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    OPIOID ANALGESIC PREPARATION OF SOLID AND AT LEAST TWO-PHASE AND ITS PRODUCTION
    1.
    发明专利
    OPIOID ANALGESIC PREPARATION OF SOLID AND AT LEAST TWO-PHASE AND ITS PRODUCTION 失效

    公开(公告)号：JPH10251149A

    公开(公告)日：1998-09-22

    申请号：JP6096198

    申请日：1998-03-12

    Applicant: BASF AG

    Inventor： BERNDL GUNTHER DR ,  ROSENBERG JOERG DR ,  BREITENBACH JOERG DR

    IPC: A61K9/00 ,  A61K9/24 ,  A61K9/52 ,  A61K31/485

    Abstract: PROBLEM TO BE SOLVED: To obtain a preparation capable of satisfying both to rapidly raise the level of an active ingredient and to slowly release the active ingredient by including opioids in two or more solid phases, respectively, and specifying the releasing amounts of the opioids. SOLUTION: A solid material comprising two or more phases is formed, and at least one kind of opioid is added to the matrix of each phase. The releasing amount (measured by the detection of UV light at 270nm by a ph. Eur. paddle method at 100rpm in a 0.1 hydrochloric acid at 37 deg.C) in a test tube is controlled to >=50wt.% after 1hr. The releasing amount is preferably controlled to 55-80wt.% after 1hr, 58-85wt.% after 2hr, 60-95wt.% after 4hr, and 65-100wt.% after 8hr. The two or more phases are preferably divided into rapidly releasing phases and slowly releasing phases in dependence on the differences of the individual matrix compositions. The opioid is preferably hydromorphone, morphine, tramadol, etc.

    PRODUCTION OF SOLID MEDICINE MOLDING
    2.
    发明专利
    PRODUCTION OF SOLID MEDICINE MOLDING 失效

    公开(公告)号：JPH1057450A

    公开(公告)日：1998-03-03

    申请号：JP19539097

    申请日：1997-07-22

    Applicant: BASF AG

    Inventor： ZETTLER HANS DIETER ,  SCHIESL MICHAEL ,  BREITENBACH JOERG DR ,  ROSENBERG JOERG DR

    IPC: A61J3/10 ,  A61J3/06 ,  A61K9/20 ,  B30B11/22

    Abstract: PROBLEM TO BE SOLVED: To embody an easy and cost effective process for producing solid medicine moldings particularly to specified shapes by dividing extrudate to molded goods in a first stage and rounding these molded goods in a plastic state in a second stage. SOLUTION: A mixture composed of a polymer/active component for production of tablets is produced by a simultaneously rotating two-screw extrusion molding machine. The plastic compsn. is extruded and is received by a circulating belt conveyor. A sensor operates a cutting device when the sensor checks the start point of the extrudate. The columnar molded goods 13 are temporarily stored in a collector 18 and are, in succession, supplied through a drilling slide gate 20 to a rounding tool 21. An arc-shaped driver 22 supports and moves the molded goods 13 during this time and rotates the molded goods round the longitudinal axis. The flat ends of the molded goods pass the heated rounding tool during this time. Two metallic jaws are moved in the same direction as the direction of the longitudinal axis of the molded goods 13 and the center of the dents of the segment type of a spherical shape is arranged on the longitudinal axis.

    PRODUCTION OF SLAT OF PHARMACEUTICALLY ACTIVE MATERIAL
    4.
    发明专利
    PRODUCTION OF SLAT OF PHARMACEUTICALLY ACTIVE MATERIAL 失效

    公开(公告)号：JPH1072400A

    公开(公告)日：1998-03-17

    申请号：JP16085497

    申请日：1997-06-18

    Applicant: BASF AG

    Inventor： BREITENBACH JOERG DR ,  ROSENBERG JOERG DR ,  NEUMANN JOERG DR ,  ZEIDLER JUERGEN DR ,  SIMON DIRK DR ,  DIENER RALPH DR

    IPC: A61K31/19 ,  A61K9/16 ,  A61K31/00 ,  B01J19/00 ,  C07C51/41 ,  C07C57/30 ,  C07C229/26

    Abstract: PROBLEM TO BE SOLVED: To provide a method for producing a salt of a pharmaceutically active material without lowering a quality, especially fluidity by reacting an acid with a base in a molten liquid so that the acid may be reacted with at least stoichiometric amount of the base in an extruder. SOLUTION: The objective salt of a pharmaceutically active material is obtained by reacting (A) a carboxylic acid with (B) a base in a molten liquid so that the acid may be reacted with at least stoichiometric amount of the base in an extruder. The method is preferably used for production of a salt of a derivative of salicylic acid, e.g. acetylasalicylic acid, or an arylcarboxylic acid, e.g. diclofenac, tolmetin or zomepirac. A basic α-aminocarboxylic acid, especially ricin, a base of an alkali(ne earth) metal, etc., are preferable as the component B. The amount of the above base is at least stoichiometric amount, preferably 1-40mol% excess based on the acid.

    PRODUCTION OF SOLID PREPARATION
    6.
    发明专利
    PRODUCTION OF SOLID PREPARATION 失效

    公开(公告)号：JP2000128775A

    公开(公告)日：2000-05-09

    申请号：JP29149199

    申请日：1999-10-13

    Applicant: BASF AG

    Inventor： KOTHRADE STEPHAN DR ,  BREITENBACH JOERG DR ,  KRULL HARALD ,  KESSLER THOMAS ,  LANGE ARMIN ,  MAIER WERNER ,  REINHOLD ULRICH

    IPC: A61K9/16 ,  A61K9/20 ,  A61K31/192

    Abstract: PROBLEM TO BE SOLVED: To prepare solid preparations where a high molecular weight polymeric binder can be employed and the delayed release of an active ingredient is made possible by producing a plastic mixture of a specific polymeric binder, medicament active principle or the like under a specific condition and by molding the mixture so as to have a necessary dosage form. SOLUTION: The objective preparations are prepared by producing a plastic mixture of at least one kind selected from pharmaceutically acceptable polymeric binders having >75 K value (preferably homopolymer or a copolymer from vinylpyrrolidone) and at least one kind selected from medicament active principles, (e.g. ibuprofen or the like) and, optionally, a customary adjuvant under the condition of temperature (preferably

    MANUFACTURE OF AT LEAST TWO-PHASE SOLID BLENDED MEDICINE SHAPE AND THIS BLENDED MEDICINE SHAPE
    7.
    发明专利
    MANUFACTURE OF AT LEAST TWO-PHASE SOLID BLENDED MEDICINE SHAPE AND THIS BLENDED MEDICINE SHAPE 失效

    公开(公告)号：JPH10314279A

    公开(公告)日：1998-12-02

    申请号：JP6095798

    申请日：1998-03-12

    Applicant: BASF AG

    Inventor： ZEIDLER JUERGEN DR ,  ROSENBERG JOERG DR ,  BREITENBACH JOERG DR ,  KLEINKE ANDREAS DR ,  MAIER WERNER

    IPC: A61J3/10 ,  A61K9/20 ,  A61K47/26 ,  A61K47/30 ,  B30B11/16

    Abstract: PROBLEM TO BE SOLVED: To manufacture a solid blended medicine shape in a large variation width by housing a solid preparation in a plastic material, and containing a single active substance in melt and/or the preparation when a medicine shape is molded from the melt composed of a high molecular weight binding agent. SOLUTION: Melt composed of a high molecular weight binding agent (for example, alkyl cellulose, hydroxyalkyl cellulose or the like) and an-active substance is molded. When this is molded, a single solid preparation containing the active substance is put in a plastic material. In a molding process, metal mold rollers 1 and 2 are rotated in the opposite direction, and a strand 3 from an extruder is composed of an active substance containing high molecular weight binding agent, and is sent into the two rollers 1 and 2 in the arrow direction. At the same time, melt composed of an active substance containing high molecular weight binding agent B is sent into a recess of the roller 1 from a supply device 4. Since the roller 1 is cooled, the melt immediately coagulates. A tablet is punched from the strand 3 by opposite directional rotation of the rollers 1 and 2.

    10.
    发明专利
    未知

    公开(公告)号：DE19629753A1

    公开(公告)日：1998-01-29

    申请号：DE19629753

    申请日：1996-07-23

    Applicant: BASF AG

    Inventor： ZETTLER HANS DIETER ,  SCHIESL MICHAEL ,  BREITENBACH JOERG DR ,  ROSENBERG JOERG DR

    IPC: A61J3/10 ,  A61J3/06 ,  A61K9/20 ,  B30B11/22

    Abstract: Production of solid medicament comprises mixing and melting at least one polymeric binder, at least one pharmaceutical active agent (A) and optionally conventional additives, in the absence of solvents, to give a plastic mixture and shaping the mixture by extrusion. The shaping is carried out in two stages: (i) dividing the extrudate into shaped articles; and (ii) rounding the articles while in a plastic state.

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