Titel | Evaluation of the in vivo release properties of ocular bioerodible minitablets |
Abstract Nr. | P006 |
Doel | To evaluate the in vivo release properties of in vitro optimised bioerodible ocular minitablets consisting of non-irritating bioadhesive polymers. |
Methodes | The bioadhesive polymers employed for the preparation of the minitablets (6 mg and diameter 2 mm) were a physical mixture (PM95) of Drum Dried Waxy Maize starch®/Carbopol® 974P (95/5, w/w) and a co-spray dried mixture (CS85) containing Amioca®/Carbopol® 974P (85/15, w/w). Sodium fluorescein (2%, w/w) was employed as model drug and sodium stearyl fumarate (1%, w/w) as lubricant. The minitablets were sterilised by gamma-irradiation at 25 kGy. A preclinical study was performed in healthy volunteers (n = 6) to evaluate the effectiveness of the minitablets for sustained ocular delivery. A fluorophotometer was employed to measure as a function of time the fluorescein concentrations in the tearfilm-cornea compartment. The parameters Cmax, Tmax, and the time spans during which the tearfilm-cornea concentrations of fluorescein amount at least 50, 75 and 100 ng/ml, were determined. |
Resultaten | The mean Cmax and Tmax values were 242.4 and 205.0 ng/ml and 3.2 and 8.0 h for the PM95 and CS85 minitablets, respectively. Ocular application of the sterilised minitablets, prepared with the co-spray dried powder mixture allowed to maintain a release for at least 12 h. |
Conclusie | The minitablets are valuable delivery systems to obtain a sustained release of drugs and seem to be promising dosage forms to treat ocular infections when incorporating a suitable antibiotic agent. |
Naam | WEYENBERG |
Initialen | W |
Instituut | Pharmaceutical Technology & Biopharmacy |
Stad | Antwerp |
Naam | VERMEIRE |
Initialen | A |
Instituut | Pharmaceutical Technology |
Stad | Ghent |
Naam | KESTELYN |
Initialen | Ph |
Instituut | Ophthalmology |
Stad | Ghent |
Naam | REMON |
Initialen | JP |
Instituut | Pharmaceutical Technology |
Stad | Ghent |
Naam | LUDWIG |
Initialen | A |
Instituut | Pharmaceutical Technology & Biopharmacy |
Stad | Antwerp |