The main objective of the present study is to develop a selfmicellizing solid dispersion(SMSD)system of cyclosporine A(CsA)using an amphiphilic copolymer,poly[MPC-co-BMA](pMB)to improve the biopharmaceutical propertie...The main objective of the present study is to develop a selfmicellizing solid dispersion(SMSD)system of cyclosporine A(CsA)using an amphiphilic copolymer,poly[MPC-co-BMA](pMB)to improve the biopharmaceutical properties of CsA(Fig.1A).Unlike conventional carrier compounds,pMB would perform the bifunctional ability as both polymeric carrier of solid dispersion system and solubilizer derived from a high micellizing property,which could be considered beneficial for the production of highly water soluble formulation of poorly water soluble compound[1].Improvement in the aqueous solubility has been believed to be a key consideration for acquiring potent pharmacological effects of BCS class II drug like CsA.展开更多
Nanosizing by wet beads milling is one of the methods to improve the solubility of poorlywater soluble compounds[1,2].Hydrophilic polymers,such as Hydroxypropylcellulose-SSL(HPC),Polyvinylalcohol(PVA),and Polyvinylpyr...Nanosizing by wet beads milling is one of the methods to improve the solubility of poorlywater soluble compounds[1,2].Hydrophilic polymers,such as Hydroxypropylcellulose-SSL(HPC),Polyvinylalcohol(PVA),and Polyvinylpyrrolidone-K30(PVP)etc.are used as dispersion stabilizer to prevent aggregation of nanoparticles.However,there are many compounds that cannot be dispersed by ordinary dispersion stabilizers.In this study,we used Povacoat?as a dispersion stabilizer for several poorly water soluble compounds milled to nanoparticles.The influences of aggregation of the nanoparticles on the dissolution behavior and the oral absorption of the compoundswere studied using formulations with high and low dispersion characters.展开更多
Nanosizing by wet beads milling is a method to improve the solubility of poorly water soluble compounds[1,2].Mebendazole(MBZ)is a well-known anthelmintic drug in wide clinical use.There were some reports that MBZ had ...Nanosizing by wet beads milling is a method to improve the solubility of poorly water soluble compounds[1,2].Mebendazole(MBZ)is a well-known anthelmintic drug in wide clinical use.There were some reports that MBZ had the anticancer effect in preclinical study.However,the bioavailability of MEB is low(<10%)due to the poor solubility in water(0.5μg/mL).The present study aimed to develop the nanocrystal formulations of MEB to improve dissolution behavior and enhance oral absorption.展开更多
文摘The main objective of the present study is to develop a selfmicellizing solid dispersion(SMSD)system of cyclosporine A(CsA)using an amphiphilic copolymer,poly[MPC-co-BMA](pMB)to improve the biopharmaceutical properties of CsA(Fig.1A).Unlike conventional carrier compounds,pMB would perform the bifunctional ability as both polymeric carrier of solid dispersion system and solubilizer derived from a high micellizing property,which could be considered beneficial for the production of highly water soluble formulation of poorly water soluble compound[1].Improvement in the aqueous solubility has been believed to be a key consideration for acquiring potent pharmacological effects of BCS class II drug like CsA.
文摘Nanosizing by wet beads milling is one of the methods to improve the solubility of poorlywater soluble compounds[1,2].Hydrophilic polymers,such as Hydroxypropylcellulose-SSL(HPC),Polyvinylalcohol(PVA),and Polyvinylpyrrolidone-K30(PVP)etc.are used as dispersion stabilizer to prevent aggregation of nanoparticles.However,there are many compounds that cannot be dispersed by ordinary dispersion stabilizers.In this study,we used Povacoat?as a dispersion stabilizer for several poorly water soluble compounds milled to nanoparticles.The influences of aggregation of the nanoparticles on the dissolution behavior and the oral absorption of the compoundswere studied using formulations with high and low dispersion characters.
文摘Nanosizing by wet beads milling is a method to improve the solubility of poorly water soluble compounds[1,2].Mebendazole(MBZ)is a well-known anthelmintic drug in wide clinical use.There were some reports that MBZ had the anticancer effect in preclinical study.However,the bioavailability of MEB is low(<10%)due to the poor solubility in water(0.5μg/mL).The present study aimed to develop the nanocrystal formulations of MEB to improve dissolution behavior and enhance oral absorption.
