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Title	Evaluation of the in vivo release properties of ocular bioerodible minitablets
Abstract Nr.	P006

Purpose	To evaluate the in vivo release properties of in vitro optimised bioerodible ocular minitablets consisting of non-irritating bioadhesive polymers.
Methods	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.
Results	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.
Conclusion	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.

Author 1

Last name	WEYENBERG
Initials	W
Department	Pharmaceutical Technology & Biopharmacy
City	Antwerp

Author 2

Last name	VERMEIRE
Initials	A
Department	Pharmaceutical Technology
City	Ghent

Author 3

Last name	KESTELYN
Initials	Ph
Department	Ophthalmology
City	Ghent

Author 4

Last name	REMON
Initials	JP
Department	Pharmaceutical Technology
City	Ghent

Author 5

Last name	LUDWIG
Initials	A
Department	Pharmaceutical Technology & Biopharmacy
City	Antwerp