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Protein-based pharmacological active substance composition, and preparation method and applications thereof

A pharmacological activity, protein technology, applied in the direction of drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problem of not improving the biodistribution of paclitaxel molecules and blood circulation time, and achieve the enrichment effect and biodistribution improvement, inhibited growth, Strong anti-proliferative effect

Inactive Publication Date: 2015-07-08
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, Abraxane powder dissociates rapidly in clinical use to form single albumin-sized particles with a size less than 10 nm, which does not improve the biodistribution and blood circulation time of paclitaxel molecules (Chem.Soc.Rev., 2012, 41, 2971-3010 )

Method used

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  • Protein-based pharmacological active substance composition, and preparation method and applications thereof
  • Protein-based pharmacological active substance composition, and preparation method and applications thereof
  • Protein-based pharmacological active substance composition, and preparation method and applications thereof

Examples

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preparation example Construction

[0055] The preparation method of the pharmacologically active substance preparation provided by the present invention for in vivo delivery comprises:

[0056] An aqueous medium in which a pharmacologically active substance, a water-miscible organic solvent, and a protein is mixed to obtain a mixture (without surfactants in the mixture) and subjected to pressures ranging from 3,000 to 30,000 psi 2 in the high pressure homogenizer. The organic solvent can be selectively removed from the mixture after being subjected to high shear conditions; it can also be selectively removed from the mixture before being subjected to high shear conditions.

[0057] The above-mentioned process of forming the mixture can be that the organic solution is added to the aqueous solution, and the aqueous solution can also be added to the organic solvent. The conditions in the mixing process can be ultrasonic, magnetic stirring, mechanical stirring, homogenization or high shear agitator, There could also...

preparation example 1

[0074] The purpose of this example is to demonstrate the homogeneous preparation of nanoparticles using high pressure. Dissolve 30 mg of paclitaxel (Paclitaxel) in 3.0 ml of ethanol. To the solution was added 27.0 ml of an aqueous solution of human serum albumin (1% w / v). The resulting mixture was placed in a Rotary evaporator and evaporated at 40°C under reduced pressure (30mmHG) for 20-30 minutes to remove ethanol. Homogenization was then performed at low RPM for 5 minutes to form a coarse emulsion, which was then transferred to a high pressure homogenizer (Avestin). Then at 9000-18000 psi 2 (psi) at least five more high-pressure homogenization cycles. The resulting dispersion was translucent, and the paclitaxel particles generally had a diameter of less than 200 nm (quantitative statistics, Malvern Zetasizer). Without adding any antifreeze, the dispersion was freeze-dried to form a dry powder. The dry powder can be reconstituted with sterile water or physiological sali...

preparation example 2

[0076]The purpose of this example is to demonstrate the use of cavitation and high shear stress in sonication for the preparation of paclitaxel nanoparticles. Dissolve 20 mg paclitaxel in 2.0 ml ethanol. Add 4.0 ml of human serum albumin solution (5% w / v) to the solution. The mixture was homogenized at low RPM for 5 minutes to form a coarse emulsion, which was then transferred to a 40 kHz sonication cell. Sonicate for 1 min at 60-90% power, level 0. The mixture was then transferred to a rotary evaporator and evaporated at 40°C under reduced pressure (30 mmHg) for 20-30 minutes to remove the organic solvent. Paclitaxel microparticles were obtained, typically less than 200 nm in diameter (quantitative statistics, Malvern Zetasizer). Without adding any antifreeze, the dispersion was freeze-dried to form a dry powder. The dry powder can be reconstituted with sterile water or physiological saline, and the particle size in the reconstituted solution remains below 200nm.

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Abstract

A protein-based pharmaceutical active substance composition, the preparation method therefor, and the use thereof. The pharmaceutical active substance delivery system comprises solid or liquid pharmaceutical active substance and particulates composed of protein coating, wherein the protein coating includes free protein associated therewith, the part of pharmaceutical active substance is wrapped in the protein coating and the other part of pharmaceutical active substance is associated with the free protein, the particles have an average particle diameter of 10-200nm. Maximum kinetic hydrated particle size is over 10nm when the particles are dispersed in an aqueous solution. The pharmaceutical active substance delivery system will not quickly dissociate to the size of 10nm or less when it is dissolved and diluted by the injection, thus the effect of enrichment in the tumor site and the bio-distribution are improved.

Description

technical field [0001] The present invention relates to a drug delivery system, in particular to a pharmacologically active substance delivery system, in particular to a protein-based pharmacologically active substance composition and its preparation method and application. Background technique [0002] Intravenous drug delivery is quickly and directly balanced with blood flow carrying the drug to the rest of the body. In order to avoid the peak concentration of the drug in the blood vessel in a short time after injection, the drug is carried in a stable carrier, and the drug can be gradually released in the blood vessel after the pulse dose of intravenous injection. [0003] However, on the one hand, many common clinical drugs are highly hydrophobic and difficult to disperse in an aqueous liquid environment, resulting in difficulties in administration methods and drug absorption. When administered intravenously, co-solvents such as Cremphor need to be used, and the use of ...

Claims

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Application Information

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IPC IPC(8): A61K47/42A61K9/16A61K31/337A61P35/00
CPCA61K9/14A61K9/0019A61K9/1075A61K9/5052A61K9/5169A61K31/337A61P35/00
Inventor 梁兴杰安菲菲柳娟
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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