Inhaler for basic pharmaceutical agents and method for the production thereof

Abstract

A device for the administration of basic active agents, such as nicotine, to the human or animal body. The active agents are administered by inhalation. The device comprises a first preparation containing a nicotine base or/and a further basic active agent and, a second or further preparations. At least one preparation contains at least one volatile acid suitable for inhalation.

1 . A device for the administration of basic active agents, particularly nicotine, to the human or animal body by inhalation, wherein said device 
 comprises a first preparation containing at least one of a nicotine base and another basic active agent; and    at least one additional preparation, at least one of said at least one additional preparation containing at least one volatile acid suitable for inhalation, wherein said device has a first air inlet aperture for air stream flow, a second air inlet aperture for air stream flow and an air outlet aperture, said air inlet apertures and said air outlet aperture having a conduit cross-section, wherein the air stream flowing in through the first inlet aperture predominantly flows over the said first preparation and that the air stream flowing in through the second inlet opening predominantly flows over said at least one additional preparation, the two air streams combining later in a common flow path and escaping from the device through said outlet aperture.    
     
     
         2 . The device according to  claim 1 , wherein said first preparation and said at least one additional preparation are applied at separate locations within the device.  
     
     
         3 . The device according to  claim 1 , wherein said first preparation contains at least one of a nicotine base and another basic active agent in combination with at least one solvent suitable for inhalation.  
     
     
         4 . The device according to  claim 1 , wherein said at least one volatile acid is contained in the preparation in combination with at least one solvent suitable for inhalation.  
     
     
         5 . The device according to  claim 1 , wherein said at least one volatile inhalable acid is selected from the group consisting of acetic acid, lactic acid, malic acid and propionic acid.  
     
     
         6 . The device according to  claim 1 , wherein said device releases said nicotine base and said at least one volatile acid during the inhalation process in approximately equimolar quantities from said first preparation and said at least one additional preparation.  
     
     
         7 . The device according to  claim 1 , wherein during an inspiration process, which lasts from 1to 10 seconds and which reaches a velocity of inspiration of 0.1 to 1 l/min, said device releases 5 to 250 μg of said nicotine base or of another basic active agent from said preparation into the inspired air.  
     
     
         8 . The device according to  claim 1 , wherein aerosol particles are formed in the internal space of said device during inhalation, and wherein the size of said particles is less than 10 μm.  
     
     
         9 . The device according to  claim 1 , wherein said preparation and said at least one additional preparation contain at least one further additive which is volatile and is suitable for inhalation.  
     
     
         10 . The device according to  claim 1 , wherein at least one of said nicotine base-containing preparation or acid(s)-containing preparation comprises a polymer matrix wherein the active agent or the acid(s) are contained in dissolved or dispersed form.  
     
     
         11 . The device according to  claim 10 , wherein the polymer matrix is based on polymers selected from the group consisting of polyethylenes, polypropylenes, silicone polymers (polydimethylsiloxanes) and poly(meth)acrylates.  
     
     
         12 . The device according to  claim 1 , wherein said device is at least partially, made from a material which is impermeable to the active agent(s).  
     
     
         13 . The device according to  claim 1 , wherein after production of said device and during storage of said device, said device is covered with a peelable protective layer which is impermeable to the basic active agent(s), to form a compartment containing the active agent(s) and a compartment containing the acid(s), both compartments being separated from each other in a gas-tight manner and being sealed from the ambient air.  
     
     
         14 . The device according to  claim 1 , wherein the conduit cross-sections of the air inlet apertures and of the air outlet aperture are dimensioned such that the negative differential pressure present in the oral cavity during the inspiration process is at most 300 Pa.  
     
     
         15 . The device according to  claim 1 , wherein said device comprises at least one formed part produced by deep-drawing wherein oblong recessions are provided for defining a first air supply channel and a second air supply channel, said first air supply channel and said second air supply channel being combined to form an air outlet channel.  
     
     
         16 . The device according to  claim 15 , wherein said device comprises an upper part and a bottom part, each formed by deep-drawing, said upper part and said bottom part being provided with said recessions and being connected with each other and being opposite one another to form said first air supply channel with an air inlet apertures, said second air supply channel with an air inlet aperture and an air outlet channel with an air outlet aperture.  
     
     
         17 . The device according to  claim 1 , wherein said first preparation is located in the oblong recess forming the first air supply channel, and said second preparation is located in the oblong recess forming the second air supply channel, wherein said first preparation and said at least one additional preparation are applied in the vicinity of the respective air inlet opening.  
     
     
         18 . A method for the production of a device according to  claim 1 , said method comprising the following steps: 
 producing a formed part by deep-drawing, said formed part comprising a first oblong, concave recess for receiving a first preparation, and a second oblong, concave recess for receiving a second preparation;    introducing a predetermined amount of said first preparation, containing a nicotine base or another basic active agent, into said first recess; and    introducing a predetermined amount of said second preparation, containing acid(s), into said second recess to produce a filled formed part.    
     
     
         19 . The method according to  claim 18 , wherein the filled formed part is covered with a peelable protective layer impermeable to the basic substance(s), such that a compartment containing the active agent(s) and a compartment containing the acid(s) are formed by the peelable layer, both compartments being separated from each other in a gas-tight manner and being sealed from the ambient air.  
     
     
         20 . The method according to  claim 18 , wherein during production of the formed part, said method further comprises forming a further oblong, concave recess by deep-drawing which is connected with said two other recesses and for forming an air outlet channel.  
     
     
         21 . The method according to  claim 20 , wherein the filled formed part is connected with a formed part serving as the upper part and having oblong recesses corresponding to those of said filled formed part, the respective, superimposed recesses forming a first air supply channel with an air inlet aperture, a second air supply channel with an air inlet opening, and an air outlet channel with an air outlet aperture.  
     
     
         22 . Use of an inhaler according to  claim 1  for smoking cessation or for smokeless satisfaction of the craving for nicotine in cases of situational necessity.  
     
     
         23 . Use of an inhaler according to  claim 1  for simultaneous inhalation of a basic active agent and one or more volatile acid compounds.  
     
     
         24 . The device according to  claim 3 , wherein said another basic active agent in combination with at least one solvent suitable for inhalation is ethanol.  
     
     
         25 . The device according to  claim 4 , wherein said at least one solvent suitable for inhalation is ethanol.  
     
     
         26 . The device according to  claim 7 , wherein said device releases 10 to 100 μg, of said nicotine base or of another basic active agent from said preparation into the inspired air.  
     
     
         27 . The device according to  claim 9 , wherein said at least one further additive which is volatile and is suitable for inhalation is menthol.  
     
     
         28 . The device according to  claim 12 , wherein said device is entirely made from a material which is impermeable to the active agent(s).  
     
     
         29 . The device according to  claim 12 , wherein said material which is impermeable to the active agent(s) is a polyester material which is coated with at least one of a copolymer of acrylonitrile and methacrylate, and a metal foil(s) or a combination of the mentioned materials.  
     
     
         30 . The device according to  claim 14 , wherein the conduit cross-sections of the air inlet apertures and of the air outlet aperture are dimensioned such that the negative differential pressure present in the oral cavity during the inspiration process is at most 200 Pa.