Abstract: A pharmaceutical composition contains an acid addition salt of a basic drug and a fatty acid or bile acid. The acid addition salts thus formed exhibit enhanced transmucosal and transdermal penetration of the basic drug. The acid addition salts, an inclusion complex containing said salts and a use of said salts are also disclosed.
Type:
Grant
Filed:
April 19, 1999
Date of Patent:
July 3, 2001
Assignee:
Farmarc Nederland B.V.
Inventors:
Lawrence John Penkler, Luéta-Ann De Kock, Darryl Vanstone Whittaker
Abstract: A process for the optical resolution of racemic 3-(p-chlorophenyl)glutaramide (GAM) into its R isomer R--COOH and its S isomer S--COOH, which process includes the steps of either:(1) reacting racemic 3-(p-chlorophenyl)-glutaramide dissolved in a suitable solvent with S-(-)-.alpha.-methylbenzylamine of the formula H.sub.2 N--S'(2) precipitating out of the solution of step (1) R--CO.sub.2.sup.-.H.sub.3.sup.+ N--S';(3) dissolving the precipitate of step (2) in water, with the addition of a suitable acid; and(4) precipitating out of the solution of step (3) R--COOH; or(5) reacting racemic -3-(p-chlorophenyl)-glutaramide dissolved in a suitable solvent with R-(+)-.alpha.-methylbenzylamine of the formula H.sub.2 N--R';(6) precipitating out of the solution of step (5) S--CO.sub.2.sup.-.H.sub.3.sup.+ N--R';(7) dissolving the precipitate of step (6) in water, with the addition of a suitable acid, and(8) precipitating out of the solution of step (7) S--COOH.
Type:
Grant
Filed:
June 19, 1998
Date of Patent:
April 18, 2000
Assignee:
Farmarc Nederland B.V.
Inventors:
Alexander Franciscus Wildervanck, Mino Rodolfo Caira, Janet Lesley Scott, Liugi Renzo Nassimbeni, Rainer Clauss, Barratt Robert Dixon Easter
Abstract: This invention is directed towards pellets and a process for manufacturing pellets of diltiazem HCl having a dissolution kinetic independent from pH.