Carmustine precursor liposome powder injection formulation and process for preparing
A technology of precursor lipid and carmustine, which is applied in liposome delivery, amide active ingredients, drug combination, etc., can solve the problems of affecting clinical treatment effect, reducing the immune function of the body, and patients can not continue to use drugs, etc., to achieve Avoid chronic decomposition, improve therapeutic effect, effect of small particle size
Inactive Publication Date: 2004-08-18
谷松兰 +4
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Problems solved by technology
It has a good curative effect on malignant brain tumors, brain and spinal cord metastasis of malignant tumors, and leukemia with invasion of the central nervous system. The bone marrow hematopoietic system inhibits the regeneration of white blood cells and platelets, and reduces the immune function of the body, so that patients cannot continue to take medication and affect the clinical treatment effect
Carmustine aqueous injection is easy to decompose and has poor stability in long-term storage
Method used
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Experimental program
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Effect test
Embodiment
[0020] Weigh 1.5 grams of carmustine, 4.5 grams of lecithin and 0.8 grams of cholesterol and dissolve them in ether, place for 1 hour, filter with a 0.22F type mixed fiber membrane, and add the filtrate to 20 grams of mannitol as a support agent in two times, Shake and shake to mix evenly, vacuum dry to recover ether, the vacuum degree is -0.08Mpa, then put the solid in a vacuum desiccator and vacuum dry for 20 hours to obtain loose light yellow carmustine powder injection.
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The precursor liposome powder for injection preparation has Carmustine in 3-12 wt% as main material and other components including phospholipid 19-25 wt%, sterol 3.5-6.5 wt% and support agent 54-73 wt%. Carmustine, phospholipid and sterol are compounded into solution; the solution is added into the support agent powder gradually and the mixture is vacuum dried to form Carmustine powder for injection preparation. Before use, the Carmustine powder for injection preparation is mixed with water for injection to form Carmustine liposome injection preparation. The injection preparation has Carmustine coated in double-layer liposome film of phospholipid and sterol and thus less toxic side effect of Carmustine to human body, so that it may be used continuously for raised cancer treating effect.
Description
Technical field [0001] The invention relates to the preparation of carmustine proliposome powder injection preparation. Carmustine (Carmustine C 5 h 9 o 2 N 2 Cl 2 ) as the main raw material and formulated into proliposome powder injection. Background technique [0002] Carmustine (Carmustine) injection (carmustine injection) recorded on page 127 of the Chinese Pharmacopoeia is a sterile polyethylene glycol 400 solution of carmustine, wherein the labeled amount of carmustine is 90.0-110.0 %, the drug has high ester solubility and is easy to pass through the blood-brain barrier. It has a good curative effect on malignant brain tumors, brain and spinal cord metastasis of malignant tumors, and leukemia with invasion of the central nervous system. The bone marrow hematopoietic system inhibits the regeneration of white blood cells and platelets and reduces the immune function of the body, thus making it impossible for patients to continue taking medication and affecting th...
Claims
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Inventor 谷松兰李玉英邓皓云沈志林黄瑞川
Owner 谷松兰
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