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Preparation process of irinotecan hydrochloride liposome for injection

A technology of irinotecan hydrochloride and Kang lipid, applied in the directions of liposome delivery, drug combination, anti-tumor drugs, etc., can solve the problems of spasm and paresthesia, neutropenia, affecting clinical use, etc., to avoid Adverse reactions, stable properties, safe and reliable effects

Inactive Publication Date: 2007-07-11
XIAN LIBANG PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Irinotecan can be dissolved in water, but its metabolite irinotecan hydrochloride is its active ingredient, and it can produce serious adverse reactions during metabolism, such as: delayed diarrhea, nausea, vomiting, and can cause neutral Neutropenia, dyspnea, muscle contraction, spasm and paresthesia, etc. These adverse reactions seriously affect the clinical use

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Embodiment 1: small laboratory test

[0012] (1) film method prepares irinotecan hydrochloride liposome

[0013] prescription:

[0014] Egg yolk phosphatidylcholine 2.12g (2.789473684mmol)

[0015] Cardiolipin 12.00g (15mmol)

[0016] Cholesterol 5.88g (15.23316062mmol)

[0017] Chloroform 13.00mL

[0018] 200mL

[0019] Preparation method: dissolve egg yolk phosphatidylcholine, cardiolipin, cholesterol and irinotecan hydrochloride in the organic solvent chloroform until the solution is clear and transparent, vacuumize the rotary evaporator to remove the organic solvent chloroform and form a lipid film, irinotecan hydrochloride 1.5 g of sucrose solution was hydrated in 200 mL, passed through 400 nm, 200 nm, and 100 nm membranes with uniform particle size respectively to prepare drug-loaded liposomes, which were freeze-dried and stored at 2-4°C.

Embodiment 2

[0020] Embodiment 2: pH gradient method preparation

[0021] (1) Preparation of blank liposomes

[0022] prescription:

[0023] Phosphatidylcholine 10.605g (13.95394737mmol)

[0024] Cholesterol 4.395g (11.38601036mmol)

[0025] Ethanol 24.75mL

[0026] tert-butanol 24.75mL

[0027] citric acid buffer

[0028] 150mL

[0029] Preparation method: Dissolve phosphatidylcholine and cholesterol in a 1:1 (v / v) mixed solvent of ethanol and tert-butanol until the solution is clear and transparent. Lipid solution and citrate buffer were mixed in a gradient pump at a volume ratio of 1:4 to prepare proliposomes. The gradient pump is connected to the extruder, and five 100nm polycarbonate films are laid in the extruder. The mixed proliposomes are extruded with a uniform particle size by an extruder, and the outflowing liposome mixed solution is ultrafiltered through an ultrafilter immediately, and 750 mL of citric acid buffer (pH=4.0) is continuously added in the ...

Embodiment 3

[0034] Embodiment 3: scale up production process

[0035] (1) Preparation of blank liposomes

[0036] prescription:

[0037] Cardiolipin 211.8g (278.6842105mmol)

[0038] Cholesterol 88.2g (228.4974093mmol)

[0039] Ethanol 495mL

[0040] tert-butanol 495mL

[0041] Citrate buffer 3000mL

[0042] 3000mL

[0043] Preparation method: Dissolve cardiolipin and cholesterol in a mixed solvent of ethanol and tert-butanol 1:1 (v / v) until the solution is clear and transparent. Lipid solution and citrate buffer were mixed in a gradient pump at a volume ratio of 1:4 to prepare proliposomes. The gradient pump is connected to the extruder, and five 100nm polycarbonate films are laid in the extruder. The mixed proliposomes are extruded with a uniform particle size by an extruder, and the outflowing liposome mixed solution is ultrafiltered through an ultrafilter immediately, and 15 L of citric acid buffer (pH=4.0) is continuously added in the middle, and the...

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Abstract

The invention relates to a method for producing injection alcaine liposome, wherein it comprises that: dissolving liposome mixture into organic solvent; mixing liposome solution with buffer solution; compressing it via panlite film into uniform diameter, filtering out the organic solvent, to obtain blank liposome, adding alcaine solution, using pH adjuster to adjust pH value to alkali, to prepare the carrier liposome; or dissolving phosphatide, cholestrin and alcaine into organic solvent; atomizing and drying, vacuum drying or other method to remove organic solvent, to film the liposome; adding hydrating solution with drug to form carrier liposome. The inventive liposome has 50-200nm diameter and more than 95% package rate, with stable property.

Description

technical field [0001] The invention relates to a preparation method of liposome, in particular to a preparation method of irinotecan hydrochloride liposome for injection. Background technique [0002] Irinotecan hydrochloride is a semi-synthetic derivative of camptothecin. Camptothecin can specifically bind totoisomerase I, which induces reversible single-strand breaks, thereby unwinding the DNA double-strand structure; irinotecan metabolite SN-38 can bind totoisomerase I-DNA The complex binds, thereby preventing religation of the broken single strands. Existing studies suggest that the cytotoxicity of irinotecan is due to the interaction between replicase and topoisomerase I-DNA-SN-38 triple complex during DNA synthesis, which causes DNA double-strand breaks. Mammalian cells cannot efficiently repair such DNA double-strand breaks. In this way, the purpose of killing tumor cells is achieved. [0003] Irinotecan can be dissolved in water, but its metabolite irinotecan hy...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/4745A61P35/00
Inventor 佐建锋王九成黄馨惠傅经国魏春龙胡忍乐
Owner XIAN LIBANG PHARMA TECH
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