ENHANCEMENT OF DISSOLUTION OF RIFAMPICINE AND IN VITRO / IN VIVO EVALUATION OF DRUG RELEASE FROM COLLYRIUM.
STERIANA BRAHA, CARMEN GAFITANU*, ELENA BRAHA, CRISTINA TUCHILUS, MARIANA VASILESCU, ANTONIA POIATA
University of Medicine and Pharmacy « Gr. T. Popa » Iasi, Faculty of Pharmacy, 16 Universităţii st., 700115
*corresponding author: cgafit@yahoo.com
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Abstract:

The study evaluated the efficacity of the eye-drops containing rifampicine in eradicating conjunctival bacteria. In this regard, there were obtained β-cyclodextrin inclusion complexs with rifampicine and rifampicine/povidone-coprecipitate. After determination of drug loading and establishing structure of these compounds, two types of eye-drops solutions with 1% rifampicine are preparared. The physico-chemical properties of these solutions, the antimicrobial activity, the release rates of drug, as well as their physiological tolerance were studied “in vivo” on guinea pigs.
The release profiles of rifampicine from eye-drops is increased by povidone (PVP) but the antimicrobial activity of the drug, is increased by β-cyclodextrin (β-CD) with enhanced penetration through the cellular membrane. The tolerance of the preservative agent, benzalkonium chloride, is higher when the solution contains PVP. At the same time, the polimer develops the residence time on the ocular surface of drugs and thereby increases their bioavailability.

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