viii New Patents

4865849

TABLET FOR PHARMACEUTICAL USE ABLE TO RELEASE ACTIVE SUBSTANCES AT SUCCESSIVE

TIMES

Ubaldo Conte, Aid La Manna, Paol Colombo, Busto Arsizio, Italy assigned to Pharmidea

A tablet for pharmaceutical use able to release active substances at successive times, comprising at least; a first layer containing a portion of the active substance with suitable excipients, a bar- rier layer of polymer material gellable and/or soluble in water and/or aqueous liquids, which is interposed between said first layer and a third layer containing the remaining portion of active substance with suitable excipients, said barrier layer and said third layer being housed in a casing consisting of polymer material im- permeable and insoluble in water or soluble in an alkaline environment. That part of the active substance not inserted in the casing is im- mediately available for dissolving, whereas the part inserted in the casing is available only after dissolution or rupture of the barrier layer and/or after solubilization of the casing.

4865851

PHARMACEUTICAL COMPOSITION COMPRISING

CEFUROXIME AXETIL

pounds to desired sites in the body, e.g. skeletal muscle or the heart. The pharmaceutically active compound can be a protease inhibitor, a cardioactive drug for combating arrythmia, etc. The linkage is chemical through one or more alcohol, carboxyl or amine groups using rea- gents such as glutaraldehyde, dicarboxylic acid anhydrides and acid halides and carbodiimides. Carnitine derivatives are also incorporated into liposomes which are then used as carriers of ac- tive pharmaceutical agents.

4866044

SOLUBILIZED COMPOSITION OF POORLY-SOLUBLE

PHARMACEUTICAL PRODUCT

Jun Sato, Katsumi Matsuzaki, Yoshiharu Mat- sukura, Hyogo, Japan assigned to Takeda Chemical Industries Ltd

3-(n-Octadecylcarbamoyloxy) 2- methoxypropyl 2-thiazolioethyi phosphate solubilized with use of a salt of salicyclic acid or/and a salt of a bile acid can be administered by stable injection without causing precipitation. A composition containing a reducing sulfur com- pound or a sequestering agent besides the above mentioned ingredients can be stored for a long term even at room temperature as well as a cold place.

4866062

Michael James, Leonard Elliott, Bishop's Stort- ford, United Kingdom assigned to Glaxo Group Limited

Cefuroxime axetil in particulate form is coated with an integral coating of a lipid or mixture of iipids which serves to mask the bitter taste of cefuroxime axetil but disperses or dissolves on contact with gastrointestinal fluid. The resulting particles may be incorporated into pharma- ceutical compositions for oral administration, for instance aqueous suspensions.

1,4-DISUBSTITUTED PIPERAZINES,

PHARMACEUTICAL COMPOSITIONS THEREOF AND

METHOD OF USE

Edi Toth, Bel Kiss, Jozsef Turley, Eva Palosi, Istvan Hajdu, Laszlo GrooDora Szporny, Erz- sebet Lapis, Istvan Laszlovszky, Budapest, Hungary assigned to Richter Gedeon Vegyeszeti Gyar

4866040

AMINOCARNITINE DIRECTED PHARMACEUTICAL AGENTS

Alfred Stracher, Leo Kesner

Carnitine, aminocarnitine and cysteic acid serve as carriers to bring pharmaceutically active corn-

The invention relates to novel 1,4-disubstituted piperazine derivatives of the general formula (I), pharmaceutically acceptable acid addition salts thereof, pharmaceutical compositions con- taining them and a process for their preparation. In the general formula (I) See Patent for Chem- ical Structure (I) See Patent for Tabular Presentation RI and R2 are the same or different and stand for hydrogen or halogen or a lower alkyl, trihalomethyl or lower alkoxy group. The