Abstract: Disclosed are a decoquinate liposome, a preparation method therefor and a use thereof. The preparation raw materials for the decoquinate liposome comprise the following components in parts by weight: 1 part of decoquinate and 2-20 parts of lecithin. The liposome is stable, shows favorable malaria resistance effects in-vivo and in-vitro with respect to animal bodies, can be used for quickly relieving the conditions of malaria, particularly subtertian malaria, and is safe. The preparation method is simple and feasible, and has the potential for mass production.

Abstract: Hot-melt extrusion for producing solid solution comprising nanoparticle formulation of decoquinate is disclosed. Aqueous phase comprising the nanoparticles of hot-melt extruding products is homogeneous and stable. Provided is the composition comprising the solid solution of decoquinate and a method of hot-melt extrusion for producing this composition comprising the solid dispersion of decoquinate. Furthermore, provided is the solid solution comprising nanosized decoquinate formulation having improved water solubility and enhanced delivery of decoquinate in digestive system for absorption, increasing bioavailability, and the efficacy against malaria at the liver stage.

Abstract: Implants comprising an antimalarial agent such as decoquinate or another therapeutic drug are disclosed. The implants can be in the form of a complex comprising a drug, a lipid or lipids and optionally a polymer carrier. The present invention provides methods for preparing implants wherein the implants comprise decoquinate or another therapeutic drug, and a lipid or lipids such as cholesterol, monoglycerides, or diglycerides, and optionally a small percentage of a biocompatible polymer based on the total implant weight. The implants are useful for releasing a therapeutic drug at a constant level and maintaining a prophylactic or therapeutic level of the drug in a subject, for preventing a malarial infection or treating other diseases or disorders.

Abstract: Hot-melt extrusion for producing solid solution comprising nanoparticle formulation of decoquinate is disclosed. Aqueous phase comprising the nanoparticles of hot-melt extruding products is homogeneous and stable. Provided is the composition comprising the solid solution of decoquinate and a method of hot-melt extrusion for producing this composition comprising the solid dispersion of decoquinate. Furthermore, provided is the solid solution comprising nanosized decoquinate formulation having improved water solubility and enhanced delivery of decoquinate in digestive system for absorption, increasing bioavailability, and the efficacy against malaria at the liver stage.

Abstract: Implants comprising an antimalarial agent such as decoquinate or another therapeutic drug are disclosed. The implants can be in the form of a complex comprising a drug, a lipid or lipids and optionally a polymer carrier. The present invention provides methods for preparing implants wherein the implants comprise decoquinate or another therapeutic drug, and a lipid or lipids such as cholesterol, monoglycerides, or diglycerides, and optionally a small percentage of a biocompatible polymer based on the total implant weight. The implants are useful for releasing a therapeutic drug at a constant level and maintaining a prophylactic or therapeutic level of the drug in a subject, for preventing a malarial infection or treating other diseases or disorders.

Abstract: The present invention relates to a hot melt extrusion composition, a process for preparing a hot melt extruded product using the hot melt extrusion composition, a solid dispersion of decoquinate, and pharmaceutical uses of the composition and the solid dispersion of decoquinate. The hot melt extrusion composition comprises 5 to 30% of decoquinate, 60 to 90% of a polymeric carrier and 0 to 10% of a surfactant. The hot melt extrusion composition can be melted into a liquid at a temperature below the melting point of decoquinate to achieve complete mixing, effectively avoiding the possible thermal decomposition of decoquinate and other components of the composition during the hot-melt process, thus retaining their original structures and pharmacodynamic activity.

Abstract: The present invention relates to a hot melt extrusion composition, a process for preparing a hot melt extruded product using the hot melt extrusion composition, a solid dispersion of decoquinate, and pharmaceutical uses of the composition and the solid dispersion of decoquinate. The hot melt extrusion composition comprises 5 to 30% of decoquinate, 60 to 90% of a polymeric carrier and 0 to 10% of a surfactant. The hot melt extrusion composition can be melted into a liquid at a temperature below the melting point of decoquinate to achieve complete mixing, effectively avoiding the possible thermal decomposition of decoquinate and other components of the composition during the hot-melt process, thus retaining their original structures and pharmacodynamic activity.