196 results about "Dasatinib" patented technology

The invention discloses a dasatinib polymorphic substance. In addition, the invention also discloses a preparation method and a medicinal composition of the dasatinib polymorphic substance. The dasatinib polymorphic substance provided by the invention has the advantages of good physicochemical property and good stability, is more suitable for industrial scale preparation, and the like.

A stable amorphous form of dasatinib of Formula (I) wherein amorphous dasatinib after exposure to a relative humidity of 75% at 40 ° C. or 60% at 25 ° C. for a period of at least three months doesn't change to crystalline form and a process for the preparation of the amorphous form of dasatinib of Formula (I).

Polymorph I of dasatinib monohydrate and Polymorph II of dasatinib, their preparation methods and pharmaceutical compositions containing the same are provided. These polymorphs have better physicochemical properties, are more stable and are more suitable for industrial scale production.

The present invention provides crystalline form of (R)-propylene glycol solvate of dasatinib and crystalline form of (S)-propylene glycol solvate of dasatinib.

The present invention primarily relates to salts of Dasatinib, wherein the salts are in amorphous form. The salts described herein preferably comprise a cation of a compound of formula 1and an anion of a second compound selected from the group consisting of glutaric acid, nicotinic acid and saccharin. The invention is further related to pharmaceutical compositions comprising such a salt. Furthermore, the invention relates to processes for preparing said salts. The invention also relates to several aspects of using said salt or pharmaceutical composition to treat a disease.

The invention relates to the technical field of medicines, in particular to a crystal III of Dasatinib monohydrate, its preparation method and pharmaceutical composition. The crystal III of Dasatinib monohydrate provided in the invention is very stable under the conditions of illumination, high temperature, high humidity and accelerated testing. The pharmaceutical composition of crystal III of Dasatinib monohydrate has good dissolubility, and can be stable under high temperature conditions. In addition, compared with prior art, the preparation method provided in the invention has the advantages of simple operation and controllable quality.

The invention relates to a dasatinib pharmaceutical composition which comprises dasatinib and pharmaceutical auxiliary materials, wherein the auxiliary materials comprise pregelatinized starch and bonding agent. The dasatinib pharmaceutical composition comprises the following concrete components in percentage by weight: 1-20% of dasatinib, 20-35% of pregelatinized starch and 60-79% of bonding agent, wherein the bonding agent is selected from one or mixture of microcrystalline cellulose, hydroxypropyl cellulose sodium, hydroxymethyl cellulose sodium and hydroxypropyl cellulose. The preparation method of the dasatinib pharmaceutical composition comprises the following steps: weighing the dasatinib, pregelatinized starch and bonding agent according to component proportions; sieving the dasatinib by a sieve with 100 meshes, sieving the pregelatinized starch and bonding agent by a sieve with 80 meshes, and uniformly mixing the dasatinib and the sieved auxiliary materials to obtain powder; and directly pressing the powder to obtain the dasatinib pharmaceutical composition. Because the pregelatinized starch is adopted, the product quality and product stability are greatly improved. The dasatinib pharmaceutical composition is a new preparation which has the advantages of better liquidity, higher stability and low hygroscopicity and is suitable for clinical pharmaceutical applications.

The anticancer medicine composition containing tyrosine kinase inhibitor is slow released injection and slow released implant. The effective anticancer components include tyrosine kinase inhibitor selected from Erbitux, Iressa, Tarceva, Sunitinib, Trastuzumab, etc, and / or composition selected from Docetaxel, deacetyl taxol, taxol, etc. The slow releasing supplementary material is selected from p(LAEG-EOP), p(DAPG-EOP), etc. The released injection and slow released implant may be injected or set in tumor for slow releasing to maintain effective medicine concentration for over 50 days, and has obviously lowered systemic reaction on the medicine and capacity of enhancing the chemotherapeutic and radiotherapeutic effect.