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IPC IPC(8): A01N43/40
CPCA61K9/1652A61K9/4808A61K31/4439A61P31/14A61P31/18A61P43/00A61K47/50A61K31/44A61K47/38C07D401/06A61K9/1682
Inventor M.罗温格尔A.S.塔塔瓦蒂P.J.马萨奇K.J.M.普勒格C.J.布卢姆K.A.布鲁克哈特J.M.鲍曼
Owner MERCK SHARP & DOHME BV
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