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A combined nano-preparation of camptothecins and taxanes and its preparation

A nano-formulation, camptothecin technology, applied in the direction of drug combination, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc.

Active Publication Date: 2020-05-22
YANTAI LANNACHENG BIOTECHNOLOGY CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In view of the above-mentioned background, it is necessary to develop a kind of nano-preparation, which can solve the problem of the combination of camptothecin and paclitaxel

Method used

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  • A combined nano-preparation of camptothecins and taxanes and its preparation
  • A combined nano-preparation of camptothecins and taxanes and its preparation
  • A combined nano-preparation of camptothecins and taxanes and its preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1: Assembly of CPT-ss-EB and Paclitaxel

[0041] Dissolve CPT-ss-EB and paclitaxel in methanol at a mass ratio of 1:0.5, then drop into the stirring aqueous solution, and then volatilize the methanol in a fume hood to obtain an aqueous solution of nanoparticles, and use a centrifuge to centrifuge at 4000 rpm After 4 minutes, the white precipitate (unassembled paclitaxel) was removed, and the remaining paclitaxel content was detected by high performance liquid chromatography. After testing, the final molar ratio of CPT-ss-EB and paclitaxel in the obtained nanoparticles was 1:0.67, and the hydrated diameter of the nanoparticles was 141±16nm. The nanoparticles were very stable in water and no visible precipitation was seen for 2 months.

Embodiment 2

[0042] Example 2: Assembly of CPT-ss-EB and Paclitaxel

[0043] CPT-ss-EB and paclitaxel were dissolved in methanol at a mass ratio of 1:1, then dropped into the stirring aqueous solution, and then dialyzed to remove methanol to obtain an aqueous solution of nanoparticles, which was centrifuged at 4000 speeds for 4 minutes in a centrifuge, The white precipitate (unassembled paclitaxel) was removed, and the remaining paclitaxel content was detected by high performance liquid chromatography. After testing, the final molar ratio of CPT-ss-EB and paclitaxel in the obtained nanoparticles was 1:1.30, and the hydrated diameter of the nanoparticles was 156±39nm. The nanoparticles were very stable in water and no visible precipitation was seen for 2 months.

Embodiment 3

[0044] Example 3: Assembly of CPT-ss-EB and Paclitaxel

[0045] Dissolve CPT-ss-EB and paclitaxel in ethanol at a mass ratio of 1:2, then volatilize the ethanol, add an aqueous solution, shake or sonicate to obtain nanoparticles, and use a centrifuge to centrifuge at 4000 speed for 4 minutes to remove the white Precipitate (unassembled paclitaxel) and detect remaining paclitaxel content using HPLC. After testing, the final molar ratio of CPT-ss-EB and paclitaxel in the obtained nanoparticles was 1:2.17, and the hydrated diameter of the nanoparticles was 142±43nm. The nanoparticles were very stable in water and no visible precipitation was seen for 2 months.

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PUM

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Abstract

The invention provides a combined nano preparation of camptothecin and yew medicines and preparation of combined nano preparation. The combined nano preparation is of a nano structure formed by physically coating a yew medicine with amphipathic medicine molecules of formula (I) as shown in the specification as a carrier, in the formula, the mole ratio of the amphipathic medicine molecules to the yew medicine is 1:(0.5-3); in the formula I, R1 is a camptothecin or a derivative group thereof; R2 is one of formulae as shown in the specification; R3 is one of formulae as shown in the specification X is one of S or -CH2-; n1 and n2 are both integers of 0-10. The combined nano preparation provided by the invention does not need an extra surfactant, and the formed nano structure is very high in medicine carrying capacity and very good in dispersibility and stability. After intravenous injection, camptothecin and yew medicines are respectively combined with proteins, and then stable albumin-medicine compositions can be formed.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a small-molecule amphiphilic drug formed from camptothecin and Evans blue, which is used as a combined preparation of a pharmaceutical adjuvant and other chemotherapeutic drugs, and a preparation method thereof. Background technique [0002] Cancer is one of the leading causes of morbidity and death worldwide. According to the World Health Organization, there were about 14 million new cases worldwide in 2012, and the number of new cases is expected to increase by about 70% in the next two decades. Cancer is the second leading cause of death worldwide, killing 8.8 million people in 2015. Globally, nearly one in six deaths is due to cancer, with approximately 70% of cancer deaths occurring in low- and middle-income countries. Currently, chemotherapy is one of the main treatments for cancer. Combination drugs are one of the most common means of chemotherapy....

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K47/54A61K9/51A61K47/22A61K31/4745A61P35/00A61K31/337
CPCA61K9/5123A61K31/337A61K31/4745A61K2300/00
Inventor 陈小元张福武
Owner YANTAI LANNACHENG BIOTECHNOLOGY CO LTD