Method for preparing romidepsin lipidosome

A technology of romide liposide and romide liposome is applied in the field of preparing romide liposome liposomes, and achieves the effects of low cost, simple process and improved targeting.

Active Publication Date: 2013-05-22
广州迈凯安生物医药研究院有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, domestic research

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  • Method for preparing romidepsin lipidosome

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Experimental program
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Effect test

Embodiment 1

[0035] Example 1: Please refer to figure 1 The present invention discloses a method for preparing romidate peptide liposomes, including the following processes:

[0036] Romidate peptide liposome prescription:

[0037] Romidopeptide

[0038] The preparation process of romidate peptide liposomes: the prescription amount of soybean phospholipid for injection, cholesterol, vitamin E, and romidate peptide are dissolved in 1:1 chloroform-methanol and poured into a pear-shaped bottle. Rotary evaporator at 30 rpm, Under the condition of 40℃ water bath, the organic solvent was removed under reduced pressure, and a uniform film was formed on the bottle wall; the prescription amount of sucrose was dissolved in 100ml of phosphate buffer with PH value of 6.8, poured into a pear-shaped bottle, 30rpm, Hydration is complete in a water bath at 25°C; the liposomes obtained are passed through a high-pressure homogenizer at a pressure of 900 bar and the number of cycles is 3 times to obtain lipos...

Embodiment 2

[0039] Example 2: Please refer to figure 1 The present invention discloses a method for preparing romidate peptide liposomes, including the following processes:

[0040] Romidate peptide liposome prescription:

[0041] Romidopeptide

[0042] The preparation process of romidate peptide liposomes: Dissolve the prescribed amount of soybean phospholipid for injection, cholesterol, vitamin E and romidate peptide in 1:3 chloroform-methanol and pour it into a pear-shaped bottle, and set it on a rotary evaporator at 40 rpm, Under the condition of 45℃ water bath, the organic solvent was removed under reduced pressure to form a uniform film on the bottle wall; the prescription amount of sucrose was dissolved in 150ml of phosphate buffer with PH value of 6.8, poured into a pear-shaped bottle, 40rpm, rotary evaporator, Hydrate completely under 35℃ water bath conditions. Pass the obtained liposomes through a high-pressure homogenizer with a pressure of 700 bar and 5 cycles to obtain liposom...

Embodiment 3

[0043] Example 3: Please refer to figure 1 The present invention discloses a method for preparing romidate peptide liposomes, including the following processes:

[0044] Romidate peptide liposome prescription:

[0045] Romidopeptide

0.3g

Soybean Phospholipids for Injection

5g

Cholesterol

1g

Sucrose

2g

Vitamin E

0.3g

PH value of 6.8 phosphate buffer

200ml

[0046] The preparation process of romidate peptide liposomes: the prescription amount of soybean phospholipid for injection, cholesterol, vitamin E and romidate peptide are dissolved in 1:5 chloroform-methanol and poured into a pear-shaped bottle. Under the condition of 50℃ water bath, the organic solvent was removed under reduced pressure to form a uniform film on the bottle wall; the prescription amount of sucrose was dissolved in 200ml of phosphate buffer with PH value of 6.8, poured into a pear-shaped bottle, 50rpm, rotary evaporator, Hydration is complete in a water bath at 45°C. The liposomes obtained are pa...

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Abstract

The invention discloses a method for preparing romidepsin lipidosome. The romidepsin lipidosome is prepared by using a film dispersion method through regarding cholesterol as a stabilizer, cane sugar as a cryoprotectant and vitamin E as an antioxidant, wherein the particle size of the lipidosome is made to be smaller than 120nm and the encapsulation efficiency is made to be greater than 85% by a high pressure homogenization method at the same time. The romidepsin lipidosome prepared by the method is capable of reducing the degradation of romidepsin, prolonging the administration time, improving the adaptability of patients, improving the targeting of romidepsin, increasing the anti-tumor effect, and reducing the toxic and side effects of drugs as all ingredients in the formula are physically compatible materials with high safety. Moreover, the method for preparing romidepsin lipidosome disclosed by the invention has the advantages of simple process and low cost, and is suitable for industrial production.

Description

Technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a method for preparing romidate peptide liposomes. Background technique [0002] Romidepsin is a histone deacetylase (HDAC) inhibitor. It can cause histone hyperacetylation, thereby affecting cell gene expression. In some cancer cells, excessive The histone deacetylase can inhibit the activation of genes that regulate normal cell activity. Therefore, lowering the activity of the enzyme can activate these genes and cause the growth of cancer cells to slow or stop. [0003] Liposomes are multilamellar vesicles formed when amphiphilic phospholipids and other amphoteric compounds such as cholesterol are dispersed in the water phase. Each layer is a lipid bilayer, and the inside of the vesicle is the water phase. The liposome structure is suitable for degradation in vivo, non-toxic and non-immunogenic. A large amount of experimental data proves that liposomes as drug carriers h...

Claims

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Application Information

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IPC IPC(8): A61K38/12A61K9/127A61P35/00
Inventor 肖文花安鸿江文敏
Owner 广州迈凯安生物医药研究院有限公司
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