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A long-circulating liposome of hydroxycamptothecin

A long-circulation liposome and hydroxycamptothecin technology, which is applied in liposome delivery, medical preparations of non-active ingredients, organic active ingredients, etc., can solve the problem of no long-circulation materials, unpublished models, difficult applications, etc. problems, to achieve the effect of expanding the scope of application, increasing the drug loading dose, and saving production costs

Inactive Publication Date: 2016-04-20
UNIV OF JINAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to the long chain length of polyethylene glycol in this patent, TPGS2000 is somewhat different from the currently commercially available TPGS with a polyethylene glycol molecular weight of 1000. There is no commercially available product at present, and it is difficult to be widely popularized.
Another Chinese patent (Patent Document 2: Publication No. CN101548951A) discloses a hydroxycamptothecin nanoliposome and its preparation method. The liposome is prepared by a high-pressure homogenization method, and poloxamer is used in its prescription , due to the large number of poloxamer models and different properties, the patent has not published its model and is difficult to apply. In addition, there is no long-circulation material in the patent prescription, which belongs to the category of ordinary liposomes

Method used

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  • A long-circulating liposome of hydroxycamptothecin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1: Preparation of hydroxycamptothecin long-circulating liposomes

[0029] The prescription is composed of: hydroxycamptothecin 0.4g, soybean lecithin 7.5g, cholesterol 1.0g, TPGS 1.5g, poloxamer 1881.0g.

[0030] Preparation Process

[0031] (1) Formation of lipid film: Weigh 0.4g of hydroxycamptothecin, 7.5g of soybean lecithin, 1.0g of cholesterol, 1.5g of TPGS, and 1881.0g of poloxamer in a small beaker, add 40ml of absolute ethanol, add Gently stir with a magnet until completely dissolved to obtain a clear solution. Transfer the above clarified mixed solution into a 500ml round bottom flask, add a little glass beads, keep the temperature of the water bath at 55°C, and slowly rotate and evaporate under reduced pressure on a rotary evaporator. After the solvent evaporates, continue vacuum evaporation for 2h until the organic Solvent, at this time a uniform transparent lipid film was formed on the wall of the flask.

[0032] (2) Hydration: Add 40ml of pho...

Embodiment 2

[0038] Embodiment 2: Preparation of hydroxycamptothecin long-circulating liposomes

[0039] The prescription is composed of: hydroxycamptothecin 0.3g, soybean lecithin 3.0g, hydrogenated soybean lecithin 0.3g, cholesterol 1.5g, TPGS 1.5g, poloxamer 1882.0g.

[0040] Preparation Process

[0041] (1) Formation of lipid film: Weigh 0.3g of hydroxycamptothecin, 3.0g of soybean lecithin, 0.3g of hydrogenated soybean lecithin, 1.5g of cholesterol, 1.5g of TPGS, and 1882.0g of poloxamer in a small beaker, Add 40ml of chloroform, add a magnet and stir gently until completely dissolved to obtain a clear solution. Transfer the above clarified mixed solution into a 500ml round-bottom flask, add a little glass beads, keep the water melting temperature at 60°C, and slowly rotate and evaporate under reduced pressure on a rotary evaporator. After the solvent evaporates, continue vacuum evaporation for 3h, and remove the flask from Remove it from the rotary evaporator and put it in a vacuum...

Embodiment 3

[0045] Embodiment 3: the preparation of hydroxycamptothecin long circulation liposome

[0046] The prescription consists of: hydroxycamptothecin 1.0g, egg yolk lecithin 19.0g, hydrogenated soybean lecithin 1.0g, cholesterol 3.0g, TPGS 5.0g, poloxamer 1882.5g.

[0047] Preparation Process

[0048] (1) Formation of lipid film: Weigh 1.0g of hydroxycamptothecin, 19.0g of egg yolk lecithin, 1.0g of hydrogenated soybean lecithin, 3.0g of cholesterol, 5.0g of TPGS, and 1882.5g of poloxamer in a beaker, add Add 100ml of absolute ethanol, add a magnet and stir gently until completely dissolved to obtain a clear solution. The above-mentioned clarification mixed solution is transferred in the 1000ml round-bottomed flask, and the following steps are the same as the "formation of lipid film" in Example 2.

[0049] (2) Hydration: 100 ml of phosphate buffer solution was added to the above-mentioned flask where the lipid film was formed, and the following steps were the same as "hydration"...

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Abstract

The invention discloses a hydroxycamptothecine long-circulating liposome and a preparation method thereof. The hydroxycamptothecine long-circulating liposome is prepared from the following components in parts by weight: 1 part of hydroxycamptothecine, 5-30 parts of phospholipid, 1-5 parts of cholesterol, 1-20 parts of TPGS (tocopherol polyethylene glycol succinate), 1-8 parts of poloxamer188. The hydroxycamptothecine long-circulating liposome prepared by the method is proper in grain diameter, high in encapsulation, low in raw material price and simple in process, and is suitable for industrial production.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a hydroxycamptothecin long-circulation liposome and a preparation method thereof. Background technique [0002] Hydroxycamptothecin (HCPT) is a trace alkaloid extracted from the unique plant camptothecin in my country. Due to its extremely low content, it is now more derived by hydroxylation at the 10-position of camptothecin. Since camptothecin compounds were discovered in 1966, they have been paid attention to and paid attention to because of their excellent anti-tumor effects. Compared with camptothecin, hydroxycamptothecin has the advantages of higher anticancer efficacy and less side effects, and has strong application value in the treatment of gastric cancer, liver cancer, leukemia, breast cancer, and head and neck tumors. Widely used in clinical practice. [0003] Studies have shown that the anti-tumor activity of camptothecin compounds is mainly exerted by inh...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/77A61K9/127A61K9/19A61K47/24A61K47/34A61P35/00A61K31/4745
Inventor 王海龙刘善奎谭晓军
Owner UNIV OF JINAN
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