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, LOMBARDI BORGIA S, SFORZINI A, BERGAMANTE V, CESCHEL GC, FINI A., et al. (2004). Mucoadhesive tablets for buccal administration containing sodium nimesulide. DRUG DELIVERY, 11, 225-230 [10.1080/10717540490446017].
Mucoadhesive tablets for buccal administration containing sodium nimesulide.
MAFFEI, PAOLA;LOMBARDI BORGIA, SIMONE;SFORZINI, ANNALISA;BERGAMANTE, VALENTINA;CESCHEL, GIANCARLO;FINI, ADAMO;
2004
Abstract
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 drugI documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.