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Effect of Cyclodextrin Complexation on the Pharmacokinetic and Biopharmaceutical Properties of Meloxicam

Very Rapid Onset of Action
The novel formulation of meloxicam / ß-cyclodextrin inclusion complex makes meloxicam immediately bioavailable. Upon administration, an association-dissociation equilibrium is rapidly established with free individual meloxicam molecules readily available for absorption (in contrast to clumping which usually occurs with conventional tablet and capsule forms).

CD.M CD + M
meloxicam / ß-cyclodextrin inclusion complex
  ß-cyclodextrin molecule
  single meloxicam molecule

Single meloxicam melocules are instantaneously absorbed and the equilibrium is rapidly shifted to the right hand side.

Enhancement of the Pharmacological Effect
As with a rapid onset of action, the administration of meloxicam / ß-cyclodextrin inclusion complex increases the intensity of therapeutic effects. This is greatly noticed by the patients as a rapid relief of symptoms such as pain and inflammation.


Gastroprotective Effect

As each meloxicam molecule is included within the cavity of a ß-cyclodextrin molecule, thus eliminating the direct irritant local effect on the GIT linings. This is reflected by a fewer patients complaints regarding GI adverse effects.


 
 
 
 
 
 
 
 
 
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