Mucoadhesive tablets for buccal administration containing sodium nimesulide.
The possibility of improving the flux of nimesulide across the buccal mucosa using the drug in the form of a sodium salt was investigated in our study. The salt form may increase to flux across buccal membrane, starting from a suspension; its lower permeation coefficient is compensated by a higher concentration gradient. The salt was inserted into a mucoadhesive tablet for buccal administration. The tablets were designed to prevent the loss of the drug into the saliva by means of a protective layer and placed on the area not in contact with the mucosa. Ten volunteers were used. The in vitro release from mucoadhesive tablets was examined through a porcine buccal mucosa, using a standard Franz cell, modified for present purposes. The advantages of a higher concentration gradient for the flux, related to a higher solubility of the salt, and to a sufficiently high permeation coefficient of the drug, despite the ionized form, could not be completely exploited, because the composition of the formulation destroys the chemical form of the drug.
Maffei
P
P
Pharmaceutical Sciences Department, University of Bologna, Bologna, Italy.
Lombardi Borgia
S
S
Sforzini
A
A
Bergamante
V
V
Ceschel
G C
GC
Fini
A
A
Ronchi
C
C
D000269:Adhesives / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D000278:Administration, Buccal; D000818:Animals; D002626:Chemistry, Pharmaceutical; D008297:Male; D009061:Mouth Mucosa / Q000187:drug effects* / Q000378:metabolism; D012972:Sodium Hydroxide / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D013449:Sulfonamides / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D013552:Swine; D013607:Tablets
D000269:Adhesives; D013449:Sulfonamides; D013607:Tablets; D012972:Sodium Hydroxide; C012655:nimesulide