7 results about "Lurasidone" patented technology

The invention discloses a lumepirone long-acting microsphere sustained-release preparation without a release stagnation period in an early stage, which comprises a lumepirone active ingredient and a medicinal polymer auxiliary material in a mass ratio of (1: 4)-(1: 1), the medicinal polymer auxiliary material is at least one of glycolide-lactide copolymers with the weight-average molecular weight of 5000-150000 Da, and the molar ratio of lactic acid units to glycolic acid units of the glycolide-lactide copolymers is (50: 50)-(95: 5). The lumepirone long-acting microsphere sustained-release preparation without a release arrest phase in the early stage is obtained by specially limiting drying conditions in liquid and medicinal polymer auxiliary materials, the release of the lumepirone long-acting microsphere sustained-release preparation can be maintained for 2 weeks to 1 month without oral administration of the long-acting sustained-release microspheres of lumepirone capsules, the safety and effectiveness of the medicine are met, and the sustained-release preparation is suitable for clinical application. Meanwhile, the problems of early-stage long-time stagnant release and early-stage burst release of the long-acting microsphere preparation can be solved, the compliance can be effectively improved, convenience is provided for patients to the maximum extent, and the economic cost is reduced.

The present invention provides a solid dispersion comprising lurasidone or a pharmaceutically acceptable salt thereof and a carrier. The carrier material includes polyvinyl acetate phthalate (PVAP), polyvinyl alcohol (PVA), cellulose acetate phthalate (CAP), mesoporous silica, hydroxypropyl methylcellulose (HPMC), polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer, acrylic resin, hydroxypropyl cellulose (HPC), povidone, copovidone, ethylcellulose, polyoxyethylene glycol, hypromellose acetate succinate (HPMCAS), hypromellose phthalate (HPMCP), or a combination thereof.

The invention provides an application of lurasidone or a pharmaceutically acceptable salt thereof in preparation of a medicine for preventing and / or treating diabetes individual bone injury healing disorder. The hyperglycemia environment causes excessive secretion of lipocalin-2 (LCN2) by activating a phosphopentose pathway of neutrophil, thereby inhibiting osteogenic differentiation of skeletal stem cells. According to the application of the lurasidone or the pharmaceutically acceptable salt thereof in the preparation of the medicine for preventing and / or treating the diabetic individual bone injury healing disorder, in the application provided by the invention, the lurasidone can specifically inhibit the metabolic pathway and the secretion of LCN2, remodel an immune microenvironment beneficial to repair, and promote the healing of the diabetic individual bone injury. The formation of callus under the condition of diabetes mellitus is obviously accelerated and the mineral density of bone is improved.

This application relates to combination compositions for use in treatment of depression, and which can alleviate the anxiogenic side effects of certain antidepressant and antipsychotic medications. Methods for treatment of depression and medicament side effects, particular anxiety, akathisia, and associated suicidality are also described herein.

The utility model discloses a device capable of preventing lurasidone tablets from rotating in a conical hopper, relates to the technical field of lurasidone tablet can particles, and aims to solve the problems that the tablets cannot fall into a plastic bottle within a specified time due to the fact that the tablets continuously rotate along the smooth inner wall of a shattering protective cover when the tablets freely fall in an existing can particle device, and the tablets cannot fall into the plastic bottle within the specified time. According to the key points of the technical scheme, the tablet falling protection device comprises a tablet falling protection cover, an inner insertion plate is inserted into the tablet falling protection cover, the cross section of the inner insertion plate is in a cross shape, and the tablet falling protection cover is in a conical barrel shape; the side edge of the inner inserting plate is provided with an inclined edge with the same conical angle as the conical shattering protection cover, a heating cover is installed on the outer portion of the shattering protection cover in a covering and buckling mode and is in a conical shape, and the conical angle of the heating cover is matched with the conical angle of the shattering protection cover. And the effects that the tablets can be prevented from sliding on the inner wall of the shattering protective cover, and the tablets can fall into the plastic bottle within the set time are achieved.

Some embodiments of the present disclosure provide solid dispersions comprising lurasidone, or a pharmaceutically acceptable salt thereof, and a carrier. The carrier is prepared from the following materials: polyvinyl acetate phthalate (PVAP), polyvinyl alcohol (PVA), cellulose acetate phthalate (CAP), mesoporous silicon oxide, hydroxypropyl methyl cellulose (HPMC), a polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol grafted copolymer, acrylic resin, hydroxypropyl cellulose (HPC), polyvinylpyrrolidone, copovidone and ethyl cellulose; the composition may be selected from the group consisting of hydroxypropyl methyl cellulose, hydroxypropyl methyl cellulose, polyethylene glycol, hydroxypropyl methyl cellulose succinate (HPMCAS), hydroxypropyl methyl cellulose phthalate (HPMCP), or a combination thereof.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a compound and application thereof as a 5-HT2AR receptor antagonist and a 5-HT1AR agonist. According to the method, the rational design of structure guidance is carried out on the basis of the structure basis and the interaction mode of key targets such as lurasidone and 5-HT1AR, 5-HT2AR and the like. A novel compound is successfully obtained by retaining a core pharmacophore MID and iteratively optimizing benzothiazole, piperazine and cyclohexyl regions. According to the compound, the affinity to DRD2 is eliminated, and meanwhile, the agonistic activity to 5-HT1AR and the antagonistic effect to 5-HT2AR are reserved.