The stability of the shapes of crystal growth face and dissolution face in a two-dimensional mathematical model of crystal growth from solution under microgravity is studied. It is proved that the stable shapes of cry...The stability of the shapes of crystal growth face and dissolution face in a two-dimensional mathematical model of crystal growth from solution under microgravity is studied. It is proved that the stable shapes of crystal growth face and dissolution face do exist, which are suitably shaped curves with their upper parts inclined backward properly.The stable shapes of crystal growth faces and dissolution faces are calculated for various values of parameters, Ra, Pr and Sc. It is shown that the stronger the convection relative to the diffusion in solution is, the more backward the upperparts of the stable crystal growth face and dissolution face are inclined. The orientation and the shape of dissolution face hardly affect the stable shape of crystal growth face and vice versa.展开更多
The solid forms of drugs play a central role in controlling their physicochemical properties and consequently the bioavailability. Multiple types of drug solid forms have been developed to achieve the desirable pharma...The solid forms of drugs play a central role in controlling their physicochemical properties and consequently the bioavailability. Multiple types of drug solid forms have been developed to achieve the desirable pharmaceutical profiles, but new solid forms will provide more options for the solid-state property optimization and hence are highly desirable. This review focuses on a new pharmaceutical solid form, drug-polymer inclusion complexes (ICs), and summarizes their structural features, structure- property relationships, as well as potential pharmaceutical applications展开更多
The solid form of drugs plays a central role in optimizing the physicochemical properties of drugs,and new solid forms will provide more options to achieve the desirable pharmaceutical profiles of drugs.Recently,certa...The solid form of drugs plays a central role in optimizing the physicochemical properties of drugs,and new solid forms will provide more options to achieve the desirable pharmaceutical profiles of drugs.Recently,certain drugs have been found to form crystalline inclusion complexes(ICs) with multiple types of linear polymers,representing a new subcategory of pharmaceutical solids.In this study,we used diflunisal(DIF) as the model drug host and extended the guest of drug/polymer ICs from homopolymers to block copolymers of poly(ethylene glycol)(PEG) and poly(s-caprolactone)(PCL).The block length in the guest copolymers showed a significant influence on the formation,thermal stability and dissolution behavior of the DIF ICs.Though the PEG block could hardly be included alone,it could indeed be included in the DIF ICs when the PCL block was long enough.The increase of the PCL block length produced IC crystals with improved thermal stability.The dissolution profiles of DIF/block copolymer ICs exhibited gradually decreased aqueous solubility and dissolution rate with the increasing PCL block length.These results demonstrate the possibility of using drug/polymer ICs to modulate the desired pharmaceutical profiles of drugs in a predictable and controllable manner.展开更多
文摘The stability of the shapes of crystal growth face and dissolution face in a two-dimensional mathematical model of crystal growth from solution under microgravity is studied. It is proved that the stable shapes of crystal growth face and dissolution face do exist, which are suitably shaped curves with their upper parts inclined backward properly.The stable shapes of crystal growth faces and dissolution faces are calculated for various values of parameters, Ra, Pr and Sc. It is shown that the stronger the convection relative to the diffusion in solution is, the more backward the upperparts of the stable crystal growth face and dissolution face are inclined. The orientation and the shape of dissolution face hardly affect the stable shape of crystal growth face and vice versa.
基金supported by the National Natural Science Foundation of China (No. 21434008)
文摘The solid forms of drugs play a central role in controlling their physicochemical properties and consequently the bioavailability. Multiple types of drug solid forms have been developed to achieve the desirable pharmaceutical profiles, but new solid forms will provide more options for the solid-state property optimization and hence are highly desirable. This review focuses on a new pharmaceutical solid form, drug-polymer inclusion complexes (ICs), and summarizes their structural features, structure- property relationships, as well as potential pharmaceutical applications
基金financially supported by the National Natural Science Foundation of China(Nos.21434008,21374054)National Basic Research Program of China(973 Program,No.2014CB932202)
文摘The solid form of drugs plays a central role in optimizing the physicochemical properties of drugs,and new solid forms will provide more options to achieve the desirable pharmaceutical profiles of drugs.Recently,certain drugs have been found to form crystalline inclusion complexes(ICs) with multiple types of linear polymers,representing a new subcategory of pharmaceutical solids.In this study,we used diflunisal(DIF) as the model drug host and extended the guest of drug/polymer ICs from homopolymers to block copolymers of poly(ethylene glycol)(PEG) and poly(s-caprolactone)(PCL).The block length in the guest copolymers showed a significant influence on the formation,thermal stability and dissolution behavior of the DIF ICs.Though the PEG block could hardly be included alone,it could indeed be included in the DIF ICs when the PCL block was long enough.The increase of the PCL block length produced IC crystals with improved thermal stability.The dissolution profiles of DIF/block copolymer ICs exhibited gradually decreased aqueous solubility and dissolution rate with the increasing PCL block length.These results demonstrate the possibility of using drug/polymer ICs to modulate the desired pharmaceutical profiles of drugs in a predictable and controllable manner.