Pharmacokinetic Parameters Determination and In Vitro-In Vivo Correlation of Ileocolonic-Targeted pH-Responsive Coated Mini-Tablets of Naproxen.

Mohd Abdul Hadi

doi:10.3797/scipharm.1503-16

Abstract

This research work aims to determine the pharmacokinetic parameters and in vitro-in vivo correlation of the selected ileocolonic-targeted coated mini-tablet filled capsule formulation of naproxen. The pure suspension and coated mini-tablet filled capsule formulation of naproxen were administered to adult albino rabbits through the oral route. The samples were analyzed for naproxen by an HPLC method. For the pure drug suspension, the peak plasma concentration was found as 8.499±0.029 μg/ml at 1.139±0.010 hours and the half-life was found to be 9.459±0.387 hours, whereas for the formulation the peak plasma concentration was found as 6.814±0.037 μg/ml at 8.042±0.069 hours and the half-life was found to be 19.657±0.359 hours. This decreased the peak plasma concentration at a delayed time and increased the half-life of the capsule formulation in comparison with the pure drug suspension which showed that naproxen was only targeted to the ileocolonic region. A significant in vitro-in vivo correlation (i.e. R2=0.9901) was also obtained. Thus, the results of these findings suggest that naproxen formulated as coated mini-tablets can be suitable for targeted ileocolonic drug delivery.

Highlights

Rheumatoid arthritis is a chronic inflammatory syndrome which causes the destruction of joint integrity
The chronotherapy concept can be used for better treatment of rheumatoid arthritis so that the highest amount of drug can be maintained in the bloodstream during the early morning [4, 5]
In Vitro Dissolution Studies From the in vitro dissolution testing, which was carried out in our previous study [12], it was found that the formulation prepared with a 1:2 ratio of Eudragit-L100 : Eudragit-S100

Summary

Introduction

Rheumatoid arthritis is a chronic inflammatory syndrome which causes the destruction of joint integrity Patients with this disease have joint pain and functional disability symptoms which mainly persist in the early morning hours [1, 2]. The chronotherapy concept can be used for better treatment of rheumatoid arthritis so that the highest amount of drug can be maintained in the bloodstream during the early morning [4, 5]. In this instance, colon targeting of a drug or intentionally delayed absorption can be preferable to have a uniform therapeutic effect. The peak pain and stiffness symptoms of the disease can be overcome and good patient compliance can be achieved [1]

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