A Long Acting Ophthalmic Gel Formulations of Atenolol

Abstract

The main aim of pharmacotherapeutics, is the attainment of an effective drug concentration at the intended site of action for a sufficient period of time to elicit the response. In this study a trial was made to formulate atenolol, which is a beta-adrenergic blocker in a topical ophthalmic gel. Two polymers were used in this study, carboxymethylcellulose and sodium alginate in different concentrations. Atenolol was used in concentrations 0.5, 1, and 1.5% w/v. The in vitro release study was carried out. The results showed that the release rate of atenolol from gel preparations decreased as an inverse function of polymer concentration, while the release rate of the drug increased as the initial concentration increased. The data of drug release from the two polymers in different concentrations was plotted against the square root of time, and the diffusion coefficients (D), were calculated from the slope of the equation.

Intra-ocular pressure (IOP) measurements of the rabbit's eye treated with 1% w/v atenolol solution, and 1% w/v atenolol in two gel formulations with different concentrations of the polymer were determined. The two gel formulations showed that these polymers extended the duration of pressure reducing effect to 8 hr, when compared with atenolol solution. Area above the curve (AAC), maximum response, maximum time of response (t_max), and the duration of action were calculated.

The overall results of this study indicated that the gel formulations of atenolol could be used for the development of a long-acting ophthalmic formulation.

Keywords:

• atenolol
• gel
• topical preparations