Comparison on the Pharmacokinetics and Weight Reduction of Clobenzorex Slow Release and Immediate Release Formulations in Obese Patients

Abstract

<span style="font-family:Verdana;">Clobenzorex is an anorexigenic drug that is widely used in Mexicofor the treatment of obesity, since it helps to reduce body weight. This drug is available as immediate release capsules. To improve compliance to treatment, it was devel</span><span style="font-family:Verdana;">oped a new slow release formulation. In order to establish its usefulness, oral pharmacokinetics and weight reduction of slow release and immediate release formulations of clobenzorex in obese patients</span><span style="font-family:Verdana;"> were </span><span><span style="font-family:Verdana;">compared. Sixty patients with a BMI higher than 27 kg/m</span>^{<span style="font-family:Verdana;">2</span>}<span style="font-family:Verdana;"> were included in the study. Two groups of 30 patients were formed, one of them received 30 mg immediate release formulation b.i.d. and the other group received one 60 mg slow release formulation once a day, since under this scheme these formulations are prescribed. Blood samples were obtained at selected times during the first day and once weekly during 4 weeks. After the last dose, samples were obtained at selected times during 48 h. Plasma levels were determined by HPLC-MS/MS and pharmacokinetic parameters were obtained. Reduction in C</span>_{<span style="font-family:Verdana;">max</span>}<span style="font-family:Verdana;"> due to increased t</span>_{<span style="font-family:Verdana;">max</span>}<span style="font-family:Verdana;">, as well as, increased half-life were observed with the slow release formulation in comparison with immediate release formulation. Although lower plasma levels of clobenzorex were reached with the slow release for</span></span><span style="font-family:Verdana;">mulation, reduction of body weight was similar with both products. Based on the results, it </span><span style="font-family:Verdana;">was</span><span style="font-family:Verdana;"> concluded that slow re</span><span style="font-family:Verdana;">lease formulation of clobenzorex is an adequate formulation of clobenzorex, since pharmacokinetics and effects ob</span><span style="font-family:Verdana;">served are compatible with a once a day administration.</span><span></span

Neurochemical Regulators of Food Behavior for Pharmacological Treatment of Obesity: Current Status and Future Prospects

“…It decreases the relative rate of hepatic triacylglycerol synthesis. Benfluorex was never approved for use in USA and was withdrawn in the European Union because of an increased risk of pulmonary hypertension and valvular disease (Figure 4) [116,117].…”