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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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