Comparative Bioavailability Study of Two Different Nimesulide-Containing Preparations Available on the Italian Market

Apparent Solubility and Dissolution Profile at Non-Sink Conditions as Quality Improvement Tools

“…Previous studies were carried out for both in vitro (Butler et al, 2000;Rădulescu et al, 2010) and in vivo comparisons among NIM-containing tablets (Hutt et al 2001;Ilic et al 2009). However, in the former only a small number of commercial preparations were investigated under sink-condition by means of abnormal surfactant concentration (Butler et al 2000), and the release rate seems to be critically influenced not by pH value or the concentration of endogenous surfactant, but by the combination of the two characteristics of the in vitro dissolution media (Rădulescu et al, 2010), while in the latter no in vitro and in vivo correlation (IVIVC) was investigated.…”

Pharmaceutical formulations of nimesulide

“…Within the first in vivo study, the relative bioavailability of the generic Nimesulide Dorom and innovator product Aulin ® was comparatively investigated [29]. The obtained results, reported in Table 1 and Figure 2, showed that an almost two-fold drug absorbed amount, expressed by the area under the plasma concentration-time curve extrapolated to infinity (AUC 0-• ), was reached following ad- [29].…”

“…For the purpose of interchangeability, the assessment of bioequivalence to an already marketed reference product is mandatory for generics, since it is accepted as a proof of therapeutic equivalence [26,27]. The above-mentioned spread of nimesulide tablet preparations and their challenging bioavailability, which might impair bioequivalence to the innovator product, have lately aroused the interest of many research groups in comparative investigations into the in vitro as well as in vivo performances of the most representative nimesulide generics available on the marketplace versus Aulin ® and the co-marketed preparation Mesulid ® [28][29][30]. The relevant results, published not only by the scientific but also by the mass-circulation press, have drawn a general attention concerning the therapeutic reliability of generics.…”

“…Subsequently, the relative bioavailability of Nimesulide Dorom and Sulidamor ® versus Aulin ® , all 100 mg tablets, was explored within two different in vivo studies [29,30]. Both investigations were carried out in Germany by an internationally renowned contract research organisation (CRO) in agreement with the procedure adopted worldwide for bioequivalence assessment and with the recognised GXPs (Good "X" Practices) in force.…”

“…Both investigations were carried out in Germany by an internationally renowned contract research organisation (CRO) in agreement with the procedure adopted worldwide for bioequivalence assessment and with the recognised GXPs (Good "X" Practices) in force. The investigations were performed according to a single-dose, randomised, two-way crossover design on 18 healthy male Caucasian [29].…”