4866040 aminocarnitine directed pharmaceutical agents

1
Gen. Pharmac. Vol. 21, No. 4, pp. i-xxiii, 1990 Pergamon Press pie. Printed in Great Britain NEW PATENTS This Section contains abstracts and, where appropriate, illustrations of recently issued United States patents and published patent applications filed from over 30 countries under the Patent Cooperation Treaty. This information was obtained from recent additions to the Pergamon PATSEARCH ~ online database in accordance with interest profiles developed by the Editors. Further information about Pergamon PATSEARCH ~ can be obtained from Pergamon Orbit InfoLine Inc., 8000 Westpark Drive, McLean, Virginia 22102 U.S.A. Copies of complete patents announced in thl ° Section are available from Pergamon Orbit InfoLine Inc. for $8 per copy. Payment with order is required. Orders outside North America add $2 for air postage. Order by patent number for Pergamon Orbit InfoLine only. 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 geilable 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 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 lipids 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. 4866O4O AMINOCARNITINE DIRECTED PHARMACEUTICAL AGENTS Alfred Stracher, Leo Kesner Carnitine, aminocarnitine and cysteic acid serve as carriers to bring pharmaceutically active com- 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-thiazolioethyl phosphate solubilized with use

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Page 1: 4866040 Aminocarnitine directed pharmaceutical agents

Gen. Pharmac. Vol. 21, No. 4, pp. i-xxiii, 1990 Pergamon Press pie. Printed in Great Britain

NEW PATENTS

This Section contains abstracts and, where appropriate, illustrations of recently issued United States patents and published patent applications filed from over 30 countries under the Patent Cooperation Treaty. This information was obtained from recent additions to the Pergamon PATSEARCH ~ online database in accordance with interest profiles developed by the Editors. Further information about Pergamon PATSEARCH ~ can be obtained from Pergamon Orbit InfoLine Inc., 8000 Westpark Drive, McLean, Virginia 22102 U.S.A.

Copies of complete patents announced in thl ° Section are available from Pergamon Orbit InfoLine Inc. for $8 per copy. Payment with order is required. Orders outside North America add $2 for air postage. Order by patent number for Pergamon Orbit InfoLine only.

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 geilable 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

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

lipids 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.

4866O4O

AMINOCARNITINE DIRECTED PHARMACEUTICAL AGENTS

Alfred Stracher, Leo Kesner

Carnitine, aminocarnitine and cysteic acid serve as carriers to bring pharmaceutically active com- 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-thiazolioethyl phosphate solubilized with use