首页> 外国专利> 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

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

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.
机译:1.一种脂质体阿霉素制剂,其包含脂质体载体和可能的药学上可接受的辅助物质。其特征在于,脂质体载体由鸡蛋卵磷脂(PC),氢化卵卵磷脂(HPC)和间苯二酚衍生物(RL)的重量比为1∶1∶2的混合物构成。 5.一种生产脂质体阿霉素的制剂的方法,其包含脂质体载体和药学上可接受的辅助物质,其特征在于包囊度超过95%。其特征在于将阿霉素或其盐在有机溶剂中的溶液与脂质载体组分的溶液合并,所述脂质载体组分的溶液按重量计包含卵卵磷脂(PC),氢化卵卵磷脂(HPC)和间苯二酚衍生物(RL)。在相同或其他有机溶剂中的比例为1:1:2。溶剂被排出。脂质层分布在有机溶剂中,进行冷处理和冻干。然后将冻干物与水接触以获得原始的多层脂质体制剂。通过进行另外的物理过程使其稳定,以获得尺寸为50-200nm,优选100-200nm,并且包封度超过95%的校准的单层脂质体的悬浮液。然后,将脂质体悬浮液冻干。 8.用于肠胃外给药的抗肿瘤药物混合物,其包含治疗有效量的脂质体制剂形式的阿霉素。其特征在于,脂质体制剂含有相对于脂质体载体的脂质成分为1:5〜1:15的重量比的盐酸阿霉素。载体由卵磷脂(PC),氢化卵卵磷脂(HPC)和间苯二酚衍生物(RL)组成,其重量比为1:1:2,并且可以包含其他可药用载体和/或辅助物质。

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