Abstract:
A medicament core which contains a super disintegrant or an effervescent couple including a foaming agent and a pharmaceutically acceptable acid activator, which core is partially covered by preformed shell coverings shaped to expose at least a part of the core for activation upon exposure to bodily fluids.

Description:
CROSS-REFERENCE TO RELATED APPLICATIONS 
       [0001]    This application claims priority under 35 U.S.C. § 119(e) on U.S. Provisional Application No. 60/609,313 entitled QUICK DISSOLVE CAPSULE AND METHOD OF MANUFACTURING, filed on Sep. 13, 2004, by Ronald L. Perry et al., the entire disclosure of which is incorporated herein by reference. 
     
    
     BACKGROUND OF THE INVENTION 
       [0002]    The present invention relates to a press-fit fast release caplet having gelatin covered ends leaving an uncovered center band. 
         [0003]    Gelatin covered caplets have become a popular dosage form for medicaments and provide tamper-resistant safety as well as easy swallowability. Several methods have evolved for the gelatin covering of caplets, including the dip-coating of caplets with a gelatin solution, the encapsulating of gelatin capsules utilizing an encapsulation machine and process as disclosed in U.S. Pat. No. 6,209,296 and in copending U.S. patent application Ser. No. 10/899,924, filed on Jul. 27, 2004, entitled TABLET ENCAPSULATING MACHINE. Also, caplets have been employed in which gelatin shells are hydrated and subsequently shrink-fitted onto a caplet to provide a caplet core which is fully enclosed by gelatin capsule shells. U.S. Pat. Nos. 5,415,868 and 5,824,338 are examples of such dosage forms. 
         [0004]    In order for a medicament to enter the bloodstream of a patient, it is necessary for the gelatin covering of gelatin covered medicaments to dissolve, typically in the stomach, which takes a certain period of time before the medicament can effectively be assimilated by the person&#39;s body. Although uncoated medicaments are faster acting, they tend to be less easily swallowed than medicaments having a gelatin covering. 
         [0005]    It would be desirable, therefore, to provide a medicament which has the ease of swallowability of a gelatin-covered caplet and yet the relatively rapid release of medicament as in uncoated caplets. 
       SUMMARY OF THE INVENTION 
       [0006]    The medicament of the present invention and its method of manufacture solves this need by providing a medicament core which contains a super disintegrant or an effervescent couple including a foaming agent and a pharmaceutically acceptable acid activator, which core is partially covered by a gelatin covering such that at least a part of the core is exposed for activation upon exposure to bodily fluids. 
         [0007]    In the preferred embodiment of the invention, the medicament core is a caplet shaped core with gelatin capsule shells press-fit from opposite ends thereof, leaving a gap exposing the core between the facing ends of the gelatin capsule shells. Also in the preferred embodiment of the invention, the gelatin capsule shells are press-fit onto opposite ends of the caplet core, leaving a gap of from about 3 to about 4 mm between the facing ends of the gelatin capsule shells. The medicament, therefore, provides a gelatin covering for at least part of the medicament and an exposed core which causes the caplet to split and rapidly dissolve to release its active ingredients before the gelatin dissolves, resulting in a quick accessibility of the medicament to the patient. 
         [0008]    These and other features, objects and advantages of the present invention will become apparent upon reading the following description thereof together with reference to the accompanying drawings. 
     
    
     
       BRIEF DESCRIPTION OF THE DRAWINGS  
         [0009]      FIG. 1  is an exploded perspective view of a medicament embodying the present invention; 
           [0010]      FIG. 2  is a top plan view of the assembled medicament shown in  FIG. 1 ; 
           [0011]      FIG. 3  is an end view of one of the gelatin capsule shells; 
           [0012]      FIG. 4  is a block diagram of the method of manufacturing the medicament shown in  FIGS. 1 and 2 ; 
           [0013]      FIG. 5  is an exploded perspective view of an alternative form of a medicament embodying the present invention; and 
           [0014]      FIG. 6  is a side elevational view of the medicament of  FIG. 5 . 
       
    
    
     DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENT 
       [0015]    Referring initially to  FIG. 1 , there is shown a medicament  10  embodying the present invention which is in the form of caplet-shaped core  12 , a first gelatin capsule shell  14 , and a second gelatin capsule shell  16  for partially encapsulating the core  12 . As seen in  FIG. 2 , the capsule shells  14  and  16  do not abut when press-fitted onto core  12  but rather leave a gap having a width identified by the dimension X in  FIG. 2  of from about 3 to 4 mm exposing the core to bodily fluids when the medicament is taken by a patient. The capsule shells  14  and  16  are conventional gelatin capsules which are commercially available but which are shorter than a typical capsule shell to leave the exposed peripheral band  15  of core  12 , as seen in  FIG. 2 . 
         [0016]    In one embodiment of the invention, the core  12  had an overall length of about 0.85 inches, with each capsule shell  14  and  16  having a length indicated by dimensions A and B in  FIG. 2  of about 0.356 inches. Band  15 , dimension “X” in this embodiment, was about 0.138 inches. Although capsule shells  14 ,  16  are preferably of equal length, they could be of different lengths, thus shifting the peripheral band  15  along the longitudinal axis of the core  12 . Core  12  can contain any desired active ingredient as the medicament. As an example only, the core  12  may contain an analgesic including non-steroidal anti-inflammatory drugs (NSAIDs) including but not limited to aspirin, ibuprofen, acetaminophen, naproxen sodium, and the like, or combinations of such medicaments with antihistamines such as chlorpheniramine maleate, dextromethorphan, pseudoephedrine, or anti-tussive agents. The medicament of core  12 , however, is not limited to these specific examples. In addition to the active ingredients and typical excipients and binders for compactability, core  12  also includes one of a super disintegrant or an effervescent couple typically comprising a foaming agent, such as bicarbonate of soda, and a pharmaceutically acceptable acid activator, such as citric acid. Examples of core materials are given below: 
       EXAMPLE 1 
       [0017]      
         [0000]    
       
         
               
               
               
               
             
               
               
               
               
             
           
               
                   
                   
               
               
                   
                 Ingredients 
                 mg/tab 
                 % 
               
               
                   
                   
               
             
             
               
                   
               
             
          
           
               
                   
                 APAP Compap Course L 
                 555.500 
                 88.174603 
               
               
                   
                 (90% acetaminophen) 
               
               
                   
                 Copovidone S-630 
                 11.500 
                 1.825397 
               
               
                   
                 Crospovidone XL 
                 63.000 
                 10.000000 
               
               
                   
                   
               
             
          
         
       
     
       EXAMPLE 2 
       [0018]      
         [0000]    
       
         
               
               
               
               
             
               
               
               
               
             
           
               
                   
                   
               
               
                   
                 Ingredients 
                 mg/tab 
                 % 
               
               
                   
                   
               
             
             
               
                   
               
             
          
           
               
                   
                 APAP Compap Course L 
                 555.500 
                 87.757 
               
               
                   
                 (90% acetaminophen) 
               
               
                   
                 Microcryst Cellulose 
                 14.500 
                 2.291 
               
               
                   
                 Crospovidone XL 
                 63.000 
                 9.953 
               
               
                   
                   
               
             
          
         
       
     
       EXAMPLE 3 
       [0019]      
         [0000]    
       
         
               
               
               
               
             
               
               
               
               
             
           
               
                   
                   
               
               
                   
                 Ingredients 
                 mg/tab 
                 % 
               
               
                   
                   
               
             
             
               
                   
               
             
          
           
               
                   
                 APAP Compap Course L 
                 555.500 
                 81.811 
               
               
                   
                 (90% acetaminophen) 
               
               
                   
                 Microcryst Cellulose 
                 14.500 
                 2.135 
               
               
                   
                 Sod Bicarb #2 F-gran 
                 54.500 
                 8.027 
               
               
                   
                 Citric Acid Anhydrs 
                 54.500 
                 8.027 
               
               
                   
                   
               
             
          
         
       
     
       EXAMPLE 4 
       [0020]      
         [0000]    
       
         
               
               
               
               
             
               
               
               
               
             
           
               
                   
                   
               
               
                   
                 Ingredients 
                 mg/tab 
                 % 
               
               
                   
                   
               
             
             
               
                   
               
             
          
           
               
                   
                 APAP Compap Course L 
                 555.500 
                 77.910 
               
               
                   
                 (90% acetaminophen) 
               
               
                   
                 Microcryst Cellulose 
                 14.500 
                 2.034 
               
               
                   
                 Crospovidone XL 
                 34.000 
                 4.769 
               
               
                   
                 Sod Bicarb #2 F-gran 
                 54.500 
                 7.644 
               
               
                   
                 Citric Acid Anhydrs 
                 54.500 
                 7.644 
               
               
                   
                   
               
             
          
         
       
     
         [0021]    The core, as shown in  FIG. 4 , is manufactured in step  20  by a typical tableting press, which compresses the active and inactive ingredients into preferably an elongated caplet-shaped core  12 , as seen in  FIG. 1 , although other tablet forms may also be employed. Upon the forming of the core, typically it is coated with a hydroxy propylmethocellulose (HPMC) or hydroxy propocellulose (HPC) to provide a protective coating and add surface strength to the core for subsequent handling. The coating step  22  is typically accomplished by spray coating, pan coating, or the like. Subsequently, the capsule shell halves  14  and  16  are formed, as shown by step  24  in  FIG. 4 , typically by dip-coating pins in baths of gelatin to a depth (in one embodiment) of approximately 0.356 inches with an internal diameter as shown by dimension Y in  FIG. 3 , for a core of approximately 0.25 inches in diameter of about 0.256 inches +/−0.003 inches. The capsule shells  14 ,  16  will typically be of different colors which function to identify the type of medicament involved. 
         [0022]    The thickness of the capsule shells  14  and  16  is conventional. Shells  14  and  16  are subsequently press-fit onto the core  12  as illustrated by step  26  in  FIG. 4 , utilizing a commercially available press-fit machine, such as one available from I.M.A. North America Model No. Zanasi 70c. During the press-fitting process, the shortened capsule shells  14  and  16  leave the peripheral band  15 , as seen in  FIG. 2 , exposing the core  12  to the bodily fluids upon swallowing medicament  10 . This band  15  of exposed core rapidly dissolves under the influence of the super disintegrant or effervescent couple to break the medicament  10  into halves at the center location of band  15  prior to dissolving of gelatin core capsule shells  14  and  16 , thereby allowing the active ingredient contained within core  12  to be rapidly assimilated by the body for providing quick relief from symptoms for which the medicament is being taken. 
         [0023]    The exact dimensions of the caplet and gelatin capsule shells can be varied as long as they interfit with one another to press-fit or otherwise attach the capsule shell halves to the core in such a manner as the core includes an exposed area. Further, the medicament can be manufactured with an elongated capsule shell which leaves one end of the medicament exposed as opposed to a center band, although the center band is preferred. Further, other shapes of tablet cores may be employed with a suitable gelatin covering which exposes a sufficient surface area of the medicament such that the super disintegrant or effervescent couple will effectively release the active ingredients into the body more quickly than an entirely gelatin covered medicament. Also, capsule shell halves  14  and  16  can be made of materials other than gelatin. Such materials include inter alia polyvinyl alcohol, starches, alginates, acrylates, polyvinyl pyrrolidone, cellulose derivates, and polysiloxanes. 
         [0024]    Referring now to  FIGS. 5 and 6 , there is shown an alternative dosage form  30  which incorporates a conventional tablet-shaped core  32  which is conventionally press manufactured by compacting the pharmaceutical active ingredients and excipients, such as employed in the caplet-shaped core  12 . The core is partially covered by a pair of shells  34  and  36 , which are formed by a molding or stamping process generally in the shape of hemispheres which have truncated peripheral edges  35  and  37 , respectively, which leaves a gap identified by reference X in  FIG. 6  of from 3 mm to 4 mm for exposing the edge of core  32  to bodily fluids when administered. In order to adhere the shells  34 ,  36  to core  32 , a pharmaceutically acceptable adhesive  38 ,  39  is applied to the interior surface of the shells  34 ,  36  prior to the shells being placed over core  32  for adhering the shells to the core. The adhesive  38 ,  39  can be dots of liquid gelatin, which are appropriately placed within the shells or other pharmaceutically acceptable adhesive and may be applied by a dropper or other conventional methods for applying a liquid adhesive. Alternatively, an adhesive coating can be spray coated on the interior of the preformed gelatin shells  34 ,  36 , after which they are pressed onto the shell  32  on opposite sides thereof and allowed to dry. The shells  34 ,  36  may have a moisture content after forming which allows them to readily fit over core  32  and, upon curing the adhesive and drying the shells, they tend to shrink onto and assist the adhesive in holding the shells in tight engagement with the core  32 . Depending on the core shape, the generally hemispherical shells  34 ,  36  may include a dome section, such as  41  and  43 , respectively, and a vertically extending band section  42  and  45 , respectively, as shown in  FIG. 6 . The material of shells  34 ,  36  can be the same as that disclosed in the embodiment of  FIGS. 1-4 , as are the ingredients of the core  32 . As in the first embodiment shells  34 ,  36  may be of different colors to color code the type of medicament being partially covered by the shells. 
         [0025]    It will become apparent to those skilled in the art that various modifications to the preferred embodiments of the invention as described herein can be made without departing from the spirit or scope of the invention as defined by the appended claims.