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Oligopeptide used for increasing solubilities of paclitaxel or similar medicines based on paclitaxel structure

A paclitaxel and solubility technology, applied in the direction of drug combinations, peptides, anti-tumor drugs, etc., can solve the problem of low oral bioavailability

Inactive Publication Date: 2013-12-04
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, CN1671370A discloses the use of mucoadhesive lipid-glycerol monooleate as the main component of oral delivery of paclitaxel, which solves the problems of paclitaxel precipitation and low oral bioavailability in the clinical preparation of marketed injections

Method used

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  • Oligopeptide used for increasing solubilities of paclitaxel or similar medicines based on paclitaxel structure
  • Oligopeptide used for increasing solubilities of paclitaxel or similar medicines based on paclitaxel structure
  • Oligopeptide used for increasing solubilities of paclitaxel or similar medicines based on paclitaxel structure

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Embodiment 1: the preparation of oligopeptide

[0058] The amino acid monomer [Trp(L), Trp(D), Phe(L), Phe(L), Ala(L), Ser(L), Gly(L), Arg(L), Glu, Lys(L) ), Asp(L)] are properly combined and connected to form various sequences.

[0059] Under the Amber software, the temperature of the above-mentioned various sequences was gradually raised in a recessive water environment with a step size of 50K, and then the molecular dynamics was stabilized at 300K for 250ns, and finally a stable oligopeptide conformation was obtained; using the docking software Auto Dock Vina docks the optimized oligopeptide molecule onto the paclitaxel molecule. Obtain a rough complex conformation and estimated binding free energy. For the AutoDock Vina program, the search space was limited to the center of the paclitaxel molecule, In the region, 10 optimal conformations were generated each time, and a total of 5 parallel operations were performed, and the conformation with the lowest binding fr...

Embodiment 2

[0066] Example 2: Solubilization preparation and determination of oligopeptide U1

[0067] Solubilization preparation of oligopeptide U1:

[0068]

[0069] Preparation and assay steps:

[0070] 1) Use absolute ethanol with 80% ethanol aqueous solution.

[0071] 2) Weigh 15mg of paclitaxel, dissolve it with ethanol aqueous solution and dilute to 1.5mg·mL -1 solution.

[0072] 3) Weigh 25mg U1, dissolve it in water and dilute to get 2.5mg·mL -1 solution.

[0073] 4) According to the volume ratio of 1:1, measure the two solutions into conical flasks with stoppers, place the conical flasks on a magnetic stirrer, 60°C, 300r·min -1 , stirred for 4 hours.

[0074] 5) Transfer the liquid in the Erlenmeyer flask to a round-bottomed flask, vacuum rotary evaporation, remove the polar organic solvent, transfer the residue to a 5mL volumetric flask with water several times, and make to volume.

[0075] 6) After the above solution was passed through a 0.22 μm filter membrane, 20 μL ...

Embodiment 3

[0077] Example 3: Solubilization preparation and determination of oligopeptide U2

[0078] Solubilization preparation of oligopeptide U2:

[0079]

[0080]

[0081] Preparation and assay steps:

[0082] 1) Use absolute ethanol with 80% ethanol aqueous solution.

[0083] 2) Weigh 15mg of paclitaxel, dissolve it with ethanol aqueous solution and dilute to 1.5mg·mL -1 solution.

[0084] 3) Weigh 25mg U2, dissolve it in water and dilute to get 2.5mg·mL -1 solution.

[0085] 4) According to the volume ratio of 1:1, measure the two solutions into conical flasks with stoppers, place the conical flasks on a magnetic stirrer, 60°C, 300r·min -1 , stirred for 4 hours.

[0086] 5) Transfer the liquid in the Erlenmeyer flask to a round-bottomed flask, vacuum rotary evaporation, remove the polar organic solvent, transfer the residue to a 5mL volumetric flask with water several times, and make to volume.

[0087] 6) After the above solution was passed through a 0.22 μm filter me...

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Abstract

The invention discloses an oligopeptide used for increasing solubilities of paclitaxel or similar medicines based on the paclitaxel structure in a manner of non-covalent supermolecule interaction, compounds of the oligopeptide and paclitaxel or similar medicines based on the paclitaxel structure, a preparation method and a method for increasing solubilities of paclitaxel or similar medicines based on the paclitaxel structure. The oligopeptide has excellent solubilization to paclitaxel. After solubilization treatment is carried out for paclitaxel by the oligopeptide, the solubility of paclitaxel in water is raised remarkably compared to the saturated solubility thereof.

Description

technical field [0001] The present invention relates to the field of pharmaceutical preparations, more specifically, the present invention relates to an oligopeptide that uses non-covalent supramolecular interaction to increase the solubility of paclitaxel or similar drugs based on the structure of paclitaxel, and the combination of the above oligopeptide with paclitaxel or paclitaxel Structure-based drug-like complexes and methods for their preparation, and methods for increasing the solubility of paclitaxel or paclitaxel-based drug-like compounds. Background technique [0002] Many drugs such as paclitaxel (PTX) have good activity, but due to their poor water solubility, they often lead to extremely low bioavailability or cannot be formulated into solutions for injection. In order to increase the bioavailability of such drugs, it is necessary to increase the solubility of these drugs in water. Conventional methods currently used to solubilize these poorly soluble drugs in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06A61K47/48A61K47/42A61K31/337A61P35/00
Inventor 张继稳郭涛李海燕
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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