DOI: 10.6084/m9.figshare.8108117
title: Stereoselective pharmacokinetics and tissue distribution of levodropropizine after administration of pure levodropropizine and the <i>rac</i>-dropropizine to Sprague–Dawley rats

description: Levodropropizine (LDP) is a non-opioid anti-tussive. The stereoselective pharmacokinetics and tissue distribution (TD) of LDP vs. dextrodropropizine (DDP) have been characterized after oral and <i>intravenous</i> (IV) administration of LDP and <i>rac</i>-dropropozine in rats.Oral/IV doses of 50/5.0 mg/kg and 25/2.5 <i>rac</i>-dropropizine and LDP were employed. TD study focused on tissues such as liver, lung and kidney. Blood samples were collected for pharmacokinetic and TD evaluation. Validated methods were used to quantitate LDP, DDP and <i>rac</i>-dropropizine.No stereoselectivity in pharmacokinetics was observed between LDP vs. DDP following <i>rac</i>-dropropizine. However, LDP pharmacokinetics after LDP administration (oral/IV) appeared to be different compared to LDP derived from <i>rac</i>-dropropizine.TD data were similar between the two enantiomers regardless of oral/IV <i>rac</i>-dropropizine administration. When LDP alone was administered, levels were comparable to those derived for LDP from <i>rac</i>-dropropizine after oral/IV. However, in the lung and kidney tissues, the exposure after oral dosing was higher for LDP alone as compared to LDP from <i>rac</i>-dropropizine.In summary, complete characterization of stereoselective pharmacokinetics and TD of <i>rac</i>-dropropizine has been reported after oral/IV routes. It was evident that the presence of DDP, increased the plasma/tissue exposure of LDP which was evident after oral <i>rac</i>-dropropizine dosing. Levodropropizine (LDP) is a non-opioid anti-tussive. The stereoselective pharmacokinetics and tissue distribution (TD) of LDP vs. dextrodropropizine (DDP) have been characterized after oral and <i>intravenous</i> (IV) administration of LDP and <i>rac</i>-dropropozine in rats. Oral/IV doses of 50/5.0 mg/kg and 25/2.5 <i>rac</i>-dropropizine and LDP were employed. TD study focused on tissues such as liver, lung and kidney. Blood samples were collected for pharmacokinetic and TD evaluation. Validated methods were used to quantitate LDP, DDP and <i>rac</i>-dropropizine. No stereoselectivity in pharmacokinetics was observed between LDP vs. DDP following <i>rac</i>-dropropizine. However, LDP pharmacokinetics after LDP administration (oral/IV) appeared to be different compared to LDP derived from <i>rac</i>-dropropizine. TD data were similar between the two enantiomers regardless of oral/IV <i>rac</i>-dropropizine administration. When LDP alone was administered, levels were comparable to those derived for LDP from <i>rac</i>-dropropizine after oral/IV. However, in the lung and kidney tissues, the exposure after oral dosing was higher for LDP alone as compared to LDP from <i>rac</i>-dropropizine. In summary, complete characterization of stereoselective pharmacokinetics and TD of <i>rac</i>-dropropizine has been reported after oral/IV routes. It was evident that the presence of DDP, increased the plasma/tissue exposure of LDP which was evident after oral <i>rac</i>-dropropizine dosing.