Abstract: A risperidone sustained release microsphere formulation is provided. The microsphere formulation includes risperidone or 9-hydroxy risperidone or salts thereof, and a polymer blend having a first uncapped lactide-glycolide copolymer and a second uncapped lactide-glycolide copolymer, in which the first uncapped lactide-glycolide copolymer is a copolymer with a high intrinsic viscosity and the second uncapped lactide-glycolide copolymer is a copolymer with a low intrinsic viscosity. The sustained release micro sphere formulation according to an embodiment of the present disclosure is suitable for large-scale industrialized production with improved stability, the in vivo release behavior of which will not change after long-term storage.

Abstract: A risperidone sustained release microsphere formulation is provided. The microsphere formulation includes risperidone or 9-hydroxy risperidone or salts thereof, and a polymer blend having a first uncapped lactide-glycolide copolymer and a second uncapped lactide-glycolide copolymer, in which the first uncapped lactide-glycolide copolymer is a copolymer with a high intrinsic viscosity and the second uncapped lactide-glycolide copolymer is a copolymer with a low intrinsic viscosity. The sustained release micro sphere formulation according to an embodiment of the present disclosure is suitable for large-scale industrialized production with improved stability, the in vivo release behavior of which will not change after long-term storage.

Abstract: A risperidone sustained release microsphere formulation is provided. The microsphere formulation includes risperidone or 9-hydroxy risperidone or salts thereof, and a polymer blend having a first uncapped lactide-glycolide copolymer and a second uncapped lactide-glycolide copolymer, in which the first uncapped lactide-glycolide copolymer is a copolymer with a high intrinsic viscosity and the second uncapped lactide-glycolide copolymer is a copolymer with a low intrinsic viscosity. The sustained release micro sphere formulation according to an embodiment of the present disclosure is suitable for large-scale industrialized production with improved stability, the in vivo release behavior of which will not change after long-term storage.

Abstract: A risperidone sustained release microsphere formulation is provided. The microsphere formulation comprise risperidone or 9-hydroxy risperidone or salts thereof, and a polymer blend having a first uncapped lactide-glycolide copolymer and a second uncapped lactide-glycolide copolymer, in which the first uncapped lactide-glycolide copolymer is a copolymer with a high intrinsic viscosity and the second uncapped lactide-glycolide copolymer is a copolymer with a low intrinsic viscosity. The sustained release micro sphere formulation according to an embodiment of the present disclosure is suitable for large-scale industrialized production with improved stability, the in vivo release behavior of which will not change after long-term storage.

Abstract: A supercritical carbon dioxide-assisted solid-phase grafting modification method for polypropylene, comprises swelling polypropylene for 0.5 to 10 hours in supercritical carbon dioxide having dissolved vinyl monomer and an initiator, then slowly relieving the pressure; moving the polypropylene that has undergone the swelling process into a reaction kettle, and adding xylene as an interface agent, the mass of xylene being 1% of the polypropylene; increasing the temperature to between 65° C. and 165° C. under normal pressure, and reacting 1 to 10 hours to obtain modified polypropylene; the swelling permeation temperature during the swelling process is from 31° C. to 60° C., the swelling pressure is from 7.5 to 12 MPa; the initiator is an azo compound or a peroxide. In the present method, the grafting rate reaches 5.4%, the thermal property, polarity, and mechanical property all improve substantially, and hydrophilic property is substantially enhanced.

Abstract: A risperidone sustained release microsphere formulation is provided. The microsphere formulation comprise risperidone or 9-hydroxy risperidone or salts thereof, and a polymer blend having a first uncapped lactide-glycolide copolymer and a second uncapped lactide-glycolide copolymer, in which the first uncapped lactide-glycolide copolymer is a copolymer with a high intrinsic viscosity and the second uncapped lactide-glycolide copolymer is a copolymer with a low intrinsic viscosity. The sustained release micro sphere formulation according to an embodiment of the present disclosure is suitable for large-scale industrialized production with improved stability, the in vivo release behavior of which will not change after long-term storage.

Abstract: The present application relates to methods for growing crystals of both the uncomplexed and complexed forms of ?-secretase (BACE) polypeptide. The present application also relates to crystalline forms of uncomplexed BACE and the three-dimensional structure of BACE, as determined from the crystals. In addition, the present application relates to the use of crystalline forms of BACE to identify ligands, preferably inhibitors (antagonists), which bind to, and preferably inhibit the enzymatic activity of, BACE. Furthermore, the present application relates to nucleic acid sequences encoding BACE polypeptide, and methods for making BACE in greater quantity than prior methods, resulting in more effective crystallization.

Abstract: The present invention relates to Pregnane X receptor (PXR) polypeptides and crystals that are useful, for example, for crystallization and in assays for identification of modulators of PXR.

Abstract: The present invention relates, inter alia, to PXR polypeptides and crystals that are useful, for example, for crystallization and in assays for identification of modulators of PXR.

Abstract: The present invention relates, inter alia, to PXR polypeptides and crystals that are useful, for example, for crystallization and in assays for identification of modulators of PXR.

Abstract: The present application relates to methods for growing crystals of both the uncomplexed and complexed forms of ?-secretase (BACE) polypeptide. The present application also relates to crystalline forms of uncomplexed BACE and the three-dimensional structure of BACE, as determined from the crystals. In addition, the present application relates to the use of crystalline forms of BACE to identify ligands, preferably inhibitors (antagonists), which bind to, and preferably inhibit the enzymatic activity of, BACE. Furthermore, the present application relates to nucleic acid sequences encoding BACE polypeptide, and methods for making BACE in greater quantity than prior methods, resulting in more effective crystallization.

Abstract: The present application relates to methods for growing crystals of both the uncomplexed and complexed forms of ?-secretase (BACE) polypeptide. The present application also relates to crystalline forms of uncomplexed BACE and the three-dimensional structure of BACE, as determined from the crystals. In addition, the present application relates to the use of crystalline forms of BACE to identify ligands, preferably inhibitors (antagonists), which bind to, and preferably inhibit the enzymatic activity of, BACE. Furthermore, the present application relates to nucleic acid sequences encoding human BACE polypeptide, and methods for making BACE in greater quantity than prior methods, resulting in more effective crystallization.

Abstract: The present invention discloses purified polypeptides that comprise an active ADAM33 catalytic domain. In addition, the present invention discloses nucleic acids that encode the polypeptides of the present invention. The present invention also discloses methods of growing X-ray diffractable crystals of polypeptides comprising the active ADAM33 catalytic domain. In addition, the present invention discloses methods of using the X-ray diffractable crystals of ADAM33 in structure-based drug design to identify compounds that can modulate the enzymatic activity of ADAM33. The present invention also discloses methods of treating respiratory disorders by administering therapeutic amounts of the ADAM33 catalytic domain.

Abstract: The present invention discloses purified polypeptides that comprise an active ADAM33 catalytic domain. In addition, the present invention discloses nucleic acids that encode the polypeptides of the present invention. The present invention also discloses methods of growing X-ray diffractable crystals of polypeptides comprising the active ADAM33 catalytic domain. In addition, the present invention discloses methods of using the X-ray diffractable crystals of ADAM33 in structure-based drug design to identify compounds that can modulate the enzymatic activity of ADAM33. The present invention also discloses methods of treating respiratory disorders by administering therapeutic amounts of the ADAM33 catalytic domain.

Abstract: The present invention discloses purified polypeptides that comprise an active human ADAM33 catalytic domain. In addition, the present invention discloses nucleic acids that encode the polypeptides of the present invention. The present invention also discloses methods of growing X-ray diffractable crystals of polypeptides comprising the active human ADAM33 catalytic domain. The present invention further discloses a crystalline form of a catalytic domain of human ADAM33. In addition, the present invention discloses methods of using the X-ray diffractable crystals of human ADAM33 in structure based drug design to identify compounds that can modulate the enzymatic activity of human ADAM33. The present invention also discloses methods of treating respiratory disorders by administering therapeutic amounts of the human ADAMS33 catalytic domain.

Abstract: The present application relates to methods for growing crystals of both the uncomplexed and complexed forms of ?-secretase (BACE) polypeptide. The present application also relates to crystalline forms of uncomplexed BACE and the three-dimensional structure of BACE, as determined from the crystals. In addition, the present application relates to the use of crystalline forms of BACE to identify ligands, preferably inhibitors (antagonists), which bind to, and preferably inhibit the enzymatic activity of, BACE. Furthermore, the present application relates to nucleic acid sequences encoding BACE polypeptide, and methods for making BACE in greater quantity than prior methods, resulting in more effective crystallization.

Abstract: The present invention discloses purified polypeptides that comprise an active ADAM33 catalytic domain. In addition, the present invention discloses nucleic acids that encode the polypeptides of the present invention. The present invention also discloses methods of growing X-ray diffractable crystals of polypeptides comprising the active ADAM33 catalytic domain. In addition, the present invention discloses methods of using the X-ray diffractable crystals of ADAM33 in structure-based drug design to identify compounds that can modulate the enzymatic activity of ADAM33. The present invention also discloses methods of treating respiratory disorders by administering therapeutic amounts of the ADAM33 catalytic domain.

Abstract: The present invention discloses purified polypeptides that comprise an active ADAM33 catalytic domain. In addition, the present invention discloses nucleic acids that encode the polypeptides of the present invention. The present invention also discloses methods of growing X-ray diffractable crystals of polypeptides comprising the active ADAM33 catalytic domain. In addition, the present invention discloses methods of using the X-ray diffractable crystals of ADAM33 in structure-based drug design to identify compounds that can modulate the enzymatic activity of ADAM33. The present invention also discloses methods of treating respiratory disorders by administering therapeutic amounts of the ADAM33 catalytic domain.

Abstract: The present application relates to methods for growing crystals of both the uncomplexed and complexed forms of ?-secretase (BACE) polypeptide. Polypeptides used herein are derived from human BACE which is also known by the synonyms “mamapsin 2”, “human ?-site APP-cleaving enzyme, and Asp2”. The present application also relates to crystalline forms of uncomplexed BACE and the three-dimensional structure of BACE, as determined from the crystals. In addition, the present application relates to the use of crystalline forms of BACE to identify ligands, preferably inhibitors (antagonists), which bind to, and preferably inhibit the enzymatic activity of, BACE. Furthermore, the present application relates to nucleic acid sequences encoding BACE polypeptide, and methods for making BACE in greater quantity than prior methods, resulting in more effective crystallization.

Abstract: The present invention discloses purified polypeptides that comprise an active ADAM33 catalytic domain. In addition, the present invention discloses nucleic acids that encode the polypeptides of the present invention. The present invention also discloses methods of growing X-ray diffractable crystals of polypeptides comprising the active ADAM33 catalytic domain. The present invention further discloses a crystalline form of a catalytic domain of ADAM33. In addition, the present invention discloses methods of using the X-ray diffractable crystals of ADAM33 in structure based drug design to identify compounds that can modulate the enzymatic activity of ADAM33. The present invention also discloses methods of treating respiratory disorders by administering therapeutic amounts of the ADAM33 catalytic domain.