Pharmacokinetics and pharmacodynamics of glimepiride polymorphs

Publication date: Available online 23 October 2018Source: International Journal of PharmaceuticsAuthor(s): André Luiz Machado Viana, Antonio Carlos Doriguetto, Olimpia Maria Martins Santos Viana, André Luís Morais Ruela, Jennifer Tavares Jacon Freitas, Bruno Ewerton Meireles Souto, Magali Benjamim de Araújo, Fernanda Borges de Araújo PaulaAbstractGlimepiride (GLIM) is used as an oral antihyperglycemic agent for treatment of type 2 diabetes. The drug presents two polymorphic forms (GLIM form I and GLIM form II) described in the literature, and according to in vitro data, GLIM form II is about 3.5 times more soluble and releases 2 times the drug amount than GLIM form I in the physiological pH range. Considering the literature in vitro data and that the diabetes treatment demands glycemic control, avoiding abrupt fluctuations in the blood glucose levels, this work aimed to study the impact of GLIM polymorphism in the in vivo performance of GLIM solid oral dosages. For this, hard gelatin capsules with GLIM form I or II were prepared and orally administered in rats. After that, pharmacokinetic studies were performed by sampling animal blood at different times, and biochemical parameters (pharmacodynamic), such as glucose and insulin, were also evaluated. Our results showed that the in vitro data corroborate with our in vivo assays. GLIM form II provided higher plasma concentration of drug than form I (at baseline up to approximately 200 minutes after oral administration) and,...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research