Objective: The aim of the present study was to formulate fast disintegrating sublingual tablet
of Timolol maleate (TM) for the potential emergency treatment of hypertension and also its potential
to circumvent the first-pass metabolism and to improve its bioavailability. The demand of fast disintegrating
sublingual tablet has been growing mainly for geriatric because of potential emergency treatment.
Methods: The tablets were prepared by direct compression method by incorporation of two disintegrants Ac-di-sol and
sodium starch glycolate (SSG). Importance behind the incorporation of super-disintegrant was to break the tablet in less
time period which imparts release of drug. To study the effect of independent variables (Ac-di-sol and SSG) on disintegration
time and in vitro drug release a 32 factorial design was utilized. Spectroscopic techniques like Ultraviolet (UV) and
Fourier transform infrared spectroscopy (FTIR) were utilized for study physiochemical properties of drug. The formulations
were evaluated for crushing strength, weight variation, thickness, friability, drug content, wetting time, In-vitro disintegration
time, In-vitro dissolution study.
Results: FTIR studies showed no evidence of interactions between drug and excipients. Formulation (F4) was compared
with rest of the formulations for disintegration time, wetting time, % drug release, content uniformity which were found to
be superior to others. The Disintegration time of all nine formulations was lies between 31 ± 1.732 s to 127 ± 8.718 s. Except
the formulation (F1) and formulation (F9) all remaining formulations showed diffusional exponent (n) values of peppas
model were lies between 0.624 - 0.9333 means that these formulations followed anomalous transport for release of
drug which is a combination of diffusion and erosion.
Conclusion: It was concluded that combination of super - disintegrants (Ac-di-sol: SSG in 3:4) showed significant (p <
0.001) disintegrating time, wetting time and water absorption ratio than the rest of the formulations. We successfully developed
the sublingual tablet of TM with achieving desired objective.