ACID-ADDITIVE SALTS OF TERBINAFINE AND MALIC ACID, METHOD FOR THEIR PREPARING AND PHARMACEUTICAL COMPOSITION FOR TREATMENT OF FUNGAL INFECTION Russian patent published in 2006 - IPC C07C211/30 A61K31/135 A61P41/00 A01N33/12 A01P3/00 

Abstract RU 2289570 C2

FIELD: organic chemistry, chemical technology, medicine, pharmacy.

SUBSTANCE: invention relates to a novel terbinafine salt of the formula (I):

with malic acid possessing an antimycotic activity and to a method for its preparing and pharmaceutical composition used in treatment of fungal infection. L-(-)-bimalate is the most preferable form of salt. Method for preparing salt involves interaction of compound of the formula (I) as a free base with the corresponding form of malic acid. Pharmaceutical composition comprises indicated salt in combination with at least one pharmaceutically acceptable carrier or excipient. Pharmaceutical composition can be prepared as a solution or lacquer for nails. Proposed salt shows improved pharmacokinetic properties that makes its to be preferable in preparing pharmaceutical compositions adopted for systemic and topical using.

EFFECT: improved preparing method, improved and valuable properties of salt and pharmaceutical composition.

8 cl, 6 dwg, 5 ex

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RU 2 289 570 C2

Authors

Zhiron Dan'El'

Rebe Zhan-Lui

Khirsh Shtefan

Dates

2006-12-20Published

2002-02-06Filed