Clofarabine injection and preparation method thereof
A technology of clofarabine and injection, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc. It can solve the problems of insignificant changes in solubility, difficulty in ensuring solution clarity, and particle precipitation, etc. problems, to achieve the effect of high concentration, convenient clinical use, and rapid dissolution
Active Publication Date: 2011-08-03
鲁南新时代生物技术有限公司
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Problems solved by technology
However, the inventor found through a large number of tests that after adding alkaline substances such as sodium hydroxide and sodium carbonate to make it into a salt, the solubility of clofarabine increased, but the clarity of the solution was difficult to ensure, and the solubility of this product did not change after adding the acid. obvious
[0008] Chinese patent CN1101152204A mentions that adding sodium chloride or glucose to its prescription can increase the dissolution rate of clofarabine, but the inventors found that the injections prepared according to this patent also have particle precipitation during long-term storage.
[0009] In summary, the clofarabine injection reported in the prior art has certain limitations in enhancing the water solubility of clofarabine and solving the problem of particle precipitation in aqueous solution
Method used
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Embodiment 1
[0020] Embodiment 1 Preparation of Clofarabine Injection
[0021] Clofarabine 2g
[0023] Propylene glycol 1g
[0024] Water for injection 2000mL
[0025] Preparation method: Measure 1500 mL of water for injection, add 1g of propylene glycol, stir to dissolve, add 18g of sodium chloride, stir to dissolve, then add 2g of clofarabine powder with a particle size of 20-60 μm screened by ultrafine grinding technology , stir to make it dissolve, use medicinal hydrochloric acid to adjust the pH to 4.5-7.5, add 0.1% activated carbon for needles, filter with a 0.22 μm filter membrane after stirring, add water for injection to 2000 mL, and fill each 20 mL bottle with 121 Sterilize at ℃ for 15 minutes, inspect and package under light.
Embodiment 2
[0032] Embodiment 2 Stability investigation of clofarabine injection of the present invention
[0033] 【an examination】
[0034] Properties This product is a colorless clear liquid.
[0035] The pH value should be 4.5-7.5 (Appendix VI H of the Chinese Pharmacopoeia 2010 Edition).
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Abstract
The invention relates to a clofarabine injection and a preparation method thereof. The clofarabine injection comprises the following components in part by weight: 20 parts of clofarabine, 180 parts of sodium chloride, 10 parts of propylene glycol, water for injection and hydrochloric acid serving as a pH regulator, wherein the water for injection is added until the concentration of the clofarabine is between 0.08 and 0.12 percent, and the pH regulator is added until the pH value of the injection is between 4.5 and 7.5. Compared with the prior art, the clofarabine injection prepared by the method has the advantages that the clofarabine injection is more stable, and particles are not separated out in the standing process. In addition, the invention provides a method for increasing the solubility of the clofarabine. In the process for preparing the clofarabine injection by the method, the clofarabine has a high dissolution speed and concentration, and is convenient to use clinically.
Description
[0001] technical field [0002] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a clofarabine injection and a preparation method thereof. Background technique [0003] Acute leukemia accounts for 30% of childhood tumors, among which acute lymphoblastic leukemia (ALL) is the most common, accounting for about 80%. A considerable number of children cannot achieve or maintain complete remission to the existing drug treatment, resulting in poor prognosis and decreased long-term survival rate, and the prognosis of adult acute leukemia is even worse than that of children. It is an important and effective class of cytotoxic drugs. [0004] Clofarabine was developed by the Southern Research Institute in Birmingham, Alabama, USA, and authorized by British Bioenvision Company and American Ilex Oncology Company to jointly develop it. Due to its remarkable efficacy in phase II clinical trials, in December 2004, FDA Clofarabine (...
Claims
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IPC IPC(8): A61K9/08A61K31/7076A61K47/10A61K47/02A61P35/02
Inventor 赵志全冯中张丽萍石其德赵震震
Owner 鲁南新时代生物技术有限公司