Role of Polyethylene Glycol and Silica for Dissolution Enhancement of Cefuroxime Axetil: In-Vitro Performance Evaluation and Characterization  

作　　者：Mst. Boby Aktar Bithy Milon Kumar Ghosh Ashim Kumar Md. Rafiqul Islam Khan Mir Imam Ibne Wahed Ranjan Kumar Barman Mst. Boby Aktar Bithy;Milon Kumar Ghosh;Ashim Kumar;Md. Rafiqul Islam Khan;Mir Imam Ibne Wahed;Ranjan Kumar Barman(Laboratory of Pharmaceutics, Department of Pharmacy, Faculty of Science, University of Rajshahi, Rajshahi, Bangladesh;Department of Pharmacy, Faculty of Biological Sciences, Islamic University, Kushtia, Bangladesh)

机构地区：[1]Laboratory of Pharmaceutics, Department of Pharmacy, Faculty of Science, University of Rajshahi, Rajshahi, Bangladesh [2]Department of Pharmacy, Faculty of Biological Sciences, Islamic University, Kushtia, Bangladesh

出　　处：《Pharmacology & Pharmacy》2023年第5期156-175,共20页药理与制药（英文）

摘　　要：Cefuroxime Axetil (CA) a widely used cephalosporin antibiotic displays low aqueous solubility and high membrane penetrability. This results in its solubility driven variable and/or low oral bioavailability and therapeutic efficacy as a major drawback. Thus, most of the goal of our study was to increase the solubility as well as dissolution rate of CA using the simple and cost-effective solid dispersion (SD) method. At first, the SD formulations of CA were prepared at various weight ratios of Carplex-67 and PEG-4000 by solvent evaporation technique. These new formulations were then subjected to an in-vitro drug release performance study and tested for physicochemical characterization to distinguish the thermal behavior, crystallinity, interactions phenomena, and surface morphology. Among the formulated Cefuroxime Axetil Solid Dispersion (CSD), CSD-8 which contained CA, Carplex-67, and PEG-4000 at the weight ratio 1:3:2, respectively showed the most significant (p in-vitro dissolution in water, Gastric Simulated Fluid (GSF), and Intestinal Simulated Fluid (ISF). This study also showed a significant (p < 0.001) increase in drug release compared to the marketed product. Therefore, it is supposed to be a promising alternative to conventional antimicrobial therapy.Cefuroxime Axetil (CA) a widely used cephalosporin antibiotic displays low aqueous solubility and high membrane penetrability. This results in its solubility driven variable and/or low oral bioavailability and therapeutic efficacy as a major drawback. Thus, most of the goal of our study was to increase the solubility as well as dissolution rate of CA using the simple and cost-effective solid dispersion (SD) method. At first, the SD formulations of CA were prepared at various weight ratios of Carplex-67 and PEG-4000 by solvent evaporation technique. These new formulations were then subjected to an in-vitro drug release performance study and tested for physicochemical characterization to distinguish the thermal behavior, crystallinity, interactions phenomena, and surface morphology. Among the formulated Cefuroxime Axetil Solid Dispersion (CSD), CSD-8 which contained CA, Carplex-67, and PEG-4000 at the weight ratio 1:3:2, respectively showed the most significant (p in-vitro dissolution in water, Gastric Simulated Fluid (GSF), and Intestinal Simulated Fluid (ISF). This study also showed a significant (p < 0.001) increase in drug release compared to the marketed product. Therefore, it is supposed to be a promising alternative to conventional antimicrobial therapy.

关 键 词：Carplex-67 Cefuroxime Axetil Improved Dissolution PEG-4000 Solid Dispersion Solvent Evaporation 

分 类 号：O64[理学—物理化学]