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Nano-carrier medicine for liver cancer precise targeted treatment and preparation method thereof

A targeted therapy and nano-carrier technology, which is applied in the fields of pharmaceutical formula, drug combination, drug delivery, etc., can solve the problems of poor absorption and release control, inability to achieve precise and effective treatment of liver cancer, poor targeting effect, etc., and achieve good release effect

Inactive Publication Date: 2018-09-25
CHENDU NEW KELI CHEM SCI CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Lenvatinib, which is currently widely used in the treatment of liver diseases, has defects such as poor targeting effect and poor absorption and release control, and cannot achieve precise and effective treatment of liver cancer

Method used

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  • Nano-carrier medicine for liver cancer precise targeted treatment and preparation method thereof
  • Nano-carrier medicine for liver cancer precise targeted treatment and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] (1) Disperse lenvatinib original drug 4-[3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy]-7-methoxy-6-quinolinecarboxamide crystals in methanol and urea , forming a dispersion;

[0033] In the dispersion liquid, by weight, wherein: lenvatinib 24 weight parts, methanol 55 weight parts, urea 21 weight parts;

[0034] (2) Add soluble divalent metal salts, soluble trivalent metal salts, and low-concentration hydrogen peroxide solution to the dispersion prepared in step (1), and heat while stirring to carry out condensation and reflux reaction, so that lenvatinib can be carried on the The hydrotalcite-like macroscopic interlayer; the soluble divalent metal salt is ferrous chloride; the soluble trivalent metal salt is ferric chloride; the mass concentration of low-concentration hydrogen peroxide solution is 7%; the stirring speed is 110r / min; The heating temperature is 86°C and the time is 4h;

[0035] In the reflux reaction system, in parts by weight, including: 60 parts...

Embodiment 2

[0039] (1) Disperse lenvatinib original drug 4-[3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy]-7-methoxy-6-quinolinecarboxamide crystals in methanol and urea , forming a dispersion;

[0040] In the dispersion liquid, in parts by weight, wherein: 22 parts by weight of lenvatinib, 59 parts by weight of methanol, and 19 parts by weight of urea;

[0041] (2) Add soluble divalent metal salts, soluble trivalent metal salts, and low-concentration hydrogen peroxide solution to the dispersion prepared in step (1), and heat while stirring to carry out condensation and reflux reaction, so that lenvatinib can be carried on the The hydrotalcite-like macroscopic interlayer; the soluble divalent metal salt is calcium chloride; the soluble trivalent metal salt is ferric bromide; the mass concentration of low-concentration hydrogen peroxide solution is 6%; the stirring speed is 95r / min; the heating of reflux reaction The temperature is 82°C, and the time is 4.5h;

[0042] In the reflux r...

Embodiment 3

[0046] (1) Disperse lenvatinib original drug 4-[3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy]-7-methoxy-6-quinolinecarboxamide crystals in methanol and urea , forming a dispersion;

[0047] In the dispersion liquid, in parts by weight, wherein: 28 parts by weight of lenvatinib, 51 parts by weight of methanol, and 21 parts by weight of urea;

[0048] (2) Add soluble divalent metal salts, soluble trivalent metal salts, and low-concentration hydrogen peroxide solution to the dispersion prepared in step (1), and heat while stirring to carry out condensation and reflux reaction, so that lenvatinib can be carried on the The hydrotalcite-like macroscopic interlayer; the soluble divalent metal salt is magnesium chloride; the soluble trivalent metal salt is ferric nitrate; the mass concentration of the low-concentration hydrogen peroxide solution is 7%; the stirring speed is 115r / min; the heating temperature of the reflux reaction is 88 ℃, the time is 3.5h;

[0049] In the reflu...

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Abstract

The invention relates to the field of carrier medicine, and discloses nanometer carrier medicine for liver cancer precise targeted treatment and a preparation method thereof. The method comprises thefollowing preparation processes of (1) adding Lenvatinib raw medicine into methyl alcohol and urea to form a dispersion solution; (2) adding soluble bivalent metal salts, soluble trivalent metal saltand low-concentration hydrogen peroxide solution; performing stirring and heating for condensing backflow reaction; (3) using a sulfamic acid water solution for anionic intercalation modification; after the completion, performing washing and drying by distillation; preparing nanometer grade liver cancer precise targeted carrier medicine. The nanometer carrier medicine prepared by the method has the advantages that the Lenvatinib is used; the modified hydrotalcite has the functional performance of light, electricity, magnetism, biology and the like, the cell barrier targeted medication of the nano-carrier medicine can be effectively realized; the absorption and release control effect is good; the medicine can be widely used for liver cancer treatment.

Description

technical field [0001] The invention relates to the field of carrier drugs, and discloses a nano carrier drug for precise targeted therapy of liver cancer and a preparation method thereof. Background technique [0002] In recent years, cancer is a disease that seriously affects human health. Chemotherapy is the main method for treating tumors. However, chemotherapy has serious adverse reactions. At the same time, traditional anticancer drugs also attack normal cells while killing tumor cells. Traditional anticancer drugs lack It is selective, widely distributed in the body, and has large toxic and side effects on normal tissues and organs under therapeutic doses, which brings great pain to patients and poor curative effect. How to release anticancer drugs only in tumor tissue without affecting normal cells is an urgent problem to be solved. At present, precision medicine has become the first choice for the treatment of tumors. [0003] Precise targeted therapy is a treatme...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/02A61K31/47A61P35/00
CPCA61K9/0087A61K31/47A61K47/02A61P35/00
Inventor 陈庆曾军堂
Owner CHENDU NEW KELI CHEM SCI CO LTD
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