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LYPOSOMIC PREPARATION OF DOXORUBICIN, METHOD OF OBTAINING SUCH PREPARATION OF HIGH ENCAPSULATION DEGREE AND ANTICARCINOGENIC PHARMACEUTICAL COMPOSITION CONTAINING SAME
LYPOSOMIC PREPARATION OF DOXORUBICIN, METHOD OF OBTAINING SUCH PREPARATION OF HIGH ENCAPSULATION DEGREE AND ANTICARCINOGENIC PHARMACEUTICAL COMPOSITION CONTAINING SAME
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机译:阿霉素的溶酶法制备,高浓缩度的制备方法和包含相同成分的抗癌药药理学组成
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摘要
1. A liposome doxorubicine preparation, containing a liposome carrier and, possibly, pharmaceutically acceptable auxiliary substances. It is characterised in that the liposome carrier is constituted by a mixture of egg lecitin (PC), hydrogenated egg lecitin (HPC) and a resorcinol derivative (RL) in the weight ratio of 1:1:2. 5. A method of producing a liposome doxorubicine preparation, containing a liposome carrier and pharmaceutically acceptable auxiliary substances, characterised by the encapsulation degree exceeding 95 percent. It is characterised in that a solution of doxorubicine or its salt in an organic solvent is combined with the solution of the lipid carrier components, containing egg lecithin (PC), hydrogenated egg lecitin (HPC) and a resorcinol derivative (RL) in the weight ratio of 1:1:2, in the same or other organic solvent. Solvents are expelled. The lipid layer is distributed in an organic solvent, subjected to cold treatment and lyophilization. The liophilizate is then contacted with water to obtain the original multilamellar liposome preparation. It is stabilized by subjecting to additional physical processes, to obtain a suspension of calibrated unilamellar liposomes with the size of 50-200 nm, preferably 100-200 nm, and the encapsulation degree exceeding 95 percent. Then, the liposome suspension is lyophilised. 8. An antitumorous pharmaceutical mixture for parenteral administration, comprising a therapeutically effective amount of doxorubicine in the form of a liposome preparation. It is characterised in that the liposome preparation contains doxorubicine hydrochloride in the weight ration between 1:5 and 1:15 with respect to the lipid components of the liposome carrier. The carrier consists of egg lecitin (PC), hydrogenated egg lecithin (HPC) and a resorcinol derivative (RL) at the weight ratio of 1:1:2, and it can contain additional pharmaceutically acceptable carriers and/or auxiliary substances.
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