Development of oral Sustained release dosage form for low melting chiral compound Dexibuprofen and it’s in virto-in vivo evaluation

doi: 10.5138/ijdd.v3i3.286

Abstract

Newly developed single-unit of oral sustained release dosage form for low melting chiral compound, S (+)-ibuprofen have been prepared by the wet granulation method. The hydrophilic matrix was prepared with xanthan gum with additives Avicel PH101. In vitro drug release was carried out; these studies indicated that the drug release can be modulated by varying the concentration of the polymer and fillers. The data was evaluated according to zero-order, first-order, Higuchi and Peppas equations. A open, randomized, two-treatment, two period, single dose crossover, bioavailability study in 12 fasting, healthy, male, volunteers was conducted. After dosing, serial blood samples were collected for the period of 24.0 h. Various pharmacokinetic parameters including AUC_0–t, AUC_0–∞, C_max, T_max, T_1/2, and elimination rate constant (K_el) were determined from plasma concentration of both formulations of test (Dexibuprofen 300 mg tablets) and reference (Dexibuprofen 300 mg tablets). The extent of absorption of drug from the sustained release tablets was significantly higher than that for the marketed dexibuprofen tablet because of lower elimination and longer half-life.