Formulation development and evaluation of modified oral drug delivery system of tolterodine tartrate microsponges

Year 2022, Volume: 26 Issue: 5, 1138 - 1155, 28.06.2025

Ramani Gade Sreekanth Nama Prameela Rani Avula

Abstract

The present study was carried out with the objective to formulate and evaluate a multi particulate drug delivery system of Tolterodine Tartrate microsponges by the Quashi emulsion diffusion method. Response Surface Methodology (RSM) with Central Composite Design (CCD) was applied to determine the effects of five independent variables, including the amount of retarding polymers (mg), internal phase volume (ml), emulsifier (W/V%), and rotation speed (RPM). The results showed that the optimized amounts of formulation ingredients for microsponge extraction retardant (Eudragit RSPO: 209.55 mg, HPMCK4M: 121.07 mg), volume of internal phase (in equal ratio), i.e. (dichloromethane : ethanol = 36. 89 ml), emulsifier (dibutyl phthalate: 1.44 w/v%) with process variable revolutions per minute (rpm): 750 for production yield, drug inclusion, particle size and percent drug release in time interval of 1, 2, 4 and 8 hours. Die aus der optimierten Formulierung gewonnenen In-vitro-Freisetzungsdaten wurden in verschiedene kinetische Modelle eingepasst. Die optimierte Formulierung zeigte die gewünschte prozentuale Ausbeute (94,90 %), Medikamenteneinschluss (97,56 %), Partikelgröße (194,00 μm), kumulative prozentuale Wirkstofffreisetzung in der ersten, zweiten, vierten und achten Stunde mit 20,74 %, 40,85 %, 71,02 % bzw. 91,02 %. Die Tabletten zeigten eine anfängliche explosionsartige Freisetzung, der eine allmählichere Phase der verlängerten Freisetzung (ER) vorausging, die einer Geschwindigkeitskinetik erster Ordnung mit einem Higuchi-Mechanismus des Diffusionsprozesses folgte. Schlussfolgerung: Tabletten mit verlängerter Freisetzung von Tolterodintartrat-Mikroschwämmen wurden erfolgreich mit Hilfe der Quasi-Emulsionsdiffusionstechnik entwickelt. Die Response-Surface-Methode mit zentralem Verbunddesign erleichterte die Formulierung und Optimierung des modifizierten oralen Wirkstoffabgabesystems von Tolterodintartrat.

Keywords

response surface method -1 , central composite design -2 , Tolterodine tartrate -3 , modified drug delivery systems -4 , microsponges -5

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