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Irinotecan hydrochloride lipidosome and preparation method thereof

A technology of healthy lipids and liposomes, which is applied in the field of medicine, can solve the problems of unsatisfactory stability and particle size, etc., and achieve the effect of good therapeutic effect, better therapeutic effect and high drug loading capacity

Inactive Publication Date: 2016-05-04
QINGDAO CHENDA BIOLOGICAL SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The prescriptions recorded in the existing patent documents have good effects, but if they are prepared into preparations suitable for human use, they are still unsatisfactory in terms of stability, particle size, etc.

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027]

[0028] Preparation:

[0029] a. Prepare blank liposomes by ethanol injection method: dissolve the prescribed amount of hydrogenated soybean lecithin, dipalmitoylphosphatidylethanolamine, cholesterol and Pluronic L61 with absolute ethanol to form solution A, and stir in a water bath at 60°C. Solution A injects and dissolves PEG2000-distearic acid phosphatidylethanolamine concentration and is in the ammonium sulfate solution hydration medium of 0.2mol / L, high-speed (rotating speed is 20000rpm) stirring, then high-pressure homogenization under 20000psi 4 times, with 0.3 The mol / L sucrose aqueous solution is replaced by 15 times the volume of ammonium sulfate except the aqueous phase through a tangential flow ultrafiltration system (membrane molecular weight 50kDa, flow rate 200ml / min, pressure 2.0bar), to obtain blank liposomes;

[0030] b. Add irinotecan hydrochloride aqueous solution to the blank liposomes obtained in step a, adjust the pH of the external phase to 7...

Embodiment 2

[0032]

[0033] The preparation method is the same as in Example 1.

Embodiment 3

[0035]

[0036] The preparation method is the same as in Example 1.

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Abstract

The invention belongs to the technical field of medicine and particularly discloses an irinotecan hydrochloride lipidosome and a preparation method thereof. The lipidosome is prepared from irinotecan hydrochloride, hydrogenated soybean lecithin, hydrogenated soybean lecithin, PEG2000-distearic phosphatidyl ethanolamine, pluronic L61, cholesterol and the like. The lipidosome is high in encapsulation efficiency, good in stability and high in safety and is suitable for industrialized popularization and application.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a liposome of irinotecan hydrochloride and a preparation method thereof. Background technique [0002] Irinotecan hydrochloride (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. [0003] The saturated lactone ring in the structure of irinotecan hydrochloride is pH-dependent, and will reversibly transform into its carboxylate form under physiological conditions, thereby weakening the antitumor activity. The dosage form currently available on the market is irinotecan hydrochloride intravenous drip injection concentrate, and the drug name is Campto. Clinically, after intravenous admin...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/14A61K47/24A61K47/28A61K47/34A61K31/4745A61P35/00
CPCA61K9/127A61K9/0019A61K9/145A61K31/4745A61K47/24A61K47/28A61K47/34
Inventor 陈令浩
Owner QINGDAO CHENDA BIOLOGICAL SCI & TECH
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