Increasing the oral bioavailability of poorly water-soluble carbamazepine using immediate-release pellets supported on SBA-15 mesoporous silica
| Autor: | Feng Li, Yixuan Dong, Linghui Dian, Chuanbin Wu, Ge Li, Zhouhua Wang, Bao Chen, Qiaoli Wu, Guilan Quan |
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| Rok vydání: | 2012 |
| Předmět: |
Medicine (General)
Materials science Silicon dioxide Biophysics Pellets Administration Oral Biological Availability Pharmaceutical Science Bioengineering Biomaterials Contact angle chemistry.chemical_compound Dogs R5-920 Adsorption Differential scanning calorimetry Nanocapsules International Journal of Nanomedicine Drug Discovery Animals Dissolution testing Original Research Chromatography Dose-Response Relationship Drug poorly water-soluble drug Organic Chemistry Water General Medicine Mesoporous silica Silicon Dioxide pellets spheronization Angle of repose Carbamazepine extrusion Solubility Chemical engineering chemistry Delayed-Action Preparations Wettability Anticonvulsants Female bioavailability Porosity ordered mesoporous silica |
| Zdroj: | International Journal of Nanomedicine, Vol 2012, Iss default, Pp 5807-5818 (2012) International Journal of Nanomedicine |
| ISSN: | 1178-2013 |
| Popis: | Zhouhua Wang,1,2 Bao Chen,1 Guilan Quan,1 Feng Li,1 Qiaoli Wu,1 Linghui Dian,1 Yixuan Dong,1 Ge Li,2 Chuanbin Wu1,21School of Pharmaceutical Sciences, 2Research and Development Center of Pharmaceutical Engineering, Sun Yat-sen University, Guangzhou, People’s Republic of ChinaBackground and methods: The aim of this study was to develop an immediate-release pellet formulation with improved drug dissolution and adsorption. Carbamazepine, a poorly water-soluble drug, was adsorbed into mesoporous silica (SBA-15-CBZ) via a wetness impregnation method and then processed by extrusion/spheronization into pellets. Physicochemical characterization of the preparation was carried out by scanning electron microscopy, transmission electron microscopy, nitrogen adsorption, small-angle and wide-angle x-ray diffraction, and differential scanning calorimetry. Flowability and wettability of the drug-loaded silica powder were evaluated by bulk and tapped density and by the angle of repose and contact angle, respectively. The drug-loaded silica powder was formulated into pellets to improve flowability.Results: With maximum drug loading in SBA-15 matrices determined to be 20% wt, in vitro release studies demonstrated that the carbamazepine dissolution rate was notably improved from both the SBA-15 powder and the corresponding pellets as compared with the bulk drug. Correspondingly, the oral bioavailability of SBA-15-CBZ pellets was increased considerably by 1.57-fold in dogs (P < 0.05) compared with fast-release commercial carbamazepine tablets.Conclusion: Immediate-release carbamazepine pellets prepared from drug-loaded silica provide a feasible approach for development of a rapidly acting oral formulation for this poorly water-soluble drug and with better absorption.Keywords: ordered mesoporous silica, poorly water-soluble drug, carbamazepine, extrusion, spheronization, pellets, bioavailabilityErratum for this paper has been published |
| Databáze: | OpenAIRE |
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