Taxotere nano preparation carried by albumin and phospholipid and method preparing same
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A technology of docetaxel and nano-preparation, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., which can solve the problems of poor water solubility of docetaxel and eliminate allergies Response, stability improvement, safety improvement effect
Inactive Publication Date: 2011-06-01
孙璐
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[0004] The present invention solves the problem of poor water solubility of existing docetaxel drugs
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specific Embodiment approach 1
[0021] Specific embodiment one: this embodiment is made up of docetaxel, albumin, phospholipid, vitamin E, lyophilized excipient and acid buffer salt by weight percentage, docetaxel is 1~15% by weight percentage, white 10-43% of protein, 10-43% of phospholipid, 1-10% of vitamin E, 1-20% of lyophilized excipient and 1-15% of acid buffer salt, adding organic solvent, adopting high-pressure uniform The solid powder preparation of 100-700 nanometers is prepared by the preparation process of quality and freeze-drying.
specific Embodiment approach 2
[0022] Specific embodiment two: the difference between this embodiment and specific embodiment one is that the percentage by weight of docetaxel is 8%, albumin is 30%, phospholipid is 30%, vitamin E is 5%, and the freeze-drying excipient is 15% and 12% acid buffer salt, add 35ml of ethanol, and adopt high-pressure homogenization and freeze-drying preparation techniques to prepare powder preparations with a diameter of 100-700 nanometers.
specific Embodiment approach 3
[0023] Embodiment 3: The albumin described in this embodiment adopts human serum albumin, bovine serum albumin or albumin obtained through biotechnology. But not limited to those listed above.
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Abstract
The invention provides a taxotere nano preparation with albumin and phospholipid acting as carriers and a preparation method thereof, which relate to an anticancer medicament preparation and preparation thereof and solve the problems that the taxotere medicament is poor in water solubility, has toxic and side effect, especially has high irritability and hemolysis, and can cause severe anaphylaxis symptoms when used in intravenous injection. The taxotere nano preparation comprises the following components in percentage by weight: docetaxel 1% to 15%, albumin of 10% to 43%, 10% to 43% of phospholipids, vitamin E about 1% to 10%, freeze-dried excipient about 1% to 20% and acid buffer salt about 1% to 15%, and is prepared by adding solvent in the compositions and using a high pressure homogenization method and a freeze-drying technology. In the taxotere nano preparation, auxiliaries and solvents which bring about an allergic reaction of a human body are not used, thereby eliminating the allergic reaction caused by solvents and Tween-80 accessories, greatly improving the safety of taxotere solid nano medicament preparation and patient medication compliance. By using the preparation method, the stability of pharmaceutical preparation is greatly improved, thereby being beneficial to storage and transportation of medicaments.
Description
technical field [0001] The present invention relates to antitumor medicine and its preparation. It specifically relates to a docetaxel solid nano preparation with albumin and phospholipid as a carrier and a preparation method thereof. Background technique [0002] Docetaxel, also known as docetaxel, English name docetaxel, its chemical name is [2aR-(2aα, 4β, 4αβ, 6β, 9α, (aR', βS'), 11α, 12α, 12a α, 12bα) ]-β-[[(1,1-dimethylethoxy)carbonyl]amino]-α-carbonylphenylpropanoic acid [12b-acetoxy-12-benzoyloxy-2a,3,4,4a, 5,6,9,10,11,12,12a,12b-dodecahydro-4,6,11-trihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11- Methylene-1H-cyclodecapenta-[3,4]benzo[1,2-b]oxetan-9-yl]ester. Molecular formula is C 43 h 53 NO 14 , the molecular weight is 807.89. Docetaxel is a paclitaxel anti-tumor drug, which plays an anti-tumor effect by interfering with the microtubule network necessary for cell mitosis and interphase cell functions. Docetaxel can bind to free tubulin, promote the assembly of ...
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