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Bone targeting vector and medicament

A bone targeting and drug technology, applied in the field of targeted drugs of drugs, can solve the problems of weak tumor killing effect and low drug loading, and achieve the effects of easy control of conditions, good biocompatibility and fast response speed.

Inactive Publication Date: 2012-01-25
蔡林 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This idea was proposed by Chen Fangzhou et al., who used the osteophilic drug tetracycline (Tetracyline, TC) as a targeting substance, and oxidized dextran (Dextran) as an intermediate, connecting tetracycline and adriamycin (Adr1amycin, ADM) grafted On the polymer, the complex ADM-DEX-TC was prepared, but the synthetic complex was not characterized, and the drug loading was low, and the killing effect on tumors was weaker than that of the raw drug ADM

Method used

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  • Bone targeting vector and medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1: Synthesis of oxidized dextran

[0035] Weigh 10.0g of dextran (T-40) and 13.5g of sodium periodate, and dissolve them in 200ml and 150ml of pH4.4 phosphate buffer solution respectively to obtain dextran solution and sodium periodate solution. Add the sodium solution into the dextran solution, stir at room temperature at 1500r / min in the dark for 4.5 hours, immediately add 4.5ml of glycerol, continue stirring at room temperature at 1500r / min for 15 minutes, place the reaction mixture in a dialyzer with a cut-off molecular weight of 3500 The bag was dialyzed at 4°C for 48 hours with distilled water as the medium, and the dialysate was freeze-dried to obtain 5.1 g of oxidized dextran. oxidized dextran 1 HNMR spectrum see figure 1 , 1 HNMR (600MHz, DMSO): δ H =9.61 ppm is the peak generated by aldehyde protons.

Embodiment 2

[0036] Example 2: Synthesis of Bisphosphonate Oxidized Dextran Bone Targeting Drug Carrier

[0037] Take 0.6mmol AEDP and dissolve it in 10ml distilled water. Weigh 100 mg of oxidized dextran (with an aldehyde group content of about 1.0 mmol), dissolve it in 5 ml of distilled water, add AEDP solution to it, incubate at 4 °C for 24 h, place the reaction mixture in a dialysis bag with a cut-off molecular weight of 3500, and distilled water The medium was dialyzed at 4°C in the dark for 48 hours to remove unbound AEDP, and the dialysate was freeze-dried to obtain a white powdery bone-targeting drug carrier.

[0038] 1 HNMR (600MHz, DMSO): δ H =1.47 ppm multiple peaks appear, should be -CH on AEDP 3 introduce. δ H The peak at =7.72 ppm is the peak generated by the Schiffer base structure -HC=N-proton. (see attached figure 2 )

Embodiment 3

[0039] Example 3: Synthesis of bone-targeted pazufloxacin AEDP-Dex-PFX

[0040] Step 1 is the same as in Example 1.

[0041] Step 2: Take 0.6mmol AEDP and dissolve it in 10ml distilled water. Weigh 100mg of oxidized dextran (with an aldehyde content of about 1.0mmol), dissolve it in 5ml of distilled water, add the AEDP solution, and incubate at 4°C for 24h.

[0042] Step 3: Weigh 20 mg of PFX: dissolve it in 10 ml of distilled water with equimolar hydrochloric acid, add it to the above reaction solution, stir with magnetic force, and incubate at 4°C in the dark for 24 hours. Finally, the reaction solution was passed through a Sephadex G-50 gel column, and the first fraction was collected and freeze-dried to obtain a pale yellow powder product bone-targeted pazufloxacin, with a drug loading of 3.38% and an in vitro HA adsorption rate of 89.12%. %.

[0043] 1 HNMR (600MHz, DMSO): δ H =1.30 is the methylene proton peak of cyclopropane on PFX; δ H The multiple peaks at =1.53...

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Abstract

The invention discloses a bone targeting medicinal vector and medicament. The bone targeting medicament vector is prepared by the following steps of: oxidizing glucan into glucan oxide containing a poly-aldehyde group with sodium periodate; and making diphosphonic acid containing an amino group react with the glucan oxide containing the poly-aldehyde group. The medicament with a bone targeting property is obtained by the following steps of: making the bone targeting medicament vector react with a medicament containing an amino group; and connecting the glucan oxide containing the poly-aldehyde group serving as an intermediate with diphosphonic acid with a bone guiding function and other medicaments (except diphosphonic acid) containing amino groups, wherein the prepared bone targeting medicament has high bone affinity and large medicament loading capacity when the reaction mass ratio of the diphosphonic acid to the glucan oxide aldehyde group is (0.4-0.6):1. The bone targeting medicament acts on bone tissues in an oriented way under the guiding action of the diphosphonic acid, and has different treating effects by loading different medicaments. The bone targeting medicament has the advantages of large medicament loading capacity, high bone affinity, simple synthesizing steps and easiness for controlling conditions.

Description

technical field [0001] The invention relates to the technical field of drug targeting drugs, in particular to bone tissue targeting carriers and bone targeting drugs. Background technique [0002] Bone is a special connective tissue composed of a large amount of calcified intercellular substance and cells. The calcified intercellular substance is the bone matrix, in which the content of inorganic salt accounts for 65-70% of the dry weight, and its main component is hydroxyapatite Stone (hydroxyapative, HA). Therefore, bone tissue has high hardness, poor permeability, and special physiological and biochemical processes. For general drug treatment, it is difficult for drugs to reach the lesion effectively, resulting in low local drug concentration and ineffective effects. And increasing the administration concentration will increase the toxic and side effects on other tissues and organs. The drug treatment of bone tissue-related diseases, such as osteoporosis, osteomyeli...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36A61P31/04A61K31/704A61P35/00A61P19/08A61K31/5383A61K47/48
Inventor 蔡林余黎
Owner 蔡林
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