Irinotecan or irinotecan hydrochloride lipidosome and preparation method thereof

A technology of irinotecan hydrochloride and irinotecan, which is applied in liposome delivery, pharmaceutical formulation, liquid delivery, etc., can solve the problems of liposome stability and unsatisfactory particle size, and achieve toxicity reduction, inhibition The effect of increasing tumor rate and stabilizing properties

Active Publication Date: 2013-05-29
JIANGSU HENGRUI MEDICINE CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Although the prescriptions recorded in the above-mentioned patent documents have better effects, if prepared into a preparation suitable for human use, the liposomes are still unsatisfactory in terms of stability, particle size, etc.

Method used

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  • Irinotecan or irinotecan hydrochloride lipidosome and preparation method thereof
  • Irinotecan or irinotecan hydrochloride lipidosome and preparation method thereof
  • Irinotecan or irinotecan hydrochloride lipidosome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] prescription

[0057]

[0058] Preparation:

[0059] Dissolve the prescribed amount of hydrogenated soybean lecithin (HSPC) and cholesterol (CHOL) in an appropriate amount of absolute ethanol to obtain a lipid solution, mix it with 100ml of ammonium sulfate solution, and remove the ethanol under reduced pressure to obtain a crude blank liposome. Afterwards, use a high-pressure homogenizer at 1000 bar to homogenize for 5 cycles, and then extrude liposomes through extrusion equipment to control their particle size (two 0.1 μm extrusion films are laid on the extruder and extruded 5 times). Then add the prepared DSPE-PEG 2000 aqueous solution, and incubate for 20 minutes with agitation. The blank liposome was dialyzed by a tangential flow ultrafiltration device, and water for injection was supplemented continuously in the middle to obtain the blank liposome.

[0060] Prepare an aqueous solution of irinotecan hydrochloride with water for injection, add it to the above...

Embodiment 2

[0068] prescription

[0069]

[0070] Preparation:

[0071] Dissolve the hydrogenated soybean lecithin and cholesterol of the prescribed amount in an appropriate amount of absolute ethanol to obtain a lipid solution, mix it with 100ml of ammonium sulfate solution, and remove the ethanol under reduced pressure to obtain a crude blank liposome. Afterwards, use a high-pressure homogenizer at 1000 bar to homogenize for 5 cycles, and then extrude liposomes through extrusion equipment to control their particle size (extruder spreads 2 sheets of 0.1 μm extrusion film and extrudes 5 times). Then add the prepared DSPE-PEG 2000 aqueous solution, and incubate for 20 minutes with agitation. The blank liposome was dialyzed by a tangential flow ultrafiltration device, and water for injection was supplemented continuously in the middle to obtain the blank liposome.

[0072] Prepare an aqueous solution of irinotecan hydrochloride with water for injection, add it to the above-mentioned ...

Embodiment 3

[0074] The blank liposome prescription and preparation method are the same as in Example 2, except that the weight ratios of irinotecan hydrochloride and HSPC are 1:1.5, 1:2, 1:3.5, 1:4 and 1:5 respectively. Preparation of liposomes, encapsulation efficiency and particle size of irinotecan hydrochloride liposome samples are shown in the table below.

[0075]

[0076] The results showed that when the ratio of irinotecan hydrochloride and HSPC was 1:1.5, the encapsulation efficiency was significantly reduced, and when the ratio was 1:5, the drug loading decreased significantly, and it was not suitable for preparation into clinically applied preparations. The encapsulation efficiency and drug loading are higher when the ratio is between 1:2 and 1:4.

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PUM

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Abstract

The invention discloses an irinotecan or irinotecan hydrochloride lipidosome and a preparation method thereof. The lipidosome contains irinotecan or irinotecan hydrochloride, neutral phospholipid and cholesterol, wherein the weight ratio of the cholesterol to the neutral phospholipid is 1:(3-5), and the irinotecan or irinotecan hydrochloride lipidosome is prepared by an ion gradient method.

Description

[0001] This application is a divisional application of the Chinese patent application with the application number 200980154026.9, the application date is December 3, 2009, and the invention title is "Irinotecan or Irinotecan Hydrochloride Liposome and Preparation Method thereof". technical field [0002] The invention relates to an irinotecan or irinotecan hydrochloride liposome and a preparation method thereof, as well as an injection containing the liposome and a preparation method thereof. Background technique [0003] Irinotecan is a semisynthetic derivative of camptothecin. Camptothecin can specifically bind totoisomerase I, which induces reversible single-strand breaks, thereby unwinding the DNA double-strand structure; irinotecan and its active metabolite SN-38 can bind totoisomerase The I-DNA complex binds, thereby preventing religation of the broken single strands. Existing studies suggest that the cytotoxic effect of irinotecan is due to the interaction between re...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/10A61K9/19A61K31/4745A61K47/34A61K47/24A61P35/00
Inventor 仝新勇雷国锋余成霞陈亮
Owner JIANGSU HENGRUI MEDICINE CO LTD
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