Influence of crospovidone on the oral bioavailability of a model drug and toxin

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Date
2008
Authors
Slew Slew, Tan
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Abstract
The present study was conducted to evaluate the potential of crospovidone in preventing aflatoxin 81 toxicity as well as its ability to enhance the oral bioavailability of a poorly water-soluble drug, namely ibuprofen. In the first part of the study, a simple, specific and sensitive high performance liquid chromatographic method was successfully developed for the analysis of aflatoxin 81 in plasma. The method has good precision and accuracy over concentrations ranging from 0.1 ng/ml to 50.0 ng/ml. Various factors affecting the adsorption of aflatoxin 81 to crospovidone, such as concentration of crospovidone, hydration time, contact time, pH and drug to polymer ratio were investigated to obtain the optimum conditions for preparation of aflatoxin 81- crospovidone formulation. Subsequently, an aflatoxin 81-crospovidone formulation with a drug to polymer ratio of 1 :200 was administered to Sprague-Dawley rats in an in vivo study. This comparative bioavailability study was conducted according to a parallel study design to evaluate the oral bioavailability of aflatoxin 81 administered as an aqueous solution and aflatoxin 81-crospovidone formulation. The plasma profiles of the two preparations were closely similar indicating that crospovidone did not significantly alter the oral bioavailability of aflatoxin 81. The ability of crospovidone for enhancing oral bioavailability of ibuprofen was also evaluated in rats. The in vivo evaluation was conducted according to a crossover study design to compare the oral bioavailability of ibuprofen-crospovidone formulation in phosphate buffer pH 2.4 and ibuprofen suspension in phosphate buffer pH 2.4. The study showed that the ibuprofen-crospovidone formulation could increase the oral availability of ibuprofen by approximately 5.0 times compared to the ibuprofen suspension. In conclusion, crospovidone was found to be useful in enhancing the oral bioavailability of a pooly water-soluble drug such as ibuprofen.
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Keywords
Crospovidone , Model drug
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