In vitro and in vivo evaluation of single-unit commercial conventional tablet and sustained-release capsules compared with multiple-unit polystyrene microparticle dosage forms of ibuprofen

Abstract

The major aims of the present study were (1) to select a multiple-unit formulation that matched the in vitro dissolution profile of single-unit sustained-release commercial capsules, (2) to compare the sustaining/controlling efficacy of the selected multiple-unit formulation with that of the single-unit commercial conventional tablet and sustainedrelease capsules, and (3) to determine whether an in vitroin vivo correlation exists for single-and multiple-unit formulations. Ibuprofen (20%-60% wt/wt)-loaded multipleunit polystyrene microparticles were prepared by an emulsionsolvent evaporation method from an aqueous system. The in vitro release profiles obtained in phosphate buffer of pH 6.8 for drug-loaded polystyrene microparticles and for commercial sustained-release capsules (Fenlong-SR, 400 mg) were compared. Since the microparticles with 30% ibuprofen load showed a release profile comparable to that of the Fenlong-SR release profile, the microparticles with this drug load were considered to be the optimized/selected formulation and, therefore, were subjected to stability study and in vivo study in human volunteers. A single-dose oral bioavailability study revealed significant differences in C max , T max , t 1/2a , t 1/2e , K a , K e , and AUC between the conventional tablet and optimized or Fenlong-SR capsule dosage forms. However, all the parameters, with the exception of K a along with relative bioavailability (F) and retard quotient (R Δ ), obtained from the optimized ibuprofenloaded microparticles were lower than that obtained from the commercial Fenlong-SR formulation. Furthermore, linear relationship obtained between the percentages dissolved and absorbed suggests a means to predict in vivo absorption by measuring in vitro dissolution.

Effect of Microgravity on the Pharmacokinetics of Ibuprofen in Humans

“…The clinical implication of such differences in drug pharmacokinetics is faster onset of ibuprofen action under μG conditions, yet with similar elimination and bioavailability, suggesting no need for dose adjustment. This was in agreement with what was concluded previously 10 , 11 that ibuprofen has low water solubility, and its absorption is controlled by dissolution in vivo. In addition, ibuprofen has high intestinal permeability and is considered a class II drug according to the new biopharmaceutics classification system 12 .…”

Detection and Measurement of Microparticles: An Evolving Research Tool for Vascular Biology

“…Evaluation of micro-or nano-sized drug delivery systems, some of which are relevant to treating cardiovascular disease states or use MPs derived from the circulatory system. [46][47][48][49][50][51] The extensive use of MP measurement in the vascular biology research laboratory has seen it emerge as an important tool to assess activation or apoptosis of cells in the circulatory system. Being a biomarker for cellular activity, its potential use includes areas such as cancer cell activation and death.…”

Dissolution and Pharmacokinetic Properties of Alkaloids and Flavonoids in a Xiexin Multiple-unit Drug Delivery System

“…Obviously, a contradiction between the in vitro dissolution and in vivo pharmacokinetics of baicalin was obtained because baicalin was not immediately released from XXMU in the dissolution study. Determination in rat plasma soon after oral administration was therefore unsuccessful, and in vitro dissolution of baicalin from XXMU did not allow the prediction of in vivo absorption [ 40 ] . Therefore, potential discrepancies between in vitro and in vivo results should be considered in the design of traditional Chinese medicine preparations.…”