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.
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.
Abstract:
Verfahren zur Herstellung von Salzen von Säuregruppen tragenden pharmazeutischen Wirkstoffen durch Umsetzung der Carbonsäuren mit einer Base in der Schmelze, indem man die Säuren mit einer mindestens stöchiometrischen Menge einer Base im Extruder umsetzt.
Abstract:
Preparation of a salt of a pharmaceutically active carboxylic acid compound comprises reacting the acid in an extruder with ≥ 1 stoichiometric equivalent of a base in melt form.
Abstract:
The invention concerns solid medicaments obtained by extrusion with subsequent shaping of a solvent-free melt, containing in addition to one or a plurality of active substances: A) between 10 and 90 wt.% of a thermoplastically processable water-soluble polymer; B) between 5 and 85 wt.% isomalt; and C) between 0 and 5 wt.% lecithin, the total of all the contents equalling 100 wt.%.