Optimized release of dexamethasone and gentamicin from a soluble ocular insert for the treatment of external ophthalmic infections.
In the case of external ophthalmic infections, repeated instillations of antibiotics are required to reach therapeutic level, above the minimal inhibitory concentration (MIC). An additional administration of a corticosteroid is often needed, in order to limit the precorneal damages caused by the infection. However, repeated administration of a corticosteroid can increase intraocular pressure and thus lead to glaucoma. To overcome the disadvantages of separated and repeated instillations of two products and to avoid the side effects of dexamethasone, a soluble insert containing gentamicin sulfate and dexamethasone phosphate was developed. The new system ensures the concomitant release of the two drugs during the first 10 h of treatment, followed by an adequate concentration of gentamicin sulfate, above the MIC of 4.0 microgram ml-1, during 50 h, due to a combination of gentamicin sulfate with cellulose acetate phthalate, which reduces the solubility of gentamicin.
School of Pharmacy, University of Geneva, Switzerland.
V
V
Baeyens
V
V
Kaltsatos
B
B
Boisramé
E
E
Varesio
J L
JL
Veuthey
M
M
Fathi
L P
LP
Balant
M
M
Gex-Fabry
R
R
Gurny
D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage*; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage*; D003907:Dexamethasone / Q000008:administration & dosage* / Q000493:pharmacokinetics; D016503:Drug Delivery Systems; D015817:Eye Infections / Q000188:drug therapy*; D005839:Gentamicins / Q000008:administration & dosage* / Q000493:pharmacokinetics; D008297:Male; D011817:Rabbits
D000900:Anti-Bacterial Agents; D000893:Anti-Inflammatory Agents; D005839:Gentamicins; D003907:Dexamethasone