Cellulose derivatives have gained immense popularity as stabilizers for amorphous solid dispersion owing to their diverse physicochemical properties. More than 20 amorphous solid dispersion-based products that have be...Cellulose derivatives have gained immense popularity as stabilizers for amorphous solid dispersion owing to their diverse physicochemical properties. More than 20 amorphous solid dispersion-based products that have been approved for marketing consist of cellulose derivatives as stabilizers, thus highlighting their importance in generation of amorphous solid dispersions. These polymers offer numerous advantages like drug solubilization, crystallization inhibition and improvement in release patterns of drugs. Exploring their potential and exploiting their chemistry and p H responsive behaviour have led to the synthesis of new derivatives that has broadened the scope of the use of cellulose derivatives in amorphous formulation development. The present review aims to provide an overview of different mechanisms by which these cellulose derivatives inhibit the crystallization of drugs in the solid state and from supersaturated solution. A summary of different categories of cellulose derivatives along with the newly explored polymers has been provided. A special segment on strengths, weaknesses, opportunities, and threats(SWOT) analysis and critical quality attributes(CQAs) which affect the performance of the cellulose based amorphous solid dispersion will aid the researchers in identifying the major challenges in the development of cellulose based solid dispersion and serve as a guide for further formulation development.展开更多
Formulation of poorly water-soluble crystalline drugs in their amorphous counterpart is a common approach to enhance their biodisponibility. In this study, the amorphous forms of ketoprofen and flurbiprofen were obtai...Formulation of poorly water-soluble crystalline drugs in their amorphous counterpart is a common approach to enhance their biodisponibility. In this study, the amorphous forms of ketoprofen and flurbiprofen were obtained by supercooling of the melt in a DSC （differential scanning calorimetry） apparatus and then investigated, especially under the stability point of view. The average rate of molecular motions at any given temperature is probably the most important parameter to know for amorphous pharmaceutical materials, and it was used to explain and predict the stability of ketoprofen and flurbiprofen. A quantitative estimate of the product＇s behaviour upon storage is obtained with additional data, such as the heat capacity of crystalline and amorphous samples and the distribution of molecular relaxation times. Amorphous flurbiprofen demonstrated greater physical stability at any aging temperature tested, when compared to ketoprofen and a different dependence from aging temperature. Both amorphous drugs could he classified as ＂fragile＂ ones.展开更多
基金financial support from the De-partment of Pharmaceuticals(Do P),Ministry of Chemicals and Fertilizers,Govt.of India
文摘Cellulose derivatives have gained immense popularity as stabilizers for amorphous solid dispersion owing to their diverse physicochemical properties. More than 20 amorphous solid dispersion-based products that have been approved for marketing consist of cellulose derivatives as stabilizers, thus highlighting their importance in generation of amorphous solid dispersions. These polymers offer numerous advantages like drug solubilization, crystallization inhibition and improvement in release patterns of drugs. Exploring their potential and exploiting their chemistry and p H responsive behaviour have led to the synthesis of new derivatives that has broadened the scope of the use of cellulose derivatives in amorphous formulation development. The present review aims to provide an overview of different mechanisms by which these cellulose derivatives inhibit the crystallization of drugs in the solid state and from supersaturated solution. A summary of different categories of cellulose derivatives along with the newly explored polymers has been provided. A special segment on strengths, weaknesses, opportunities, and threats(SWOT) analysis and critical quality attributes(CQAs) which affect the performance of the cellulose based amorphous solid dispersion will aid the researchers in identifying the major challenges in the development of cellulose based solid dispersion and serve as a guide for further formulation development.
文摘Formulation of poorly water-soluble crystalline drugs in their amorphous counterpart is a common approach to enhance their biodisponibility. In this study, the amorphous forms of ketoprofen and flurbiprofen were obtained by supercooling of the melt in a DSC （differential scanning calorimetry） apparatus and then investigated, especially under the stability point of view. The average rate of molecular motions at any given temperature is probably the most important parameter to know for amorphous pharmaceutical materials, and it was used to explain and predict the stability of ketoprofen and flurbiprofen. A quantitative estimate of the product＇s behaviour upon storage is obtained with additional data, such as the heat capacity of crystalline and amorphous samples and the distribution of molecular relaxation times. Amorphous flurbiprofen demonstrated greater physical stability at any aging temperature tested, when compared to ketoprofen and a different dependence from aging temperature. Both amorphous drugs could he classified as ＂fragile＂ ones.
