Protein conjugate and pharmaceutical compositions thereof

A protein coupling and conjugate technology, which can be used in drug combinations, animal/human proteins, albumin peptides, etc., and can solve the problems of weak nanocrystalline stability and performance.

Inactive Publication Date: 2009-02-04
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Human serum albumin has achieved great success as the carrier of paclitaxel nanosuspension for injection, but there are still shortcomings: on the one hand, Abraxane is a passive targeting agent, and further research can be made into an active targeting agent to improve targeting. On the other hand, in our study, we found that the stability of nanocrystals to drugs other than paclitaxel and cyclosporine A is weak

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Preparation of Folic Acid-Bovine Serum Albumin Conjugate by Ultrasonic Treatment

[0066] Treat 30.0ml bovine serum albumin (1%, w / v) and cystine-modified folic acid (0.1%, w / v) solution in a 60kHz ultrasonic processor for 2 minutes, dilute with water, and have a molecular weight of 10,000 The ultrafiltration membrane is ultrafiltered, and the concentrate is freeze-dried to obtain folate-coupled bovine serum albumin.

Embodiment 2

[0068] Preparation of oligomeric hyaluronic acid-human serum albumin conjugate by high pressure homogenization method

[0069] 200.0ml of human serum albumin (1%, w / v) and cystine modified oligomeric hyaluronic acid (0.1%, w / v, molecular weight of oligomeric hyaluronic acid is 3500, cystine coupling degree is 10%) The solution is transferred to the high-pressure homogenizer, the high-pressure homogenization cycle is 5 times, the homogenate is diluted with water, the ultrafiltration membrane with a molecular weight of 30,000 is ultrafiltered, and the concentrated solution is freeze-dried to obtain the oligomeric hyaluronic acid coupling Human serum albumin.

Embodiment 3

[0071] Preparation of paclitaxel nano-suspension containing folic acid-human serum albumin conjugate by high pressure homogenization method

[0072] Dissolve 200mg Paclitaxel in 2.7ml chloroform and 0.3ml absolute ethanol, add 97.0ml human serum albumin (3%, w / v) and cystine modified folic acid (0.3%, w / v) ) Aqueous solution, the mixture is homogenized at a low speed for 5 minutes to form a crude emulsion, and then transferred to a high-pressure homogenizer, the high-pressure homogenization cycle is 8 times, and the homogenate is evaporated at 40°C under reduced pressure for 20 minutes The dichloromethane is quickly removed, and the resulting dispersion is translucent. The diameter of paclitaxel particles is generally 130-160nm, diluted with water, and ultrafiltration with an ultrafiltration membrane with a molecular weight of 10,000. The concentrate is freeze-dried for 48 hours without any freezing Dry proppant. The obtained cake is easily reconstituted into the original dispersi...

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Abstract

The invention discloses a novel protein conjugate which is the conjugate of proteins and endogenous substances modified by cystine or cysteine. Besides, the invention also discloses a drug combination comprising the protein conjugate and the preparation method of the protein conjugate and the drug combination comprising the protein conjugate. The invention does not relate to toxic organic solvents and catalysts, reactions are simple and easy, and products are easy for separation, refinement and quality control, and moreover, the active targeting property of the obtained drug combination is improved.

Description

Technical field [0001] The present invention relates to pharmaceutical preparation technology, and more specifically, to a novel protein conjugate, a preparation method thereof, and a pharmaceutical composition containing the protein conjugate. Background technique [0002] In drug research, it is found that nearly 40% of drugs are poorly soluble in water, and some drugs are even insoluble in organic solvents, resulting in low bioavailability. In the preparation process, the use of cyclodextrin inclusion technology, surfactant solubilization, emulsion, microemulsion and solid dispersion technology can solve the problem of low bioavailability of some insoluble drugs, but there are still a large number of drugs due to bioavailability. Due to the degree of problems, it was abandoned. And nanosuspension technology provides these drugs with an opportunity to reproduce their own value. Nano suspension is a submicron colloidal dispersion system formed by using a small amount of surfacta...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/765C07K1/10A61K47/48A61K31/337A61P35/00A61K47/42
Inventor 高缘张建军吕慧侠
Owner CHINA PHARM UNIV
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