Pharmaceutical compositions containing at least one NSAID having increased bioavailability

DETAILED DESCRIPTION OF THE INVENTION The incorporation of Piperine, its metabolites or structural analogues or isomers thereof with NSAIDs particularly Nimesulide or derivatives thereof results in a synergistic composition having unexpected increased bioavailability of NSAIDs particularly Nimesulide and derivatives thereof.
Therefore the invention does not involve simple mixing of the components.
It is also to be noted that Piperine or has no pharmacological properties but when mixed with NSAIDs particularly Nimesulide or derivatives thereof results in a synergistic effect on said NSIADs particularly Nimesulide causing enhanced activity and bio-availibilty thereof.
Piperine, (E, E) 1-[5-(1,3-benzodioxyl-5-yl)-1-oxo-2,4-pentadenyl] piperidine is the main constituent of many Piper species.
It is mostly obtained from Piper longum (3-5%) or Piper nigrum (3-9%) which are cultivated commercially.
Piperine has the formula: ##STR2## Examples of its metabolites are as follows: ##STR3## Piperine as a parent molecule and/or one or more of its metabolites and/or analogues thereof may have a role in enhancing bio-availability of drugs.
Examples of Piperine analogues are derivatives in which the piperidine ring is substituted, e.
g.
by an amino group, or esters (e.
g.
C.
sub.
1-6 alkyl esters) of metabolites containing an OH group.
Piperine forms monoclinic prisms from ethanol mp 130.
degree.
C.
It is tasteless at first but induces a burning sensation after a few seconds.
It is neutral to litmus (pKa 12.
22).
It is soluble in benzene, chloroform, ether, ethyl acetate, dichloromethane, alcohol, acetic acid and insoluble in water, pet.
ether.
On alkaline hydrolysis it furnishes a base piperidine and the acid viz.
piperic acid, mp 216.
degree.
C.
It may be synthesized by condensing the two components under proper conditions.
It has the following spectral characteristics: UV (methanol): max 340 mu (32,000).
IR(KBr): 1633, 1610, 1580, 1510, 1440, 1250, 1190, 1130, 1030, 995, 930, 842 cm.
sup.
-1.
Piperine is commercially available