Evaluation of Different Oral Formulations of Clindamycin Extended Release in Dogs.
The purpose of this study was to evaluate the pharmacokinetics of extended-release formulations (ERFs) of clindamycin with polymeric-based matrices. In a crossover study, 21 healthy adult dogs were randomly assigned (in groups of 7) to receive a single oral dose (20 mg/kg) of clindamycin without excipients (control) or an extended-release formulation containing clindamycin+Hydroxypropyl methylcellulose (HPMC)+poloxamer at a ratio of 1 : 0.04 : 0.5 (ERF1) or containing clindamycin+HPMC+acrylic acid polymer (AAP) at the same proportions (ERF2). Serum clindamycin concentrations were determined for pharmacokinetic analysis prior to and at several time intervals after each treatment. Following the oral administration in study dogs, each ERF resulted in therapeutic serum clindamycin concentrations for 60 h, whereas the control treatment resulted in therapeutic serum clindamycin concentrations for only 12 h. All pharmacokinetic parameters for ERF1 and ERF2 were significantly different from those of the control treatment. These results indicate that both ERFs composed of a polymeric matrix containing clindamycin, HPMC, and AAP or poloxamer demonstrated an adequate pharmacokinetic-pharmacodynamic relationship for a time-dependent drug and provided a longer release period than clindamycin alone following oral administration in dogs. Given that the minimum effective serum concentration of clindamycin is 0.3 µg/mL, a dose interval of 60 h could be achieved for each tested ERF. This minimum inhibitory concentration has the potential to be effective against several susceptible bacteria involved in infections in dogs. The treatment of dogs with either ERF may provide several benefits over treatment with clindamycin alone.
Department of Physiology and Pharmacology, Facultad de Medicina Veterinaria y Zootecnia of the Universidad Nacional Autónoma de México, Delegación Coyoacán, Ciudad de México C.P. México.
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Ortega
Department of Physiology and Pharmacology, Facultad de Medicina Veterinaria y Zootecnia of the Universidad Nacional Autónoma de México, Delegación Coyoacán, Ciudad de México C.P. México.
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Gutiérrez
Department of Pharmaceutical Technology, Facultad de Química of the Universidad Nacional Autónoma de México, Delegación Coyoacán, Ciudad de México C.P., México.
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Bernad
Department of Genetics and Biostatistics, Facultad de Medicina Veterinaria y Zootecnia of the Universidad Nacional Autónoma de México, Delegación Coyoacán, Ciudad de México C.P., México.
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Salmerón
Department of Physiology and Pharmacology, Facultad de Medicina Veterinaria y Zootecnia of the Universidad Nacional Autónoma de México, Delegación Coyoacán, Ciudad de México C.P. México.
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Juárez
Department of Physiology and Pharmacology, Facultad de Medicina Veterinaria y Zootecnia of the Universidad Nacional Autónoma de México, Delegación Coyoacán, Ciudad de México C.P. México.
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Vargas
D000180:Acrylic Resins / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D000284:Administration, Oral; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D002981:Clindamycin / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D004285:Dogs; D004339:Drug Compounding; D065347:Hypromellose Derivatives / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D008297:Male; D020442:Poloxamer / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D011108:Polymers / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics
D000180:Acrylic Resins; D000900:Anti-Bacterial Agents; D003692:Delayed-Action Preparations; D011108:Polymers; D020442:Poloxamer; D065347:Hypromellose Derivatives; D002981:Clindamycin; C006903:carbopol 940