Pirarubicin freeze-dry preparations and preparation method thereof
A technology for pirarubicin and freeze-dried preparations, which is applied in the field of pirarubicin liposome freeze-dried preparations and their preparation, can solve the problems of poor preparation stability, poor anti-tumor activity, large toxic and side effects of the reticuloendothelial system, etc. problems, to achieve the effect of improving stability, improving anti-tumor activity, and reducing toxic and side effects
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Embodiment 1
[0030] Pirarubicin 10g
[0031] Hydrogenated Soy Lecithin 63g
[0032] Cholesterol 35g
[0033] PEG2000-Dipalmitoylphosphatidylethanolamine 4g
[0034] Poloxamer 188 1.5g
[0035] a-Tocopherol 40mg
[0036] Sucrose 625g
[0037] Preparation method: Dissolve the prescribed amount of pirarubicin, hydrogenated soybean lecithin, cholesterol, PEG2000-dipalmitoylphosphatidylethanolamine and a-tocopherol in absolute ethanol, remove the absolute ethanol by rotary evaporation to make a uniform lipid film. The lipid film was hydrated with PH7.4 phosphate buffer containing the prescribed amount of poloxamer 188 and sucrose in a constant temperature water bath at 60°C with nitrogen gas for 30 minutes, then transferred to an ice bath to cool, and then was homogenized with a high-pressure milk homogenizer (high-pressure homogenizer). 408kg / cm 2 2 times, low pressure 102kg / cm 2 1 time) Dispersion treatment, filtration with 200nm microporous membrane, and lyophilization in a lyophiliz...
Embodiment 2
[0066] Pirarubicin Hydrochloride 12g
[0067] Hydrogenated Soy Lecithin 75g
[0068] Cholesterol 42g
[0069] PEG2000-Dipalmitoylphosphatidylethanolamine 5g
[0070] Poloxamer 188 2g
[0071] a-Tocopherol 50mg
[0072] Sucrose 900g
[0073] Preparation method: Dissolve the prescribed amount of pirarubicin hydrochloride, hydrogenated soybean lecithin, cholesterol, PEG2000-dipalmitoylphosphatidylethanolamine and a-tocopherol in absolute ethanol, and remove the absolute ethanol by rotary evaporation to make a uniform lipid The lipid film was hydrated with PH6.5 phosphate buffer solution containing the prescribed amount of poloxamer 188 and sucrose, filled with nitrogen in a constant temperature water bath at 50°C for 60 minutes, then transferred to an ice bath to cool, and then homogenized with a high-pressure milk homogenizer. (high pressure 510kg / cm 2 2 times, low pressure 102kg / cm 2 1 time) Dispersion treatment, filtration with 100nm microporous membrane, and lyophiliza...
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