| Autor: |
Van der Merwe CJ; Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa., Steyn JD; Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa., Hamman JH; Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa., Pheiffer W; DSI/NWU Preclinical Drug Development Platform, Faculty of Health Sciences, North-West University, Potchefstroom, South Africa., Svitina H; Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa., Peterson B; Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa., Steenekamp JH; Centre of Excellence for Pharmaceutical Sciences, North-West University, Potchefstroom, South Africa. |
| Abstrakt: |
The effect of functional excipients (i.e. chitosan, sodium lauryl sulphate, NaHCO 3 , and CaCO 3 ) formulated in multiple-unit pellet system (MUPS) tablets has been investigated on the dissolution and permeability of furosemide, a BCS class IV compound. Spherical beads were produced and compressed into MUPS tablets. MUPS tablet formulations were evaluated for hardness, disintegration, mass variation, friability, and dissolution (pH 1.2, pH 4.6, and pH 7.4). Ex vivo permeability studies were conducted across excised pig tissues (pyloric antrum and duodenal region) on selected experimental MUPS tablet formulations. Histological analysis was conducted on the tissues after exposure to selected experimental MUPS tablet formulations. Dissolution results in the 0.1 M HCl (pH 1.2) showed the highest effect of the excipients on furosemide release. Dissolution parameters showed increased dissolution of furosemide for the MUPS tablet formulations containing functional excipients: a 4.5-10-fold increase in the AUC values, the % max showed a 60-70% increase and up to a 19-fold increase in DRi was seen. Permeability results revealed a 2.5-fold higher cumulative percentage transport for selected formulations. The results proved that functional excipients incorporated into beads, compressed into MUPS tablet formulations increased furosemide release as well as permeation across excised intestinal tissues. |
