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Cyanoacrylate material carrying antitumor drug

A technology of cyanoacrylate and cyanoacrylate diester is applied in the field of cyanoacrylate materials, which can solve the problems of easy overflow of liquid drugs and failure to achieve long-term administration.

Inactive Publication Date: 2019-06-21
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, in the scheme of intratumoral injection, there are two risk issues that need to be paid special attention to. One is that the liquid drug is easy to overflow after injection into the tumor because the intratumoral pressure is higher than that of normal tissue. Afterwards, the drug is easy to spread from the tumor site to other tissues quickly, and the purpose of long-acting drug administration cannot be achieved

Method used

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  • Cyanoacrylate material carrying antitumor drug
  • Cyanoacrylate material carrying antitumor drug
  • Cyanoacrylate material carrying antitumor drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0114] The preparation of embodiment 1 formula glue

[0115] Using cyanoacrylate monomers BCA, MOE-CA, CA-TEG-CA, CA-PEG 600 -CA, CA-PEG 2000 -CA, according to the recipe in Table 1 to prepare formula glue. Under the condition of nitrogen protection, the corresponding monomer components are mixed by stirring, shaking, etc., and a clear and transparent formula glue can be obtained. The formula glue is polymerized at normal temperature and pressure in the air to form a glue block. The degradation rate and bonding strength of the rubber blocks were tested, and the results are shown in Table 1.

[0116] The structure of each monomer is as follows:

[0117]

[0118] BCA R=-CH 2 -CH 2 -CH 2 -CH 3 CA-TEG-CA W=-(CH 2 CH 2 O) 3 -CH 2 CH 2 -

[0119] MOE-CA R=-CH 2 -CH 2 -O-CH 3 CA-PEG 600 -CA W=PEG 600

[0120] MOEOE-CA R=-CH 2 -CH 2 -O-CH 2 -CH 2 -O-CH 3 CA-PEG 2000 -CA W=PEG 2000

[0121] Table 1 The composition of the formula glue and the degradatio...

Embodiment 2

[0127] The preparation of embodiment 2 drug-loaded glue

[0128] The formula glue in Table 1 was mixed with fluorouracil, curcumin, doxorubicin, paclitaxel, and docetaxel respectively, and each drug was used in multiple mass ratios (0.1%, 0.25%, 0.5%, 0.75%, 1%, 1.25%, 1.5%, 2%, 2.5%), clear and transparent drug-loaded gel solutions can be obtained.

Embodiment 3

[0129] The in vitro drug release test of the drug-loaded glue of embodiment 3 different monomer formulations

[0130] Take the drug-loaded gel solution containing 1.25% fluorouracil as an example. Add 1.25% by mass fluorouracil to the formulated gels of groups A, F, G, I, J, K, and M, and mix them uniformly to obtain drug-loaded gels in the form of clear solutions. Take 0.1g drug-loaded gel solution and polymerize it into a gel block (area 2.5×1cm 2 ), placed in 50mL PBS solution (pH7.4), and then put the solution containing the gel pieces into a constant temperature shaker (SHZ-82A, JINTAN RONGHUA, China, 60rpm) at 37°C. Samples were taken at a certain time point to test the fluorouracil content in the solution, and then the drug release amount of each group was calculated. Determination of the content of fluorouracil: firstly, through the method of high performance liquid phase, different concentrations of standard products are configured, and the peak area-concentration s...

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Abstract

The invention relate to the field of biomedicine and materials, in particular to a cyanoacrylate material carrying an antitumor drug. The invention particularly relates to a composition containing anantitumor drug and a cyanoacrylate, as well as a pharmaceutical preparation containing the composition, such as a pharmaceutical preparation suitable for intra-tumor injection.

Description

technical field [0001] The invention relates to the fields of biomedicine and materials, in particular to a cyanoacrylate material loaded with antitumor drugs. Background technique [0002] Intratumoral injection therapy is a new tumor treatment plan developed in recent years. By injecting drugs directly into the tumor to make it play the role of fixed-point therapy, it can avoid or alleviate the first-pass effect that oral and intravenous injections need to face to a certain extent. and systemic side effects. In some parts that can be reached without using open surgical instruments, and some parts that are not conducive to surgical resection, or when the postoperative aesthetics are considered, the treatment plan of intratumoral injection of drugs has unique advantages. [0003] The tumor fusion virus therapy that has been approved for marketing, such as Amgen's IMLYGIC, domestic Jinyousheng, Ankerui and other new drugs, all use intratumoral injection. In addition, a numb...

Claims

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Application Information

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IPC IPC(8): A61K47/18A61K45/00A61P35/00
CPCA61K9/08A61K45/00A61K47/18A61K47/32A61P35/00
Inventor 徐亮张涛张伟刘克良
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A