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Formula and preparation process of specific targeting medicament for treating pancreatic cancer

A preparation process, a technology for pancreatic cancer, applied in the direction of medical formula, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of unsatisfactory treatment effect of pancreatic cancer, and achieve the purpose of strengthening targeted therapy Effect, improve targeted therapy effect, good effect of sustained release performance

Pending Publication Date: 2020-07-10
类承斌
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, targeted therapy has achieved very good curative effects in colorectal cancer, lung cancer and other cancers, but the therapeutic effect of targeted drug therapy in pancreatic cancer is not very satisfactory

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] S1. Compound X-76, namely 43-O-(2-(4-(diethylaminomethyl)-1H-1,2,3-triazol-1-yl)acetyl)oxyrapamycin Soluble in maleic acid, as the organic phase, the modified magnetic carboxymethyl chitosan nano-microspheres are made into an aqueous dispersion, as the water phase, wherein the modified magnetic carboxymethyl chitosan nano-microspheres The concentration of the resulting aqueous dispersion is 0.2%, and the weight ratio of the modified magnetic carboxymethyl chitosan nanospheres to the compound X-76 is 1:18;

[0023] S2. Add the organic phase obtained in step S1 into the water phase while stirring, and stir at 20° C. for 8 hours at a stirring speed of 600 rpm to obtain a mixture;

[0024] S3, using deionized water to wash the mixture obtained in step S2, and then collect the microspheres by magnetic separation, wherein the steps of washing with deionized water and magnetic separation are repeated 5 times;

[0025] S4. Freeze-dry the microspheres obtained in step S3. The f...

Embodiment 2

[0027] S1. Compound X-76, namely 43-O-(2-(4-(diethylaminomethyl)-1H-1,2,3-triazol-1-yl)acetyl)oxyrapamycin Soluble in maleic acid, as the organic phase, the modified magnetic carboxymethyl chitosan nano-microspheres are made into an aqueous dispersion, as the water phase, wherein the modified magnetic carboxymethyl chitosan nano-microspheres The concentration of the resulting aqueous dispersion is 0.2%, and the weight ratio of the modified magnetic carboxymethyl chitosan nanospheres to the compound X-76 is 1:20;

[0028] Wherein, the preparation of the modified magnetic carboxymethyl chitosan nano drug-loaded microspheres, the specific steps are as follows: first, the magnetic Fe coated with oleic acid 3 o 4 Nanoparticles are dispersed in cyclohexane as an oil phase; secondly, an aqueous solution of carboxymethyl chitosan with a mass volume concentration of 1.5% is added to the oil phase as an aqueous phase, wherein the oleic acid-wrapped magnetic Fe 3 o 4 The volume ratio ...

Embodiment 3

[0033] S1. Compound X-76, namely 43-O-(2-(4-(diethylaminomethyl)-1H-1,2,3-triazol-1-yl)acetyl)oxyrapamycin Soluble in maleic acid, as the organic phase, the modified magnetic carboxymethyl chitosan nano-microspheres are made into an aqueous dispersion, as the water phase, wherein the modified magnetic carboxymethyl chitosan nano-microspheres The concentration of the resulting aqueous dispersion is 0.2%, and the weight ratio of the modified magnetic carboxymethyl chitosan nanospheres to the compound X-76 is 1:16;

[0034] Wherein, the preparation of the modified magnetic carboxymethyl chitosan nano drug-loaded microspheres, the specific steps are as follows: first, the magnetic Fe coated with oleic acid 3 o 4 Nanoparticles are dispersed in cyclohexane as an oil phase; secondly, an aqueous solution of carboxymethyl chitosan with a mass volume concentration of 1.8% is added to the oil phase as an aqueous phase, wherein the magnetic Fe encapsulated by oleic acid 3 o 4 The volum...

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Abstract

The invention discloses a formula of a specific targeting medicament for treating pancreatic cancer. The specific targeting medicament comprises the following components: a compound X-76, namely 43-O-(2-(4-(diethylaminomethyl)-1H-1,2,3-triazol-1-yl)acetyl)oxyrapamycin, and modified magnetic carboxymethyl chitosan nano microspheres, wherein the weight ratio of the compound X-76 to the modified magnetic carboxymethyl chitosan nano microspheres is 1:(15-20). According to the invention, the compound X-76 / modified magnetic carboxymethyl chitosan nano drug-carrying microspheres can have superparamagnetism, can selectively reach and be positioned at a tumor target area to release the medicament under guidance of an external magnetic field through vein medication, arterial catheter medication, oral medication or direct injection, so that the targeted therapeutic effect of the compound X-76 is improved, and comprehensive control of temperature, time and stirring speed in a preparation process is improved. Therefore, that the diameter of the compound X-76 / modified magnetic carboxymethyl chitosan nano drug-carrying microspheres is small (35+ / -2 nm), slow release performance is good, and simultaneously the targeted therapeutic effect of the medicament on pancreatic cancer cells PANC-1 is enhanced.

Description

technical field [0001] The invention relates to the technical field of targeted anticancer agents, in particular to a formulation of a specific targeted agent for treating pancreatic cancer and a preparation process thereof. Background technique [0002] Pancreatic cancer is a highly malignant tumor of the digestive tract that is difficult to diagnose and treat. About 90% of pancreatic cancers are ductal adenocarcinomas originating from the ductal epithelium. Its morbidity and mortality have increased significantly in recent years. The 5-year survival rate is <1%, and it is one of the malignant tumors with the worst prognosis. The early diagnosis rate of pancreatic cancer is not high, the surgical mortality rate is high, and the cure rate is very low. The incidence of this disease is higher in men than in women, with a male to female ratio of 1.5 to 2:1. Male patients are far more common than premenopausal women, and the incidence of postmenopausal women is similar to t...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/12A61K47/02A61K47/36A61K31/439A61P35/00
CPCA61K9/1617A61K9/1611A61K9/1652A61K31/439A61P35/00
Inventor 类承斌张文杜文燕
Owner 类承斌
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