摘要:
The present invention relates to alkaline earth metal salts of bosentan, anyhdrous bosentan, polymorphic forms thereof, amorphous bosentan and processes for preparing them. The present invention further relates to a process for the preparation of bosentan and its pharmaceutically acceptable salts.
摘要:
A process for the preparation of carvedilol of formula (I) (I) either in enantiomeric substantially pure form, or as an enantiomeric mixture, optionally as a pharmaceutically acceptable salt thereof, which process comprises reacting 2,3-eopxypropoxy carbazole of formula (II) (II) or the R or S enantiomer thereof, with N-[2-(2-methoxy-phenoxy)ethyl]-benzylamine of formula (V) (V) to yield benzyl carvedilol of formula (VI) (VI) which is debenzylated by catalytic hydrogenation to yield carvedilol of formula (I), either in enantiomeric substantially pure form, or as an enantiomeric mixture, and if desired reacting the thus formed carvedilol of formula (I) with an inorganic or organic acid to yield a pharmaceutically acceptable salt thereof, and/or, if desired, separating the enantiomers. The above process is characterised in that reaction of said 2,3-epoxypropoxy carbazole of formula (II) with said N-[2-(2-methoxy-phenoxy)ethyl]-benzylamine of formula (V) is carried out in water as the reaction medium. The present invention further provides carvedilol of formula (I) prepared by a process as described above, and pharmaceutical compositions containing the same and therapeutic uses thereof.
摘要:
A pharmaceutical formulation which comprises azelastine, or a pharmaceutically acceptable salt, solvate or physiologically functional derivative thereof, and ciclesonide.
摘要:
An inhaler device (2) is for the inhalation of particulate substances is provided. The device comprises a housing (5) having first and second openings, a first air passageway (11) being defined through said housing between said first and second openings, an extraction member (40) extending from said housing and having a second air passageway (46) formed therein, and an airflow directing means (16) proximate one of said first and second openings.
摘要:
A process for the preparation of valganciclovir with triacetyl ganciclovir (V) as a starting material, comprising the following steps: selective hydrolysis, reacting with a coupling agent and a solvent, followed by hydrolysis under basic conditions and hydrogenolysis in the presence of a catalyst.
摘要:
One-pot process for the preparation of nateglinide, which process comprises reacting an alkyl ester of D-phenylalanine of formula (II) where R represents C1-4 alkyl, typically methyl, either as the free base or in salt form (typically the hydrochloride), with trans-4-isopropylcyclohexanecarboxylic acid of formula (III) where X represents hydroxy or halo, typically chloro, to obtain a C1-4 alkyl ester of nateglinide of formula (IV), preferably the methyl ester of nateglinide followed by hydrolysis to yield nateglinide of formula (I).
摘要:
Transdermal spray formulations containing a pharmaceutically active agent and methods for administering the same are provided. The formulations comprise the pharmaceutically active agent, a VP/VA copolymer and a non-aqueous vehicle. The formulations further comprise an anti-nucleating agent to prevent recrystallization of the pharmaceutically active agent and a penetration enhancer to increase the rate of drug delivery through the skin. Upon application to the skin, the present formulations dry to provide a film at the site of treatment.
摘要:
Anhydrous crystalline fexofenadine hydrochloride Form C, crystalline fexofenadine acetate monohydrate Form D, crystalline fexofenadine acetate dihydrate Form E and crystalline fexofenadine free base monohydrate Form F, processes of preparing the same, pharmaceutical compositions thereof, therapeutic uses thereof and methods of treatment therewith.
摘要:
A process of preparing finasteride Form (I), which process comprises dissolving finasteride in a solvent, replacing the solvent partially or substantially completely with a nonsolvent and thereafter isolating finasteride Form (I). There is also provided finasteride Form (I) prepared in accordance with the present invention, and the therapeutic use thereof in the inhibition of 5-alpha reductase, and pharmaceutical compositions containing the same.