4897270 Pharmaceutical compositions

1
New Patents High oil phase pharmaceutical vehicles in the form of an emulsion system having an oil phase content of from about 35% to about 65%, wherein the emulsion system comprises from ab- out 1~ to about 13~ of an aikylated PVP copolymer, from about 1~o to about 70/0 of an emulsifier, and a solvent system. The solvent sys- tem comprises from about 4~o to about 18~o of a C4-C22 fatty acid, alcohol or ester thereof, from about 2~o to about 25~/o of a glycol ester or diester, and from 0°~ to about 13%o of a branched chain ester of a C4-C22 carboxylic acid. The pharmaceutical vehicles are useful in sunscreen formulations, and especially those containing higher concentrations of benzophenone-3. When such higher concentrations are used, it is advantageous to add up to about 10~'/o of a branched chain ester of a C4-C22 carboxylic acid. 4897270 PHARMACEUTICAL COMPOSITIONS David S Deutsch, Jamshed Anwar, London, United Kingdom assigned to Glaxo Group Limited A pharmaceutical tablet is described which com- prises a tablet core containing the antibiotic cefuroxime axetil and a film coat which serves to mask the bitter taste of the cefuroxime axetil upon oral administration. It has been found that conventional film-coated tablets reduce the bio- availability of cefuroxime axetil and the inven- tion overcomes this by control of the film coat rupture time and use of a tablet core which dis- integrates immediately following rupture of the film coat. 4897267 MICROPARTICLES COMPRISING A BIODEGRADABLE POLYMER CONTROLLING THE RELEASE OF AN ANTIMALARIA ACTIVE PRINCIPLE, PHARMACEUTICAL COMPOSITIONS COMPRISING IT AND PROCESS FOR ITS PREPARATION Jose Pirson Philippe Bontemps, Jean-Bernard Falmagne, Robert Jerome, Philippe Teyssie, Luc Delattre, Brigitte Evrard. Xhendremael, Bel- gium assigned to Ire-Celltarg S A The present invention relates to microparticles containing an active principle against malaria, such as primaquine, one of its amino acid derivatives, or their conjugates with a hepatotro- pic vector or their pharmaceutically acceptable salts, and a biocompatible and biodegradable polymer controlling the kinetics of release of the active principle, like (DL)polylactide. The inven- tion also relates to pharmaceutical compositions comprising microcapsules according to the in- vention. Lastly, the invention relates to pro- cesses for the preparation of microparticles as mentioned above, the processes comprising: dis- solving the polymer in a volatile solvent, adding to this solution the active principle and possibly a substance regulating the size of the micro- particles, and at the end of evaporation, recovering the microparticles by centrifugation and filtration. 4897398 HYDROCHLORIDES OF CHLORIDES OF 2-AMINOALKYL- 9-HYDROXY ELLIPTICINIUM DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM Pierre Gros, Emili Crisafulli, Gu Mazue, Mont- pellier, France assigned to Sanofi; Centre Na- tional de la Recherche Scientifique (C N R S The invention relates to the 2-aminoalkyl-9 hydroxyellipticinium chloride hydrochloride of formula: See Patent for Chemical Structure in which Z represents hydrogen or a lower alkyl group, Alk represents a lower alkylene group and Am represents a di(lower alkyl)amino, pyrrolidino or piperidino group. These com- pounds are useful as antitumour agents. 4897399 HETEROTERTRACYCLIC LACTAM DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHOD OF TREATING IMPAIRED MEMORY AND LEARNING Jan W F Wasley assigned to Ciba-Geigy Corp Disclosed are the compounds of formula I: See Patent for Chemical Structure (I) wherein R l-R3

Transcript of 4897270 Pharmaceutical compositions

Page 1: 4897270 Pharmaceutical compositions

New Patents

High oil phase pharmaceutical vehicles in the form of an emulsion system having an oil phase content of from about 35% to about 65%, wherein the emulsion system comprises from ab- out 1~ to about 13~ of an aikylated PVP copolymer, from about 1~o to about 70/0 of an emulsifier, and a solvent system. The solvent sys- tem comprises from about 4~o to about 18~o of a C4-C22 fatty acid, alcohol or ester thereof, from about 2~o to about 25~/o of a glycol ester or diester, and from 0°~ to about 13%o of a branched chain ester of a C4-C22 carboxylic acid. The pharmaceutical vehicles are useful in sunscreen formulations, and especially those containing higher concentrations of benzophenone-3. When such higher concentrations are used, it is advantageous to add up to about 10~'/o of a branched chain ester of a C4-C22 carboxylic acid.

4897270

PHARMACEUTICAL COMPOSITIONS

David S Deutsch, Jamshed Anwar, London, United Kingdom assigned to Glaxo Group Limited

A pharmaceutical tablet is described which com- prises a tablet core containing the antibiotic cefuroxime axetil and a film coat which serves to mask the bitter taste of the cefuroxime axetil upon oral administration. It has been found that conventional film-coated tablets reduce the bio- availability of cefuroxime axetil and the inven- tion overcomes this by control of the film coat rupture time and use of a tablet core which dis- integrates immediately following rupture of the film coat.

4897267

MICROPARTICLES COMPRISING A BIODEGRADABLE POLYMER CONTROLLING THE RELEASE OF AN ANTIMALARIA ACTIVE

PRINCIPLE, PHARMACEUTICAL COMPOSITIONS COMPRISING IT

AND PROCESS FOR ITS PREPARATION

Jose Pirson Philippe Bontemps, Jean-Bernard Falmagne, Robert Jerome, Philippe Teyssie, Luc Delattre, Brigitte Evrard. Xhendremael, Bel- gium assigned to Ire-Celltarg S A

The present invention relates to microparticles containing an active principle against malaria, such as primaquine, one of its amino acid derivatives, or their conjugates with a hepatotro- pic vector or their pharmaceutically acceptable salts, and a biocompatible and biodegradable polymer controlling the kinetics of release of the active principle, like (DL)polylactide. The inven- tion also relates to pharmaceutical compositions comprising microcapsules according to the in- vention. Lastly, the invention relates to pro- cesses for the preparation of microparticles as mentioned above, the processes comprising: dis- solving the polymer in a volatile solvent, adding to this solution the active principle and possibly a substance regulating the size of the micro- particles, and at the end of evaporation, recovering the microparticles by centrifugation and filtration.

4897398

HYDROCHLORIDES OF CHLORIDES OF 2-AMINOALKYL-

9-HYDROXY ELLIPTICINIUM DERIVATIVES AND PHARMACEUTICAL

COMPOSITIONS CONTAINING THEM

Pierre Gros, Emili Crisafulli, Gu Mazue, Mont- pellier, France assigned to Sanofi; Centre Na- tional de la Recherche Scientifique (C N R S

The invention relates to the 2-aminoalkyl-9 hydroxyellipticinium chloride hydrochloride of formula: See Patent for Chemical Structure in which Z represents hydrogen or a lower alkyl group, Alk represents a lower alkylene group and Am represents a di(lower alkyl)amino, pyrrolidino or piperidino group. These com- pounds are useful as antitumour agents.

4897399

HETEROTERTRACYCLIC LACTAM DERIVATIVES,

PHARMACEUTICAL COMPOSITIONS, AND METHOD

OF TREATING IMPAIRED MEMORY AND LEARNING

Jan W F Wasley assigned to Ciba-Geigy Corp

Disclosed are the compounds of formula I: See Patent for Chemical Structure (I) wherein R l-R3