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Irinotecan hydrochloride lipid nanoparticles injection

A technology of healthy lipids and nanoparticles, which is applied in the field of medicine to achieve the effects of improving stability, excellent dissolution, and good drug release

Inactive Publication Date: 2012-10-03
灵康药业集团股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] However, the challenge in preparing lipid nanoparticles lies in the selection of appropriate ingredients and preparation methods

Method used

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  • Irinotecan hydrochloride lipid nanoparticles injection
  • Irinotecan hydrochloride lipid nanoparticles injection
  • Irinotecan hydrochloride lipid nanoparticles injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Preparation of Example 1 Irinotecan Hydrochloride Lipid Nanoparticle Injection

[0070] The ingredients used are as follows:

[0071]

[0072] Adopt following production process to prepare irinotecan hydrochloride lipid nanoparticle sheet:

[0073] (1) Add 240g lecithin into 800ml pH7.0 phosphate buffer solution, heat in a constant temperature water bath at 50°C, stir to dissolve completely, then add 200ml ethanol solution in which 50g irinotecan hydrochloride and 120g stearic acid are dissolved, Stir fully to dissolve and form a mixed phase;

[0074] (2) Dissolve 320g PEG400 and 80g glycerin in 1000ml water, heat in a constant temperature water bath at 50°C, stir to dissolve, and form a water phase;

[0075] (3) Slowly add the organic phase to the stirring water phase, keep the temperature at 50°C, and continue stirring for 1 hour;

[0076] (4) Remove the organic solvent under reduced pressure to obtain translucent colostrum;

[0077] (5) Quickly add the colos...

Embodiment 2

[0079] Preparation of Example 2 Irinotecan Hydrochloride Lipid Nanoparticle Injection

[0080] The ingredients used are as follows:

[0081]

[0082]

[0083] Adopt the following production process to prepare irinotecan hydrochloride lipid nanoparticle capsules:

[0084] (1) Add 600g lecithin to 1000ml pH7.0 phosphate buffer solution, heat in a constant temperature water bath at 50°C, stir to dissolve completely, then add 300ml ethanol solution in which 100g irinotecan hydrochloride and 300g stearic acid are dissolved, Stir fully to dissolve and form a mixed phase;

[0085] (2) Dissolve 800g PEG400 and 200g glycerin in 1000ml water, heat in a constant temperature water bath at 50°C, stir to dissolve, and form a water phase;

[0086] (3) Slowly add the organic phase to the stirring water phase, keep the temperature at 50°C, and continue stirring for 1 hour;

[0087] (4) Remove the organic solvent under reduced pressure to obtain translucent colostrum;

[0088] (5) Q...

Embodiment 3

[0090] Preparation of Example 3 Irinotecan Hydrochloride Lipid Nanoparticle Injection

[0091] The ingredients used are as follows:

[0092]

[0093] Adopt following production process to prepare irinotecan hydrochloride lipid nanoparticle particle:

[0094] (1) Add 600g lecithin to 1500ml pH7.0 phosphate buffer solution, heat in a constant temperature water bath at 50°C, stir to dissolve completely, then add 300ml ethanol solution in which 100g irinotecan hydrochloride and 300g stearic acid are dissolved, Stir fully to dissolve and form a mixed phase;

[0095] (2) Dissolve 800g PEG400 and 200g glycerin in 2000ml water, heat in a constant temperature water bath at 50°C, stir to dissolve, and form a water phase;

[0096] (3) Slowly add the organic phase to the stirring water phase, keep the temperature at 50°C, and continue stirring for 1 hour;

[0097] (4) Remove the organic solvent under reduced pressure to obtain translucent colostrum;

[0098] (5) Quickly add the c...

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Abstract

The invention discloses an irinotecan hydrochloride lipid nanoparticles injection and a preparation method thereof. Mixed phase is formed by dissolving irinotecan hydrochloride and stearic acid in organic solvent and dissolving lecithin in buffer salt solution; aqueous solution of PEG (polyethylene glycol) 400, glycerol and trehalose is adopted as aqueous phase; and then irinotecan hydrochloride is loaded in lipid nanoparticles by combining stirring emulsification and high-pressure emulsion homogenizing to obtain the irinotecan hydrochloride lipid nanoparticles injection. The inventive lipid nanoparticles preparation has the advantages of high drug loading rate, uniform particle size, long drug retention time in blood circulation, better sustained-release and controlled-release effect, simple preparation method and device, easy operation, improved product quality, reduced toxic and side effects, and suitability for industrialized production.

Description

technical field [0001] The invention relates to a new injection of irinotecan hydrochloride, in particular to a lipid nanoparticle injection of irinotecan hydrochloride, which belongs to the technical field of medicine. Background technique [0002] Irinotecan hydrochloride, chemical name: (+)-(4S)-4,11-diethyl-4-hydroxy-9[(4-piperidinylpiperidine)carbonyl]-1Hpyrano[3, 4,6,7]indoxazin[1,2b]quinoline-3,14-(4H-12H)-dione hydrochloride trihydrate, molecular formula: C 33 h 38 N 4 o 6 ·HCl·3H 2 O, the molecular weight is 677.19, the structural formula is as follows [0003] [0004] Irinotecan (CPT-11) is a camptothecin derivative isolated from natural plants. It is a water-soluble anti-tumor raw material drug and a broad-spectrum tumor drug recently listed abroad. For the treatment of tumors, advanced colon cancer, rectal cancer, small cell lung cancer, cervical cancer, ovarian cancer and non-Hodgkinson lymphoma. When used in combination with other antitumor drugs, th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K9/19A61K31/4745A61K47/34A61P35/00
Inventor 陶灵刚
Owner 灵康药业集团股份有限公司
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