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Hydroxycamptothecine long-circulating liposome

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of non-active ingredients, organic active ingredients, etc., can solve the problem of no long-circulation materials, unpublished models, difficult applications, etc.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: 2014-04-02
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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  • Hydroxycamptothecine long-circulating liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0029] The prescription consisted of: hydroxycamptothecin 0.4 g, soybean lecithin 7.5 g, cholesterol 1.0 g, TPGS 1.5 g, and poloxamer 188 1.0 g.

[0030] Preparation Process

[0031] (1) Formation of lipid film: Weigh 0.4 g of hydroxycamptothecin, 7.5 g of soybean lecithin, 1.0 g of cholesterol, 1.5 g of TPGS, and 1.0 g of poloxamer 188 in a small beaker, add 40 ml of absolute ethanol , add a magnet and gently stir until completely dissolved to obtain a clear solution. Transfer the above clarified mixed solution into a 500 ml round-bottomed flask, add a little glass beads, keep the temperature of the water bath at 55°C, slowly rotate and evaporate under reduced pressure on a rotary evaporator, and continue vacuum evaporation for 2 h until the solvent evaporates to dryness. The organic solvent was removed, at which point a uniform, clear lipid film formed on the flask walls.

[0032] (2) Hyd...

Embodiment 2

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

[0039] The prescription consisted of: hydroxycamptothecin 0.3 g, soybean lecithin 3.0 g, hydrogenated soybean lecithin 0.3 g, cholesterol 1.5 g, TPGS 1.5 g, and poloxamer 188 2.0 g.

[0040] Preparation Process

[0041] (1) Formation of lipid film: Weigh 0.3 g of hydroxycamptothecin, 3.0 g of soybean lecithin, 0.3 g of hydrogenated soybean lecithin, 1.5 g of cholesterol, 1.5 g of TPGS, and 2.0 g of poloxamer 188 in a small beaker , add 40 ml of chloroform, add a magnet and stir gently until completely dissolved to obtain a clear solution. Transfer the above clarified mixed solution into a 500 ml round bottom flask, add a little glass beads, keep the water melting temperature at 60°C, slowly rotate and evaporate under reduced pressure on a rotary evaporator, and continue vacuum evaporation for 3 h after the solvent evaporates to dryness. The flask was removed from the rotary evaporator and pl...

Embodiment 3

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

[0046] The prescription consisted of: hydroxycamptothecin 1.0 g, egg yolk lecithin 19.0 g, hydrogenated soybean lecithin 1.0 g, cholesterol 3.0 g, TPGS 5.0 g, and poloxamer 188 2.5 g.

[0047] Preparation Process

[0048] (1) Formation of lipid film: Weigh 1.0 g of hydroxycamptothecin, 19.0 g of egg yolk lecithin, 1.0 g of hydrogenated soybean lecithin, 3.0 g of cholesterol, 5.0 g of TPGS, and 2.5 g of poloxamer 188 in a beaker, Add 100 ml of absolute ethanol, add a magnet and stir gently until completely dissolved to obtain a clear solution. The above-mentioned clarified mixed solution was transferred to a 1000 ml round-bottomed flask, and the following steps were the same as in 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 sam...

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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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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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