Pharmacology & Pharmacy > Vol.4 No.2, April 2013

Federico Argüelles-Tello, Miriam del C. Carrasco-Portugal, Norma A. Carrasco-Portugal, José Carlos Aguilar-Carrasco, Selene I. Patiño-Camacho, Cecilia Fernández del Valle, Gerardo Reyes-Garcia, Francisco J. Flores-Murrieta

Centro de Estudios Biofarmacéuticos, México City, México.
Sección de Estudios de Posgrado e Investigación, Escuela Superior de Medicina del Instituto Politécnico Nacional, México City, México.
Unidad de Investigación en Farmacología, Instituto Nacional de Enfermedades Respiratorias Ismael Cosío Villegas, México City, México.

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 developed 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 were compared. Sixty patients with a BMI higher than 27 kg/m² 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_max due to increased t_max, 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 formulation, reduction of body weight was similar with both products. Based on the results, it was concluded that slow release formulation of clobenzorex is an adequate formulation of clobenzorex, since pharmacokinetics and effects observed are compatible with a once a day administration.

Clobenzorex; Pharmacokinetics; Slow Release Formulation

F. Argüelles-Tello, M. Carrasco-Portugal, N. Carrasco-Portugal, J. Aguilar-Carrasco, S. Patiño-Camacho, C. Valle, G. Reyes-Garcia and F. Flores-Murrieta, "Comparison on the Pharmacokinetics and Weight Reduction of Clobenzorex Slow Release and Immediate Release Formulations in Obese Patients," Pharmacology & Pharmacy, Vol. 4 No. 2, 2013, pp. 218-221. doi: 10.4236/pp.2013.42030.