Irinotecan hydrochloride liposome pharmaceutical composition and preparation method thereof

A technology of irinotecan hydrochloride and its composition, which is applied in the field of liposome composition and its preparation, can solve the problems of instability and easy degradation, and achieve the effect of stable drug loading and high encapsulation efficiency

Active Publication Date: 2016-07-27
NANJING LUYE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At the same time, it overcomes the defect that CPT-11 is unstable...

Method used

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  • Irinotecan hydrochloride liposome pharmaceutical composition and preparation method thereof
  • Irinotecan hydrochloride liposome pharmaceutical composition and preparation method thereof
  • Irinotecan hydrochloride liposome pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1 irinotecan hydrochloride liposome injection

[0042] Table 1: The ratio of each prescription of irinotecan hydrochloride liposome injection

[0043]

[0044] Preparation:

[0045] Put the prescribed amount of hydrogenated soybean phosphatidylcholine, distearoylphosphatidylcholine, cholesterol, and DSPE-mPEG2000 in a 500ml round-bottomed flask, add 200ml of absolute ethanol to dissolve, and reduce the temperature on a rotary evaporator at 55-60°C. Ethanol is removed by pressure steaming, so that the lipid forms a uniform lipid film at the bottom of the flask, and the film is washed by rotation with 100ml0.25mol / L ammonium sulfate aqueous solution, and then the granules are extruded successively through 0.4, 0.2, 0.1 μm by a homogenizer (each 3 times), a tangential flow ultrafiltration device was used to remove unwrapped ammonium sulfate, and water for injection was constantly replenished during the ultrafiltration process to obtain blank liposomes.

[0...

Embodiment 2

[0060] Embodiment 2 irinotecan hydrochloride liposome injection

[0061] Table 4: Prescription ratio of irinotecan hydrochloride liposome injection

[0062] Irinotecan Hydrochloride

[0063] Preparation:

[0064] Weigh the prescribed amount of hydrogenated soybean phosphatidylcholine, distearoylphosphatidylcholine, cholesterol, and DSPE-mPEG2000, put them in a 500ml round bottom flask, add 200ml of absolute ethanol to dissolve, and reduce the temperature on a rotary evaporator at 55-60°C. Ethanol was evaporated under pressure to make the lipid form a uniform lipid film at the bottom of the flask, and the film was washed with 100ml of 0.25mol / L ammonium sulfate aqueous solution, and then the whole grain was extruded through a homogenizer at 0.4, 0.2, and 0.1 μm in sequence ( Each time 3 times), a tangential flow ultrafiltration device was used to remove unwrapped ammonium sulfate, and water for injection was continuously replenished during the ultrafiltration process...

Embodiment 3

[0070] Table 6: Prescription ratio of irinotecan hydrochloride liposome injection

[0071] Irinotecan Hydrochloride

0.4g

Hydrogenated Soy Phosphatidylcholine

1.44g

Distearoylphosphatidylcholine

0.48g

cholesterol

0.5g

DSPE-mPEG3350

0.4g

ammonium sulfate

5g

Mannitol

10g

Disodium phosphate

0.38g

Sodium dihydrogen phosphate

0.65g

Water for Injection

Add to required volume

[0072] Preparation:

[0073] Weigh the prescribed amount of hydrogenated soybean phosphatidylcholine, distearoylphosphatidylcholine, cholesterol, DSPE-mPEG3350 and add 50ml of absolute ethanol to dissolve, then inject 100ml of 0.25mol / L ammonium sulfate kept in a 60°C water bath through a peristaltic pump in the aqueous solution, and then through a homogenizer to extrude granules through 0.4, 0.2, and 0.1 μm successively (3 times each). A tangential flow ultrafiltration device is used to r...

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Abstract

The invention provides an irinotecan hydrochloride liposome pharmaceutical composition and a preparation method thereof. The irinotecan hydrochloride liposome pharmaceutical composition comprises irinotecan hydrochloride, hydrogenated soy phosphatidylcholine (HSPC), distearoyl phosphatidylcholine (DSPC), cholesterol (CHol) and Phosphatidylethanolamine Pegol. The irinotecan hydrochloride liposome pharmaceutical composition obtained through the preparation method has a high encapsulation rate, a high drug loading amount and good stability.

Description

technical field [0001] The invention relates to a liposome composition and a preparation method thereof, in particular to an irinotecan hydrochloride liposome pharmaceutical composition and a preparation method thereof. Background technique [0002] Camptothecin drugs achieve their cytotoxic effect by inhibiting DNATopo-I, an essential enzyme in cell survival. Irinotecan hydrochloride (Irinotecan, CPT-11), as a water-soluble derivative of camptothecin, solved the problem of water solubility by modifying the structure of camptothecin on the one hand; The ester ring makes the drug effect significantly higher than that of hydroxycamptothecin injection. CPT-11 is a prodrug that needs to be catalyzed by carboxylesterase in tissues to generate an active metabolite SN-38 to be effective. [0003] CPT-11 was developed by Japan, and Phase I clinical trials began in 1987. Large-scale Phase III clinical trials have shown that it is an effective drug for the treatment of metastatic co...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/4745A61K47/24A61P35/00
Inventor 李锦张国喜陈文忠程光
Owner NANJING LUYE PHARMA
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