Effect of iontophoresis and penetration enhancers on transdermal absorption of metopimazine.
BACKGROUND
Metopimazine is an antiemetic drug already used by oral and rectal administration. It would be interesting to develop a new formulation for a transdermal administration.


OBJECTIVE
The objective of this study was to determine the influence of iontophoresis on the metopimazine transdermal absorption and the possible synergistic enhancement with chemical enhancers.


METHODS
Transdermal transport of metopimazine was studied in vitro in a Franz cell with pig skin according to the following protocol: 1h of iontophoresis followed by 7h of passive diffusion. Different current densities were applied: 0, 0.125, 0.25 and 0.5 mA/cm(2). Chemical enhancers used as solvent dilution were ethanol, propylene glycol and isopropyl myristate. Metopimazine was assayed by HPLC. Fourier transform infrared spectroscopy was used to determinate the interaction between chemical enhancers and stratum corneum.


RESULTS
The iontophoresis has increased the percutaneous absorption of metopimazine and has decreased the lag time with 3.85+/-0.90 microg/(cm(2)h) and 1.9h for 0.5 mA/cm(2) and with 0.27+/-0.20 microg/(cm(2)h) and >8h for passive diffusion. Transdermal transport has been increased with current density and with isopropyl myristate and was not modified by ethanol or propylene glycol.


CONCLUSIONS
Results indicated that iontophoresis is an effective method for transdermal administration of metopimazine.
Bounoure
Frédéric
F
Laboratoire de Pharmacie Galénique, ADEN EA 3234, Faculté de Médecine Pharmacie, 22 bd Gambetta, 76136 Rouen Cedex, France.
Lahiani Skiba
Malika
M
Besnard
Madeleine
M
Arnaud
Philippe
P
Mallet
Eric
E
Skiba
Mohamed
M
D000818:Animals; D000932:Antiemetics / Q000493:pharmacokinetics*; D000431:Ethanol / Q000494:pharmacology; D007478:Iontophoresis; D007540:Isonipecotic Acids / Q000493:pharmacokinetics*; D019946:Propylene Glycol / Q000494:pharmacology; D012869:Skin Absorption; D017550:Spectroscopy, Fourier Transform Infrared; D013552:Swine
D000932:Antiemetics; D007540:Isonipecotic Acids; C005260:metopimazine; D000431:Ethanol; D019946:Propylene Glycol