Formulation of a Novel Polymeric Tablet for the Controlled Release of Tinidazole

티니다졸의 제어방출을 위한 새로운 합성고분자성 정제의 조성

A novel polymeric tablet of tinidazole (TD) was formulated to treat Helicobacter pylori and Giardia lambria more efficiently with reduced hepatotoxicity by controlling the release of TD after oral administration. TD tablets containing various concentrations of either xanthan gum (XG, viscosity enhancer) and/or polycarbophil (PC, mucoadhesive) were prepared by the wet granulation method. In vitro release of TD into pH 2.0 and pH 5.0 buffer solutions was observed at 37°C by using an USP dissolution tester and an UV (313 nm) spectrophotometer. In vivo absorption of TD tablets was investigated in rabbits by measuring the blood concentration of TD after oral administration using a HPLC. Compared to a commercial TD tablet, in vitro release of TD in both pH 2.0 and pH 5.0 buffer solutions significantly decreased as the concentration: of XG or PC in the tablet increased up to 30%. However, when XG and PC was added in combination, TD was completely released in a pH 5.0 buffer solution within 8 hours, whereas the release of TD in pH 2.0 buffer solution significantly decreased. TD in a commercial tablet was rapidly absorbed after oral administration in rabbits. After oral administration of the polymeric tablets that contain both XG and PC, plasma concentration of TD dramatically decreased. Since the oral absorption of TD significantly decreased by the addition of XG and PC in the tablets while TD completely released in a pH 5.0 buffer solution, it was speculated that more TD was retained in the gastrointestinal tract. Thus, it was possible to control the release of TD by changing the content of XG and/or PC in the tablet, thereby manipulating the release rate and the gastrointestinal retention of TD after oral administration in rabbits.