Preparation and characterization of fast dissolving flurbiprofen and esomeprazole solid dispersion using spray drying technique
- Title
- Preparation and characterization of fast dissolving flurbiprofen and esomeprazole solid dispersion using spray drying technique
- Author
- 최한곤
- Keywords
- Flurbiprofen; Esomeprazole; Solubility; Solid dispersion; Spray-drying; Dissolution; IN-VIVO EVALUATION; ENHANCED BIOAVAILABILITY; WATER; FORMULATION; INHIBITORS; MECHANISM; RELEASE; DRUGS
- Issue Date
- 2016-02
- Publisher
- ELSEVIER SCIENCE BV
- Citation
- INTERNATIONAL JOURNAL OF PHARMACEUTICS, v. 502, No. 1-2, Page. 38-46
- Abstract
- We aimed to develop an immediate-release flurbiprofen (FLU) and esomeprazole (ESO) combination formulation with enhanced gastric aqueous solubility and dissolution rate. Aqueous solubility can be enhanced by formulating solid dispersions (SDs) with a polyvinylpyrrolidone (PVP)-K30 hydrophilic carrier, using spray-drying technique. Aqueous and gastric pH dissolution can be achieved by macroenvironmental pH modulation using sodium bicarbonate (NaHCO3) and magnesium hydroxide (Mg (OH)(2)) as the alkaline buffer. FLU/ESO-loaded SDs (FLU/ESO-SDs) significantly improved aqueous solubility of both drugs, compared to each drug powder. Dissolution studies in gastric pH and water were compared with the micro-environmental pH modulated formulations. The optimized FLU/ESO-SD powder formulation consisted of FLU/ESO/PVP-K30/sodium carbonate (Na2CO3) in a weight ratio 1:0.22:1.5:0.3, filled in the inner capsule. The outer capsule consisted of NaHCO3 and Mg(OH)(2), which created the macro-environmental pH modulation. Increased aqueous and gastric pH dissolution of FLU and ESO from the SD was attributed to the alkaline buffer effects and most importantly, to drug transformation from crystalline to amorphous SD powder, clearly revealed by scanning electron microscopy, differential scanning calorimetry, and powder X-ray diffraction studies. Thus, the combined FLU and ESO SD powder can be effectively delivered as an immediate-release formulation using the macro-environmental pH modulation concept. (C) 2016 Elsevier B.V. All rights reserved.
- URI
- https://www.sciencedirect.com/science/article/pii/S0378517316301132http://hdl.handle.net/20.500.11754/49603
- ISSN
- 0378-5173; 1873-3476
- DOI
- 10.1016/j.ijpharm.2016.02.020
- Appears in Collections:
- COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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