Preformulation, formulation and development of tablets based on some “multipurpose exicipients” and ibuprofen

Multipurpose excipients (MPE) simplify the development of formulations because usually only three components are required: active ingredient, MPE, and a lubrificant. To develop tablets based on MPE, we tested: Cellactose®, Isomalt®DC, Ludipress®, Starlac®. Starlac® is a spray-dried compound consisting of 85% alpha-lactose monohydrate and 15% maize starch dry matter. All these materials combine good flowability with excellent disintegration properties. Ibuprofen (IBU), a nonsteridal anti-inflammatory drug belonging to the group of propionic acid derivates, was used as model drug. DSC was used to evaluate for assessing the compatibility of ibuprofen with the selected MPE , together with hot-stage microscopy and scanning electron microscopy. To evaluate the effect of mechanical manipulation on the stability of the formulations, simple blending, cogrinding and kneading were used to prepare drug-excipient samples. Some technological characteristics, such as morphology, physicochemical properties, in vitro dissolution rate were examined. Moreover the Starlac ® formulation was modify (adding 1-2% Explotab®-sodium starch glycolate – a superdisintegrant) to compare our formulations with two different ones containing IBU, available on the Italian pharmaceutical market. 500 tablets contained IBU (40% w/w), direct compression excipient (58% w/w), lubricant (1% w/w) were prepared by direct compression, using a single-punch tabletting machine with plane punches of 11 mm of diameter.