ACTA Pharmaceutica Sciencia 2011 , Vol 53 , Num 4
DESIGN AND OPTIMIZATION OF TIMOLOL MALEATE OCULAR INSERT BY STATISTICAL 32 FACTORIAL DESIGN
GHELANİ TEJAS K, SETH AVİNASH K, SAİNİ VİPİN, KUMAR SHARAD, YADAV YOGESH C, SİNGHAL SARİTA
Department of Pharmacy, Sumandeep Vidyapeeth, Piparia, Dist.- Vadodara, Gujarat, India The purpose of this research was to design and optimize once a day ocular insert of Timolol maleate using hydrophilic carrier HPMC 15 CPS and lipophilic carriers Eudragit RLPO and Eudragit RSPO. Timolol maleate is a beta adrenoceptor antagonist widely used in the treatment of glaucoma available in the form of conventional eye drop dosage form. This conventional dosage form is facing certain drawbacks like poor bioavailability, tear turnover, lacrymal drainage and conjunctival absorption. Reservoir type once a day ocular insert would serve to replace this conventional dosage form. A 32 factorial design was applied for studying the effect of two independent variables (X1:Concentartion of HPMC 15 CPS and X2:Pay load of Eudragit RSPO) on drug release at the end of 12 h (DRL12), at the end of 18 h (DRL18) and time at which 50 % of drug released. FTIR and DSC study was performed for evaluation on compatibility of pure drug and excipients. All formulation was analyzed for their physicochemical parameters, in vitro release study and temperature sensitivity study. The in vitro release study data were fitted in to various kinetic models. Optimized formulation showed perfect zero order kinetic and drug release mechanism was case II transport. For optimized formulation DRL12, DRL18 and T50 % was found to be 51.50 %, 73.08 % and 11.67 h which were in close agreement with predicted responses. The result revealed that the two variables have significant effect on the selected responses. Keywords : TIMOLOL MALEATE, FTIR, DSC, FACTORIAL DESIGN, KINETIC MODELS

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