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LIPOSOMES OF IRINOTEKAN OR ITS SALTS, METHOD FOR PRODUCING THEM

机译:伊利替康或其盐的脂质体,其制备方法

摘要

1. Liposomes of irinotecan or irinotecan hydrochloride, characterized in that these liposomes contain irinotecan or irinotecan hydrochloride, neutral phospholipid and cholesterol, and the mass ratio of cholesterol to neutral phospholipid is 1: 3-5.2. Liposomes according to claim 1, characterized in that the mass ratio of neutral phospholipid to irinotecan or irinotecan hydrochloride is: 3. Liposomes according to claim 1, characterized in that the neutral phospholipid comprises hydrogenated soybean phosphatidylcholine. Liposomes according to claim 3, characterized in that the neutral phospholipid is a hydrogenated soybean phosphatidylcholine. Liposomes according to claim 1, characterized in that the ratio of cholesterol to neutral phospholipid is 1: 3.5-4.5, preferably 1: 4.6. Liposomes according to claim 1, characterized in that they are obtained by the ion gradient method. Liposomes according to claim 6, characterized in that they have an ionic gradient formed by a buffer between the internal aqueous phase and the external aqueous phase of liposomes, preferably the internal aqueous phase of liposomes has a higher ionic concentration than the external aqueous phase. Liposomes according to claim 1, characterized in that they further comprise a lipid derivative of a hydrophilic polymer, preferably polyethylene glycol2000-distearoylphosphatidylethanolamine (DSPE-PEG). The liposomes of claim 8, characterized in that the mass ratio of the lipid derivative of the hydrophilic polymer to irinotecan or irinotecan hydrochloride is 0.2-0.4.10. Liposomes according to any one of claims 1 to 9, characterized in that they additionally contain a charged phospholipid, which is selected
机译:1.伊立替康或盐酸伊立替康的脂质体,其特征在于,这些脂质体包含伊立替康或盐酸伊立替康的脂质,中性磷脂和胆固醇,胆固醇与中性磷脂的质量比为1:3-5.2。 2.根据权利要求1所述的脂质体,其特征在于,中性磷脂与伊立替康或盐酸伊立替康盐酸盐的质量比为:3.根据权利要求1所述的脂质体,其特征在于,所述中性磷脂包括氢化大豆磷脂酰胆碱。 4.根据权利要求3所述的脂质体,其特征在于,所述中性磷脂是氢化大豆磷脂酰胆碱。 2.根据权利要求1的脂质体,其特征在于胆固醇与中性磷脂的比例为1∶3.5-4.5,优选1∶4.6。 2.根据权利要求1的脂质体,其特征在于它们是通过离子梯度法获得的。 7.根据权利要求6的脂质体,其特征在于它们具有由脂质体的内部水相和外部水相之间的缓冲剂形成的离子梯度,优选脂质体的内部水相具有比外部水相更高的离子浓度。 2.根据权利要求1的脂质体,其特征在于它们还包含亲水性聚合物的脂质衍生物,优选聚乙二醇2000-二硬脂酰磷脂酰乙醇胺(DSPE-PEG)。 9.根据权利要求8所述的脂质体,其特征在于,所述亲水性聚合物的脂质衍生物与伊立替康或盐酸伊立替康盐酸盐的质量比为0.2〜0.4.10。 10.根据权利要求1至9中任一项的脂质体,其特征在于它们还含有带电荷的磷脂,其选自

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