Bortezomib lyophilized powder for injection and preparation process thereof

Abstract

The invention provides bortezomib lyophilized powder for injection. The bortezomib lyophilized powder for injection comprises the following raw materials in parts by weight: 0.1 to 0.3 part of bortezomib, 3 to 10 parts of acetonitrile, 1 to 3 parts of mannitol and 87 to 94 parts of water. A preparation process comprises the following steps: fully dissolving the raw material medicines in an acetonitrile-aqueous solution, and then putting the mixed solution into the auxiliary material, namely a mannitol solution; the bortezomib is in sufficient contact with the mannitol solution in a dissolved state to rapidly form boric acid ester, so that the problem of poor solubility of the bortezomib raw material is solved under the premise of small use amount of an organic solvent, and the stability ofan intermediate product and a preparation is improved.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a bortezomib freeze-dried powder for injection. Background technique [0002] Bortezomib is a new type of antineoplastic drug, trade name Velcade, developed by Millennium Pharmaceutical Company of the United States. The solubility of the bulk drug of bortezomib in water is only 0.52mg / ml, and the solubility of the bulk drug is low, which cannot reach the prescription concentration. Therefore, it is necessary to use an appropriate co-solvent, and on this basis to obtain a finished preparation with good stability. [0003] Chinese patent CN102784114, a bortezomib freeze-dried powder injection and its preparation method, by mixing and grinding bortezomib and excipients, the two are fully contacted and mixed to promote the dissolution of the raw material bortezomib, and at the same time add antioxidants to increase its stability. Chinese patent CN103142509, the composition contai...

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