Orally dosed pharmaceutical compositions comprising a delivery agent in micronized form

Abstract

Solid pharmaceutical compositions and methods of their use suitable for the oral delivery of pharmacologically active agents, e.g. peptides, comprising a therapeutically-effective amount of a pharmacologically active agent; a crospovidone or povidone; and a delivery agent for said pharmacologically active agent are disclosed. The compositions utilize micronized forms of the delivery agent which provides enhanced bioavailability of pharmacologically active agents, particularly calcitonin.

1 . A solid pharmaceutical composition suitable for the oral delivery of a pharmacologically active agent comprising 
 a. a therapeutically-effective amount of a pharmacologically active agent;    b. pharmaceutically acceptable inactive excipients, and    c. a delivery agent for said pharmacologically active agent, wherein said delivery agent is in micronized form.    
   
   
       2 . A composition according to  claim 1  wherein the active agent is a peptide.  
   
   
       3 . A composition according to  claim 2  wherein the peptide is a calcitonin.  
   
   
       4 . A composition according to  claim 3  wherein the calcitonin is salmon calcitonin.  
   
   
       5 . A composition according to  claim 1  wherein said inactive excipients are selected from the group consisting of crospovidone and povidone.  
   
   
       6 . A composition according to  claim 1  wherein the delivery agent is selected from the group consisting of 5-CNAC, SNAD, and SNAC.  
   
   
       7 . A composition according to  claim 1  wherein the delivery agent is selected from the group consisting of a disodium salt of 5-CNAC, a disodium salt of SNAD, and a disodium salt of SNAC.  
   
   
       8 . A composition according to  claim 1  which additionally includes a diluent.  
   
   
       9 . A composition according to  claim 8  wherein the diluent is microcrystalline cellulose.  
   
   
       10 . A composition according to  claim 1  which additionally includes a lubricant.  
   
   
       11 . A composition according to  claim 10  wherein the lubricant is magnesium stearate.  
   
   
       12 . A method for enhancing the oral bioavailability of a pharmacologically active agent, said method comprising administering to a patient in need of a pharmacologically active agent, an effective amount of a pharmaceutical composition according to  claim 1 .  
   
   
       13 . A method of treatment of bone related diseases and calcium disorders comprising administering to a patient in need of such treatment a therapeutically effective amount of a composition according to  claim 1 , wherein said pharmacologically active agent is a bone active agent.  
   
   
       14 . A method according to  claim 13 , wherein said pharmacologically active agent is calcitonin.  
   
   
       15 . A method according to  claim 14  wherein said calcitonin is salmon calcitonin.  
   
   
       16 . (canceled)