Novel nano preparation with stable protein and preparation method and use thereof

A protein and application technology, applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problems of small rearrangement and cross-linking, unfavorable production, long time, etc., and achieve a stable shell , stable production and low loss

Inactive Publication Date: 2009-03-18
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the method of patent 200310123461.X to prepare the nano-preparation with albumin as the carrier still has disadvantages: due to the rearrangement of the disulfide bonds between the molecules of human serum albumin under high pressure and high shear force, the interaction between the protein molecules Combined, the high-pressure homogenization takes a long time, on the one hand, the stability of the drug will be affected, especially paclitaxel and other thermally unstable drugs are easy to degrade, and the loss of high-pressure homogenization equipment is also great; on the other hand, disulfide in albumin The number of bonds is limited, so the ratio of rearrangement and cross-linking between protein molecules around the drug nanocrystal is small, and the shell formed is not stable. The drug nanocrystal will still aggregate into larger particles within 24 hours, which is not conducive to stable production

Method used

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  • Novel nano preparation with stable protein and preparation method and use thereof
  • Novel nano preparation with stable protein and preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] (prepared by the method of patent 200310123461.X) 30mg paclitaxel (Paclitaxel) was dissolved in 3.0ml dichloromethane, 27.0ml human serum albumin (1%, w / v, the same below) was added to the solution, and the mixture was heated at a low speed Homogenize for 5 minutes to form a coarse emulsion, and then transfer it to a high-pressure homogenizer (Avestin). Evaporate under reduced pressure for 20 minutes at °C to remove chloroform quickly to obtain a translucent dispersion. The average diameter of paclitaxel particles is 190 nm, and freeze-dry for 48 hours without adding any freeze-dried proppant. The obtained cake is easy to reconstitute the original dispersion liquid after adding sterile water or physiological saline, and the particle size after reconstitution is the same as that before freeze-drying, and precipitation occurs after the dispersion liquid is stable for 16 hours.

[0033] (prepared by the method of the present invention) 30mg paclitaxel (Paclitaxel) and 3mg ...

Embodiment 2

[0036] 200mg of paclitaxel (Paclitaxel) was dissolved in 3.7ml of chloroform and 0.3ml of absolute ethanol, added 97.0ml of aqueous solution containing human serum albumin (3%) and sodium dimercaptosuccinate (0.02%), and the mixture was Homogenize for 5 minutes at a rotating speed to form a coarse emulsion, then transfer it to a high-pressure homogenizer, circulate 4 to 5 times for high-pressure homogenization, evaporate the homogenate at 40°C for 20 minutes under reduced pressure, and quickly remove chloroform , to obtain a translucent dispersion, the average diameter of paclitaxel particles is generally 130 ~ 160nm, diluted with water, ultrafiltration with a molecular weight of 10,000 ultrafiltration membrane, the concentrated solution was freeze-dried for 48 hours, without adding any freeze-dried proppant. The obtained cake can easily reconstitute the original dispersion after adding sterile water or physiological saline, and the particle size after reconstitution is the sam...

Embodiment 3

[0038] 200mg paclitaxel (Paclitaxel) and 20mg dimercaptopropanol were dissolved in 3.7ml of chloroform and 0.3ml of absolute ethanol, and 97.0ml of human serum albumin (3%) solution was added, and the mixture was homogenized for 5 minutes at a low speed. To form a crude emulsion, then transfer it to a high-pressure homogenizer, and circulate the high-pressure homogenization for 4 to 5 times. The homogenized liquid is evaporated under reduced pressure at 40°C for 20 minutes, and the chloroform is quickly removed. The obtained dispersion is half Transparent, the average diameter of paclitaxel particles is generally 130-150nm, diluted with water, ultrafiltration with an ultrafiltration membrane with a molecular weight of 10,000, and the concentrated solution was freeze-dried for 48 hours without adding any freeze-dried proppant. The obtained cake can easily reconstitute the original dispersion after adding sterile water or physiological saline, and the particle size after reconsti...

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Abstract

The invention discloses a novel nano preparation with stable protein, as well as a preparation method and a purpose thereof. The invention is characterized in that: a protein coating is formed from albumin and other materials containing sulphydryl or disulfide bond through the cross linking of the disulfide bond; the protein coating contains free protein or protein derivatives which associate(s) with the protein coating, wherein, part of insoluble drugs are contained in the protein coating and part of such drugs are associated with the free protein or the protein derivatives, and the average diameter of protein coating particles is not more than 1 micron. The purpose of the preparation is to send water insoluble drugs into the bodies of living things.

Description

Technical field: [0001] The invention relates to the field of pharmaceutical preparations, specifically a novel protein-stabilized nano-preparation and its preparation method and application. Background technique: [0002] In drug research, it is found that a large number of drugs are insoluble in water, and some drugs are even insoluble in organic solvents, making it difficult to administer them. In the preparation process, the use of cyclodextrin inclusion technology, surfactant solubilization, emulsion, microemulsion and solid dispersion technology can solve the dissolution problem of some insoluble drugs, but there are still a large number of drugs that are discarded due to dissolution problems use. [0003] In 2005, the FDA approved Abraxane, a paclitaxel product developed by American Pharmaceutical Partners, which uses human serum albumin (HSA) as a carrier. Abraxane has significant advantages over paclitaxel injection (Taxol). The product is a nano-preparation of pa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/42A61K47/48A61K31/337A61P35/00A61K47/64
Inventor 周建平张振海吕慧侠
Owner CHINA PHARM UNIV
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