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Protein conjugate and pharmaceutical compositions thereof

A protein 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: 2012-07-04
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 the molecular weight is 10,000 The ultrafiltration membrane is ultrafiltered, and the concentrate is freeze-dried to obtain folic acid-coupled bovine serum albumin.

Embodiment 2

[0068] Preparation of Oligomeric Hyaluronic Acid-Human Serum Albumin Conjugate by High Pressure Homogenization

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

Embodiment 3

[0071] Preparation of Paclitaxel Nanosuspension Containing Folic Acid-Human Serum Albumin Conjugate by High Pressure Homogenization

[0072] Dissolve 200mg of paclitaxel (Paclitaxel) in 2.7ml of chloroform and 0.3ml of absolute ethanol, add 97.0ml of human serum albumin (3%, w / v) and cystine-modified folic acid (0.3%, w / v ) aqueous solution, the mixture was homogenized at low speed for 5 minutes to form a coarse emulsion, which was then transferred to a high-pressure homogenizer for 8 cycles of high-pressure homogenization, and the homogenate was evaporated at 40°C for 20 minutes under reduced pressure Quickly remove dichloromethane, the obtained dispersion is translucent, the diameter of paclitaxel particles is generally 130 ~ 160nm, dilute with water, ultrafiltration with an ultrafiltration membrane with a molecular weight of 10,000, and freeze dry the concentrate for 48 hours without adding any frozen dry proppant. The obtained cake can easily reconstitute the original dis...

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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, 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 insoluble 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. It was abandoned due to the degree of problems. The nanosuspension technology provides these drugs with the opportunity to reproduce their own value. Nanosuspension is a submicron colloidal dispersion system formed by stabilizing pure drug particles with...

Claims

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Application Information

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Patent Type & Authority Patents(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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