NEW AMORPHOUS BOSENTAN AND METHOD FOR PRODUCING THE SAME

PROBLEM TO BE SOLVED: To improve the bioavailability of bosentan which is N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)-pyrimidin-4-yl]-4-tert-butylbenzene sulfonamide, is an endothelin receptor antagonist, and is used as a treating agent for pulmonary arterial hypertension by improv...

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Main Authors HIRAI YOSUKE, SAKAI HITOSHI, OSHIO NAOTAKA, TANAKA NOBUKAZU, SANADA KUNIO
Format Patent
LanguageEnglish
Published 19.01.2012
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:PROBLEM TO BE SOLVED: To improve the bioavailability of bosentan which is N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(2-pyrimidinyl)-pyrimidin-4-yl]-4-tert-butylbenzene sulfonamide, is an endothelin receptor antagonist, and is used as a treating agent for pulmonary arterial hypertension by improving the solubility in water since bosentan is a sparingly soluble drug, and to obtain a method for industrially simply improving the bioavailability.SOLUTION: By making bosentan into amorphous bosentan by a solvent method, a melting method, a mechanochemical method or the like, the amorphous bosentan can be more simply produced in a shorter time than by the conventional production methods and furthermore, the solubility can be improved.
Bibliography:Application Number: JP20100153304