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A kind of cisplatin liposome preparation and its preparation method and application

A technology of liposome preparation and cisplatin, which is applied in the field of pharmaceutical preparations, can solve problems such as unsatisfactory effects, easy leakage of drugs, and inability to release, so as to improve bioavailability, reduce drug dosage, and reduce toxic and side effects

Active Publication Date: 2018-12-25
山东瑞银生物工程有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although there are many studies on liposomes of platinum-based drugs at present, their effects are not very satisfactory, mainly due to the problems of low encapsulation efficiency, easy leakage of drugs, and inactivation or inability to release part of cisplatin encapsulated in liposomes (Meric , Rixe, Khayat. Metastatic malignant melanoma. Drugs Today (Barc), 2003, 39 (S-C): 17.)

Method used

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  • A kind of cisplatin liposome preparation and its preparation method and application
  • A kind of cisplatin liposome preparation and its preparation method and application
  • A kind of cisplatin liposome preparation and its preparation method and application

Examples

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Effect test

Embodiment 1

[0047] A kind of cisplatin liposome preparation, its preparation method step is as follows:

[0048] a) Preparation of blank liposomes

[0049] Put 1000mg of egg yolk lecithin, 620mg of oleic acid, 240mg of cholesterol and 140mg of Tween-80 in a 10ml beaker, add 3ml of absolute ethanol and magnetically stir in a water bath at 40°C to dissolve, and inject the resulting ethanol solution into the preheated In 100ml aqueous sodium hydroxide solution at 30°C (formed by adding water to sodium hydroxide, NaOH:oleic acid=85:100mol / mol), after stirring for 30min at 30°C, pass through a liposome extruder A polycarbonate membrane with a pore size of 100 nm was used three times to obtain a blank liposome suspension.

[0050] b) Preparation of cisplatin liposome preparation

[0051] Place the above blank liposome suspension in a shaker, preheat at 50°C for 30 minutes; weigh 450mg of cisplatin and add it to the above blank liposome suspension, shake at 50°C, 180r / min, and avoid light 1h,...

Embodiment 2

[0053] A kind of cisplatin liposome preparation, its preparation method step is as follows:

[0054] a) Preparation of blank liposomes

[0055] Put 1000mg of egg yolk lecithin, 620mg of oleic acid, 240mg of cholesterol and 140mg of Tween-80 in a 10ml beaker, add 3ml of absolute ethanol and magnetically stir in a water bath at 40°C to dissolve, and inject the resulting ethanol solution into the preheated In the 100ml sodium hydroxide aqueous solution (NaOH: oleic acid=85:100mol / mol) of 30 ℃, after continuing to stir 30min under the condition of 30 ℃, be that 100nm polycarbonate membrane is 3 times with liposome extruder aperture , to obtain a blank liposome suspension.

[0056] b) Preparation of cisplatin liposome preparation

[0057] Place the above blank liposome suspension in a shaker, preheat at 50°C for 30 minutes; weigh 600mg of cisplatin and add it to the above blank liposome suspension, shake at 50°C, 180r / min, and avoid light 1h, discard the precipitate, and use a l...

Embodiment 3

[0059] A kind of cisplatin liposome preparation, its preparation method step is as follows:

[0060] a) Preparation of blank liposomes

[0061] Put 1000mg of egg yolk lecithin, 620mg of oleic acid, 240mg of cholesterol and 140mg of Tween-80 in a 10ml beaker, add 3ml of absolute ethanol and magnetically stir in a water bath at 40°C to dissolve, and inject the resulting ethanol solution into the preheated In the 100ml sodium hydroxide aqueous solution (NaOH: oleic acid=85:100mol / mol) of 30 ℃, after continuing to stir 30min under the condition of 30 ℃, be that 100nm polycarbonate membrane is 3 times with liposome extruder aperture , to obtain a blank liposome suspension.

[0062] b) Preparation of cisplatin liposome preparation

[0063] Place the above blank liposome suspension in a shaker, preheat at 50°C for 30 minutes; weigh 750mg of cisplatin and add it to the above blank liposome suspension, shake at 50°C, 180r / min, and avoid light 1h, discard the precipitate, and use a l...

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Abstract

The invention relates to the technical field of medicinal preparations, and concretely discloses a cisplatin-liposome preparation, and a preparation method and an application thereof. An improved formula and the improved method in the above technical scheme make the cisplatin liposome improve the bioavailability of cisplatin medicines and prolong the detention time of the medicines in bodies, and also make cisplatin be enriched in cancerous organs, thereby the dosage is reduced, curative effects are enhanced, the toxic and side effects of the medicines are reduced, and the medicines are suitable for treating various tumor diseases.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a cisplatin liposome preparation and its preparation method and application. Background technique [0002] Cisplatin (cisplatin, DDP) was first prepared in 1844. It was not until 1967 that Rosenberg, a professor at Michigan State University in the United States, discovered that its cis-isomerization had anticancer effects, and it was applied clinically in 1969. Launched in the United States in 1978. [0003] Cisplatin is the first platinum-based drug. Cisplatin is a complex of heavy metal platinum. There are 2 chlorine atoms and 2 ammonia molecules around the central platinum atom, and it has the properties of a bifunctional alkylating agent. In the human body, chlorine can be hydrolyzed to form active positively charged hydration molecules, which then react with nucleic acids and proteins, causing DNA inter-strand or intra-strand cross-links, or forming DNA-...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K33/24A61K47/28A61P35/00
Inventor 葛建郑宜红金燕刘文双徐传瑞马建义王朝东
Owner 山东瑞银生物工程有限公司
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