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7-ethyl-10-hydroxycamptothecine liposome freeze-dried powder injection and preparation method thereof

A technology of hydroxycamptothecin and hydroxycamptothecin, applied in the field of 7-ethyl-10-hydroxycamptothecin liposome freeze-dried powder injection and its preparation, can solve the problem of low anti-tumor activity, limited application, and high toxicity and other problems to achieve the effect of prolonging the metabolic time, eliminating side effects, and reducing irritation

Inactive Publication Date: 2010-11-03
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Camptothecin derivatives with new structures have shown great potential in the treatment of cancer. Although there are camptothecin, 10-hydroxycamptothecin, irinotecan and topotecan in China, the clinical use of camptothecin and 10- Hydroxycamptothecin is an unmodified natural product with high toxicity and low antitumor activity, which limits its clinical application
Although the two new camptothecin derivative drugs approved by the FDA, irinotecan and topotecan, have been successfully imitated in my country, they have applied for patents in my country, which limits their application

Method used

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  • 7-ethyl-10-hydroxycamptothecine liposome freeze-dried powder injection and preparation method thereof
  • 7-ethyl-10-hydroxycamptothecine liposome freeze-dried powder injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] (1) Dissolve 30 grams of soybean lecithin (injection grade), 10 grams of cholesterol (injection grade), and 2 grams of α-tocopherol in 2000 ml of ethanol (analytical pure), vacuum rotary transfer organic solvent, and place in a vacuum constant temperature drying oven overnight The residual organic solvent was evaporated to prepare dry lipid film, and the above operations were all completed under sterile conditions.

[0053] (2) Dissolve 1.67 grams of 7-ethyl-10-hydroxycamptothecin and 100 grams of sucrose (injection grade) in 1000 ml of sodium carbonate-sodium bicarbonate buffered saline solution (pH=9.9) at a hydration temperature of 45°C Next, use the above-mentioned alkaline buffered saline solution to hydrate the lipid dry film, and after the hydration is complete, use a milk homogenizer to reduce the particle size to 100-200nm to obtain drug-containing liposomes. All the above operations were completed under sterile conditions.

[0054] (3) Vacuum freeze-dry drug-...

Embodiment 2

[0056] (1) Dissolve 40 grams of sphingomyelin (injection grade), 10 grams of cholesterol (injection grade), and 2 grams of α-tocopherol in 2000 ml of ethanol (analytical pure), vacuum rotary transfer organic solvent, and place in a vacuum constant temperature drying oven The residual organic solvent was evaporated overnight to prepare a dry lipid film. The above operations were all completed under sterile conditions.

[0057] (2) Dissolve 2 grams of 7-ethyl-10-hydroxycamptothecin and 200 grams of trehalose (injection grade) in 2000 ml of potassium dihydrogen phosphate-sodium hydroxide buffer solution (pH=9.9) Hydrate the lipid dry film with the above-mentioned alkaline buffered saline solution at the temperature of 100 °C, and reduce the particle size to 100-200 nm with a homogenizer after the hydration is complete, to obtain the drug-containing liposome. All the above operations were completed under sterile conditions.

[0058] (3) Vacuum freeze-drying of the drug-containing...

Embodiment 3

[0060] (1) Dissolve 30 grams of phosphatidylcholine (injection grade), 10 grams of cholesterol (injection grade), and 2 grams of α-tocopherol in 2000 ml of ethanol (analytical pure), vacuum rotary transfer organic solvent, and vacuum constant temperature drying oven Leave it overnight to evaporate the residual organic solvent to prepare a lipid dry film. The above operations are all completed under sterile conditions.

[0061] (2) Dissolve 1 g of 7-ethyl-10-hydroxycamptothecin and 300 g of lactose (injection grade) in 3000 ml of barbiturate sodium-hydrochloric acid buffer solution (pH=9.9) at a hydration temperature of 45°C The dry lipid film is hydrated with the above-mentioned alkaline buffered saline solution, and after the hydration is complete, the particle size is reduced to 100-200nm with a homogenizer to obtain the drug-containing liposome. The above operations were all done under sterile conditions.

[0062] (3) Vacuum freeze-drying drug-containing liposome solution ...

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Abstract

The invention belongs to the medical technical field, and discloses 7-ethyl-10-hydroxycamptothecine liposome freeze-dried powder injection and a preparation method thereof. The 7-ethyl-10-hydroxycamptothecine liposome freeze-dried powder injection comprises the following components: 1-10g of 7-ethyl-10-hydroxycamptothecine, 30-60g of phospholipids, 10-40g of cholesterol, 2-8g of VE, 100-300g of a freeze drying protectant, 2000-8000ml of an organic solvent, 1000-4000ml of alkaline buffer salt solution and 1000-4000ml of acid buffer salt solution. The preparation method comprises the following steps: dissolving liposoluble components in the organic solvent and water-soluble components in the alkaline buffer salt; transferring the organic solvent, and then adding the alkaline buffer salt for hydration; and carrying freeze drying in vacuum, re-dissolving with the acid buffer salt, incubating, filtering, sterilizing, and carrying out freeze drying again to obtain the 7-ethyl-10-hydroxycamptothecine liposome freeze-dried powder injection for injection. The invention solves the problems of low solubility and fast in-vivo metabolism of the 7-ethyl-10-hydroxycamptothecine, thus lowering toxic reaction, eliminating side reaction, having higher target distribution characteristics, prolonging metabolism time and improving solubility and bioavailability.

Description

technical field [0001] The technical field of the present invention relates to the design and preparation of new dosage forms of anticancer drugs, and provides a 7-ethyl-10-hydroxycamptothecin liposome freeze-dried powder injection and its preparation method Background technique [0002] 7-Ethyl-10-hydroxycamptothecin is the main metabolite of camptothecin anticancer drugs in the body. Studies have shown that it has a good anticancer effect, and its cytotoxicity is 200-2000 times that of irinotecan. 7-Ethyl-10-Hydroxycamptothecin is a fat-water insoluble compound, and it is metabolized rapidly in both PBS and plasma solutions. It is lipophilic in acid solution and hydrophilic in alkaline solution. It is considered to use this characteristic to prepare liposome injection to improve solubility and stability in vivo. [0003] When the liposome is delivered to the tumor blood vessels, it can enter the tumor tissue through the capillary epithelial tissue gap, so as to achieve a ...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/4745A61K47/28A61P35/00
Inventor 王淑君叶田田
Owner SHENYANG PHARMA UNIVERSITY
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