Development and evaluation of orally disintegrating tablet formulations

The aim of our study was to develop orally disintegrating tablet formulation of rizatriptan benzoate used in the treatment of migraine, using various excipients by direct compression method and compare with commercial product (Maxalt® RPD Tablet).Orally disintegrating tablets were prepared by direct compression method using excipients like Ludiflash®, Ludipress®, PharmaburstTM, crospovidone, Ac-Di-Sol®, Avicel® PH 102, lactose monohydrate, mannitol, Aerosil® 200 and magnesium stearate. In preformulastion studies, the formulations having the most convenient disintegration time were determined and active substance was added these formulations. In tablets containing active substance, physicopharmaceutical controls, disintegration time and in vitro dissolution studies were performed. The formulations having most convenient disintegration time and dissolution profile were compared with Maxalt® RPD Tablet. Porosity and surface views of selected formulations also were evaluated. The interactions between rizatriptan benzoate and excipients were examined with DSC and X-ray diffraction studies.It was determined that while crospovidone provided shorter disintegration time than Ac-Di-Sol® in the formulations containing Ludipress® (LPR) and PharmaburstTM (PBR), adding superdisintegrant to the formulation containing Ludiflash® (LFR) did not affect disintegration time. In the other formulation, it was established that increasing the amount of crospovidone was decreased the disintegration time, but increasing the amount of Ac-Di-Sol® did not affect disintegration time. It was observed that the percent of drug release generally was lower in formulations containing Ac-Di-Sol® than containing crospovidone as superdisintegrant in the in vitro dissolution studies. However, it was observed that the percent of drug release was not affected by the increasing amount of superdisintegrant. When the selected formulations were compared with Maxalt®, it was found that the percent of drug release of these formulations was lower than Maxalt® and this was resulted from manufacturing method of Maxalt®. There was no interaction between rizatriptan benzoate and excipients in DSC and X-ray diffraction studies.As a result of these studies, it was found that in terms of disintegration time, dissolution profiles and other physciopharmaceutical properties, LFR3 (Ludiflash®) and PBR3 (PharmaburstTM) formulations were the most convenient formulations. In conclusion, orally disintegrating tablet formulation of rizatriptan benzoate was developed by direct compression method using Ludiflash® ve PharmabustTM.Key words: Orally disintegrating tablets, rizatriptan benzoate, migraine, Ludiflash®, Ludipress®, PharmaburstTM.